Design, Development and in Vitro Evaluation of Controlled Release Gel for Topical Delivery of Quetiapine Using Box- Behnken Design

The purpose of this work was to develop and characterize a vesicular drug carrier for topical delivery of Quetiapine to overcome the problems related with oral route that is high first pass metabolism and fluctuating drug plasma concentration. The effects of key formulation variables on entrapment efficiency (EE %), vesicle size and in vitro drug permeation were studied using a BoxBehnken design. Liposomes bearing Quetiapine were prepared by using saturated lipids like 1, 2-Dipalmitoyl-sn-glycero-3-phosphocholine (DPPC) and 1, 2-Distearoyl-sn-glycero-3-phosphocholine (DSPC) with relatively less stability problems through rotary evaporation method. The liposomal formulation was characterized for various parameters including EE %, vesicles shape, size distribution, lamellarity, in vitro release study, skin permeation and stability studies. Firstly liposomal suspension was prepared and then previously prepared suspension was incorporated in carbopol 940P gel with an objective of enhancing stability of liposome by avoiding aggregation of vesicles and for better skin permeation. The encapsulation efficiency of drug was found to be ranging from 60.59±4.54% to 83.56±2.97%. Nano liposomes were found to have mean particle size of 405.8±1.1 nm and zeta potential of −10.9±1.54 mV. The optimized liposomal gel showed the desired controlled release of drug uptil 12 h and J flux was also found to be higher than the plain gel of drug. The stability studies proved that both liposome suspension and gel were stable uptil 6 months. Finally, from the research work it could be concluded that the liposome accentuates the transdermal flux of Quetiapine and could be used as an effective carrier for transdermal delivery. INTRODUCTION: In last two decades, number of innovative microparticulate carrier systems viz. microemulsion, nanoemulsion, nanoparticles, liposomes, ethosomes etc. have been reported for improving delivery of drug to the skin. Yet in the dermatological field, liposomes were used initially because of their moisturizing and restoring action. Later their capability of enclosing many different biological materials and of delivering them to the epidermal cells or even deeper cell layers was investigated . Liposomes are enclosed spherical vesicles that are organized in one or several concentric phospholipid bilayers with an internal aqueous phase. After development liposomal technology has made considerable progress. Several important liposomal formulations for the treatment of different diseases are now available commercially or are in advanced Correspondence to Author: