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Preparation and cytotoxicity of 2-methoxyestradiol-loaded solid lipid nanoparticles.
MedLine Citation:
PMID:  22027535     Owner:  NLM     Status:  Publisher    
Abstract/OtherAbstract:
The objective of this study was to prepare 2-methoxyestradiol (2-ME)-loaded solid lipid nanoparticles (SLN) by hot homogenization-ultrasonication and evaluate their cytotoxicity on three cell lines, breast cancer [Michigan Cancer Foundation-7 (MCF-7)], prostatic carcinoma (PC-3), and glioma (SK-N-SH), by the sulforhodamineB method. The particle sizes and zeta potentials of the prepared SLN were around 120 nm and -40 mV, respectively. Differential scanning calorimetry (DSC) measurements revealed that the monostearin and 2-ME existed in solid and amorphous states in the SLN prepared, respectively. The high drug entrapment efficiency (>85%) indicated that most 2-ME was incorporated in the SLN. An in-vitro drug release study showed that 2-ME was released from the SLN in a slow but time-dependent manner. The cytotoxicity of 2-ME in SLN on each cell line was significantly enhanced compared with the solution. 2-ME SLN composed of Tween80 was approximately 17-fold more effective on PC-3 cells and 6.7-fold more effective on SK-N-SH cells than in the solution, whereas a lower sensitivity was achieved on MCF-7 cells. In each cell line, the cellular uptake percentages of 2-ME in SLN were much higher than the solution, respectively. In addition, surfactants may exert different effects on the cytotoxicity of 2-ME SLN depending on the cell line. The above assay demonstrated that SLN could significantly enhance the cytotoxicity of 2-ME compared with the free drug because of the increased cellular internalization and concentration of 2-ME. The results suggested that SLN could be an excellent carrier candidate to entrap 2-ME for improving the effectiveness of tumor chemotherapy.
Authors:
Xinhong Guo; Yabing Xing; Qian Mei; Hongling Zhang; Zhenzhong Zhang; Fude Cui
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Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2011-10-24
Journal Detail:
Title:  Anti-cancer drugs     Volume:  -     ISSN:  1473-5741     ISO Abbreviation:  -     Publication Date:  2011 Oct 
Date Detail:
Created Date:  2011-10-26     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9100823     Medline TA:  Anticancer Drugs     Country:  -    
Other Details:
Languages:  ENG     Pagination:  -     Citation Subset:  -    
Affiliation:
aSchool of Pharmacy, Zhengzhou University, Zhengzhou bDepartment of Pharmaceutical Sciences, Shenyang Pharmaceutical University, Shenyang, People's Republic of China.
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