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微针介导的维生素C经皮给药:制剂、表征、细胞毒性及稳定性增强

Microneedles mediated-dermal delivery of Vitamin C: Formulation, characterization, cytotoxicity, and enhancement of stability.

作者信息

Hamed Rania, AbuKwiak Amani D, Aburayya Rafa, Alkilani Ahlam Zaid, Hamadneh Lama, Naser Mais, Al-Adhami Yasmeen, Alhusban Ala A

机构信息

Department of Pharmacy, Faculty of Pharmacy, Al-Zaytoonah University of Jordan, Jordan, Amman, 11733, Jordan.

Department of Pharmacy, Faculty of Pharmacy, Zarqa University, Zarqa, Zarqa, 13110, Jordan.

出版信息

Heliyon. 2024 Sep 3;10(17):e37381. doi: 10.1016/j.heliyon.2024.e37381. eCollection 2024 Sep 15.

Abstract

Vitamin C (VIT C) is an antioxidant that prevents skin aging. Although dermal delivery is one of the most effective routes to transport VIT C to the skin, the impact of this route can be limited by the barrier function of the (SC). Additionally, VIT C rapidly oxidized and degraded under light and temperature. Therefore, this study provides an approach to utilizing microneedles (MNs) to improve the dermal delivery of VIT C and enhance its stability by incorporating a stabilizing system of ethylenediaminetetraacetic acid (EDTA) and sodium metabisulfite (Meta) within the MNs. Vitamin C microneedles (VIT C MNs) were fabricated using different biodegradable polymers and various concentrations of EDTA/Meta. VIT C MNs were evaluated for morphology, VIT C content, mechanical properties, dissolution rate, needles' insertion, physicochemical properties, permeation, viscosity of VIT C polymeric solutions, cytotoxicity, and stability. The results showed that VIT C MNs were uniform and mechanically strong. The recovery of VIT C in MNs was 88.3-90.0 %. The dissolution rate of MNs was <30 min. The flux of VIT C varied based on the composition of MNs. VIT C MNs demonstrated safety against human dermal fibroblasts. VIT C MNs with EDTA/Meta (0.1/0.3 %) were stable under different storage conditions for two months. In conclusion, VIT C MNs were successfully developed using biodegradable polymers, and the stabilizing system (EDTA/META) provided a stable dermal delivery system for VIT C to protect skin from aging.

摘要

维生素C(VIT C)是一种抗氧化剂,可防止皮肤衰老。尽管经皮给药是将VIT C输送到皮肤的最有效途径之一,但该途径的效果可能会受到角质层(SC)屏障功能的限制。此外,VIT C在光照和温度下会迅速氧化和降解。因此,本研究提供了一种利用微针(MNs)来改善VIT C经皮给药并通过在微针中加入乙二胺四乙酸(EDTA)和焦亚硫酸钠(Meta)的稳定系统来提高其稳定性的方法。使用不同的可生物降解聚合物和不同浓度的EDTA/Meta制备了维生素C微针(VIT C MNs)。对VIT C MNs的形态、VIT C含量、机械性能、溶解速率、针的插入情况、物理化学性质、渗透情况、VIT C聚合物溶液的粘度、细胞毒性和稳定性进行了评估。结果表明,VIT C MNs形态均匀且机械强度高。微针中VIT C的回收率为88.3-90.0%。微针的溶解速率<30分钟。VIT C的通量因微针的组成而异。VIT C MNs对人皮肤成纤维细胞显示出安全性。含有EDTA/Meta(0.1/0.3%)的VIT C MNs在不同储存条件下两个月内保持稳定。总之,使用可生物降解聚合物成功开发了VIT C MNs,稳定系统(EDTA/META)为VIT C提供了一个稳定的经皮给药系统,以保护皮肤免受衰老。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e16c/11407233/f515a4fec70d/ga1.jpg

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