In Vitro Cytotoxicity and Cellular Uptake of Tamoxifen Citrate-Loaded Polymeric Micelles

被引:3
|
作者
Nasr, Mohamed [1 ]
Hashem, Fahima [1 ]
Abdelmoniem, Raghda [1 ]
Tantawy, Norhan [1 ]
Teiama, Mohamed [1 ]
机构
[1] Helwan Univ, Fac Pharm, Dept Pharmaceut & Ind Pharm, Cairo 11790, Egypt
关键词
Pluronic polymers; polymeric micelles; tamoxifen citrate; cellular uptake; cytotoxicity; breast cancer; PLURONIC BLOCK-COPOLYMERS; WATER-SOLUBLE DRUG; MIXED MICELLES; BREAST-CANCER; VIVO EVALUATION; ORAL DELIVERY; P123; SOLUBILIZATION; OPTIMIZATION; FORMULATION;
D O I
10.1208/s12249-020-01850-6
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
The main intent of this treatise was to encapsulate tamoxifen citrate (TMXC) into polymeric micellar delivery system and evaluate the influence of TMXC-loaded micelles as a promising carrier on the in vitro cytotoxicity and cellular uptake of TMXC in treatment of breast cancer. Different formulae of polymeric micelles loaded with TMXC using mixtures of different Pluronic polymers were fabricated by thin-film hydration method and evaluated for morphology, drug entrapment efficiency, particle size, surface charge, in vitro liberation of TMXC, uptake by cancer cell lines, and cytotoxic effect against breast cancer cell lines such as MCF-7. The optimal TMXC-loaded micelles exhibited nano-sized particles and entrapped about 89.09 +/- 4.2% of TMXC. In vitro liberation study revealed an extended TMXC escape of about 70.23 +/- 5.9% over a period of 36 h. The optimized TMXC-loaded micelles formula showed enhanced cellular uptake of TMXC by 2.28 folds and showed a significant cytotoxic effect with MCF-7 breast cancer cells compared to TMXC solution. The obtained yield proposed that Pluronic micelles could be a promising potential delivery system for anticancer moieties.
引用
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页数:11
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