Optimization of self nanoemulsifying drug delivery system for poorly water-soluble drug using response surface methodology
Drug Development and Industrial Pharmacy, 2012
There is an increasing interest on self-nanoemulsifying drug delivery system (SNEDDS) for oral de... more There is an increasing interest on self-nanoemulsifying drug delivery system (SNEDDS) for oral delivery of poorly water-soluble drugs. However, development of SNEDDS is often driven by empiric, pseudo-ternary diagrams and solubility of drugs, and it is lacking a systematic approach for evaluating impact of excipients on the performance of formulations as well as the fate of drug. The aim of this study was to rationalize the SNEDDS development procedure and to get a better understanding on the role of excipients on the SNEDDS. The formulations consist of soybean oil or rapeseed oil, Cremophor(®) RH40, Maisine™ 35-1 and ethanol. Response surface methodology (RSM) was used in the development of SNEDDS. Significant advantages of RSM were found in reducing the work load and determining the impact of excipients on formulation characteristics. The most significant factor in influencing droplet size was the co-surfactant Maisine™ 35-1, the droplet size increased with increasing concentration of Maisine™ 35-1. It suggests that Maisine™ 35-1 has double functions in the SNEDDS; it functions as co-surfactant to improve the emulsification of oil, meanwhile it also works as the oil phase and results in larger droplets. A significant reduction in droplet size was interestingly observed when fenofibrate was loaded in the vehicles, probably due to the surface activity of fenofibrate, promoting the self-emulsifying process. It was evident that drug precipitation during lipolysis was not affected by the level of co-solvent ethanol in the formulation, while it had pronounced impact on drug solubilization during the initial dispersion stage.
British journal of pharmaceutical research, Jan 10, 2013
Gliclazide is an oral hypoglycemic agent used in management of non-insulin dependent diabetes mel... more Gliclazide is an oral hypoglycemic agent used in management of non-insulin dependent diabetes mellitus. Among people who are suffering from long term disorders, the major were categorized under diabetes so, a dosage form is needed to provide continuous therapy with high margin of safety & such dosage form can be achieved by microencapsulation. Gliclazide microspheres with sodium alginate (coat material, gum kondagogu, gum guar and xanthan gum (mucoadhesive agents) were prepared by orifice-ionic gelation and emulsification ionic gelation techniques varying concentrations (1:0.25, 1:0.5, 1:0.75 and 1:1). Formulations were then evaluated for surface morphology, particle shape, Carr's index, microencapsulation efficiency, drug release, mucoadhesion studies. Compatibility studies were performed by FTIR, DSC, and XRD techniques and no interactions were found between drug and excepients used. The microspheres were found spherical and free flowing with emulsion ionic gelation technique with a size range 400-600µm. % drug content and encapsulation efficiency found in the range of 55%-68% and, 86.23%-94.46% respectively. All microspheres showed good mucoadhesive property in in-vitro wash of test. In vitro drug release studies showed that the guar gum has more potentiality to retard the drug release compared to other gums and concentrations. Drug release from the microspheres was found slow following zero order release kinetics with non-fickian release mechanism stating release depended on the coat: core ratio and the method employed. The concentration of 1:1 of SA: GG (EMG 4) found suitable for preparing the controlled release formulation of gliclazide stating emulsification gelation technique is the best among followed.
Preparation and characterization of solid lipid nanoparticles II. Effect of viscosity, method of preparation and homogenization speed on Physical Characteristics of Solid Lipid Nanoparticles
Zagazig Journal of Pharmaceutical Science, Dec 1, 2010
This article is an open access article distributed under the terms and conditions of the Creative... more This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY
Zagazig Journal of Pharmaceutical Science, Jun 1, 2006
Borneol is a traditional Chinese medicine that can promote drug absorption from the gastrointesti... more Borneol is a traditional Chinese medicine that can promote drug absorption from the gastrointestinal tract and distribution to the brain. However, stomach irritation may occur when high doses of borneol are used. In the present work, gastrodin, the main bioactive ingredient of the traditional Chinese drug "Tianma" (Rhizoma Gastrodiae) was used as a model drug to explore reasonable application of borneol. Sustained-release solid dispersions (SRSDs) for co-loading gastrodin and borneol were prepared using ethylcellulose as a sustained release matrix and hydroxy-propyl methylcellulose as a retarder. The dispersion state of drug within the SRSDs was analyzed by using scanning electron microscopy, differential scanning calorimetry, and powder X-ray diffractometry. The results indicated that both gastrodin and borneol were molecularly dispersed in an amorphous form. Assay of in vitro drug release demonstrated that the dissolution profiles of gastrodin and borneol from the SRSDs both fitted the Higuchi model. Subsequently, gastric mucosa irritation and the brain targeting of the SRSDs were evaluated. Compared with the free mixture of gastrodin and borneol, brain targeting of SRSDs was slightly weaker (brain targeting index: 1.83 vs. 2.09), but stomach irritation obviously reduced. Sustained-release technology can be used to reduce stomach irritation caused by borneol while preserving sufficient transport capacity for oral brain-targeting drug delivery.
Prevalence of Depression Among Jordanian University Students During COVID-19 Pandemic
Biomedical and Pharmacology Journal
Objective: The global COVID-19 pandemic has a significant impact on individuals, physical and men... more Objective: The global COVID-19 pandemic has a significant impact on individuals, physical and mental health. This study aims to investigate the relationship between the COVID-19 pandemic and depression as a mental health problem among students of Jadara University. Methods: a cross-sectional study among Jadara University students by survey forms was conducted between 6 -12 of May 2020. The CES-D scale was used to assess depression. Result: Out of 200 participants, 45% were classified as high risk for depression and 55% as low risk for depression. Our resulting study revealed that the academic year and the professional status of the student had a significant relationship with depression. Conclusion: COVID-19 pandemic gives insight into the importance of universities and states natural resources to respond to mental health problems among the most vulnerable.
The usefulness of nanotechnology nowadays in improving the performance of different active pharma... more The usefulness of nanotechnology nowadays in improving the performance of different active pharmaceutical ingredients (API) has generated a great deal of excitement worldwide. These nano-systems offer the advantage of higher bioavailability, lower toxicity, and the ability to deliver drugs with low half-life or low permeability. Lipid nano-based carriers have been extensively used for their ability to protect the API from degradation and their safety as these used lipids are generally regarded as safe. Lipospheres and Pro-nanolipospheres are among the promising systems for the delivery of water-insoluble drugs. They are composed of aqueous dispersible particles with a rigid hydrophobic lipid centre, coated by an outer protective phospholipid exterior. These lipospheres and Pro-nanolipospheres have the advantage of being easy to scale up, high dispersibility in aqueous media, and improved physical stability, making them the perfect candidate for the delivery of different APIs using different routes including oral, parenteral, intranasal and topical routes.
International Journal of Pharmacy and Pharmaceutical Sciences, Jan 10, 2015
The aim of the current work was to look into the feasibility of planning of solid lipid nanoparti... more The aim of the current work was to look into the feasibility of planning of solid lipid nanoparticles of Glyceryl mono stearate containing Dibenzoyl peroxide, Erythromycin base, and Triamcinolone acetonide as model drugs. Methods: Solid lipid nanoparticles loaded with three model lipophilic drugs were developed by high shear hot homogenization method. The model drugs used are Dibenzoyl peroxide, Erythromycin base, and Triamcinolone acetonide. Glyceryl monostearate was used as the lipid core; Tween 20 and Tween 80 were employed as surfactants and lecithin asco-surfactant. Many formulation parameters were manipulated to receive high quality nanoparticles. The prepared solid lipid nanoparticles were evaluated by different standardphysical and imaging methods. The efficiency of drug release form prepared formulaewas studied using In vitro technique to utilize of dialysis bag technique. The stability of prepared formulae was studied by thermal procedures and infrared spectrum analysis. The physicochemical properties of the prepared formulae like particle size, drug entrapment efficiency, drug loading capacity, yield content and In vitro drug release behavior were too assessed. Results: The average particle diameter measured by a laser diffraction technique was (194.6±5.03 to 406.6±15.2 NM) for Dibenzoyl peroxide loaded solid lipid nanoparticles, (220±6.2 to 328.34±2.5) NM for Erythromycin loaded solid lipid nanoparticles and (227.3±2.5 to 480.6±24) NM for Triamcinolone acetonide loaded solid lipid nanoparticles. The entrapment efficiency and drug loading capacity, determined with ultravioletspectroscopy, were 80.5±9.45% and 0.805±0.093%, for Dibenzoyl peroxide, 96±11.5 and0.96±0.012 for Triamcinolone acetonide and 94.6±14.9 and 0.946±0.012 for Erythromycinbase respectively. It was found that model drugs showed significant faster release patterns when compared with commercially available formulations and pure drugs(p˂0. 05). Thermal analysis of prepared solid lipid nanoparticles gave indication ofsolubilization of drugs within a lipid matrix. Fourier Transform Infrared Spectroscopy (FTIR) showed the absence of new bands for loaded solid lipid nanoparticles indicating nointeraction between drugs and lipid matrix and being only dissolved in it. Electronmicroscope of scanning and transmission techniques indicated sphere form of preparedsolid lipid nanoparticles with smooth surface with size below 100 nm. Conclusion: In conclusion, it may be concluded that solid lipid nanoparticles with small particle size have high encapsulation efficiency, and relatively high loading capacity for Dibenzoyl peroxide, Erythromycin base, and Triamcinolone acetonide as model drugs can be obtained by this method.
Annona muricata L. leaves extract loaded on chitosan nanoparticles combined with methotrexate induce Cytotoxicity in A549 cancer cell line
Annona muricata Linn (AM) and methotrexate (MTX)-loaded chitosan (Ch) as a natural cationic, bio-... more Annona muricata Linn (AM) and methotrexate (MTX)-loaded chitosan (Ch) as a natural cationic, bio-degradable and biocompatible polymer were investigated for their genotoxic and cytotoxic effects in their normal and nano form. The AM-ChNP and MTX-ChNP were analyzed and characterized according to fourier transform infrared spectroscopy (FTIR), particle size, Zeta potential, transmission electron microscope (TEM) and encapsulation efficiency. The chitosan concentration (3:1) was found to be an important parameter for optimizing the dispersion of AM-ChNPs and of MTX-ChNPs nanocomposites over long time. The efficiency was found to be 87.3% and size of 100–200 nm. The stabilty of the nanocomposites offers a good sign in cancer cell line treatment. Seven groups were prepared using the A549 lung cell line: control group, A. muricata leaf extract (AM), Methotrexate (MTX), AM-ChNPs, MTX-ChNPs, AM + MTX, and AM-ChNPs + MTX-ChNPs. 3-[4,5-dimethylthiazol-2-yl]-2,5 diphenyl tetrazolium bromide ( M...
Atorvastatin-loaded pro-nanolipospheres with ameliorated oral bioavailability and antidyslipidemic activity
Colloids and Surfaces B: Biointerfaces
Despite significant advances in oral drug delivery technologies, many drugs are prone to limited ... more Despite significant advances in oral drug delivery technologies, many drugs are prone to limited oral bioavailability due to biological barriers that hinder drug absorption. Pro-nanolipospheres (PNL) are a form of delivery system that can potentiate the oral bioavailability of poorly water-soluble drugs through a variety of processes, including increased drug solubility and protecting them from degradation by intestinal or hepatic first-pass metabolism. In this study, pro-nanolipospheres were employed as a delivery vehicle for improving the oral bioavailability of the lipophilic statin, atorvastatin (ATR). Various ATR-loaded PNL formulations, composed of various pharmaceutical ingredients, were prepared by the pre-concentrate method and characterized by determining particle size, surface charge, and encapsulation efficiency. An optimized formula (ATR-PT PNL) showing the smallest particle size, highest zeta potential, and highest encapsulation efficiency was selected for further in vivo investigations. The in vivo pharmacodynamic experiments demonstrated that the optimized ATR-PT PNL formulation exerted a potent hypolipidemic effect in a Poloxamer® 407-induced hyper-lipidaemia rat model by restoring normal cholesterol and triglyceride serum levels along with alleviating serum levels of LDL while elevating serum HDL levels, compared to pure drug suspensions and marketed ATR (Lipitor®). Most importantly, oral administration of the optimized ATR-PT PNL formulation showed a dramatic increase in ATR oral bioavailability, as evinced by a 1.7- and 3.6-fold rise in systemic bioavailability when compared with oral commercial ATR suspensions (Lipitor®) and pure drug suspension, respectively. Collectively, pro-nanolipospheres might represent a promising delivery vehicle for enhancing the oral bioavailability of poorly water-soluble drugs.
The Comparison Between the Effect of Atorvastatin and Nanoparticle Atorvastatin on Rat Liver
Biomedical and Pharmacology Journal
Objective: Statins are one of the most effective drugs for reducing cholesterol and triglyceride ... more Objective: Statins are one of the most effective drugs for reducing cholesterol and triglyceride levels, which main activity includes inhibiting 3-hydroxy-3-methylglutaryl-CoA (HMG-CoA) reductase that is involved in cholesterol synthesis. However, statins are associated with several side effects; the most commonly reported ones are those related to the liver. This study was conducted to compare the impact of two formulas of Atorvastatin: Atorvastatin calcium (ATV), and Nanoparticles of Atorvastatin (NATV) on the liver. Methods: thirty Albino rats were randomly divided into three groups; control group (n=10) (standard diet), Atorvastatin group (ATV) 40 mgkg group, and Nanoparticle Atorvastatin group (NATV) 40 mgkg. After 30 days, all rat groups were sacrificed. Results: In comparison with the control group, the ATV and NATV groups had a significant increase in the activities of liver enzymes alkaline phosphatase (ALP), aspartate transaminase (AST), and alanine transaminase (ALT) (p&l...
Testicular Nanotechnology is redefining healthcare methods, and it is projected to have a signifi... more Testicular Nanotechnology is redefining healthcare methods, and it is projected to have a significant impact in the next years, resulting in improved healthcare facilities. It has paved the way for therapeutic medication delivery and diagnostics. Medical nanoparticles are materials in the nanoscale (from 1 to 100 nm) employed in the development, production, control, and use of medicinal drugs or devices employed in developing, producing, controlling, and using medicinal drugs or devices. Aside from gene therapy, nano-based medicine delivery systems benefit cancer, diabetes, infectious diseases, neurological diseases, blood diseases, and orthopaedic-related maladies. Furthermore, the development of multifunctional nanotherapeutics is potentially needed to contribute to the present therapeutic area positively. Nanomedicines are preferable to conventional therapeutic approaches in cancer as they can transmit the drug efficiently to the damaged tissues, decreasing drug toxicity. Nanotechnology-based medicines and diagnostics are more effective while posing little or no side effects. Micelles of polymeric paclitaxel and polymeric asparaginase conjugates have been advocated for treating several tumours in this vein. Nanotechnology advancements have prepared nanorobotics to be applied in various healthcare applications. As a result, this review thoroughly highlights the potential of polymeric nanoparticles, Nano-emulsions, solid lipid nanoparticles, nanostructured lipid carriers, self-micellizing anticancer lipids, dendrimer, nanocapsule, and nanosponges approaches in cancer, as well as the potentialities of various nanocarriers and nanomedicines for a variety of applications in diagnostics and drug delivery. This article reviews the most recent literature on nanotechnology, particularly cyclodextrin-based polymers, in medicinal applications. Nanosponges have shown great potential in nanotechnology and targeted medicine delivery. Because they can be employed to solubilize poorly water-soluble medicines, boost stability, extend release, and improve bioavailability, these nano-sized structures with colloidal diameters and nanosized voids can answer various questions formulation difficulties. This review focuses on nanosponge manufacturing procedures and characterization, factors affecting drug loading and release kinetics, and their use in the pharmaceutical industry.
Records of Pharmaceutical and Biomedical Sciences, 2020
Solid lipid nanoparticles (SLN) are colloidal lipid carriers, which used for improving the bioava... more Solid lipid nanoparticles (SLN) are colloidal lipid carriers, which used for improving the bioavailability of lipophilic and hydrophilic drugs. SLN are composed of biodegradable lipids such as hard fats, highly purified triglycerides, monoglycerides, complex glyceride mixtures or waxes which are solid at room temperature. In the present study, different formulation variables, including the type and quantity of lipid and surfactant were optimized for the preparation of SLN. SLN were prepared by a modified micro emulsion-based method and their particle size was evaluated. Two types of surfactants Tween 80 and Poloxamer 188 were used. Also, the monoglyceride (Glyceryl monostearate) and wax (Cetyl palmitate) were used as lipid. The optimum SLN formulae were at lipid concentration 5%. The optimum surfactant concentration was 6%. SLN with a surfactant Tween 80 were smaller in size than Poloxamer 188 SLN. Glyceryl monostearate formed a smaller size SLN than Cetyl palmitate. Increasing Glyceryl monostearate concentration in the lipid ratio resulted in the formation of small size SLN.
The objective of this study was to verify the effect of certain new biocompatible additive on the... more The objective of this study was to verify the effect of certain new biocompatible additive on the stability and feasibility of the SLN using Glyceryl monostearate as lipid matrix. Cationic Starch, which is newly modified in organic chemistry laboratories, used with different ratios to show the effect on zeta potential of formulated nanoparticles using Triamcinolone acetonide as a model drug. Method of High shear homogenization was used for preparation of SLN utilizing a rotor-stator homogenizer. It was found that particle diameter of formulated nanoparticles shifted from nanosized to micronized with increase of amount of cationic starch used (2.5 to 10% w/w), while the zeta potential reduced although showing high negative values (-36 to-27 mV), indicating stability. The loading capacity and encapsulation efficiency of produced nanoparticles were reduced with increase of amount of cationic starch used. The influence of cationic starch on drug release from prepared formulae was studied using dialysis bag technique. Fourier Transformation Infrared Spectroscopy (FTIR) showed the absence of new bands for loaded solid lipid nanoparticles indicating no interaction between drug and cationic starch. Electron microscope of scanning technique indicated sphere form of prepared solid lipid nanoparticles with smooth surface. It was concluded that retardation of in vitro release and effect on simulated in vivo permeation through human skin were affected by using different concentrations of cationic starch as excipient that meantime, be used to reduce zeta potential and act as self-flocculating agent during formulation.
This study assessed the protective effect of Zizphus jujube (ZJ) extract on 5‑FU‑induced alterati... more This study assessed the protective effect of Zizphus jujube (ZJ) extract on 5‑FU‑induced alterations in renal function markers and kidney morphology in Dawley rats. Twenty-four rats were divided randomly into four groups administrated orally with 0.9% normal saline as the control group, 5-FU (40 mg/kg daily for 5 days), ZJ (500 mg/ kg daily for 5 days), and 5-FU+ ZJ (for 6 days). further biochemical experiments carried out on blood collected from the heart. Kidney tissues were obtained for analysis of catalase (Cat), glutathione S-transfers (GST), and lipid peroxide levels as well as histology analysis. 5-FU significantly reduced the enzyme activity of Cat and GST and increased levels of lipid peroxidation and plasma creatinine levels (P < 0.005). Histopathological examination showed severe wide ischemia of proximal convoluted tubule (PCT), missing in Bowman's space, and edema in the group treated with 5-FU. In addition, pretreatment with ZJ has significantly improved levels ...
Optimization of self nanoemulsifying drug delivery system for poorly water-soluble drug using response surface methodology
Drug Development and Industrial Pharmacy, 2012
There is an increasing interest on self-nanoemulsifying drug delivery system (SNEDDS) for oral de... more There is an increasing interest on self-nanoemulsifying drug delivery system (SNEDDS) for oral delivery of poorly water-soluble drugs. However, development of SNEDDS is often driven by empiric, pseudo-ternary diagrams and solubility of drugs, and it is lacking a systematic approach for evaluating impact of excipients on the performance of formulations as well as the fate of drug. The aim of this study was to rationalize the SNEDDS development procedure and to get a better understanding on the role of excipients on the SNEDDS. The formulations consist of soybean oil or rapeseed oil, Cremophor(®) RH40, Maisine™ 35-1 and ethanol. Response surface methodology (RSM) was used in the development of SNEDDS. Significant advantages of RSM were found in reducing the work load and determining the impact of excipients on formulation characteristics. The most significant factor in influencing droplet size was the co-surfactant Maisine™ 35-1, the droplet size increased with increasing concentration of Maisine™ 35-1. It suggests that Maisine™ 35-1 has double functions in the SNEDDS; it functions as co-surfactant to improve the emulsification of oil, meanwhile it also works as the oil phase and results in larger droplets. A significant reduction in droplet size was interestingly observed when fenofibrate was loaded in the vehicles, probably due to the surface activity of fenofibrate, promoting the self-emulsifying process. It was evident that drug precipitation during lipolysis was not affected by the level of co-solvent ethanol in the formulation, while it had pronounced impact on drug solubilization during the initial dispersion stage.
British journal of pharmaceutical research, Jan 10, 2013
Gliclazide is an oral hypoglycemic agent used in management of non-insulin dependent diabetes mel... more Gliclazide is an oral hypoglycemic agent used in management of non-insulin dependent diabetes mellitus. Among people who are suffering from long term disorders, the major were categorized under diabetes so, a dosage form is needed to provide continuous therapy with high margin of safety & such dosage form can be achieved by microencapsulation. Gliclazide microspheres with sodium alginate (coat material, gum kondagogu, gum guar and xanthan gum (mucoadhesive agents) were prepared by orifice-ionic gelation and emulsification ionic gelation techniques varying concentrations (1:0.25, 1:0.5, 1:0.75 and 1:1). Formulations were then evaluated for surface morphology, particle shape, Carr's index, microencapsulation efficiency, drug release, mucoadhesion studies. Compatibility studies were performed by FTIR, DSC, and XRD techniques and no interactions were found between drug and excepients used. The microspheres were found spherical and free flowing with emulsion ionic gelation technique with a size range 400-600µm. % drug content and encapsulation efficiency found in the range of 55%-68% and, 86.23%-94.46% respectively. All microspheres showed good mucoadhesive property in in-vitro wash of test. In vitro drug release studies showed that the guar gum has more potentiality to retard the drug release compared to other gums and concentrations. Drug release from the microspheres was found slow following zero order release kinetics with non-fickian release mechanism stating release depended on the coat: core ratio and the method employed. The concentration of 1:1 of SA: GG (EMG 4) found suitable for preparing the controlled release formulation of gliclazide stating emulsification gelation technique is the best among followed.
Preparation and characterization of solid lipid nanoparticles II. Effect of viscosity, method of preparation and homogenization speed on Physical Characteristics of Solid Lipid Nanoparticles
Zagazig Journal of Pharmaceutical Science, Dec 1, 2010
This article is an open access article distributed under the terms and conditions of the Creative... more This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY
Zagazig Journal of Pharmaceutical Science, Jun 1, 2006
Borneol is a traditional Chinese medicine that can promote drug absorption from the gastrointesti... more Borneol is a traditional Chinese medicine that can promote drug absorption from the gastrointestinal tract and distribution to the brain. However, stomach irritation may occur when high doses of borneol are used. In the present work, gastrodin, the main bioactive ingredient of the traditional Chinese drug "Tianma" (Rhizoma Gastrodiae) was used as a model drug to explore reasonable application of borneol. Sustained-release solid dispersions (SRSDs) for co-loading gastrodin and borneol were prepared using ethylcellulose as a sustained release matrix and hydroxy-propyl methylcellulose as a retarder. The dispersion state of drug within the SRSDs was analyzed by using scanning electron microscopy, differential scanning calorimetry, and powder X-ray diffractometry. The results indicated that both gastrodin and borneol were molecularly dispersed in an amorphous form. Assay of in vitro drug release demonstrated that the dissolution profiles of gastrodin and borneol from the SRSDs both fitted the Higuchi model. Subsequently, gastric mucosa irritation and the brain targeting of the SRSDs were evaluated. Compared with the free mixture of gastrodin and borneol, brain targeting of SRSDs was slightly weaker (brain targeting index: 1.83 vs. 2.09), but stomach irritation obviously reduced. Sustained-release technology can be used to reduce stomach irritation caused by borneol while preserving sufficient transport capacity for oral brain-targeting drug delivery.
Prevalence of Depression Among Jordanian University Students During COVID-19 Pandemic
Biomedical and Pharmacology Journal
Objective: The global COVID-19 pandemic has a significant impact on individuals, physical and men... more Objective: The global COVID-19 pandemic has a significant impact on individuals, physical and mental health. This study aims to investigate the relationship between the COVID-19 pandemic and depression as a mental health problem among students of Jadara University. Methods: a cross-sectional study among Jadara University students by survey forms was conducted between 6 -12 of May 2020. The CES-D scale was used to assess depression. Result: Out of 200 participants, 45% were classified as high risk for depression and 55% as low risk for depression. Our resulting study revealed that the academic year and the professional status of the student had a significant relationship with depression. Conclusion: COVID-19 pandemic gives insight into the importance of universities and states natural resources to respond to mental health problems among the most vulnerable.
The usefulness of nanotechnology nowadays in improving the performance of different active pharma... more The usefulness of nanotechnology nowadays in improving the performance of different active pharmaceutical ingredients (API) has generated a great deal of excitement worldwide. These nano-systems offer the advantage of higher bioavailability, lower toxicity, and the ability to deliver drugs with low half-life or low permeability. Lipid nano-based carriers have been extensively used for their ability to protect the API from degradation and their safety as these used lipids are generally regarded as safe. Lipospheres and Pro-nanolipospheres are among the promising systems for the delivery of water-insoluble drugs. They are composed of aqueous dispersible particles with a rigid hydrophobic lipid centre, coated by an outer protective phospholipid exterior. These lipospheres and Pro-nanolipospheres have the advantage of being easy to scale up, high dispersibility in aqueous media, and improved physical stability, making them the perfect candidate for the delivery of different APIs using different routes including oral, parenteral, intranasal and topical routes.
International Journal of Pharmacy and Pharmaceutical Sciences, Jan 10, 2015
The aim of the current work was to look into the feasibility of planning of solid lipid nanoparti... more The aim of the current work was to look into the feasibility of planning of solid lipid nanoparticles of Glyceryl mono stearate containing Dibenzoyl peroxide, Erythromycin base, and Triamcinolone acetonide as model drugs. Methods: Solid lipid nanoparticles loaded with three model lipophilic drugs were developed by high shear hot homogenization method. The model drugs used are Dibenzoyl peroxide, Erythromycin base, and Triamcinolone acetonide. Glyceryl monostearate was used as the lipid core; Tween 20 and Tween 80 were employed as surfactants and lecithin asco-surfactant. Many formulation parameters were manipulated to receive high quality nanoparticles. The prepared solid lipid nanoparticles were evaluated by different standardphysical and imaging methods. The efficiency of drug release form prepared formulaewas studied using In vitro technique to utilize of dialysis bag technique. The stability of prepared formulae was studied by thermal procedures and infrared spectrum analysis. The physicochemical properties of the prepared formulae like particle size, drug entrapment efficiency, drug loading capacity, yield content and In vitro drug release behavior were too assessed. Results: The average particle diameter measured by a laser diffraction technique was (194.6±5.03 to 406.6±15.2 NM) for Dibenzoyl peroxide loaded solid lipid nanoparticles, (220±6.2 to 328.34±2.5) NM for Erythromycin loaded solid lipid nanoparticles and (227.3±2.5 to 480.6±24) NM for Triamcinolone acetonide loaded solid lipid nanoparticles. The entrapment efficiency and drug loading capacity, determined with ultravioletspectroscopy, were 80.5±9.45% and 0.805±0.093%, for Dibenzoyl peroxide, 96±11.5 and0.96±0.012 for Triamcinolone acetonide and 94.6±14.9 and 0.946±0.012 for Erythromycinbase respectively. It was found that model drugs showed significant faster release patterns when compared with commercially available formulations and pure drugs(p˂0. 05). Thermal analysis of prepared solid lipid nanoparticles gave indication ofsolubilization of drugs within a lipid matrix. Fourier Transform Infrared Spectroscopy (FTIR) showed the absence of new bands for loaded solid lipid nanoparticles indicating nointeraction between drugs and lipid matrix and being only dissolved in it. Electronmicroscope of scanning and transmission techniques indicated sphere form of preparedsolid lipid nanoparticles with smooth surface with size below 100 nm. Conclusion: In conclusion, it may be concluded that solid lipid nanoparticles with small particle size have high encapsulation efficiency, and relatively high loading capacity for Dibenzoyl peroxide, Erythromycin base, and Triamcinolone acetonide as model drugs can be obtained by this method.
Annona muricata L. leaves extract loaded on chitosan nanoparticles combined with methotrexate induce Cytotoxicity in A549 cancer cell line
Annona muricata Linn (AM) and methotrexate (MTX)-loaded chitosan (Ch) as a natural cationic, bio-... more Annona muricata Linn (AM) and methotrexate (MTX)-loaded chitosan (Ch) as a natural cationic, bio-degradable and biocompatible polymer were investigated for their genotoxic and cytotoxic effects in their normal and nano form. The AM-ChNP and MTX-ChNP were analyzed and characterized according to fourier transform infrared spectroscopy (FTIR), particle size, Zeta potential, transmission electron microscope (TEM) and encapsulation efficiency. The chitosan concentration (3:1) was found to be an important parameter for optimizing the dispersion of AM-ChNPs and of MTX-ChNPs nanocomposites over long time. The efficiency was found to be 87.3% and size of 100–200 nm. The stabilty of the nanocomposites offers a good sign in cancer cell line treatment. Seven groups were prepared using the A549 lung cell line: control group, A. muricata leaf extract (AM), Methotrexate (MTX), AM-ChNPs, MTX-ChNPs, AM + MTX, and AM-ChNPs + MTX-ChNPs. 3-[4,5-dimethylthiazol-2-yl]-2,5 diphenyl tetrazolium bromide ( M...
Atorvastatin-loaded pro-nanolipospheres with ameliorated oral bioavailability and antidyslipidemic activity
Colloids and Surfaces B: Biointerfaces
Despite significant advances in oral drug delivery technologies, many drugs are prone to limited ... more Despite significant advances in oral drug delivery technologies, many drugs are prone to limited oral bioavailability due to biological barriers that hinder drug absorption. Pro-nanolipospheres (PNL) are a form of delivery system that can potentiate the oral bioavailability of poorly water-soluble drugs through a variety of processes, including increased drug solubility and protecting them from degradation by intestinal or hepatic first-pass metabolism. In this study, pro-nanolipospheres were employed as a delivery vehicle for improving the oral bioavailability of the lipophilic statin, atorvastatin (ATR). Various ATR-loaded PNL formulations, composed of various pharmaceutical ingredients, were prepared by the pre-concentrate method and characterized by determining particle size, surface charge, and encapsulation efficiency. An optimized formula (ATR-PT PNL) showing the smallest particle size, highest zeta potential, and highest encapsulation efficiency was selected for further in vivo investigations. The in vivo pharmacodynamic experiments demonstrated that the optimized ATR-PT PNL formulation exerted a potent hypolipidemic effect in a Poloxamer® 407-induced hyper-lipidaemia rat model by restoring normal cholesterol and triglyceride serum levels along with alleviating serum levels of LDL while elevating serum HDL levels, compared to pure drug suspensions and marketed ATR (Lipitor®). Most importantly, oral administration of the optimized ATR-PT PNL formulation showed a dramatic increase in ATR oral bioavailability, as evinced by a 1.7- and 3.6-fold rise in systemic bioavailability when compared with oral commercial ATR suspensions (Lipitor®) and pure drug suspension, respectively. Collectively, pro-nanolipospheres might represent a promising delivery vehicle for enhancing the oral bioavailability of poorly water-soluble drugs.
The Comparison Between the Effect of Atorvastatin and Nanoparticle Atorvastatin on Rat Liver
Biomedical and Pharmacology Journal
Objective: Statins are one of the most effective drugs for reducing cholesterol and triglyceride ... more Objective: Statins are one of the most effective drugs for reducing cholesterol and triglyceride levels, which main activity includes inhibiting 3-hydroxy-3-methylglutaryl-CoA (HMG-CoA) reductase that is involved in cholesterol synthesis. However, statins are associated with several side effects; the most commonly reported ones are those related to the liver. This study was conducted to compare the impact of two formulas of Atorvastatin: Atorvastatin calcium (ATV), and Nanoparticles of Atorvastatin (NATV) on the liver. Methods: thirty Albino rats were randomly divided into three groups; control group (n=10) (standard diet), Atorvastatin group (ATV) 40 mgkg group, and Nanoparticle Atorvastatin group (NATV) 40 mgkg. After 30 days, all rat groups were sacrificed. Results: In comparison with the control group, the ATV and NATV groups had a significant increase in the activities of liver enzymes alkaline phosphatase (ALP), aspartate transaminase (AST), and alanine transaminase (ALT) (p&l...
Testicular Nanotechnology is redefining healthcare methods, and it is projected to have a signifi... more Testicular Nanotechnology is redefining healthcare methods, and it is projected to have a significant impact in the next years, resulting in improved healthcare facilities. It has paved the way for therapeutic medication delivery and diagnostics. Medical nanoparticles are materials in the nanoscale (from 1 to 100 nm) employed in the development, production, control, and use of medicinal drugs or devices employed in developing, producing, controlling, and using medicinal drugs or devices. Aside from gene therapy, nano-based medicine delivery systems benefit cancer, diabetes, infectious diseases, neurological diseases, blood diseases, and orthopaedic-related maladies. Furthermore, the development of multifunctional nanotherapeutics is potentially needed to contribute to the present therapeutic area positively. Nanomedicines are preferable to conventional therapeutic approaches in cancer as they can transmit the drug efficiently to the damaged tissues, decreasing drug toxicity. Nanotechnology-based medicines and diagnostics are more effective while posing little or no side effects. Micelles of polymeric paclitaxel and polymeric asparaginase conjugates have been advocated for treating several tumours in this vein. Nanotechnology advancements have prepared nanorobotics to be applied in various healthcare applications. As a result, this review thoroughly highlights the potential of polymeric nanoparticles, Nano-emulsions, solid lipid nanoparticles, nanostructured lipid carriers, self-micellizing anticancer lipids, dendrimer, nanocapsule, and nanosponges approaches in cancer, as well as the potentialities of various nanocarriers and nanomedicines for a variety of applications in diagnostics and drug delivery. This article reviews the most recent literature on nanotechnology, particularly cyclodextrin-based polymers, in medicinal applications. Nanosponges have shown great potential in nanotechnology and targeted medicine delivery. Because they can be employed to solubilize poorly water-soluble medicines, boost stability, extend release, and improve bioavailability, these nano-sized structures with colloidal diameters and nanosized voids can answer various questions formulation difficulties. This review focuses on nanosponge manufacturing procedures and characterization, factors affecting drug loading and release kinetics, and their use in the pharmaceutical industry.
Records of Pharmaceutical and Biomedical Sciences, 2020
Solid lipid nanoparticles (SLN) are colloidal lipid carriers, which used for improving the bioava... more Solid lipid nanoparticles (SLN) are colloidal lipid carriers, which used for improving the bioavailability of lipophilic and hydrophilic drugs. SLN are composed of biodegradable lipids such as hard fats, highly purified triglycerides, monoglycerides, complex glyceride mixtures or waxes which are solid at room temperature. In the present study, different formulation variables, including the type and quantity of lipid and surfactant were optimized for the preparation of SLN. SLN were prepared by a modified micro emulsion-based method and their particle size was evaluated. Two types of surfactants Tween 80 and Poloxamer 188 were used. Also, the monoglyceride (Glyceryl monostearate) and wax (Cetyl palmitate) were used as lipid. The optimum SLN formulae were at lipid concentration 5%. The optimum surfactant concentration was 6%. SLN with a surfactant Tween 80 were smaller in size than Poloxamer 188 SLN. Glyceryl monostearate formed a smaller size SLN than Cetyl palmitate. Increasing Glyceryl monostearate concentration in the lipid ratio resulted in the formation of small size SLN.
The objective of this study was to verify the effect of certain new biocompatible additive on the... more The objective of this study was to verify the effect of certain new biocompatible additive on the stability and feasibility of the SLN using Glyceryl monostearate as lipid matrix. Cationic Starch, which is newly modified in organic chemistry laboratories, used with different ratios to show the effect on zeta potential of formulated nanoparticles using Triamcinolone acetonide as a model drug. Method of High shear homogenization was used for preparation of SLN utilizing a rotor-stator homogenizer. It was found that particle diameter of formulated nanoparticles shifted from nanosized to micronized with increase of amount of cationic starch used (2.5 to 10% w/w), while the zeta potential reduced although showing high negative values (-36 to-27 mV), indicating stability. The loading capacity and encapsulation efficiency of produced nanoparticles were reduced with increase of amount of cationic starch used. The influence of cationic starch on drug release from prepared formulae was studied using dialysis bag technique. Fourier Transformation Infrared Spectroscopy (FTIR) showed the absence of new bands for loaded solid lipid nanoparticles indicating no interaction between drug and cationic starch. Electron microscope of scanning technique indicated sphere form of prepared solid lipid nanoparticles with smooth surface. It was concluded that retardation of in vitro release and effect on simulated in vivo permeation through human skin were affected by using different concentrations of cationic starch as excipient that meantime, be used to reduce zeta potential and act as self-flocculating agent during formulation.
This study assessed the protective effect of Zizphus jujube (ZJ) extract on 5‑FU‑induced alterati... more This study assessed the protective effect of Zizphus jujube (ZJ) extract on 5‑FU‑induced alterations in renal function markers and kidney morphology in Dawley rats. Twenty-four rats were divided randomly into four groups administrated orally with 0.9% normal saline as the control group, 5-FU (40 mg/kg daily for 5 days), ZJ (500 mg/ kg daily for 5 days), and 5-FU+ ZJ (for 6 days). further biochemical experiments carried out on blood collected from the heart. Kidney tissues were obtained for analysis of catalase (Cat), glutathione S-transfers (GST), and lipid peroxide levels as well as histology analysis. 5-FU significantly reduced the enzyme activity of Cat and GST and increased levels of lipid peroxidation and plasma creatinine levels (P < 0.005). Histopathological examination showed severe wide ischemia of proximal convoluted tubule (PCT), missing in Bowman's space, and edema in the group treated with 5-FU. In addition, pretreatment with ZJ has significantly improved levels ...
Uploads
Papers by Ahmed Gardouh