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首页> 外文期刊>European journal of pharmaceutics and biopharmaceutics: official journal of Arbeitsgemeinschaft fuer Pharmazeutische Verfahrenstechnik e.V >High oral bioavailability of 2-methoxyestradiol in PEG-PLGA micelles-microspheres for cancer therapy
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High oral bioavailability of 2-methoxyestradiol in PEG-PLGA micelles-microspheres for cancer therapy

机译：在PEG-PLGA胶束 - 微球中的2-甲氧基雌二醇的高口服生物利用度用于癌症治疗

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摘要

The development of effective oral preparations of 2-methoxyestradiol (2-ME) has been a worldwide problem. In this study, breakthrough progress has been made in oral delivery of 2-ME by encapsulating 2-ME micelles in pH-responsive microspheres. 2-ME micelles with small particle size (58 nm) and high drug loading (7.94 +/- 0.23%) were successfully prepared and showed slower release characteristics and 12.8 times higher cytotoxicity on 4T1 cells than free 2-ME. The pH-sensitive microspheres could slowly release 82% of 2-ME micelles for 10 h in PBS (7.4). After oral administration to rats, 2-ME-micelles-microspheres compared to 2-ME micelles could prolong significantly blood retention time (MRT) of 2-ME by 12 times and enhance oral absolute bioavailability from 49.99% to 121.68%. In vivo imaging of 4T1 tumor-bearing mice showed that retention time and intensity of the fluorescence signal in each 2 ME preparation group all were consistent with the pharmacokinetic results and intact 2-ME micelles in the microspheres could be absorbed in intestine to blood to target to tumor. Furthermore, after the 4T1 tumor-bearing mice were treated with oral 2-ME-micelles-microspheres for 21 days, the tumor growth inhibition rate achieved 94.93% and the mice weight gained significantly, indicating their high antitumor activity and low toxicity. While oral administration of 2-ME micelles and 2-ME microspheres all were ineffective under the same conditions. Therefore, micelles-microspheres might be a promising candidate for oral administration of 2-ME for cancer therapy. (C) 2017 Elsevier B.V. All rights reserved.
机译：有效口服制剂的2-甲氧基雌二醇（2-ME）的发展是全世界的问题。在这项研究中，通过在pH-响应微球中封装2-Me胶束来口服递送2-Me的突破性进展。 2-ME粒径（58nm）和高药物负载（7.94 +/- 0.23％）的2-Me胶束成功制备，并显示出较慢的释放特性和4T1细胞上的细胞毒性比Free 2-Me更高的细胞毒性12.8倍。 pH敏感的微球可以在PBS（7.4）中慢慢释放出82％的2-Me胶束10小时。在口服给予大鼠之后，与2-Me胶束相比，2-Me-​​胶束 - 微球可以延长2-Me的显着血液保留时间（MRT），以12次，增强口腔绝对生物利用度，从49.99％到121.68％。在4T1肿瘤的小鼠的体内成像表明，每种2 ME制备组中的荧光信号的保留时间和强度均与药代动力学结果一致，并且在微球中的完整2-Me胶束可以在肠中吸收到血液中以血液中的血液吸收肿瘤。此外，在用口服2-ME-胶束 - 微球处理21天后，肿瘤生长抑制率为94.93％，小鼠重量显着，表明其高抗肿瘤活性和低毒性。虽然口服给药2-Me胶束和2-Me微球，但在相同的条件下均无效。因此，胶束微球可能是口服癌症治疗口服给药的有希望的候选者。 （c）2017 Elsevier B.v.保留所有权利。

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