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Tropical Journal of Pharmaceutical Research
Pharmacotherapy Group, Faculty of Pharmacy, University of Benin, Benin City, Nigeria
ISSN: 1596-5996
EISSN: 1596-9827
Vol. 13, No. 2, 2014, pp. 199-204
Bioline Code: pr14028
Full paper language: English
Document type: Research Article
Document available free of charge

Tropical Journal of Pharmaceutical Research, Vol. 13, No. 2, 2014, pp. 199-204

 en Formulation and Release Characteristics of Zidovudine- Loaded Solidified Lipid Microparticles
Uronnachi, Emmanuel M.; Ogbonna, John D.N.; Kenechukwu, Franklin C.; Chime, Salome A.; Attama, Anthony A. & Okore, Vincent C.

Abstract

Purpose: To formulate and determine the release profile of zidovudine (AZT)-loaded solidified lipid microparticles (SLMs).
Methods: Different concentrations (0, 1, 2, 3 and 5 %w/w) of zidovudine (AZT) were formulated into microparticles in melt dispersion of Phospholipon® 90H and goat fat in the ratio 1:1, 2:1, 2:3 and 1:3 followed by lyophilization. They were characterized for particle size, yield, entrapment efficiency (EE) and loading capacity (LC). In vitro release kinetics and mechanism of release were assessed sequentially in simulated gastric fluid (SGF, pH 1.2) and simulated intestinal fluid (SIF, pH 7.2).
Results: The ratio 1: 1 formulation was the most stable in terms of physical observation. Particle size analysis indicated that the particles were irregular in shape with size ranging from 5.10 ± 0.10 to 13.40 ± 2.20 μm. Yield decreased with increase in drug concentrations in the SLMs formulations. EE data showed that the microparticles containing 1 % w/w of AZT had the highest entrapment efficiency of 74.0 ± 0.03 %. LC also decreased with increase in concentration of AZT. AZT tablet released most of its content within 5 min with a sharp decrease in the concentration but the SLMs maintained its release for 8 to 12 h in different batches
Conclusion: The results show that drug content has influence on drug release from the SLMs, but not on the mechanism of release. Furthermore, dose dumping was avoided and drug release mechanism was mostly non-Fickian while for the reference (commercial) tablet, it was Fickian.

Keywords
Phospholipon® 90H; Solidified lipid microparticles; Solidified reverse micellar microparticle; Zidovudine

 
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