Formulation of Heterolipid-Based Hollow Nanoparticles Improves the Physicochemical and Gastroprotective Properties of Cimetidine (Pages 1-15)

Chukwuebuka Umeyor1, Chioma Chike-Nwankwo1, Comfort Madueke1, Precious Orji1 and Anthony Attama2

1Nanomedicines and Drug Delivery Research Group, Department of Pharmaceutics and Pharmaceutical Technology, Faculty of Pharmaceutical Sciences, Nnamdi Azikiwe University, Awka 422001, Anambra State, Nigeria; 2Drug Delivery and Nanomedicines Research Group, Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, University of Nigeria, Nsukka 410001, Enugu State, Nigeria


Abstract: Purpose: The purpose of the present study is to improve the physicochemical and gastroprotective properties of the BCS class III drug, cimetidine using nanostructured lipid carriers (NLC); thus, improving the overall absorption and bioavailability of cimetidine.

Methods: Cimetidine-loaded NLCs were formulated by melt-fusion followed by high pressure homogenization (HPH) using rational blends of the solid lipids, Precirol® ATO5 and beeswax, and the liquid lipid, Kolliphor® ELP. In vitro physicochemical characterization (particle size, electric charge, polydispersity index, thermal analysis, particle optics, entrapment efficiency) and in vivo gastroprotective evaluations were carried out respectively.

Results: Cimetidine-loaded NLCs were stable (-31 to -37 mV), polydispersed (0.1 – 0.4) with particle sizes ranging from 113 – 153 nm. Thermal analysis confirmed that cimetidine was molecularly dispersed in the NLC due to low matrix crystallinity. In vitro release of cimetidine showed sustained release effect and entrapment efficiency (EE %) was concentration-dependent in the range of 85 – 96 %. There was improved gastric ulcer inhibition by the cimetidine-loaded nanoparticles.

Conclusion: The improved physicochemical and gastroprotective profiles obtained from the study suggest that NLC is a very promising delivery system for cimetidine.

Keywords: Cimetidine, Precirol®ATO5, Beeswax, Gastroprotective, Nanostructured lipid carrier.