Obitte N.C., Chukwu A., Onyishi V.I., Obitte B.C.N.
Dept of Pharmaceutical Technology and Industrial Pharmacy, Faculty of Pharmaceutical Sciences, University of Nigeria, Nsukka, Nigeria; Dept of Science Technology, Federal Polytechnic Offa, Kwara State, Nigeria
Obitte, N.C., Dept of Pharmaceutical Technology and Industrial Pharmacy, Faculty of Pharmaceutical Sciences, University of Nigeria, Nsukka, Nigeria; Chukwu, A., Dept of Pharmaceutical Technology and Industrial Pharmacy, Faculty of Pharmaceutical Sciences, University of Nigeria, Nsukka, Nigeria; Onyishi, V.I., Dept of Pharmaceutical Technology and Industrial Pharmacy, Faculty of Pharmaceutical Sciences, University of Nigeria, Nsukka, Nigeria; Obitte, B.C.N., Dept of Science Technology, Federal Polytechnic Offa, Kwara State, Nigeria
The need to address the problematic gastric irritation side effects and inconsistent bioavailability of most poorly soluble drugs has drawn the attention of researchers to self emulsifying drug delivery system as one of the possible solutions to these problems. Secondly self emulsifying oil formulations good as they may be could be associated with leakage from their hard gelatin capsules. This further motivated the introduction of gelling agents to address this problem. The objective of this work was to investigate some preliminary properties of Landolphia owariensis latex, including its applicability as a release modulating agent when admixed with Carbosil®, a gelling agent in Ibuprofen-loaded Palm Kernel oil (PKO)-based self-emulsifying oil formulations (SEOFs). Purification and precipitation were carried out on the oil and the latex respectively. Some physicochemical properties of the latex were also determined. SEOFs were formulated using varying concentrations of PKO, Tween 80 and Span 85 and thereafter tested for isotropicity. Drug-loaded SEOFs with or without Landolphia owariensis latex (LOL) and Carbosil-LOL admixture respectively were evaluated for stability, emulsification time, drug release, aqueous dilution, freeze thaw and drug precipitation tests. Results showed that LOL contained some phytocostituents, had a reasonable adhesive strength, and could retard aqueous permeation. Three out of nine batches of the SEOFs passed the isotropicity test, witnessed no phase separation when emulsified and diluted, and could resist drug precipitation after dilution. LOL did not at all delay drug release from SEOFs unlike LOL-Carbosil admixture. LOL-Carbosil admixture significantly (p<0.05) reduced emulsification time. There was no consistent trend in the dynamic viscosity result. Stability of the SEOFs was maintained at refrigeration temperature of 2°C. The above results indicated that LOL, an oil-soluble latex possesses excipient usefulness when incorporated into SEOFs and can therefore be used to modulate the drug retarding effect of Carbosil in their SEOF formulations while retaining Carbosil's gelling property. Industrial relevance: The major challenge confronting the biopharmaceutical properties of some nonsteroidal antiinflammatory drugs and poorly water soluble drugs include gastric irritation and poor GIT solubility/unpredictable bioavailability respectively. Self-emulsifying oil formulation is a lipid-based drug delivery system that addresses the above two challenges by fine globule-drug entrapment/solubilisation. In the GIT the o/w emulsion formed fortifies the drug enough for avoidance of direct drug-mucosal surface irritation and/or erosion and better absorption profile cum consistent bioavailability. The industrial translation of SEOF is very easy; this is because it involves very minimal and affordable machinability, devoid of complicated methodologies and tedious granulation/tableting procedures. Besides the oil component is very available, safe and inexpensive. The inclusion of carbosil® will gel the SEOF against capsular leakage while LOL latex will reduce the sustained drug release effect of Carbosil® especially for immediate release products. Landolphia owariensis latex can also be formulated as an adhesive. © 2009-2010 Healthy Synergies Publications.