Document Type

Conference Proceeding

Publication Date

7-2016

Abstract

Objectives: The aim of the present study was to examine the influence of the formulation and process variables on the entrapment efficiency of simvastatin-phospholipid complex (SPC), prepared with a goal of improving the solubility and permeability of simvastatin.

Method: The SPC was prepared using a solvent evaporation method. The influence of formulation and process variables on simvastatin entrapment was assessed using a central composite design. An additional SPC was prepared using the optimized variables from the developed quadratic model. This formulation was characterized for its physical-chemical properties. The functional attributes of the optimized SPC formulation were analyzed by apparent aqueous solubility analysis, in-vitro dissolution studies, dissolution efficiency analysis, and ex-vivo permeability studies.

Results: The factors studied were found to significantly influence on the entrapment efficiency. The developed model was validated using the optimized levels of formulation and process variables. The physical-chemical characterization confirmed a formation of the complex. The optimized SPC demonstrated over 25-fold higher aqueous solubility of simvastatin, compared to that of pure simvastatin. The optimized SPC exhibited a significantly higher rate and extent of simvastatin dissolution (>98%), compared to that of pure simvastatin (∼16%). The calculated dissolution efficiency was also found to be significantly higher for the SPC (∼54 %), compared to that of pure simvastatin (∼8%). Finally, the optimized SPC exhibited a significantly higher simvastatin permeability (>78%), compared to that of pure simvastatin (∼11%).

Implications: The present study shows that simvastatin-phospholipid complex can be a promising strategy for improving the delivery of simvastatin, and similar drugs with low aqueous solubility.

DOI

https://doi.org/10.5688/ajpe805S2

Comments

Presented at the American Association of Colleges of Pharmacy (AACP) Annual Meeting in Anaheim, California, July 23-27, 2016.

Abstract published in American Journal of Pharmaceutical Education, 2016; 80 (5) Article S2: https://www.ajpe.org/content/80/5/S2

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