NOVEL AMPHOTERICIN B NANOPARTICLES FOR SYSTEMIC MYCOSIS

描述(逐字摘自申请者摘要)：本报告的总体目标 该计划将验证SEDUM的新BiAcervateTM纳米颗粒配方 运送药物、蛋白质和DNA。当前毒品领域面临的挑战之一 今天的发展是高效地提供化学和生物药物。 稳定生物活性成分的微粒和包埋技术 将系统性毒性降至最低通常是困难和昂贵的 规模很大。景天实验室公司开发了一种新型胶囊 基于两种相反电荷生物相容聚合物凝聚的方法 用带电的药物或大分子。BiAcervateTM纳米颗粒 药物和大分子高效，在体内缓慢释放。 SEDUM现在建议通过优化配方来验证这项技术 最大化两性霉素B的掺入效率、稳定性和安全性 两性霉素B是治疗严重系统性真菌的唯一有效药物 免疫功能低下患者的感染，但其使用受到严重限制 毒性。脂质体制剂太贵了，所以不能使用 通常在一些医疗中心。候选双乙酸乙酯配方将是 评价细胞毒性和体外和体外抗真菌活性 小鼠全身性真菌感染的实验模型。 建议的商业应用： SEDUM计划通过开发以下技术进入价值140亿美元的先进药物输送系统市场 两性霉素B的新纳米制剂，这将有更大的治疗指数 而且毒副作用比传统药物更少，而且更容易和更低的成本 比脂质体形式更容易产生。两性霉素B是治疗重症患者最有效的药物 系统性真菌感染，每年困扰10万名免疫功能低下的患者。

DESCRIPTION (Verbatim from Applicant's Abstract):The overall objective of this program is to validate Sedum's new Bi-AcervateTM nanoparticle formulation for delivery of drugs, proteins and DNA. One of the current challenges in drug development today is efficient delivery of chemical and biological medicines. Microparticle and encapsulation techniques that stabilize bioactive ingredients and minimize systemic toxicity often are difficult and expensive to produce at large scale. Sedum Laboratories, Inc. has developed a novel encapsulation method based on coacervation of two oppositely charged biocompatible polymers with a charged drug or macromolecule. Bi-AcervateTM nanoparticles incorporate drugs and macromolecules with high efficiency and release them slowly in vivo. Sedum now proposes to validate this technology by optimizing the formulation to maximize incorporation efficiency, stability and safety of amphotericin B. Amphotericin B is the only drug effective against severe systemic fungal infections in immunocompromised patients, but its use is limited by severe toxicity. Liposomal preparations are so expensive that they are not used routinely in some medical centers. Candidate BiAcervate formulations will be evaluated for cytotoxicity and anti-fungal activity in vitro and in an experimental model of systemic fungal infection in mice. PROPOSED COMMERCIAL APPLICATION: Sedum proposes to enter the $14B market for advanced drug delivery systems by developing a new nanoparticle formulation of Amphotericin B. This will have a greater therapeutic index and fewer toxic side effects than conventional drugs, and will be easier and less costly to produce than liposomal forms. Amphotericin B is the most effective drug for treating severe systemic fungal infections, which afflict 100,000 immunocompromised patients a year.