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用于阴道给药的负载棕榈酸视黄酯和酮咯酸的羟丙基甲基纤维素及聚乙二醇400黏膜黏附膜的特性研究

Characterization of HPMC and PEG 400 Mucoadhesive Film Loaded with Retinyl Palmitate and Ketorolac for Intravaginal Administration.

作者信息

Hernández-González Maryel E, Rodríguez-González Claudia A, Valencia-Gómez Laura E, Hernández-Paz Juan F, Jiménez-Vega Florida, Salcedo Mauricio, Olivas-Armendáriz Imelda

机构信息

Departamento de Física y Matemáticas, Instituto de Ingeniería y Tecnología, Universidad Autónoma de Ciudad Juárez, Ciudad Juárez 32320, Mexico.

Departamento de Ciencias Químico Biológicas, Instituto de Ciencias Biomédicas, Universidad Autónoma de Ciudad Juárez, Ciudad Juárez 32315, Mexico.

出版信息

Int J Mol Sci. 2024 Nov 26;25(23):12692. doi: 10.3390/ijms252312692.

DOI:10.3390/ijms252312692
PMID:39684402
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11641465/
Abstract

Intravaginal drug administration offers several advantages over other routes, primarily bypassing the initial stages of metabolism. Additionally, this route has demonstrated both local and systemic effects. Mucoadhesive polymeric systems can be utilized to prevent dose loss due to the mucous barriers and the formation of wet cavities. This study employed various techniques to evaluate the performance and characteristics of a mucoadhesive film composed of HPMC-PEG 400 containing retinyl palmitate and ketorolac molecules. Scanning Electron Microscopy (SEM) was employed to analyze the porous structure of the film. Thermogravimetric Analysis (TGA) was conducted at different temperatures to assess thermal stability. Fourier Transform Infrared Spectroscopy (FTIR) was used to analyze the functional groups and intermolecular interactions between the film and the drug. Swelling and weight loss tests indicated that the film disintegrated within 3-4 days. UV-VIS spectroscopy was used for drug release evaluation based on the Higuchi equation. Additionally, the surface wetting properties were assessed through contact angle measurements. The system's biocompatibility was confirmed using the MTT assay. Finally, adhesion and glide tests demonstrated the film's interaction with porcine uterine tissue. This study shows that the HPMC-PEG 400 film containing retinyl palmitate molecules interacts effectively with tissue and could be considered a novel tool for treating damaged epithelial tissues.

摘要

与其他给药途径相比,阴道内给药具有多种优势,主要是绕过了代谢的初始阶段。此外,这种给药途径已显示出局部和全身作用。可利用粘膜粘附聚合物系统来防止由于粘液屏障和湿腔形成导致的剂量损失。本研究采用了各种技术来评估由含有棕榈酸视黄酯和酮咯酸分子的HPMC-PEG 400组成的粘膜粘附膜的性能和特性。使用扫描电子显微镜(SEM)分析膜的多孔结构。在不同温度下进行热重分析(TGA)以评估热稳定性。利用傅里叶变换红外光谱(FTIR)分析膜与药物之间的官能团和分子间相互作用。膨胀和失重测试表明该膜在3-4天内崩解。基于Higuchi方程,使用紫外-可见光谱进行药物释放评估。此外,通过接触角测量评估表面润湿性。使用MTT试验确认了该系统的生物相容性。最后,粘附和滑动测试证明了该膜与猪子宫组织的相互作用。这项研究表明,含有棕榈酸视黄酯分子的HPMC-PEG 400膜与组织有效相互作用,可被视为治疗受损上皮组织的一种新型工具。

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