Preparation, Characterization, and In Vivo Study of 7-Ethyl-14-Aminocamptothecin-Loaded Poly(Ethylene Glycol)2000-Poly(Lactic Acid)2000 Polymeric Micelles Against H460 Human Nonsmall Cell Lung Carcinoma

ABSTRACT This work aims to improve the solubility of 7-ethyl-14-aminocamptothecin (EACPT) by encapsulating it into monomethoxy poly(ethylene glycol) 2000 -poly(lactic acid) 2000 (MPEG-PLA) polymeric micelles. Micelles were prepared by a solid dispersion method; the properties including particle size distribution, morphology, drug loading, entrapment efficiency, crystallography property, solubility, and stability were characterized in detail. The results demonstrated that the EACPT-loaded MPEG-PLA polymeric micelle (EACPT-M) was successfully developed with a small particle size of 20.7±0.2nm, and the solubility was increased approximately 800-fold compared with free drug. In vitro release study showed sustained-release behavior of EACPT-M. Cytotoxicity assay suggested the incorporated EACPT maintained the potent antitumor effect of free drug. Furthermore, the obtained EACPT-M (1mg/mL) did not induce hemolysis in vitro . Additionally, EACPT-M exhibited significant tumor growth inhibition in H460 human tumor xenograft model. The results indicated that the EACPT-M was a water-soluble, safe, and effective delivery system for human cancer chemotherapy. © 2015 Wiley Periodicals, Inc. and the American Pharmacists Association J Pharm Sci 104:3934–3942, 2015