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 ± 0.2 nm, 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 (1 mg/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.

• Authors: Xia Cheng, Neng Qiu, Jianhong Yang, Huili Liu, Jiaolin Wen, Wenwen Wang, Zhoufeng Wang, Lijuan Chen
• Journal: Journal of pharmaceutical sciences (J Pharm Sci) Vol. 104 Issue 11 Pg. 3934-3942 (Nov 2015) ISSN: 1520-6017 [Electronic] United States
• PMID: 26306026 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
• Copyright: © 2015 Wiley Periodicals, Inc. and the American Pharmacists Association.

Chemical References

• 7-ethyl-14-aminocamptothecin
• Antineoplastic Agents
• Delayed-Action Preparations
• Micelles
• Polyesters
• Polymers
• methoxy poly(ethylene glycol)-poly(lactide)
• Lactic Acid
• Polyethylene Glycols
• poly(lactide)
• Camptothecin

Topics

• Animals
• Antineoplastic Agents (administration & dosage, pharmacology, therapeutic use)
• Camptothecin (administration & dosage, analogs & derivatives, pharmacology, therapeutic use)
• Carcinoma, Non-Small-Cell Lung (drug therapy, pathology)
• Cell Line, Tumor
• Cell Survival (drug effects)
• Delayed-Action Preparations (chemistry)
• Female
• Hep G2 Cells
• Humans
• Lactic Acid (chemistry)
• Lung (drug effects, pathology)
• Lung Neoplasms (drug therapy, pathology)
• Mice, Nude
• Micelles
• Polyesters (chemistry)
• Polyethylene Glycols (chemistry)
• Polymers (chemistry)