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In vitro properties of surface-modified solid lipid microspheres containing an antimalarial drug:halofantrine

Asian Pacific Journal of Tropical Medicine 2011年第4期4卷 253-258页

作者： Anthony A Attama collins n igbonekwu Department of Pharmaceutics University of Nigeria

Objective:To formulate and evaluate in vitro,surface-modified solid lipid microspheres containing hal of antrine using lipid matrix formed from goat fat and a phospholipid(P90H). Methods:The model drug,hal of antrine in an increasing concentration of 1%,2%,3%,4% and 5%w/w was incorporated into surface-modified solid lipid microspheres formulated by hot *** of drug concentration on the encapsulation efficiency was studied. The dispersion was evaluated using particle size,particle morphology,pH and encapsulation *** drug formulation with highest encapsulation efficiency was selected and used for the release studies and compared with the release from a commercial dosage form(Halfan~? 250 mg tablet,Claxo-Smithkline,Mayenne France) using simulated gastric fluid(SGF pH 1.2), simulated intestinal fluid(SIF pH 7.2) and phosphate buffer(pH 6.8) as biorelevant media. Results were analyzed statistically and the level of significance was taken to be Pnd spherical solid lipid microspheres were *** particle size of the dispersion was low(32.48-33.87μm) with minimal particle growth and high encapsulation efficiencies(86.8%-91.0%) after 3 *** pH of the microspheres dispersion changed appreciably after 3 *** vitro release result obtained revealed sustained and controlled drug release from the lipid microspheres compared with the tablet dosage ***: Formulation of hal of antrine as solid lipid microspheres presents a better alternative to the conventional tablet formulation as the in vitro dissolution of the highly lipophilic hal of antrine was highly improved.

关键词： Solid lipid microsphere Particle size stability Halofan trine Encapsulation efficiency Release studies In vitro evaluation

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