DESIGN, DEVELOPMENT AND IN VITRO EVALUATION OF CONTROLLED RELEASE GEL FOR TOPICAL DELIVERY OF QUETIAPINE USING BOX- BEHNKEN DESIGNAbstract
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 Box- Behnken 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.
Hardik K. Patel*, Chandni V. Shah, Viral H. Shah and Umesh M. Upadhyay
Department of Pharmaceutics, Sigma institute of Pharmacy, Baroda, Gujarat, India
24 May, 2012
21 June, 2012
29 August, 2012
01 September, 2012