Abstract |
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.
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Authors | Ming-Ji Jin, Sheng-Jun Piao, Tie-Xiong Jin, Zhe-Hu Jin, Xue-Zhe Yin, Zhong-Gao Gao |
Journal | Journal 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 |
PMID | 24496681
(Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
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Chemical References |
- Antineoplastic Agents
- Micelles
- Polyesters
- Taxoids
- Docetaxel
- polycaprolactone
- Polyethylene Glycols
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Topics |
- 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
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