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采用静电纺丝技术制备阿奇霉素纳米纤维作为控释眼科药物载体及其表征

Preparation of Azithromycin Nanofibers as Controlled Release Ophthalmic Drug Carriers Using Electrospinning Technique: and Characterization.

作者信息

Taghe Shiva, Mehrandish Saba, Mirzaeei Shahla

机构信息

Pharmaceutical Sciences Research Center, Health Institute, Kermanshah University of Medical Sciences, Kermanshah, Iran.

Nano Drug Delivery Research Center, Health Technology Institute, Kermanshah University of Medical Sciences, Kermanshah, Iran.

出版信息

Adv Pharm Bull. 2022 Mar;12(2):346-355. doi: 10.34172/apb.2022.033. Epub 2021 May 29.

DOI:10.34172/apb.2022.033
PMID:35620329
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9106962/
Abstract

Conventional topical dosage forms face with some challenges like low intraocularbioavailability, which could be overcome by application of novel drug delivery systems.Therefore, this study was conducted to prepare azithromycin (AZM)-loaded chitosan/polyvinylalcohol/polyvinyl pyrrolidone (CS/PVA-PVP) nanofibers with the prolonged antibacterialactivity by electrospinning method. After preparation of nanofibers, they were characterized in terms of physicochemicaland morphological properties. and release of the drug from nanofibers wereevaluated using microbial assay against the . Antibacterial efficacy of thenanofibers was assessed. The ophthalmic irritation test was also performed. MTT test wascarried out to evaluate cytotoxicity of the formulations. All the formulations were found to be stable with uniform thickness, weight, and drugcontent. Nanofibers had a diameter range from 119 ± 29 to 171 ± 39 nm. The inserts were nonirritantand non-toxic to the rabbits' eye. Based on the obtained results, the crosslinked AZMnanofibers showed slower and more controlled drug release in tear fluid compared to the noncrosslinkedones, within 184 hours. Our results revealed that the prepared nanofibers could be considered as suitableand non-invasive inserts for the prolonged ophthalmic delivery of AZM.

摘要

传统的局部剂型面临一些挑战,如眼内生物利用度低,而新型药物递送系统的应用可以克服这些挑战。因此,本研究旨在通过静电纺丝法制备具有延长抗菌活性的载阿奇霉素(AZM)的壳聚糖/聚乙烯醇/聚乙烯吡咯烷酮(CS/PVA-PVP)纳米纤维。纳米纤维制备后,对其物理化学和形态学性质进行了表征。并使用针对……的微生物测定法评估了药物从纳米纤维中的释放情况。评估了纳米纤维的抗菌效果。还进行了眼刺激试验。进行MTT试验以评估制剂的细胞毒性。发现所有制剂均稳定,具有均匀的厚度、重量和药物含量。纳米纤维的直径范围为119±29至171±39nm。插入物对兔眼无刺激性且无毒。基于所得结果,与未交联的纳米纤维相比,交联的AZM纳米纤维在泪液中的药物释放更缓慢且更可控,在184小时内。我们的结果表明,所制备的纳米纤维可被视为用于AZM长期眼部递送的合适且非侵入性的插入物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6569/9106962/fe6bba279a1e/apb-12-346-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6569/9106962/c6a462fa6123/apb-12-346-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6569/9106962/4df8de462d40/apb-12-346-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6569/9106962/425f1fd06950/apb-12-346-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6569/9106962/fe41801c5fec/apb-12-346-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6569/9106962/ebee874cb151/apb-12-346-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6569/9106962/fe6bba279a1e/apb-12-346-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6569/9106962/c6a462fa6123/apb-12-346-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6569/9106962/4df8de462d40/apb-12-346-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6569/9106962/425f1fd06950/apb-12-346-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6569/9106962/fe41801c5fec/apb-12-346-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6569/9106962/ebee874cb151/apb-12-346-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6569/9106962/fe6bba279a1e/apb-12-346-g006.jpg

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