New Approach to Solid Lipid Microparticles USING Biocompatible Homolipids-Templated Heterolipid Micricarriers for Cimetidine Delivery

Abstract

Tallowation refers to the modification of lipid molecules using tallow fat while P90Gylation is the modification of lipid molecules by one or more phospholipid chains. Phospholipon® 90G (P90G) contains about 94.0 % of phosphatidylcholine stabilized with 0.1 % ascorbyl palmitate and is parenterally safe (GRAS) FDA approved excipient with wide application in drug delivery including surface modification of lipid particles (templation). P90Gylated-goat fat conjugate has numerous advantages: wetting, solubilisation, drug stabilization, emulsification and modified release. Here we report an evaluation of solid lipid microparticles (SLMs) formulated from this system and compared the effect of tallowation of the P90Gylated-goat fat matrices as an alternative microcarrier system for oral cimetidine administration in ulcerated rats. The results of this study showed that the templated homolipid mixtures had more spaces in them that entrapped cimetidine than P90Gylated-goat fat conjugate alone. Outstanding amongst them were the tallowated P90Gylated-goat fat matrices generated from 1:1 admixture of goat and tallow fats which showed 45.37 % encapsulation efficiency and the 2:1 templated matrix which exhibited the highest ulcer inhibition of 81.20 % superseding that of CEMTAB® which maximally inhibited ulcer at 72.50 %.

Keywords: Solid lipid microparticles, homolipids, heterolipid, P90Gylation, tallowation, goat fat, cimetidine

Nigerian Journal of Pharmaceutical ResearchVol. 8 No 1 pp. 92 - 111 (September 2010)