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American Journal of Drug Discovery and Development
  Year: 2012 | Volume: 2 | Issue: 1 | Page No.: 1-16
DOI: 10.3923/ajdd.2012.1.16
 
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In vivo Evaluation and Application of Central Composite Design in the Optimization of Amisulpride Self-Emulsifying Drug Delivery System
Ahmed A. Aboelwafa and Amal I.A. Makhlouf

Abstract:
Amisulpride is practically insoluble in water and suffers from irregular and low bioavailability (48%). This could be due to low solubility and being a substrate for P-glycoprotein efflux. The aim of this study is to develop and statistically optimize Self-Emulsifying Drug Delivery System (SEDDS) formulation containing bio-enhancers and P-glycoprotein inhibitors components, for the improvement of dissolution and oral absorption of amisulpride; using Central Composite Rotatable Design (CCRD). Preliminary screening was carried out to determine amisulpride solubility in various oils and surfactants. Formulations were prepared using oil (Capryol-90®), two surfactants (Cremophor EL® and Labrasol®, “Smix”) and co-surfactant (Transcutol HP®). CCRD was applied for optimization. Oil percentage, Smix: co-surfactant ratio and Cremophor EL: Labrasol ratio in Smix, were selected as independent variables while mean droplet size, drug loading and light absorbance of diluted SEDDS as dependent variables. Second-order polynomial equations were fitted to data. Optimized formulation, containing 10% oil, 1.31 as Smix: co-surfactant ratio and 2 as ratio of Cremophor ®EL: Labrasol® in Smix was prepared according to software determined levels using desirability function and overlay plot. It provided drug loading of 50 mg mL-1 and released amisulpride completely within 15 min irrespective of type or pH of dissolution medium. Optimized SEDDS showed significant (p<0.01) increase in vivo bioavailability compared to drug suspension. CCRD could be considered as an efficient approach for the optimization of SEDDS. Also, the optimized SEDDS formulation demonstrated a great potential as a possible alternative to traditional oral formulations of amisulpride.
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How to cite this article:

Ahmed A. Aboelwafa and Amal I.A. Makhlouf, 2012. In vivo Evaluation and Application of Central Composite Design in the Optimization of Amisulpride Self-Emulsifying Drug Delivery System. American Journal of Drug Discovery and Development, 2: 1-16.

DOI: 10.3923/ajdd.2012.1.16

URL: https://scialert.net/abstract/?doi=ajdd.2012.1.16

 
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