Transferrin-conjugated lipid-coated PLGA nanoparticles for targeted delivery of aromatase inhibitor 7alpha-APTADD to breast cancer cells.
Transferrin-conjugated lipid-coated PLGA nanoparticles for targeted delivery of aromatase inhibitor 7alpha-APTADD to breast cancer cells.
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DOI：
10.1016/j.ijpharm.2010.02.008
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发表时间：
2010-05-10
影响因子：
5.8
通讯作者：
Lee, Robert J.
中科院分区：
文献类型：
--
作者：
Zheng, Yu;Yu, Bo;Weecharangsan, Wanlop;Piao, Longzhu;Darby, Michael;Mao, Yicheng;Koynova, Rumiana;Yang, Xiaojuan;Li, Hong;Xu, Songlin;Lee, L. James;Sugimoto, Yasuro;Brueggemeier, Robert W.;Lee, Robert J.
采用溶剂注射法制备了转铁蛋白(Tf)-脂质包衣的聚(d，L-丙交酯-乙交酯共聚物)载芳香酶抑制剂7α-(4′-amino)phenylthio-1，4-androstadiene-3，17-dione(7-α-APTADD)纳米粒。优化了处方参数，包括PLGA与脂质的比例、鸡蛋PC与TPGS的比例、药物与PLGA的比例以及合成时水与有机相的比例，以获得所需的尺寸和载药效率的纳米粒。最佳处方的载药率为36.3±3.4%，平均粒径为170.3±7.6 nm，−电位为18.9±1.5 mV。在SKBR-3乳腺癌细胞中评价了纳米颗粒对芳香化酶的抑制活性。转移因子纳米粒的IC50值为0.77~1.21 nm，IC50值为1.90~3.41 nm(n=3)。前者显著低于后者(p<；0.05)。这些结果表明，与非靶向纳米粒相比，转铁蛋白纳米粒的芳香酶抑制活性增强，这归因于转铁蛋白受体(TFR)介导的摄取。综上所述，Tf-偶联脂质包裹的PLGA纳米粒是提高芳香酶抑制剂治疗给药效率和特异性的潜在载体。
Transferrin (Tf)-conjugated lipid-coated poly(d,l-lactide-co-glycolide) (PLGA) nanoparticles carrying the aromatase inhibitor, 7α-(4′-amino)phenylthio-1,4-androstadiene-3,17-dione (7α-APTADD), were synthesized by a solvent injection method. Formulation parameters including PLGA-to-lipid, egg PC-to-TPGS, and drug-to-PLGA ratios and aqueous-to-organic phase ratio at the point of synthesis were optimized to obtain nanoparticles with desired sizes and drug loading efficiency. The optimal formulation had a drug loading efficiency of 36.3±3.4%, mean diameter of 170.3±7.6 nm and zeta potential of −18.9±1.5 mV. The aromatase inhibition activity of the nanoparticles was evaluated in SKBR-3 breast cancer cells. IC50 value of the Tf-nanoparticles was ranging from 0.77 to 1.21 nM, and IC50 value of the nanoparticles was ranging from 1.90 to 3.41 nM (n = 3). The former is significantly lower than the latter (p < 0.05). These results suggested that the aromatase inhibition activity of the Tf-nanoparticles was enhanced relative to that of the non-targeted nanoparticles, which was attributable to Tf receptor (TfR) mediated uptake. In conclusion, Tf-conjugated lipid-coated PLGA nanoparticles are potential vehicles for improving the efficiency and specificity of therapeutic delivery of aromatase inhibitors.
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影响因子：
4.9
作者：
Lu, Yanhui;Wu, Jun;Lee, Robert J.
通讯作者：
Lee, Robert J.
影响因子：
4.9
作者：
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影响因子：
5.6
作者：
INOUE, T;CAVANAUGH, PG;NICOLSON, GL
通讯作者：
NICOLSON, GL
通过将长春新碱和维拉帕米共封装在 PLGA 纳米颗粒中逆转多药耐药性。
影响因子：
4.6
作者：
Song, Xiang Rong;Cai, Zheng;Wei, Yu Quan
通讯作者：
Wei, Yu Quan