Solid lipid nanoparticle formulations of docetaxel prepared with high melting point triglycerides: in vitro and in vivo evaluation.

Abstract	Docetaxel (DCX) is a second generation taxane. It is approved by the U.S. Food and Drug Administration for the treatment of various types of cancer, including breast, non-small cell lung, and head and neck cancers. However, side effects, including those related to Tween 80, an excipient in current DCX formulations, can be severe. In the present study, we developed a novel solid lipid nanoparticle (SLN) composition of DCX. Trimyristin was selected from a list of high melting point triglycerides as the core lipid component of the SLNs, based on the rate at which the DCX was released from the SLNs and the stability of the SLNs. The trimyristin-based, PEGylated DCX-incorporated SLNs (DCX-SLNs) showed significantly higher cytotoxicity against various human and murine cancer cells in culture, as compared to DCX solubilized in a Tween 80/ethanol solution. Moreover, in a mouse model with pre-established tumors, the new DCX-SLNs were significantly more effective than DCX solubilized in a Tween 80/ethanol solution in inhibiting tumor growth without toxicity, likely because the DCX-SLNs increased the concentration of DCX in tumor tissues, but decreased the levels of DCX in major organs such as liver, spleen, heart, lung, and kidney. DCX-incorporated SLNs prepared with one or more high-melting point triglycerides may represent an improved DCX formulation.
Authors	Youssef Wahib Naguib, B Leticia Rodriguez, Xinran Li, Stephen D Hursting, Robert O Williams 3rd, Zhengrong Cui
Journal	Molecular pharmaceutics (Mol Pharm) Vol. 11 Issue 4 Pg. 1239-49 (Apr 07 2014) ISSN: 1543-8392 [Electronic] United States
PMID	24621456 (Publication Type: Journal Article, Research Support, N.I.H., Extramural, Research Support, Non-U.S. Gov't)
Chemical References	Antineoplastic Agents Dcx protein, mouse Doublecortin Protein Taxoids Triglycerides Docetaxel
Topics	Animals Antineoplastic Agents (chemistry) Cell Line, Tumor Chemistry, Pharmaceutical Docetaxel Doublecortin Protein Female Mice Mice, Inbred C57BL Nanoparticles (chemistry) Taxoids (chemistry, pharmacokinetics, pharmacology, therapeutic use) Tissue Distribution Transition Temperature Triglycerides (chemistry)

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