Formulation and Evaluation of Itraconazole Niosomal Gel

Journal of Advanced Scientific Research

The present study was aimed to investigate the delivery potential of vancomycin containing topical niosomal gel. Niosomal formulations were prepared by thin film hydration method at various ratios of Soya PC: Span 80 and were evaluated with respect to particle size, shape, entrapment efficiency, and in vitro characteristics. Average vesicle size of optimized formulation F9 was 158.85 nm. The Zeta potential was found 38.25%. Entrapment efficiency of optimized Niosome formulation (F9) was found as 78.85%. Further, niosomes were incorporated into gel base and characterized for viscosity, % entrapment, extrudability, spreadability and drug release study. It was found that viscosity of prepared gel was 3310±25 cps, % assay was 98.95±0.2 %, extrudability was 175±4 g and spreadibility (g/cm/sec) was found that 8.56±0.25 (g/cm/sec) respectively. In vitro drug release from niosome gel was carried out using franz diffusion cell method. The percentage drug release of optimized formulation was ...

2020

Dermatological conditions are known to be one of the most common medical conditions and 67-90% of fungal infections are known to be caused by Candida non-albicans. Since topicaldrug administration is the most preferred route for dermatological treatment. Unlike classic liposomal vesicles that become trapped within the top layer of stratum corneum cells, cubosomes penetrate the skin and allow improved delivery of various compounds to the deep strata of the skin or to the systemic circulation and can release therapeutic dose. Itraconazole is known to interact with 14-α demethylase interfering with the formation of ergosterol, the main component of the fungal cell membrane.Therefore, the present study is aimed to prepare a cubosomal gel of itraconazole.Cubosomal gel was prepared to increase the penetration of itraconazole into the deeper layers of the skin and hence enhancing the bioavailability by avoiding fi rst-pass metabolism. The prepared cubosomes were optimized on the basis of vesicle size, drug entrapment effi ciency,shape, appearance and in-vitro drug release study. The vesicle size of the prepared cubosomes was found to be 86.69nm and PDI was found to be and 0.258 with 37%, entrapment effi ciency, in-vitro study follows Korsemeyer-Peppas order release pattern. The appearance of the cubosomes was confi rmed by SEM and the cubosomal gel shows good pH, homogeneity, spreadability, and hardness properties. Hence, with the above results it could be interpreted that the cubosomal gel formulation of itraconazole can be a promising treatment approach for candidiasis with improved skin penetration of the drug.

2013

Topical drug administration is a localized drug delivery system anywhere in the body through ophthalmic, rectal, vaginal and skin as topical routes. Skin is one of the most readily accessible organs on human body for topical administration and is main route of topical drug delivery system. There are various skin infections caused by fungus. An antifungal medication is a pharmaceutical fungicide used to treat mycoses such as athlete’s foot ringworm, candidasis. Antifungal works by exploiting differences between mammalian and fungal cells to kill the fungal organism without dangerous effect on host. Miconazole is an imidazoles antifungal derivative and used for the treatment of local and systemic fungal infection. The oral use of miconazole is not recommended as it has many side effects. Miconazole topical gel formulation is made for better patient compliance and to reduce the dose of drug and to avoid the side effects like liver damage and kidney damage. The gel was formulated by cha...

International Journal of Science and Research Archive

Background: Griseofulvin is an antifungal drug that is currently available in the market only in oral dosage forms. So, the development of topical treatment could be advantageous for the treatment of superficial fungal infections. Though for superficial fungal treatment, the skin acts as a major target as well as a principal barrier for drug delivery. To overcome this the colloidal carrier system niosome was used. Niosomes being in the nanometer size range would allow the delivery of the drug at the desired site. Niosomes being non-ionic surfactant-based vehicles would facilitate the passage of the drugs through as skin is composed of both lipid and aqua, which would create problems for any other delivery system. Methodology: Griseofulvin belonging to the BCS Class II was formulated in the form of niosomes to enhance the drug’s solubility. In this study, optimization of niosomal formulation was done using OVAT (one variable at a time) method. Here, the CMAs (critical material attrib...

International Journal of Pharmacy and Pharmaceutical Sciences, 2023

Objective: Topical gel preparations are used for application on skin or to certain mucosal surfaces for local action or for their emollient or protective action. Topical delivery of drugs can be achieved by incorporating drugs into the hydrogel matrix for effective delivery of drugs, thus avoiding first-pass metabolism and for increased local action in pain management and skin diseases. Methods: Hydrogel is a network of polymer chains that are hydrophilic, sometimes found as a colloidal gel in which water is the dispersion medium. Miconazole nitrate (MN) is a broad-spectrum antifungal agent of the imidazole group. It has been selected as a model drug for the preparation of hydrogel. For the preparation of hydrogel, Carbopol of different grades like 934p, 971p, and 974p have been selected. Drug-polymer interaction has been carried out by FT-IR spectroscopy. Standard curve of miconazole nitrate was prepared in phosphate buffer pH 5.5 and 7.4. Physico-chemical characteristics of the hydrogel, like pH, viscosity and % swelling index, were studied. % cumulative drug permeation study through dialysis membrane was done in phosphate buffer pH 7.4. Results: The results were found to be satisfactory. Carbopols have been used in different ratios to get a number of formulations. Out of these, nine formulations have been chosen by their satisfactory physicochemical characteristics and used for the study. The average pH, viscosity, % swelling index and drug content were found to be 7.36, 1.09 x 100 cps, 23.1 and 98.36 %, respectively. Drug permeation kinetics through the dialysis membrane has been done in a Franz diffusion cell at phosphate buffer pH-7.4. The permeation of Miconazole Nitrate through the dialysis membrane was maximum in F1 and minimum in F9. The drug permeation through the dialysis membrane followed zero-order kinetics. Conclusion: A sharp correlation between the % swelling index and the Cumulative % of drug permeated through the dialysis membrane has been found. With the increase in the % swelling index over a period of 6 h the permeation decreased; thus, the swelling of the formulations is responsible to inhibit the permeation of Miconazole Nitrate through the skin.

Asian Journal of Pharmaceutical and Clinical Research, 2018

Objective: The main objective of the study was to formulate and evaluate the chitosan nanoparticles to improve the therapeutic efficacy of itraconazole by loading in nanoparticle drug delivery system. Designing the formulation of the drug itraconazole prolongs the therapeutic concentration of the drug in the blood and which will lower the frequency of dosing and also improves the efficacy of the drug. Methods: Itraconazole nanoparticles are prepared by ionic gelation method; here, chitosan is used as polymer. The formulated nanoparticles are evaluated for external morphological studies by scanning electron microscope (SEM), drug content, in vitro drug release studies, as well as infrared (IR) spectral analysis. Results: The Fourier transform IR spectra show that there was no interaction between drug and polymers; hence, they are compatible. Percentage entrapment efficiency, drug content, and percentage yield were higher for F3 formulation. The particle size analysis shows that every...

2009

Niosomes have shown promise as cheap and chemically stable drug delivery systems. Niosomes have been prepared with different molar ratios of surfactant and cholesterol and their morphological properties have been determined by scanning electron microscopy. Different batches of Fluconazole niosomal preparations were prepared by changing the surfactant concentration but keeping the cholesterol concentration constant. The surfactant used was Span 60 and the five batches of niosomal preparations prepared were in the ratios 1:1:1, 1.5:1:1, 2:1:1, 2.5:1:1 and 3:1:1 (surfactant: cholesterol: drug). Furthermore, the release profile, entrapment efficiency, size distribution and stability of these niosomes under various temperatures were studied.

Journal of Global Pharma Technology, 2010

Antifungal drug ketoconazole was encapsulated in niosome for topical application .Ketoconazole niosome were prepared by thin film hydration method technique using surfactant, cholesterol, dicetyl phosphate & drug mixture in different weight ratios. The prepared niosomes were characterized by various physicochemical parameters & evaluation of release studies of entrapped ketoconazole in niosomes were carried out by UV Visible spectrophotometric method.

Journal of Pharmacy and Pharmacology, 2004

Orally administered acetazolamide has a limited use in glaucoma due to the systemic side effects associated with its use. No topical formulation of acetazolamide is available, mainly because of it having a limited aqueous solubility and poor corneal permeation. To enhance the bioavailability of acetazolamide by the topical route and to improve the corneal permeability of the drug, niosomes of acetazolamide were prepared (employing span 60 and cholesterol) by different methods. Transmission electron microscopy (TEM) of the selected formulation was carried out to study the morphology. Niosomes were also prepared in the presence of dicetyl phosphate and stearylamine to obtain negatively and positively charged vesicles, respectively. It was found that the reverse-phase evaporation method (REV) gave the maximum drug entrapment efficiency (43.75%) as compared with ether injection (39.62%) and film hydration (31.43%) techniques. Drug entrapment efficiency varied with the charge and the percent entrapment efficiency for the REV method was 43.75, 51.23 and 36.26% for neutral, positively charged and negatively charged niosomes, respectively. Corneal permeability studies, however, showed that the percent permeation and the apparent permeability coefficient for the charged niosomes was less than the neutral ones. A bioadhesive niosomal formulation of acetazolamide was also prepared and compared with the positively charged formulation, considering that both of them would have a prolonged stay in the cul-de-sac because of their expected interactions with mucin. The formulations were also compared based on their intraocular pressure (IOP)-lowering capacity. The positively charged niosomes (REV2), although showing a good corneal permeability and pharmacodynamics were, however, found to be inappropriate in terms of the corneal cell toxicity. The bioadhesive coated formulation (REV1bio) compared well with REV2 and also showed a much lesser toxicity. Further, the IOP-lowering effect of the developed formulations was compared with that of a marketed formulation of dorzolamide 2%, a topical carbonic anhydrase inhibitor. The developed niosomal formulations of acetazolamide showed a comparable physiological effect (33% reduction of IOP in REV1bio and 37% reduction in dorzolamide) with a duration of up to 6 h (the duration being 3 h for dorzolamide). Results of the study indicate that it is possible to develop a safe (as indicated by corneal toxicity studies) and physiologically active topical niosomal formulation of acetazolamide relative in efficiency to the newer local carbonic anhydrase inhibitor, dorzolamide. The developed formulations can form a cost effective treatment plan, which is especially important in the treatment of glaucoma, a chronic ailment affecting middle-aged to old patients.

Topical drug administration is a localised drug delivery system that can be used to administer drugs to any part of the body via ophthalmic, rectal, vaginal, and cutaneous channels. The principal route of topical medication delivery is through the skin, which is one of the most easily accessible organs on the human body for topical administration. Fungus can cause a variety of skin illnesses. Antifungal medications are fungicides that are used to treat mycoses such athlete's foot, ringworm, and candidasis. Antifungal kills the fungal organism without harming the host by leveraging distinctions between mammalian and fungal cells. Hence we attempted to develop Econazole-loaded invasomes hydrogel. Invasomes were prepared by conventional thin layer evaporation technique using Phosphatidylcholine, terpene (Limonene) and ethanol. In present study was to develop and characterize Econazoleloaded invasomal drug carrier systems. Different Formulations (F1 to F6) of invasomes were prepared and evaluated for average vesicle size, zeta potential and entrapment efficiency. Drug content of econazole incorporated invasomes gel for formulation IG-1, IG-2 and IG-3 was found to be 98.85±0.15, 99.45±0.10 and 98.74±0.23 respectively. The maximum drug content was found in formulation IG-2 (99.45±0.10), select as optimized formulation. When the regression coefficient values of were compared, it was observed that 'r 2 ' values of Higuchi was maximum i.e. 0.985 hence indicating drug release from formulations was found to follow Higuchi kinetics.

The present study endeavors to prepare a niosomal gel of Cefoperazone sodium (CFS), as a novel dermal delivery for the treatment of skin infections. CFS loaded niosomes were prepared using different molar ratio of Tween 80 and Cholesterol by ether injection method using experimental design. The optimized formula was evaluated for DSC, XRPD and AFM. A niosomal gel with the optimized formulation was prepared in Carbopol 934 and were evaluated for gelling properties, in-vitro release, ex-vivo permeation and skin irritation study on rats. Quality by design was successfully executed to get stable (Zeta potential-30mV), nano sized (365.3 nm) niosomal vesicles. The niosomal gel of CFS showed a pH around 5.5, and a viscosity of 84.13±0.25 cps, enhanced permeation and no skin irritation. Hence, the study depicts that a superior site-specific delivery of CFS can be achieved with a niosomal gel of the drug in the treatment of skin infections.

Journal of Drug Targeting, 2021

The purpose of this research was to enhance the transdermal delivery of diclofenac sodium niosomal formulations. To characterise the obtained niosomes, SEM, XRPD, DSC and ATR-FTIR were employed. The size of the niosomes increased from 158.00±6.17 to 400.87±4.99 nm when cholesterol was incorporated into the formulations. It was observed that the zeta potential of niofenac varies from -25.40±1.352 to -43.13±1.171 mV when the cholesterol percentage decreased from 2% to 0.2%. The higher entrapment efficiency percentage (63.70±0.18%) was obtained for the formulations with larger particle sizes and higher cholesterol content. The optimised niofenac formulation showed a controlled release fashion where 61.71±0.59% of the drug released within 24 h. The results showed that the value of permeated diclofenac sodium through the skin layers was higher for the niofenac gel formulation (242.3±31.11 µg/cm 2 ) compared to simple gel formulation (127.40±27.80 µg/cm 2 ). Besides, niofenac formulation outperformed the anti-inflammatory activities in the formalin test compared to the control and diclofenac simple gel group. The licking time was significantly lower in both early (40.2±7.3 s) and late stages (432.4±31.7 s) for niofenac compared to conventional formulation (early stage 130.4±8.73 s and late stage 660.6±123.73 s). This study indicates that niosomal formulations can improve drug therapeutic effects by increasing drug delivery to specific sites.

Polymers

Itraconazole (ITZ) is a triazole antifungal agent characterized by broad-spectrum activity against fungal infections. The main drawback of ITZ, when applied topically, is the low skin permeability due to the stratum corneum, the outermost layer of the skin, which represents the main barrier for drug penetration. Therefore, this study aimed to prepare itraconazole as transferosomes (ITZ-TFS) to overcome the barrier function of the skin. ITZ-TFSs were prepared by thin lipid film hydration technique using different surfactants, sodium lauryl sulfate (SLS) and sodium deoxycholate (SDC). The prepared ITZ-TFS were evaluated for entrapment efficiency (EE) %, particle size, polydispersity index (PDI), zeta potential, and in vitro drug release to obtain an optimized formula. The surface morphology of the optimized formula of ITZ-TFS was determined by transmission electron microscope (TEM). The optimized formulation was prepared in the form of gel using hydroxyl propyl methyl cellulose (HPMC)...

J Pharm Pharm Sci, 2002

Purpose: A niosome based transdermal drug delivery system of Nimesulide (NIM) was developed and extensively characterized and evaluated for in-vitro performance followed by in-vivo evaluation in rats by carrageenan induced rat paw edema method. Method: Niosomes were prepared by lipid film hydration technique using tweens and spans. Preparation of niosomes was optimized for highest percent drug entrapment (PDE). The prepared niosomes were incorporated into 1% carbopol gel base and the system was evaluated for drug diffusion across human cadaver skin (HCS) using modified validated diffusion cell. The drug retention studies in niosomes were performed at refrigerated temperature (2°C -8°C) and at room temperature (25°C±2°C) for the period of 2 months. In-vivo performance of plain drug gel, niosomallyentrapped drug in carbopol gel base and marketed formulation were evaluated using acute rat paw edema method. Results: Highest mean percentage edema inhibition (PEI) was observed for niosomal nimesulide gel after 24 hours i.e. 66.68%±5.19% compared to plain drug gel i.e. 12.57%±1.78% and marketed NIM formulation i.e. 20.49%±0.91%. Conclusion: Findings of this investigation conclusively demonstrate prolongation of drug release and increase in amount of drug retention into the skin and permeation across the skin after niosomal encapsulation of NIM. Developed nimesulide niosomal gel formulation has also demonstrated enhanced anti-inflammatory activity compared to plain drug gel and marketed formulation.

Journal of Microencapsulation, 2012

In this study, different positively charged niosomal formulations containing sorbitan esters, cholesterol and cetyl trimethyl ammonium bromide were prepared by film hydration method for the entrapment of autoclaved Leishmania major (ALM). Size distribution pattern and stability of niosomes were investigated by laser light scattering method and ALM encapsulation per cent was measured by the bicinchoninic acid method. Finally, the selected formulation was used for the induction of the immune response against cutaneous leishmaniasis in BALB/c mice. Size distribution curves of all the formulations followed a log-normal pattern and the mean volume diameter was in the range 7.57-15.80 mm. The mean volume diameters were significantly increased by adding Tween to Span formulations (p 5 0.05). The percentage of ALM entrapped in all formulations varied between 14.88% and 36.65%. In contrast to ALM, in vivo studies showed that the niosomes containing ALM have a moderate effect in the prevention of cutaneous leishmaniasis in BALB/c mice.