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纳米颗粒作为抗真菌剂的安全有效递送系统:成就与挑战。

Nanoparticles as safe and effective delivery systems of antifungal agents: Achievements and challenges.

作者信息

Soliman Ghareb M

机构信息

Department of Pharmaceutics, Faculty of Pharmacy, Assiut University, Assiut, 71526, Egypt; Department of Pharmaceutics, Faculty of Pharmacy, University of Tabuk, Tabuk, Saudi Arabia.

出版信息

Int J Pharm. 2017 May 15;523(1):15-32. doi: 10.1016/j.ijpharm.2017.03.019. Epub 2017 Mar 19.

DOI:10.1016/j.ijpharm.2017.03.019
PMID:28323096
Abstract

Invasive fungal infections are becoming a major health concern in several groups of patients leading to severe morbidity and mortality. Moreover, cutaneous fungal infections are a major cause of visits to outpatient dermatology clinics. Despite the availability of several effective agents in the antifungal drug arena, their therapeutic outcome is less than optimal due to limitations related to drug physicochemical properties and toxicity. For instance, poor aqueous solubility limits the formulation options and efficacy of several azole antifungal drugs while toxicity limits the benefits of many other drugs. Nanoparticles hold great promise to overcome these limitations due to their ability to enhance drug aqueous solubility, bioavailability and antifungal efficacy. Further, drug incorporation into nanoparticles could greatly reduce its toxicity. Despite these interesting nanoparticle features, there are only few marketed nanoparticle-based antifungal drug formulations. This review sheds light on different classes of nanoparticles used in antifungal drug delivery, such as lipid-based vesicles, polymeric micelles, solid lipid nanoparticles, nanostructured lipid carriers, nanoemulsions and dendrimers with emphasis on their advantages and limitations. Translation of these nanoformulations from the lab to the clinic could be facilitated by focusing the research on overcoming problems related to nanoparticle stability, drug loading and high cost of production and standardization.

摘要

侵袭性真菌感染正成为几类患者的主要健康问题,导致严重的发病率和死亡率。此外,皮肤真菌感染是门诊皮肤科就诊的主要原因。尽管抗真菌药物领域有多种有效药物,但由于药物理化性质和毒性相关的限制,其治疗效果并不理想。例如,水溶性差限制了几种唑类抗真菌药物的剂型选择和疗效,而毒性则限制了许多其他药物的益处。纳米颗粒因其能够提高药物的水溶性、生物利用度和抗真菌疗效,有望克服这些限制。此外,将药物掺入纳米颗粒可以大大降低其毒性。尽管纳米颗粒具有这些有趣的特性,但基于纳米颗粒的抗真菌药物制剂上市的却很少。这篇综述阐述了用于抗真菌药物递送的不同类型纳米颗粒,如脂质体、聚合物胶束、固体脂质纳米粒、纳米结构脂质载体、纳米乳剂和树枝状大分子,重点介绍了它们的优缺点。通过集中研究克服与纳米颗粒稳定性、药物载量以及高生产成本和标准化相关的问题,可促进这些纳米制剂从实验室向临床的转化。

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