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脂质体作为多烯抗生素靶向递送的潜在载体系统。

Liposomes as potential carrier system for targeted delivery of polyene antibiotics.

作者信息

Naik Suresh R, Desai Sandhya K, Shah Priyank D, Wala Santosh M

机构信息

Department of Pharmacology, Sinhgad Institute of Pharmaceutical Sciences, Gat No. 309, off Mumbai- Pune Expressway, Kusgaon (Bk.), Lonavala-410401, Dist: Pune, Maharashtra, India.

出版信息

Recent Pat Inflamm Allergy Drug Discov. 2013 Sep;7(3):202-14. doi: 10.2174/1872213x113079990016.

Abstract

The development of new therapeutic modalities involves the use of drug carrier, such as liposomes, which can modify pharmacokinetic and bio-distribution of drug profile. Polyene antibiotics incorporation into liposomes improves its availability at the site, bio-distribution and therapeutic index mainly through the engulfment of liposomes by circulating monocytes/macrophages and transportation to the site of infection. Polyene antibiotics (AmB, SJA-95, HA-1-92) and other antibiotics (streptomycin, tobramycin, quinolones, anti-tubercular and anti-cancer drugs), liposomal preparations are described with possible advantages from therapeutic efficacy and toxicity point of view. The polyene macrolide antibiotics liposomal preparations proved to be more effective in the treatment of systemic mycosis. The AmB-cyclodextrin derivatives inclusion complex is a major breakthrough in liposomal preparation which can be converted into aqueous phase of liposome. Liposomal drug incorporated preparation has been one of the important areas of research for developing the existing polyene antibiotics into useful chemotherapeutic agents in clinical medicine. In recent past other antibiotics have also been incorporated into liposomes using wide variety of materials, phosphatidylethanolamine derivatives (pegylated liposomes, enzyme sensitive conjugates, fluidosomes of anti-cancer drugs and poly lactic/glycolic acid microspheres for anti-tuberculosis drugs). In addition, attempts were also made to extend the receptor mediated drug targeting and to review some relevant patents.

摘要

新治疗方式的发展涉及药物载体的使用,如脂质体,其可改变药物的药代动力学和生物分布特征。将多烯抗生素包裹于脂质体中,主要通过循环单核细胞/巨噬细胞吞噬脂质体并将其转运至感染部位,从而提高其在该部位的可用性、生物分布和治疗指数。本文从治疗效果和毒性的角度描述了多烯抗生素(两性霉素B、SJA - 95、HA - 1 - 92)和其他抗生素(链霉素、妥布霉素、喹诺酮类、抗结核药和抗癌药)的脂质体制剂及其可能的优势。多烯大环内酯类抗生素脂质体制剂在系统性真菌病的治疗中被证明更有效。两性霉素B - 环糊精衍生物包合物是脂质体制备中的一项重大突破,其可转化为脂质体的水相。将药物包裹于脂质体中的制剂一直是将现有多烯抗生素开发为临床医学中有用化疗药物的重要研究领域之一。最近,其他抗生素也已使用多种材料被包裹于脂质体中,如磷脂酰乙醇胺衍生物(聚乙二醇化脂质体、酶敏感缀合物、抗癌药的流体脂质体以及用于抗结核药的聚乳酸/乙醇酸微球)。此外,人们还尝试扩展受体介导的药物靶向并综述了一些相关专利。

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