Encapsulated paclitaxel nanoparticles exhibit enhanced anti-tumor efficacy in A549 non-small lung cancer cells.

Abstract

In the present study, paclitaxel (PTX) were encapsulated with polyethylene glycol (PEG)-polylactide (PLA)/D-α tocopheryl polyethylene glycol 1000 succinate (TPGS) (PEG-PLA/TPGS) and the enhanced anti-tumor activity of this PTX mixed micelles (PTX-MM) was evaluated in lung cancer cells. The PTX-MM prepared by a solvent evaporation method was demonstrated to have high drug-loading efficiency (23.2%), high encapsulation efficiency (76.4%), and small size (59 nm). In vitro release assay showed the slow release behavior of PTX-MM, suggesting the good stability of the PTX-MM essential for long circulation time. In vitro kinetics assay demonstrated that PTX-MM could promote absorption and increase relative bioavailability. The anti-cancer efficiency of PTX-MM was also examined by both in vitro and in vivo studies. PTX-MM exhibits obvious cytotoxicity against lung cancer cells with much lower IC50 value when compared with commercial formulated PTX or PTX + TPGS. The xenograft tumor model studies on nude mice indicated that PTX-MM inhibits tumor growth more effectively than other formulations. It was also found that most of mixed micelles were integral in tumor site to exhibit anti-cancer activity. Our results suggested that the use of PTX-MM as an anti-cancer drug may be an effective approach to treat lung cancer.

• Authors: Guojin Huang, Bao Zang, Xiaowei Wang, Gang Liu, Jianqiang Zhao
• Journal: Acta biochimica et biophysica Sinica (Acta Biochim Biophys Sin (Shanghai)) Vol. 47 Issue 12 Pg. 981-7 (Dec 2015) ISSN: 1745-7270 [Electronic] China
• PMID: 26525950 (Publication Type: Journal Article)
• Copyright: © The Author 2015. Published by ABBS Editorial Office in association with Oxford University Press on behalf of the Institute of Biochemistry and Cell Biology, Shanghai Institutes for Biological Sciences, Chinese Academy of Sciences.

Chemical References

• Antineoplastic Agents
• Micelles
• Solvents
• Paclitaxel

Topics

• A549 Cells
• Animals
• Antineoplastic Agents (administration & dosage, chemistry)
• Biological Availability
• Carcinoma, Non-Small-Cell Lung (drug therapy)
• Cell Line, Tumor
• Drug Delivery Systems
• Fluorescence Resonance Energy Transfer
• Humans
• Inhibitory Concentration 50
• Kinetics
• Lung Neoplasms (drug therapy)
• Mice
• Mice, Inbred BALB C
• Mice, Nude
• Micelles
• Nanoparticles (chemistry)
• Paclitaxel (administration & dosage)
• Solvents (chemistry)
• Xenograft Model Antitumor Assays