A B S T R A C T We are introducing design, development and preliminary feasibility study of nanoc... more A B S T R A C T We are introducing design, development and preliminary feasibility study of nanocomposites (made of Food and drug administration approved layered montmorillonite (Mt) and biodegradable polymer Poly lactic-co-glycolic acid (PLGA)), as a vehicle for oral administration of insulin. A systematic study on the variation of Mt-PLGA ratio was focused to reduce particles to the submicron size range while maintaining insulin's bioactivity. The synthesized Insulin-Mt-PLGA nanocomposites were successfully characterized with various techniques and compared with the Insulin-PLGA nanoparticles for their drug content, physico-chemical properties, in-vitro insulin release profile and cytotoxicity. High encapsulation efficiency, desirable particle size, prolonged gastric residence time, extended release of insulin in simulated gastrointestinal fluid and biocompatibility indicated the effectiveness of presence of Mt in the synthesized Mt-PLGA nanocomposites for the oral delivery of insulin. Thus, on the basis of our preliminary research findings, it could be concluded that the developed biocompatible Insulin-Mt-PLGA nanocomposites with double functionality of low pH stability and mucoadhesivity may offers promise to overcome the difficulties associated with the oral drug delivery of insulin.
Atenolol (ATN) is a widely prescribed drug for the treatment of hypertension. Due to short biolog... more Atenolol (ATN) is a widely prescribed drug for the treatment of hypertension. Due to short biological half life, low oral bioavailability and poor absorption fromthe lower gastrointestinal tract, high doses are required to maintain its therapeutic level in the blood plasma which has undesirable side effects. It seems that an increase in gastric residence time may increase the extent of absorption and bioavailability of the ATN. Therefore, to overcome the drawbacks associated with conventional oral delivery of ATN, a new drug delivery vehicle is required. The purpose of the present research was to develop montmorillonite (Mt)-poly lactic-co-glycolic acid (PLGA) nanocomposites as sustained release oral delivery vehicle for ATN. The Mt–PLGA nanocompositeswere prepared by w/o/w double emulsion solvent evaporation method by varying the ATN toMt ratio at three levels using Pluronic F68 and PLGA as stabilizing agent and matrix material respectively. Effects of these compositions on interlayer spacing of Mt–PLGA nanocomposites, particle size, morphology and in vitro drug release were evaluated. The in vitro release behavior of ATN from Mt–ATN–PLGA nanocomposites was found to be pH dependent and sustained as compared to ATN–PLGA nanoparticles, pure ATN and commercial formulation of Atenolol “ATEN- 25” over a period of 24 h. The developed clay polymer nanocomposites (CPN) showpromising ability to prolong the gastric residence time of ATN and suggest the possibility of designing the sustained release formulations with improved bioavailability and patient compliance.
In the present study, a naturally occurring clay mineral, Montmorillonite, (Mt) has been explored... more In the present study, a naturally occurring clay mineral, Montmorillonite, (Mt) has been explored as a carrier for an antihypertensive drug, atenolol. The effect of pH, time and initial drug concentration on drug loading capacity of Mt has been evaluated. The adsorption isotherm was fitted by the Langmuir model and follows the pseudo-second-order kinetics. The synthesized Mt-atenolol complexes were characterized by XRD, FTIR, TGA, DSC etc. XRD data indicates the intercalation of atenolol within the Mt layers. The release profile of the atenolol from Mt-atenolol complexes is compared with the pure atenolol, in simulated gastric and intestinal fluids. The release behaviour of atenolol from Mt-atenolol complexes appears to be in sustained manner over a period of 24 hours and reaches upto 40% and 27% in simulated gastric and intestinal fluids respectively. As compared to pure atenolol, extended gastric retention time was observed for Mt-atenolol complexes indicative of the increased extent of absorption and bioavailability of the drug. Various kinetic models were used to elucidate the drug release mechanism, the best fitting was found for Higuchi and Korsmeyer-Peppas model. The synthesized Mt-atenolol complexes have the potential for developing in to a sustained release formulation for oral drug delivery. Thus, proposing a promising formulation for oral sustained drug delivery of atenolol.
Objective of the present study is to develop MMT based PLGA nanocomposites of oral and controlled... more Objective of the present study is to develop MMT based PLGA nanocomposites of oral and controlled release carrier of 5-Fluorouracil. Double emulsion solvent evaporation method was used for nanocomposite synthesis and effect of medical clay MMT on encapsulation efficiency has been evaluated. The synthesized 5FU-PLGA-MMT nanocomposites were compared with respect to morphology, particle size, physical status of 5FU and MMT, and in vitro drug release to the corresponding biodegradable PLGA nanoparticles. Intercalation of polymer-drug moiety within the MMT layers has been supported by XRD data. Particle size of synthesized nanocomposites was found in the range of 100-200 nm, a favorable size for cellular uptake. In vitro drug release profiles of 5FU-PLGA-MMT nanocomposites in simulated gastrointestinal fluid, indicates a controlled release of 5-Fluorouracil as compared to 5FU-PLGA nanoparticles and pure 5FU for a period of 8 hours.
Short half life of propranolol hydrochloride (PPN), an antihypertensive drug is a prime requireme... more Short half life of propranolol hydrochloride (PPN), an antihypertensive drug is a prime requirement to develop a formulation which could sustain the release of PPN in the human body and also eliminate daily multiple dosage of propranolol. In this study organoclay Pluronic F68 modified montmorillonite (Mt) has been explored as a sustained release carrier for oral delivery of PPN. The developed organoclay PF68-Mt was compared for adsorption capacity of PPN with pristine Mt. A detailed and systematic study to evaluate the effect of pH, time and initial PPN concentration on drug loading capacity of organoclay PF68-Mt and pristine Mt has been evaluated. The synthesized PF68-Mt-PPN composites were characterized by XRD, FTIR, TGA techniques. XRD studies suggested the intercalation of PPN within the pristine Mt and organoclay PF68 -Mt. In vitro drug release profile of PPN from organoclay PF68-Mt composites is compared with that of pristine Mt and the pure PPN, in simulated gastric and intestinal fluids. The release profile of loaded PPN in organoclay PF68-Mt shows pH dependent release in simulated gastrointestinal fluid. The release behaviour of PPN from PF68-Mt-PPN composites was appeared to be in more sustained manner than prisine Mt and pure PPN over a period of 24 hours. This study suggests that the modification of Mt with a non ionic tri block co polymer Pluronic F68 provides better controlled on the release of PPN as compared to pristine Mt and pure drug. The obtained PF68-Mt-PPN composites with high drug loading capacity and sustained drug release characteristics supposed to be a better oral drug delivery system, for a highly hydrophilic low molecular weight antihypertensive drug PPN. The PF68-Mt-PPN composites developed have the potential to minimize the drug dosing frequency and hence improving the patient compliance. Thus, proposing a new promising formulation for oral sustained release drug delivery.
Short half life of Propranolol Hydrochloride (PPN), an antihypertensive drug is a prime requireme... more Short half life of Propranolol Hydrochloride (PPN), an antihypertensive drug is a prime requirement to develop a formulation which could extend the release of PPN in the human body and also eliminate daily multiple dosage of PPN. In this study, a system of PPN loaded Montmorillonite-Poly lactic-co-glycolic acid (Mt-PLGA) nanocomposites has been developed. PPN incorporated PLGA nanoparticles have been compared with Mt-PPN-PLGA nanocomposites. Mt was used as sustained release carrier for PPN with addition of biodegradable polymer PLGA by preparing Mt-PPN-PLGA nanocomposites by double emulsion solvent evaporation method. The drug encapsulation efficiency and drug loading capacity of synthesized products were estimated with HPLC including suitable analytical techniques to confirm the formation of clay-polymer nanocomposites (CPN). The release profile of encapsulated PPN in CPN shows pH dependent release in simulated gastrointestinal fluid for a period of 8 h. This study suggests that the methodologies used are suitable for the synthesis of Mt based PLGA nanocomposites with high drug encapsulation efficiency and controlled drug release characteristics and indicates that the Mt-PPN-PLGA nanocomposites are supposed to be better oral controlled drug delivery system, for a highly hydrophilic low molecular weight antihypertensive drug PPN to minimize the drug dosing frequency and hence improving the patient compliance.
Objective of the present study is to develop MMT based PLGA nanocomposites of oral and controlled... more Objective of the present study is to develop MMT based PLGA nanocomposites of oral and controlled release carrier of 5-Fluorouracil. Double emulsion solvent evaporation method was used for nanocomposite synthesis and effect of medical clay MMT on encapsulation efficiency has been evaluated. The synthesized 5FU-PLGA-MMT nanocomposites were compared with respect to morphology, particle size, physical status of 5FU and MMT, and in vitro drug release to the corresponding biodegradable PLGA nanoparticles. Intercalation of polymer-drug moiety within the MMT layers has been supported by XRD data. Particle size of synthesized nanocomposites was found in the range of 100-200 nm, a favorable size for cellular uptake. In vitro drug release profiles of 5FU-PLGA-MMT nanocomposites in simulated gastrointestinal fluid, indicates a controlled release of 5-Fluorouracil as compared to 5FU-PLGA nanoparticles and pure 5FU for a period of 8 hours.
Short half life of propranolol hydrochloride (PPN), an antihypertensive drug is a prime requireme... more Short half life of propranolol hydrochloride (PPN), an antihypertensive drug is a prime requirement to develop a formulation which could sustain the release of PPN in the human body and also eliminate daily multiple dosage of propranolol. In this study organoclay Pluronic F68 modified montmorillonite (Mt) has been explored as a sustained release carrier for oral delivery of PPN. The developed organoclay PF68-Mt was compared for adsorption capacity of PPN with pristine Mt. A detailed and systematic study to evaluate the effect of pH, time and initial PPN concentration on drug loading capacity of organoclay PF68-Mt and pristine Mt has been evaluated. The synthesized PF68-Mt-PPN composites were characterized by XRD, FTIR, TGA techniques. XRD studies suggested the intercalation of PPN within the pristine Mt and organoclay PF68 -Mt. In vitro drug release profile of PPN from organoclay PF68-Mt composites is compared with that of pristine Mt and the pure PPN, in simulated gastric and intestinal fluids. The release profile of loaded PPN in organoclay PF68-Mt shows pH dependent release in simulated gastrointestinal fluid. The release behaviour of PPN from PF68-Mt-PPN composites was appeared to be in more sustained manner than prisine Mt and pure PPN over a period of 24 hours. This study suggests that the modification of Mt with a non ionic tri block co polymer Pluronic F68 provides better controlled on the release of PPN as compared to pristine Mt and pure drug. The obtained PF68-Mt-PPN composites with high drug loading capacity and sustained drug release characteristics supposed to be a better oral drug delivery system, for a highly hydrophilic low molecular weight antihypertensive drug PPN. The PF68-Mt-PPN composites developed have the potential to minimize the drug dosing frequency and hence improving the patient compliance. Thus, proposing a new promising formulation for oral sustained release drug delivery.
In the present study, a naturally occurring clay mineral, Montmorillonite, (Mt) has been explored... more In the present study, a naturally occurring clay mineral, Montmorillonite, (Mt) has been explored as a carrier for an antihypertensive drug, atenolol. The effect of pH, time and initial drug concentration on drug loading capacity of Mt has been evaluated. The adsorption isotherm was fitted by the Langmuir model and follows the pseudo-second-order kinetics. The synthesized Mt-atenolol complexes were characterized by XRD, FTIR, TGA, DSC etc. XRD data indicates the intercalation of atenolol within the Mt layers. The release profile of the atenolol from Mt-atenolol complexes is compared with the pure atenolol, in simulated gastric and intestinal fluids. The release behaviour of atenolol from Mt-atenolol complexes appears to be in sustained manner over a period of 24 hours and reaches upto 40% and 27% in simulated gastric and intestinal fluids respectively. As compared to pure atenolol, extended gastric retention time was observed for Mt-atenolol complexes indicative of the increased extent of absorption and bioavailability of the drug. Various kinetic models were used to elucidate the drug release mechanism, the best fitting was found for Higuchi and Korsmeyer-Peppas model. The synthesized Mt-atenolol complexes have the potential for developing in to a sustained release formulation for oral drug delivery. Thus, proposing a promising formulation for oral sustained drug delivery of atenolol.
A B S T R A C T We are introducing design, development and preliminary feasibility study of nanoc... more A B S T R A C T We are introducing design, development and preliminary feasibility study of nanocomposites (made of Food and drug administration approved layered montmorillonite (Mt) and biodegradable polymer Poly lactic-co-glycolic acid (PLGA)), as a vehicle for oral administration of insulin. A systematic study on the variation of Mt-PLGA ratio was focused to reduce particles to the submicron size range while maintaining insulin's bioactivity. The synthesized Insulin-Mt-PLGA nanocomposites were successfully characterized with various techniques and compared with the Insulin-PLGA nanoparticles for their drug content, physico-chemical properties, in-vitro insulin release profile and cytotoxicity. High encapsulation efficiency, desirable particle size, prolonged gastric residence time, extended release of insulin in simulated gastrointestinal fluid and biocompatibility indicated the effectiveness of presence of Mt in the synthesized Mt-PLGA nanocomposites for the oral delivery of insulin. Thus, on the basis of our preliminary research findings, it could be concluded that the developed biocompatible Insulin-Mt-PLGA nanocomposites with double functionality of low pH stability and mucoadhesivity may offers promise to overcome the difficulties associated with the oral drug delivery of insulin.
Atenolol (ATN) is a widely prescribed drug for the treatment of hypertension. Due to short biolog... more Atenolol (ATN) is a widely prescribed drug for the treatment of hypertension. Due to short biological half life, low oral bioavailability and poor absorption fromthe lower gastrointestinal tract, high doses are required to maintain its therapeutic level in the blood plasma which has undesirable side effects. It seems that an increase in gastric residence time may increase the extent of absorption and bioavailability of the ATN. Therefore, to overcome the drawbacks associated with conventional oral delivery of ATN, a new drug delivery vehicle is required. The purpose of the present research was to develop montmorillonite (Mt)-poly lactic-co-glycolic acid (PLGA) nanocomposites as sustained release oral delivery vehicle for ATN. The Mt–PLGA nanocompositeswere prepared by w/o/w double emulsion solvent evaporation method by varying the ATN toMt ratio at three levels using Pluronic F68 and PLGA as stabilizing agent and matrix material respectively. Effects of these compositions on interlayer spacing of Mt–PLGA nanocomposites, particle size, morphology and in vitro drug release were evaluated. The in vitro release behavior of ATN from Mt–ATN–PLGA nanocomposites was found to be pH dependent and sustained as compared to ATN–PLGA nanoparticles, pure ATN and commercial formulation of Atenolol “ATEN- 25” over a period of 24 h. The developed clay polymer nanocomposites (CPN) showpromising ability to prolong the gastric residence time of ATN and suggest the possibility of designing the sustained release formulations with improved bioavailability and patient compliance.
In the present study, a naturally occurring clay mineral, Montmorillonite, (Mt) has been explored... more In the present study, a naturally occurring clay mineral, Montmorillonite, (Mt) has been explored as a carrier for an antihypertensive drug, atenolol. The effect of pH, time and initial drug concentration on drug loading capacity of Mt has been evaluated. The adsorption isotherm was fitted by the Langmuir model and follows the pseudo-second-order kinetics. The synthesized Mt-atenolol complexes were characterized by XRD, FTIR, TGA, DSC etc. XRD data indicates the intercalation of atenolol within the Mt layers. The release profile of the atenolol from Mt-atenolol complexes is compared with the pure atenolol, in simulated gastric and intestinal fluids. The release behaviour of atenolol from Mt-atenolol complexes appears to be in sustained manner over a period of 24 hours and reaches upto 40% and 27% in simulated gastric and intestinal fluids respectively. As compared to pure atenolol, extended gastric retention time was observed for Mt-atenolol complexes indicative of the increased extent of absorption and bioavailability of the drug. Various kinetic models were used to elucidate the drug release mechanism, the best fitting was found for Higuchi and Korsmeyer-Peppas model. The synthesized Mt-atenolol complexes have the potential for developing in to a sustained release formulation for oral drug delivery. Thus, proposing a promising formulation for oral sustained drug delivery of atenolol.
Objective of the present study is to develop MMT based PLGA nanocomposites of oral and controlled... more Objective of the present study is to develop MMT based PLGA nanocomposites of oral and controlled release carrier of 5-Fluorouracil. Double emulsion solvent evaporation method was used for nanocomposite synthesis and effect of medical clay MMT on encapsulation efficiency has been evaluated. The synthesized 5FU-PLGA-MMT nanocomposites were compared with respect to morphology, particle size, physical status of 5FU and MMT, and in vitro drug release to the corresponding biodegradable PLGA nanoparticles. Intercalation of polymer-drug moiety within the MMT layers has been supported by XRD data. Particle size of synthesized nanocomposites was found in the range of 100-200 nm, a favorable size for cellular uptake. In vitro drug release profiles of 5FU-PLGA-MMT nanocomposites in simulated gastrointestinal fluid, indicates a controlled release of 5-Fluorouracil as compared to 5FU-PLGA nanoparticles and pure 5FU for a period of 8 hours.
Short half life of propranolol hydrochloride (PPN), an antihypertensive drug is a prime requireme... more Short half life of propranolol hydrochloride (PPN), an antihypertensive drug is a prime requirement to develop a formulation which could sustain the release of PPN in the human body and also eliminate daily multiple dosage of propranolol. In this study organoclay Pluronic F68 modified montmorillonite (Mt) has been explored as a sustained release carrier for oral delivery of PPN. The developed organoclay PF68-Mt was compared for adsorption capacity of PPN with pristine Mt. A detailed and systematic study to evaluate the effect of pH, time and initial PPN concentration on drug loading capacity of organoclay PF68-Mt and pristine Mt has been evaluated. The synthesized PF68-Mt-PPN composites were characterized by XRD, FTIR, TGA techniques. XRD studies suggested the intercalation of PPN within the pristine Mt and organoclay PF68 -Mt. In vitro drug release profile of PPN from organoclay PF68-Mt composites is compared with that of pristine Mt and the pure PPN, in simulated gastric and intestinal fluids. The release profile of loaded PPN in organoclay PF68-Mt shows pH dependent release in simulated gastrointestinal fluid. The release behaviour of PPN from PF68-Mt-PPN composites was appeared to be in more sustained manner than prisine Mt and pure PPN over a period of 24 hours. This study suggests that the modification of Mt with a non ionic tri block co polymer Pluronic F68 provides better controlled on the release of PPN as compared to pristine Mt and pure drug. The obtained PF68-Mt-PPN composites with high drug loading capacity and sustained drug release characteristics supposed to be a better oral drug delivery system, for a highly hydrophilic low molecular weight antihypertensive drug PPN. The PF68-Mt-PPN composites developed have the potential to minimize the drug dosing frequency and hence improving the patient compliance. Thus, proposing a new promising formulation for oral sustained release drug delivery.
Short half life of Propranolol Hydrochloride (PPN), an antihypertensive drug is a prime requireme... more Short half life of Propranolol Hydrochloride (PPN), an antihypertensive drug is a prime requirement to develop a formulation which could extend the release of PPN in the human body and also eliminate daily multiple dosage of PPN. In this study, a system of PPN loaded Montmorillonite-Poly lactic-co-glycolic acid (Mt-PLGA) nanocomposites has been developed. PPN incorporated PLGA nanoparticles have been compared with Mt-PPN-PLGA nanocomposites. Mt was used as sustained release carrier for PPN with addition of biodegradable polymer PLGA by preparing Mt-PPN-PLGA nanocomposites by double emulsion solvent evaporation method. The drug encapsulation efficiency and drug loading capacity of synthesized products were estimated with HPLC including suitable analytical techniques to confirm the formation of clay-polymer nanocomposites (CPN). The release profile of encapsulated PPN in CPN shows pH dependent release in simulated gastrointestinal fluid for a period of 8 h. This study suggests that the methodologies used are suitable for the synthesis of Mt based PLGA nanocomposites with high drug encapsulation efficiency and controlled drug release characteristics and indicates that the Mt-PPN-PLGA nanocomposites are supposed to be better oral controlled drug delivery system, for a highly hydrophilic low molecular weight antihypertensive drug PPN to minimize the drug dosing frequency and hence improving the patient compliance.
Objective of the present study is to develop MMT based PLGA nanocomposites of oral and controlled... more Objective of the present study is to develop MMT based PLGA nanocomposites of oral and controlled release carrier of 5-Fluorouracil. Double emulsion solvent evaporation method was used for nanocomposite synthesis and effect of medical clay MMT on encapsulation efficiency has been evaluated. The synthesized 5FU-PLGA-MMT nanocomposites were compared with respect to morphology, particle size, physical status of 5FU and MMT, and in vitro drug release to the corresponding biodegradable PLGA nanoparticles. Intercalation of polymer-drug moiety within the MMT layers has been supported by XRD data. Particle size of synthesized nanocomposites was found in the range of 100-200 nm, a favorable size for cellular uptake. In vitro drug release profiles of 5FU-PLGA-MMT nanocomposites in simulated gastrointestinal fluid, indicates a controlled release of 5-Fluorouracil as compared to 5FU-PLGA nanoparticles and pure 5FU for a period of 8 hours.
Short half life of propranolol hydrochloride (PPN), an antihypertensive drug is a prime requireme... more Short half life of propranolol hydrochloride (PPN), an antihypertensive drug is a prime requirement to develop a formulation which could sustain the release of PPN in the human body and also eliminate daily multiple dosage of propranolol. In this study organoclay Pluronic F68 modified montmorillonite (Mt) has been explored as a sustained release carrier for oral delivery of PPN. The developed organoclay PF68-Mt was compared for adsorption capacity of PPN with pristine Mt. A detailed and systematic study to evaluate the effect of pH, time and initial PPN concentration on drug loading capacity of organoclay PF68-Mt and pristine Mt has been evaluated. The synthesized PF68-Mt-PPN composites were characterized by XRD, FTIR, TGA techniques. XRD studies suggested the intercalation of PPN within the pristine Mt and organoclay PF68 -Mt. In vitro drug release profile of PPN from organoclay PF68-Mt composites is compared with that of pristine Mt and the pure PPN, in simulated gastric and intestinal fluids. The release profile of loaded PPN in organoclay PF68-Mt shows pH dependent release in simulated gastrointestinal fluid. The release behaviour of PPN from PF68-Mt-PPN composites was appeared to be in more sustained manner than prisine Mt and pure PPN over a period of 24 hours. This study suggests that the modification of Mt with a non ionic tri block co polymer Pluronic F68 provides better controlled on the release of PPN as compared to pristine Mt and pure drug. The obtained PF68-Mt-PPN composites with high drug loading capacity and sustained drug release characteristics supposed to be a better oral drug delivery system, for a highly hydrophilic low molecular weight antihypertensive drug PPN. The PF68-Mt-PPN composites developed have the potential to minimize the drug dosing frequency and hence improving the patient compliance. Thus, proposing a new promising formulation for oral sustained release drug delivery.
In the present study, a naturally occurring clay mineral, Montmorillonite, (Mt) has been explored... more In the present study, a naturally occurring clay mineral, Montmorillonite, (Mt) has been explored as a carrier for an antihypertensive drug, atenolol. The effect of pH, time and initial drug concentration on drug loading capacity of Mt has been evaluated. The adsorption isotherm was fitted by the Langmuir model and follows the pseudo-second-order kinetics. The synthesized Mt-atenolol complexes were characterized by XRD, FTIR, TGA, DSC etc. XRD data indicates the intercalation of atenolol within the Mt layers. The release profile of the atenolol from Mt-atenolol complexes is compared with the pure atenolol, in simulated gastric and intestinal fluids. The release behaviour of atenolol from Mt-atenolol complexes appears to be in sustained manner over a period of 24 hours and reaches upto 40% and 27% in simulated gastric and intestinal fluids respectively. As compared to pure atenolol, extended gastric retention time was observed for Mt-atenolol complexes indicative of the increased extent of absorption and bioavailability of the drug. Various kinetic models were used to elucidate the drug release mechanism, the best fitting was found for Higuchi and Korsmeyer-Peppas model. The synthesized Mt-atenolol complexes have the potential for developing in to a sustained release formulation for oral drug delivery. Thus, proposing a promising formulation for oral sustained drug delivery of atenolol.
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oral bioavailability and poor absorption fromthe lower gastrointestinal tract, high doses are required to maintain
its therapeutic level in the blood plasma which has undesirable side effects. It seems that an increase in gastric
residence time may increase the extent of absorption and bioavailability of the ATN.
Therefore, to overcome the drawbacks associated with conventional oral delivery of ATN, a new drug delivery
vehicle is required.
The purpose of the present research was to develop montmorillonite (Mt)-poly lactic-co-glycolic acid (PLGA)
nanocomposites as sustained release oral delivery vehicle for ATN. The Mt–PLGA nanocompositeswere prepared
by w/o/w double emulsion solvent evaporation method by varying the ATN toMt ratio at three levels using Pluronic
F68 and PLGA as stabilizing agent and matrix material respectively. Effects of these compositions on interlayer spacing
of Mt–PLGA nanocomposites, particle size, morphology and in vitro drug release were evaluated.
The in vitro release behavior of ATN from Mt–ATN–PLGA nanocomposites was found to be pH dependent and
sustained as compared to ATN–PLGA nanoparticles, pure ATN and commercial formulation of Atenolol “ATEN-
25” over a period of 24 h.
The developed clay polymer nanocomposites (CPN) showpromising ability to prolong the gastric residence time
of ATN and suggest the possibility of designing the sustained release formulations with improved bioavailability
and patient compliance.
oral bioavailability and poor absorption fromthe lower gastrointestinal tract, high doses are required to maintain
its therapeutic level in the blood plasma which has undesirable side effects. It seems that an increase in gastric
residence time may increase the extent of absorption and bioavailability of the ATN.
Therefore, to overcome the drawbacks associated with conventional oral delivery of ATN, a new drug delivery
vehicle is required.
The purpose of the present research was to develop montmorillonite (Mt)-poly lactic-co-glycolic acid (PLGA)
nanocomposites as sustained release oral delivery vehicle for ATN. The Mt–PLGA nanocompositeswere prepared
by w/o/w double emulsion solvent evaporation method by varying the ATN toMt ratio at three levels using Pluronic
F68 and PLGA as stabilizing agent and matrix material respectively. Effects of these compositions on interlayer spacing
of Mt–PLGA nanocomposites, particle size, morphology and in vitro drug release were evaluated.
The in vitro release behavior of ATN from Mt–ATN–PLGA nanocomposites was found to be pH dependent and
sustained as compared to ATN–PLGA nanoparticles, pure ATN and commercial formulation of Atenolol “ATEN-
25” over a period of 24 h.
The developed clay polymer nanocomposites (CPN) showpromising ability to prolong the gastric residence time
of ATN and suggest the possibility of designing the sustained release formulations with improved bioavailability
and patient compliance.