阿奇霉素干粉制剂用于COVID-19治疗。

IF 3 4区 医学 Q2 CHEMISTRY, APPLIED Journal of microencapsulation Pub Date : 2023-06-01 DOI:10.1080/02652048.2023.2175924
Stefanie Ho Yi Chan, Khalid Sheikh, Mohammed Gulrez Zariwala, Satyanarayana Somavarapu
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引用次数: 0

摘要

阿奇霉素是一种抗生素,因其免疫调节活性而被提议用于治疗2019冠状病毒病(COVID-19)。本研究的目的是开发阿奇霉素负载聚乳酸-羟基乙酸(PLGA)纳米复合微粒的干粉配方,用于肺部递送,以改善阿奇霉素的低生物利用度。采用双乳液法制备纳米颗粒,喷雾干燥后形成纳米复合微粒。分析了包封效率和载药量,并通过粒径、zeta电位、形貌、结晶度和体外气溶胶分散性能对制剂进行了表征。壳聚糖的加入使只带中性电荷的阿奇霉素配方变成带正电荷的纳米颗粒。然而,壳聚糖的加入也增加了配方的粒径。在NGI®数据中观察到,壳聚糖相关配方的分散性有所改善。本研究表明,所有干粉制剂都能够将阿奇霉素输送到肺深部,这表明阿奇霉素通过肺部给药可能成为治疗COVID-19的有效方法。
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Dry powder formulation of azithromycin for COVID-19 therapeutics.

Azithromycin is an antibiotic proposed as a treatment for the coronavirus disease 2019 (COVID-19) due to its immunomodulatory activity. The aim of this study is to develop dry powder formulations of azithromycin-loaded poly(lactic-co-glycolic acid) (PLGA) nanocomposite microparticles for pulmonary delivery to improve the low bioavailability of azithromycin. Double emulsion method was used to produce nanoparticles, which were then spray dried to form nanocomposite microparticles. Encapsulation efficiency and drug loading were analysed, and formulations were characterised by particle size, zeta potential, morphology, crystallinity and in-vitro aerosol dispersion performance. The addition of chitosan changed the neutrally-charged azithromycin only formulation to positively-charged nanoparticles. However, the addition of chitosan also increased the particle size of the formulations. It was observed in the NGI® data that there was an improvement in dispersibility of the chitosan-related formulations. It was demonstrated in this study that all dry powder formulations were able to deliver azithromycin to the deep lung regions, which suggested the potential of using azithromycin via pulmonary drug delivery as an effective method to treat COVID-19.

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来源期刊
Journal of microencapsulation
Journal of microencapsulation 工程技术-工程:化工
CiteScore
6.30
自引率
2.60%
发文量
39
审稿时长
3 months
期刊介绍: The Journal of Microencapsulation is a well-established, peer-reviewed journal dedicated to the publication of original research findings related to the preparation, properties and uses of individually encapsulated novel small particles, as well as significant improvements to tried-and-tested techniques relevant to micro and nano particles and their use in a wide variety of industrial, engineering, pharmaceutical, biotechnology and research applications. Its scope extends beyond conventional microcapsules to all other small particulate systems such as self assembling structures that involve preparative manipulation. The journal covers: Chemistry of encapsulation materials Physics of release through the capsule wall and/or desorption from carrier Techniques of preparation, content and storage Many uses to which microcapsules are put.
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