Abstract :
The objective of the research work was to design and characterize Nanostructured Lipid Carriers (NLC)
incorporated with anticancer agent docetaxel. NLC were prepared by hot homogenization followed by
ultrasonication method using stearic acid as the solid lipid and oleic acid as the liquid lipid. Soya bean lecithin
was used as surfactant and poloxamer 188 as the cosurfactant. Optimization of the formulations was done based
on sedimentation volume, particle size, polydispersity, % entrapment efficiency and zeta potential. The
optimized batch of NG9 exhibited a particle size of 180µm, polydispersity of 0.25, %EE of 78% and zeta
potential of 41mV. Based on this it was decided that concentration of lipid at 20%, solid lipid: liquid lipid ratio
of 80:20, surfactant and cosurfactant at 4%, mannitol at 3% was the optimal proportion. The process
parameters was further optimized and the results revealed that at homogenization RPM of 6000,
homogenization time of 20min and sonication time of 10min resulted in NLC with ideal characteristics. The in
vitro release of Docetaxel from the optimized batch, NG9 was found to be almost complete with a release of
98.80 ±0.08 at 4 hours. The drug release of this batch when subjected to pharmacokinetics studies using
various models showed that the data best into zero order and Higuchi release kinetic model with a coefficient of
determination (R2
) value of 0.9972 and 0.9347. Linearity to Higuchi kinetic model indicated a diffusion
controlled drug release. The release component (n) from peppas model was found to be 0.42, which indicated
Fickian diffusion from which it can be assumed that the drug delivery system under study is a matrix device.
Keyword :
Nano structured lipid carriers (NLC), Docetaxel, Poloxamer 188, soya bean lecithin, stearic acid, and oleic acid