Subscribe Now Subscribe Today
Science Alert
 
FOLLOW US:     Facebook     Twitter
Blue
   
Curve Top
American Journal of Drug Discovery and Development
  Year: 2012 | Volume: 2 | Issue: 1 | Page No.: 1-16
DOI: 10.3923/ajdd.2012.1.16
 
Facebook Twitter Digg Reddit Linkedin StumbleUpon E-mail
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.
PDF Fulltext XML References Citation Report Citation
 RELATED ARTICLES:
  •    Optimization of Process Variables for the Batch Degradation of Phenol by Pseudomonas fluorescence Using Response Surface Methodology
  •    The Factors Affecting the Extraction Condition for Neuroprotective Activity of Centella asiatica Evaluated by Metal Chelating Activity Assay
  •    Optimization of Medium Constituents for the Production of Fructosyltransferase (Ftase) by Bacillus subtilis Using Response Surface Methodology
  •    Characterization and Stability Testing of Itraconazole Solid Dispersions Containing Crystallization Inhibitors
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
 
COMMENT ON THIS PAPER
 
 
 

 
  Navigation
 
  Online First
  Current Issue
  Previous Issues
  Editorial Board
  Submit a Manuscript
  Guide to Authors
  Subscribe to E-alerts

  Indexed In
 
  ASCI-Database
  Asian Digital Library
  Chemical Abstract Services

       

       

Science Alert
Curve Bottom