用甲基丙烯酰化、巴豆酰化和伊塔康酰化明胶与聚乙烯醇共混物制备甲硝唑阴道黏附膜

IF 3.4 4区 医学 Q2 PHARMACOLOGY & PHARMACY
Elvira O. Shatabayeva, Daulet B. Kaldybekov, Zarina A. Kenessova, Rysgul N. Tuleyeva, Sarkyt E. Kudaibergenov, Vitaliy V. Khutoryanskiy
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引用次数: 0

摘要

目的:本工作报道了明胶或其化学改性衍生物(巴豆酰化、衣康酰化和甲基丙烯酰化明胶)与聚乙烯醇(PVA)混合而成的聚合物薄膜的研制和表征。在这些配方中,甲硝唑是一种抗菌药物。方法采用聚合物溶液浇铸,溶剂蒸发法制备薄膜。利用傅里叶变换红外光谱、扫描电镜和力学性能测试对其结构和理化性质进行了研究。并对膜的厚度、折叠耐久性、表面pH值和透明度进行了评价。通过离体分离技术评估膜的粘接性能,该技术涉及新鲜切除的绵羊阴道组织。采用Franz扩散细胞进行体外累积释药研究。结果与天然明胶相比,加入不饱和官能团能改善明胶的粘接性能。体外释药实验表明,纯明胶/PVA膜的累积释药量为49±2%,而改性明胶/PVA膜(70:30)的累积释药量为~ 64-71%。结论改性明胶可作为阴道给药黏附制剂的有效赋形剂,在其他经黏膜给药系统中具有广阔的应用前景。图形抽象
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Development of Mucoadhesive Vaginal Films for Metronidazole Delivery Using Methacryloylated, Crotonoylated, and Itaconoylated Gelatin Blends with Poly(vinyl alcohol)

Purpose

This work reports the development and characterisation of polymeric films composed of gelatin or its chemically modified derivatives (crotonoylated, itaconoylated, and methacryloylated gelatins) blended with polyvinyl alcohol (PVA). Metronidazole served as an antimicrobial drug in these formulations.

Methods

The films were produced by casting aqueous solutions of polymers, followed by solvent evaporation. Their structure and physicochemical characteristics were studied using Fourier transform infrared spectroscopy, scanning electron microscopy, and mechanical testing. The thickness of the films, their folding endurance, the surface pH, and transparency were also evaluated. The mucoadhesive performance of the films was evaluated through an ex vivo detachment technique involving freshly excised sheep vaginal tissues. In vitro cumulative drug release studies were conducted using Franz diffusion cells.

Results

The results demonstrate that incorporating unsaturated functional groups into gelatin improves its mucoadhesive properties compared to native gelatin. The drug release experiments conducted in vitro showed that the cumulative release from pure gelatin/PVA films was found to be 49 ± 2%, whereas modified gelatins/PVA (70:30) films released ~ 64–71%.

Conclusion

These findings suggest that modified gelatins could serve as effective excipients in designing mucoadhesive formulations for vaginal administration, with potential applications extending to other transmucosal drug delivery systems.

Graphical Abstract

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来源期刊
AAPS PharmSciTech
AAPS PharmSciTech 医学-药学
CiteScore
6.80
自引率
3.00%
发文量
264
审稿时长
2.4 months
期刊介绍: AAPS PharmSciTech is a peer-reviewed, online-only journal committed to serving those pharmaceutical scientists and engineers interested in the research, development, and evaluation of pharmaceutical dosage forms and delivery systems, including drugs derived from biotechnology and the manufacturing science pertaining to the commercialization of such dosage forms. Because of its electronic nature, AAPS PharmSciTech aspires to utilize evolving electronic technology to enable faster and diverse mechanisms of information delivery to its readership. Submission of uninvited expert reviews and research articles are welcomed.
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