Phospholipon 90G based SLMs loaded with ibuprofen: An oral anti-inflammatory and gastrointestinal sparing evaluation in rats

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 stabili...

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Bibliographic Details
Published in:Pakistan journal of zoology 2012-12, Vol.44 (6), p.1657-1664
Main Authors: Audu, M.M. (University of Nigeria, Enugu State (Nigeria). Dept. of Pharmaceutics), Achile, P.A. (University of Nigeria, Enugu State (Nigeria). Dept. of Pharmaceutics), Amaechi, A.A. (University of Nigeria, Enugu State (Nigeria). Dept. of Pharmaceutics)
Format: Article
Language:English
Subjects:
ANTIINFLAMMATORY AGENTS
DIGESTIVE SYSTEM
DRUGS
ENCAPSULATION
Indexing in process
LABORATORY ANIMALS
LIPIDS
ORAL ADMINISTRATION
RATS
SIDE EFFECTS
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Summary: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 plus minus 0.2, 84 plus minus 0.1, and 93 plus minus 0.4 for A1-A3, while 81 plus minus 0.0, 84 plus minus 0.3 and 94 plus minus 0.1 were obtained for B1-B3, respectively. Stable, spherical and smooth SLMs of size range 21.1 plus minus 0.2 mum to 34.2 plus minus 1.4 mum were produced. The release of ibuprofen in phosphate buffer varied widely with the lipid contents. Moreover, significant (p less than 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, SLMs-based on P90G and Beeswax would likely offer a reliable means of delivering ibuprofen orally and prevent GI side effect.
ISSN:0030-9923