Effect of niosomes in the transdermal delivery of antidepressant sertraline hydrochloride

Abstract

Objective: Sertraline hydrochloride is an antidepressant that undergoes hepatic first pass effect upon oral administration. Controlled delivery for prolonged period across skin is one of the solutions to improve its therapeutic efficacy. Here, niosomes has been used as a carrier for the transdermal transport of sertraline HCl. Material and Method: Sertraline HCl Niosomes were prepared by ether injection method using surfactants such as span 40(A), span 60(B) and span 80(C) along with cholesterol at a ratio of 1:1. Four different concentrations (200:200(Aa), 250:250(Ab), 300:300(Ac) & 350:350(Ad)) of surfactant and cholesterol were used for each surfactant. The niosomes were characterized in vitro for size and surface morphology by means of particle size analyzer and scanning electron microscope (SEM) respectively. Encapsulation efficiency was determined by high performance liquid chromatography. Sertraline HCl release and skin permeation studies were carried out using franz diffusion cell. At last, the optimized formulation was subjected to physical stability studies. Results: The SEM and size distribution analysis evidenced the formation of discrete, spherical niosomes. Higher encapsulation efficiency of 53.71%±3.2%, 51.18%±2.5% and 51.92%±2.7% were obtained for Ad, Bb and Bc respectively. A maximum sertraline HCl release of 70%±2.6% was obtained for Ad which showed a permeation of 2.71%±0.157% across mouse skin. A calculated 50.2%±0.9% of sertraline HCl was assumed to get accumulated in the skin layers and the niosomes were physically stable. Conclusion: Sertraline HCl niosome showed a slow and prolonged release of sertraline HCl through the mouse skin and thus holds promise for transdermal delivery.