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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.

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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