Improved anti-tumor efficiency against prostate cancer by docetaxel-loaded PEG-PCL micelles.

This study primarily focused on the systematic assessment of both in vitro and in vivo anti-tumor effects of docetaxel-loaded polyethylene glycol (PEG)2000-polycaprolactone (PCL)2600 micelles on hormone-refractory prostate cancer (HRPC). By using solvent evaporation method, PEG-PCL was chosen to prepare doxetaxel (DTX)-loaded mPEG-PCL micelles (DTX-PMs), with the purpose of eliminating side effects of the commercial formulation (Tween 80) and prolonging the blood circulation time. The prepared DTX-PMs had an average particle size of 25.19±2.36 nm, a zeta potential of 0.64±0.15 mV, a polydispersity index of 0.56±0.03, a drug loading of (8.72±1.05)%, and an encapsulation efficiency of (98.1±8.4)%. In vitro cytotoxicity studies indicated that DTX-PMs could effectively kill LNCap-C4-2B cells and show a dose- and time-dependent efficacy. The hemolysis test showed that DTX-PMs had less hemocytolysis than the commercial product of Duopafei®. A sustained in vitro release behavior and prolonged circulation time in blood vessels were observed in the DTX-PMs. Furthermore, when compared with Duopafei®, the DTX-PMs dramatically reduced the prostate specific antigen (PSA) level and tumor growth of prostate tumor-bearing nude mice in vivo. In conclusion, the DTX-PMs can lower systemic side effects, improve anti-tumor activity with prolonged blood circulation time, and will bring an alternative to patients with HRPC.
AuthorsMing-Ji Jin, Sheng-Jun Piao, Tie-Xiong Jin, Zhe-Hu Jin, Xue-Zhe Yin, Zhong-Gao Gao
JournalJournal of Huazhong University of Science and Technology. Medical sciences = Hua zhong ke ji da xue xue bao. Yi xue Ying De wen ban = Huazhong keji daxue xuebao. Yixue Yingdewen ban (J Huazhong Univ Sci Technolog Med Sci) Vol. 34 Issue 1 Pg. 66-75 (Feb 2014) ISSN: 1672-0733 [Print] China
PMID24496681 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Chemical References
  • Antineoplastic Agents
  • Micelles
  • Polyesters
  • Taxoids
  • Docetaxel
  • polycaprolactone
  • Polyethylene Glycols
  • Animals
  • Antineoplastic Agents (pharmacokinetics, pharmacology)
  • Area Under Curve
  • Cell Line, Tumor
  • Cell Survival (drug effects)
  • Docetaxel
  • Dose-Response Relationship, Drug
  • Guinea Pigs
  • Hemolysis (drug effects)
  • Humans
  • Male
  • Mice
  • Mice, Nude
  • Micelles
  • Particle Size
  • Polyesters (chemistry)
  • Polyethylene Glycols (chemistry)
  • Prostatic Neoplasms (drug therapy, pathology)
  • Rats
  • Rats, Sprague-Dawley
  • Taxoids (chemistry, pharmacokinetics, pharmacology)
  • Treatment Outcome
  • Tumor Burden (drug effects)
  • Xenograft Model Antitumor Assays

Join CureHunter, for free Research Interface BASIC access!

Take advantage of free CureHunter research engine access to explore the best drug and treatment options for any disease. Find out why thousands of doctors, pharma researchers and patient activists around the world use CureHunter every day.
Realize the full power of the drug-disease research graph!

Choose Username:
Verify Password:
Enter Code Shown: