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.