Evaluation of the pharmacodynamic properties of indomethacin-loaded lipospheres

Abstract

Obitte N. C., Chime S. A., Attama A. A., Odo J. I. and Brown S. A.

Indomethacin has been doomed for its gastrointestinal side effects. Therefore a formulation design to avert this may redeem the censorship on indomethacin. Hence the purpose of this study was to formulate robust lipospheres (LIPs) loaded with indomethacin with a view to ameliorating or precluding established adverse events associated with this ill-fated drug. Indomethacin-loaded LIPs were prepared by melt emulsification technique using a blend of natural lipid derived from Capra hircus and synthetic lipid, Phospholipon® 90G. The effect of sodium chloride, in vitro release studies, and encapsulation efficiency were evaluated on the indomethacin lipospheres (INDLIPs). Anti-inflammatory and ulcerogenic properties of a batch of INDLIPs were also studied on healthy, adult Wistar rats. Results showed that particle size ranged between 8.0 – 30 µm and significantly (p<0.05) increased with increasing drug load up to 1mg. Eighty five percent drug release took place within 40 min and sodium chloride did not have significant impact on drug release. The Encapsulation efficiency ranged from 36-57 %. Significant (p<0.05) anti-inflammatory activity and absence of gastric lesions were observed. In conclusion, the formulation carrier (liposphere) for indomethacin promoted improved anti-inflammation and fostered gastro-protection that precluded gastric lesions.

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