The objective of this study was to formulate a niosomal in situ gel of sertraline hydrochloride for the treatment of depression.Sertraline hydrochloride is a Biopharmaceutical Classification System class II drug with ...The objective of this study was to formulate a niosomal in situ gel of sertraline hydrochloride for the treatment of depression.Sertraline hydrochloride is a Biopharmaceutical Classification System class II drug with low solubility and high permeability.This research aims to improve the bioavailability of drugs by increasing their solubility by encapsulation in niosomal vesicles incorporated into an in situ gel.Niosomes were prepared via the ether injection method using a 3^(2)full factorial design.Sertraline hydrochloride in situ gel was prepared via the cold method by using Poloxamer 407 and PVP K 30.One factor was evaluated at 3 levels,and the concentrations of surfactant Span 60(X_(1))and of cholesterol(X_(2))were selected as independent variables.The F8 batch of niosomes out of 9 formulations was found to be optimized.The average vesicle size of the niosomal suspension in the optimized F8 batch was 167.5 nm,with a zeta potential of-31.4 mV.The entrapment efficiency across the 9 batches varied from 79.6%to 90.5%,while the drug content ranged between 91.2%and 98.5%.The entrapment efficiency and drug content of the optimized batch were 90.5%and 98.5%,respectively.In vitro drug release for these batches was between 86.32%and 91.33%.The in vitro drug release and ex vivo permeation rates of the optimized batch were 88.03%and 81.74%,respectively.Thus,the application of niosomes has proven potential for intranasal delivery of sertraline hydrochloride over conventional gel formulations,and intranasal drug delivery for sertraline hydrochloride has been successfully developed.展开更多
文摘The objective of this study was to formulate a niosomal in situ gel of sertraline hydrochloride for the treatment of depression.Sertraline hydrochloride is a Biopharmaceutical Classification System class II drug with low solubility and high permeability.This research aims to improve the bioavailability of drugs by increasing their solubility by encapsulation in niosomal vesicles incorporated into an in situ gel.Niosomes were prepared via the ether injection method using a 3^(2)full factorial design.Sertraline hydrochloride in situ gel was prepared via the cold method by using Poloxamer 407 and PVP K 30.One factor was evaluated at 3 levels,and the concentrations of surfactant Span 60(X_(1))and of cholesterol(X_(2))were selected as independent variables.The F8 batch of niosomes out of 9 formulations was found to be optimized.The average vesicle size of the niosomal suspension in the optimized F8 batch was 167.5 nm,with a zeta potential of-31.4 mV.The entrapment efficiency across the 9 batches varied from 79.6%to 90.5%,while the drug content ranged between 91.2%and 98.5%.The entrapment efficiency and drug content of the optimized batch were 90.5%and 98.5%,respectively.In vitro drug release for these batches was between 86.32%and 91.33%.The in vitro drug release and ex vivo permeation rates of the optimized batch were 88.03%and 81.74%,respectively.Thus,the application of niosomes has proven potential for intranasal delivery of sertraline hydrochloride over conventional gel formulations,and intranasal drug delivery for sertraline hydrochloride has been successfully developed.
