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基于细菌纳米纤维素的局部药物递送系统:加速稳定性测试。

Topical Drug Delivery Systems Based on Bacterial Nanocellulose: Accelerated Stability Testing.

机构信息

CICECO-Aveiro Institute of Materials, Department of Chemistry, University of Aveiro, 3810-193 Aveiro, Portugal.

CBIOS-Research Center for Biosciences and Health Technologies, Lusófona University, Campo Grande 376, 1749-024 Lisbon, Portugal.

出版信息

Int J Mol Sci. 2020 Feb 13;21(4):1262. doi: 10.3390/ijms21041262.

Abstract

Bacterial nanocellulose (BNC) membranes have enormous potential as systems for topical drug delivery due to their intrinsic biocompatibility and three-dimensional nanoporous structure, which can house all kinds of active pharmaceutical ingredients (APIs). Thus, the present study investigated the long-term storage stability of BNC membranes loaded with both hydrophilic and lipophilic APIs, namely, caffeine, lidocaine, ibuprofen and diclofenac. The storage stability was evaluated under accelerated testing conditions at different temperatures and relative humidity (RH), i.e., 75% RH/40 °C, 60% RH/25 °C and 0% RH/40 °C. All systems were quite stable under these storage conditions with no significant structural and morphological changes or variations in the drug release profile. The only difference observed was in the moisture-uptake, which increased with RH due to the hydrophilic nature of BNC. Furthermore, the caffeine-loaded BNC membrane was selected for in vivo cutaneous compatibility studies, where patches were applied in the volar forearm of twenty volunteers for 24 h. The cutaneous responses were assessed by non-invasive measurements and the tests revealed good compatibility for caffeine-loaded BNC membranes. These results highlight the good storage stability of the API-loaded BNC membranes and their cutaneous compatibility, which confirms the real potential of these dermal delivery systems.

摘要

细菌纳米纤维素 (BNC) 膜由于其内在的生物相容性和三维纳米多孔结构,具有作为局部药物递送系统的巨大潜力,可容纳各种活性药物成分 (API)。因此,本研究考察了同时负载亲水性和疏水性 API(即咖啡因、利多卡因、布洛芬和双氯芬酸)的 BNC 膜的长期储存稳定性。在不同温度和相对湿度 (RH)(即 75% RH/40°C、60% RH/25°C 和 0% RH/40°C)的加速测试条件下评估了储存稳定性。所有系统在这些储存条件下都非常稳定,没有明显的结构和形态变化,也没有药物释放曲线的变化。唯一观察到的差异是水分吸收,由于 BNC 的亲水性,水分吸收随 RH 增加而增加。此外,选择负载咖啡因的 BNC 膜进行体内皮肤相容性研究,将贴片应用于二十名志愿者的掌侧前臂 24 小时。通过非侵入性测量评估皮肤反应,测试结果表明负载咖啡因的 BNC 膜具有良好的相容性。这些结果突出了 API 负载的 BNC 膜的良好储存稳定性及其皮肤相容性,证实了这些经皮递送系统的实际潜力。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1d6d/7072910/827bf31a852d/ijms-21-01262-g001.jpg

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