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含环丙沙星的壳聚糖/聚(2-乙基-2-恶唑啉)薄膜在阴道给药中的应用

Chitosan/Poly(2-ethyl-2-oxazoline) Films with Ciprofloxacin for Application in Vaginal Drug Delivery.

作者信息

Abilova Guzel K, Kaldybekov Daulet B, Irmukhametova Galiya S, Kazybayeva Diara S, Iskakbayeva Zhanar A, Kudaibergenov Sarkyt E, Khutoryanskiy Vitaliy V

机构信息

Department of Chemistry and Chemical Technology, Al-Farabi Kazakh National University, Almaty 050040, Kazakhstan.

Department of Natural Sciences, K. Zhubanov Aktobe Regional State University, 030000 Aktobe, Kazakhstan.

出版信息

Materials (Basel). 2020 Apr 6;13(7):1709. doi: 10.3390/ma13071709.

Abstract

Chitosan (CHI) and chitosan/poly(2-ethyl-2-oxazoline) (CHI/POZ)-based films were prepared by casting from aqueous solutions of polymer blends with different compositions. Ciprofloxacin was used as a model drug in these formulations. The weight, thickness, folding endurance and transparency of blend films were measured and characterised. All films had a uniform thickness (0.06 ± 0.01 mm) and exhibited sufficient flexibility. The surface pHs of films ranged from 3.76 ± 0.49 to 4.14 ± 0.32, which is within the pH range suitable for vaginal applications. The cumulative release of the drug from the films in experiments in vitro was found to be 42 ± 2% and 56 ± 1% for pure CHI and CHI/POZ (40:60) films, respectively. Drug-free chitosan/poly(2-ethyl-2-oxazoline) films showed weak antimicrobial activity against Escherichia coli. Drug-loaded CHI and CHI/POZ films showed good antimicrobial properties against both Gram-positive Staphylococcus aureus and Gram-negative bacteria Escherichia coli. Mucoadhesive properties of these films with respect to freshly excised sheep vaginal mucosa were evaluated using a tensile method. It was established that all films were mucoadhesive, but an increase in POZ content in the blend resulted in a gradual reduction of their ability to stick to vaginal mucosa. These films could potentially find applications in vaginal drug delivery.

摘要

通过从具有不同组成的聚合物共混物水溶液中浇铸制备了基于壳聚糖(CHI)和壳聚糖/聚(2-乙基-2-恶唑啉)(CHI/POZ)的薄膜。环丙沙星用作这些制剂中的模型药物。对共混薄膜的重量、厚度、耐折性和透明度进行了测量和表征。所有薄膜厚度均匀(0.06±0.01毫米),并表现出足够的柔韧性。薄膜的表面pH值范围为3.76±0.49至4.14±0.32,这在适合阴道应用的pH范围内。在体外实验中,纯CHI薄膜和CHI/POZ(40:60)薄膜中药物的累积释放率分别为42±2%和56±1%。不含药物的壳聚糖/聚(2-乙基-2-恶唑啉)薄膜对大肠杆菌显示出较弱的抗菌活性。载药的CHI和CHI/POZ薄膜对革兰氏阳性金黄色葡萄球菌和革兰氏阴性大肠杆菌均显示出良好的抗菌性能。使用拉伸法评估了这些薄膜对新鲜切除的绵羊阴道黏膜的黏膜粘附性能。结果表明,所有薄膜都具有黏膜粘附性,但共混物中POZ含量的增加导致其粘附于阴道黏膜的能力逐渐降低。这些薄膜在阴道给药方面可能具有应用潜力。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/02f3/7178655/3b0842c1bbc5/materials-13-01709-g001.jpg

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