Drug Delivery Research Unit, Department of Pharmaceutics, University of Nigeria, Nsukka, Enugu State, Nigeria
Audu, M.M., Drug Delivery Research Unit, Department of Pharmaceutics, University of Nigeria, Nsukka, Enugu State, Nigeria; Achile, P.A., Drug Delivery Research Unit, Department of Pharmaceutics, University of Nigeria, Nsukka, Enugu State, Nigeria; Amaechi, A.A., Drug Delivery Research Unit, Department of Pharmaceutics, University of Nigeria, Nsukka, Enugu State, Nigeria
To formulate and evaluate solid lipid microparticles (SLMs) intended for oral administration of ibuprofen. Ibuprofen-loaded solid lipid microparticles (SLMs) were prepared using hot emulsification method. Characterizations based on particles size and morphology, particles surface charges and stability and encapsulation efficiency (EE%) were carried out on the SLMs. In vitro release of Ibuprofen was performed in phosphate buffer while in vivo anti-inflammatory activity and GI sparing effect were carried out in rats. Maximum encapsulation efficiency (EE%) of 89±0.2, 84±0.1, and 93±0.4 for A1-A3, while 81±0.0, 84±0.3 and 94±0.1 were obtained for B1-B3, respectively. Stable, spherical and smooth SLMs of size range 21.1±0.2 μm to 34.2±1.4 μm were produced. The release of ibuprofen in phosphate buffer varied widely with the lipid contents. Moreover, significant (p<0.05) anti-inflammatory activity of 65.9, 55.9 and 85.2 % for A1-A3 and 51.3, 65.1, 72.1% for B1-B3 within 6 h respectively were observed. Maximum gastrointestinal (GI) protection of 98, 94, 72 and 71% were observed in batch A3, B3, A1and B1 as compared to 62, 69 and 10 % observed in A2, B2 and the conventional tablet. Thus, SLMsbased on P90G and Beeswax would likely offer a reliable means of delivering ibuprofen orally and prevent GI side effect. Copyright © 2012 Zoological Society of Pakistan.