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载药纳米乳凝胶的灭菌黄烷酮制剂优化及其创伤愈合活性评价。

Formulation optimization of sterilized xanthones-loaded nanoemulgels and evaluation of their wound healing activities.

机构信息

Thammasat University Research Unit in Drug, Health Product Development and Application (DHP-DA), Department of Pharmaceutical Sciences, Faculty of Pharmacy, Thammasat University, Pathum Thani 12120, Thailand.

Thammasat University Research Unit in Drug, Health Product Development and Application (DHP-DA), Department of Pharmaceutical Sciences, Faculty of Pharmacy, Thammasat University, Pathum Thani 12120, Thailand.

出版信息

Int J Pharm. 2023 Apr 5;636:122812. doi: 10.1016/j.ijpharm.2023.122812. Epub 2023 Mar 7.

DOI:10.1016/j.ijpharm.2023.122812
PMID:36894040
Abstract

Xanthones (XTs) are bioactive compounds found in mangosteen trees (Garcinia mangostana Linn.). They are used as an active ingredient in various health products. However, there is a lack of data of their application in wound healing. In particular, the topical products of XTs for wound healing; they should be sterilized to minimize the risks of wound infection from contaminated microorganisms. This study thus aimed to optimize the formulation of sterilized XTs-loaded nanoemulgel (XTs-NE-G) and to investigate their wound healing activities. The XTs-NE-Gs were prepared by mixing various gels containing sodium alginate (Alg) and Pluronic F127 (F127) into a XTs-nanoemulsion (NE) concentrate according to the face-centered central composite design. The results showed that the optimized XTs-NE-G was A5-F3 containing 5% w/w Alg and 3% w/w F127. It enhanced the proliferation-, migration rates of skin fibroblasts (HFF-1 cells) with an optimal viscosity. After blending the XTs-NE concentrate and the gel that was previously sterilized by a membrane filtration and an autoclaving technique, respectively, the sterilized A5-F3 was obtained. The sterilized A5-F3 still had effective bioactivities towards the HFF-1 cells. It promoted re-epithelialization, collagen deposition and inflammation suppression in the mice' wounds. It could thus be accepted for further investigation in clinical studies.

摘要

柚皮素(XTs)是存在于藤黄树( Garcinia mangostana Linn. )中的生物活性化合物。它们被用作各种保健品的有效成分。然而,关于它们在伤口愈合中的应用的数据却很少。特别是用于伤口愈合的 XTs 局部产品;为了尽量减少因受污染的微生物引起的伤口感染的风险,它们应该经过消毒。因此,本研究旨在优化消毒的 XTs 负载纳米乳凝胶(XTs-NE-G)的配方,并研究其伤口愈合活性。通过根据面心中央组合设计将含有海藻酸钠(Alg)和 Pluronic F127(F127)的各种凝胶混合到 XTs-纳米乳液(NE)浓缩物中,制备了 XTs-NE-Gs。结果表明,优化的 XTs-NE-G 为 A5-F3,含有 5%w/wAlg 和 3%w/wF127。它通过增加皮肤成纤维细胞(HFF-1 细胞)的增殖率和迁移率,以及最佳的粘度来增强其生物活性。在将 XTs-NE 浓缩物与先前分别通过膜过滤和高压灭菌技术消毒的凝胶混合后,得到了消毒的 A5-F3。消毒的 A5-F3 仍然对 HFF-1 细胞具有有效的生物活性。它能促进小鼠伤口的上皮再形成、胶原沉积和炎症抑制。因此,它可以进一步接受临床研究的调查。

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