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载两性霉素 B 的 MPEG-PCL 胶束的制备、表征和毒性评价及其在口腔片剂中的应用。

Preparation, characterization and toxicity evaluation of amphotericin B loaded MPEG-PCL micelles and its application for buccal tablets.

机构信息

Department of Pharmacology, Health Science Center, Xi'an Jiaotong University, No. 76 Yanta Westroad, Xi'an, 710061, People's Republic of China.

MRC Centre for Molecular Microbiology and Infection, Imperial College London, London, SW7 2AZ, UK.

出版信息

Appl Microbiol Biotechnol. 2017 Oct;101(19):7357-7370. doi: 10.1007/s00253-017-8463-6. Epub 2017 Sep 3.

Abstract

Oral candidiasis or thrush is a fungal infection due to Candida albicans, causing discomfort in areas inside mouth or tongue. The clinical application of antifungal reagent amphotericin B (AMB), which is believed to offer a better treatment for oral candidiasis, is greatly compromised by its toxicities (mainly nephrotoxicity) and poor solubility. In order to overcome these issues, we characterized AMB-loaded MPEG-PCL micelles in vitro and in vivo. In addition, the antifungal activities of AMB/MPEG-PCL micelles-loaded buccal tablet were also evaluated in vitro. We found that micelles system could significantly improve the solubility of AMB yet reduce the overall toxicity, while the buccal tablet system is capable to suppress C. albicans biofilm formation. Furthermore, the toxicity of the buccal tablet system is also reduced compared with other standard preparations. Therefore, the prepared tablet with AMB-loaded MPEG-PCL micelles as oral topical preparations has the potential to improve current treatment of superficial oral C. albicans infections.

摘要

口腔念珠菌病或鹅口疮是一种由白色念珠菌引起的真菌感染,会导致口腔内部或舌头上出现不适。抗真菌试剂两性霉素 B(AMB)的临床应用受到其毒性(主要是肾毒性)和低溶解度的严重限制,而被认为对口腔念珠菌病有更好治疗效果。为了克服这些问题,我们对 AMB 负载的 MPEG-PCL 胶束进行了体外和体内表征。此外,还评估了负载 AMB/MPEG-PCL 胶束的口腔片剂的体外抗真菌活性。我们发现胶束系统可以显著提高 AMB 的溶解度,同时降低整体毒性,而口腔片剂系统能够抑制白色念珠菌生物膜的形成。此外,与其他标准制剂相比,口腔片剂系统的毒性也降低了。因此,作为口腔局部制剂,负载 AMB 的 MPEG-PCL 胶束的口腔片剂有潜力改善当前治疗浅表口腔白色念珠菌感染的方法。

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