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Journal of Nanomaterials
Volume 2012 (2012), Article ID 358782, 10 pages
http://dx.doi.org/10.1155/2012/358782
Research Article

Formulation of LDL Targeted Nanostructured Lipid Carriers Loaded with Paclitaxel: A Detailed Study of Preparation, Freeze Drying Condition, and In Vitro Cytotoxicity

Department of Pharmaceutics, School of Pharmacy and Pharmaceutical Sciences and Isfahan Pharmaceutical Research Center, Isfahan University of Medical Sciences, Isfahan 73461-8174, Iran

Received 11 October 2012; Accepted 13 November 2012

Academic Editor: Li-Hong Liu

Copyright © 2012 Jaber Emami et al. This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

Abstract

In the present study, cholesterol nanostructured lipid carriers with various oleic acid content loaded with paclitaxel (PTX) were prepared by solvent emulsification-diffusion method using a Taguchi design. Size, zeta potential, entrapment efficiency, drug loading, and release percent of NLCs were measured. The results indicated that the most effective factors on the size were oleic acid content and surfactant percent. Zeta potential was more affected by the drug content. Drug to- lipid weight ratio was the most effective factor on entrapment efficiency and drug release from NLC. In the present work, the effect of lyophilization on the particle size and release properties of NLCs was also evaluated. The results revealed no differences between the characteristics of NLCs before and after freeze drying by using 25% w/w sorbitol as cryoprotectant. Cytotoxicity studies indicate that PTX associated with the NLC is also effective in HT-29 cell lines and enters the cancer cells selectively through the LDL receptor endocytic pathway. The IC50 values of free PTX solubilized in Cremophor EL and NLC-born PTX after 72 h exposure were  ng/mL and  ng/mL, respectively.