Solid Lipid Nanoparticles of Atovaquone Based on 24 Full-factorial Design

Document Type: Research article

Authors

School of Pharmaceutical Sciences, Universiti Sains Malaysia, 11800 Pulau Pinang, Malaysia.

Abstract

Solid lipid nanoparticles of atovaquone (ATQ-SLN) were prepared by high shear
homogenization method using tripalmitin, trilaurin, and Compritol 888 ATO as the lipid
matrices and Phospholipon 90H, Tween 80, and poloxamer 188 as the surfactants. Optimization
of the formulations was conducted using 6 sets of 24 full-factorial design based on four
independent variables that were the number of homogenizing cycles, concentration of the lipid,
concentration of the co-surfactant, and concentration of the main surfactant. The dependent
variables were particle size and polydispersity index (PdI). The homogenizing cycles showed a
negative influence on the dependent variables which reduced both the particle size and the PdI
value. Moreover, a combination of certain percentages of the main surfactant and co-surfactant
also showed a negative influence that reduced both the particle size and PdI value. Selected
formulations from each design were further characterized for the entrapment efficiency and
yield. The optimised formulation of ATQ-SLN consisted of trilaurin, Phospholipon 90H and
Tween 80 with a particle size of 89.4 ± 0.2 nm and entrapment efficiency of 83.0 ± 1.7%. The
in-vitro release evaluation of the formulation showed a complete and immediate release of ATQ
from the SLN that could be a solution to improve the poor aqueous solubility and hence poor
bioavailability of the drug.

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