包封两性霉素B：两性霉素B的口服可用性终于实现了吗？
Encochleated Amphotericin B: Is the Oral Availability of Amphotericin B Finally Reached?
作者信息
Aigner Maria, Lass-Flörl Cornelia
机构信息
Institute of Hygiene and Medical Microbiology, Medical University of Innsbruck, Schöpfstraße 41, Innsbruck A-6020, Austria.
出版信息
J Fungi (Basel). 2020 May 18;6(2):66. doi: 10.3390/jof6020066.
Abstract
As the oldest and for many decades the only available agent for the treatment of life-threatening invasive fungal diseases, amphotericin B (AmB) is known for its broad-spectrum fungicidal activity against a wide range of yeasts and molds. However, the main drawback of the present formulations remains its toxicity, the limited use to intravenous administration, and the higher costs associated with the better tolerated lipid formulations. The novel nanoparticle-based encochleated AmB (CAmB) formulation encapsulates, protects, and delivers its cargo molecule AmB in the interior of a calcium-phospholipid anhydrous crystal. Protecting AmB from harsh environmental conditions and gastrointestinal degradation, CAmB offers oral availability in conjunction with reduced toxicity. Matinas BioPharma, Bedminster, NJ is on the way to develop CAmB named MAT2203, currently undergoing Phase II clinical trials.
摘要
作为治疗危及生命的侵袭性真菌病最古老且几十年来唯一可用的药物，两性霉素B（AmB）以其对多种酵母和霉菌具有广谱杀菌活性而闻名。然而，目前制剂的主要缺点仍然是其毒性、仅限于静脉给药的使用方式以及与耐受性较好的脂质制剂相关的较高成本。新型基于纳米颗粒的包载两性霉素B（CAmB）制剂将其载药分子两性霉素B包裹、保护并递送至钙磷脂无水晶体内部。CAmB保护两性霉素B免受恶劣环境条件影响和胃肠道降解，同时具有口服可用性且毒性降低。新泽西州贝德明斯特的马蒂纳斯生物制药公司正在开发名为MAT2203的CAmB，目前正在进行II期临床试验。
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