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载白藜芦醇的微乳型温敏水凝胶用于阴道炎症的潜在局部治疗。

Resveratrol-loaded microemulsion based thermosensitive hydrogel for potential topical treatment of the vaginal inflammation.

机构信息

School of Pharmacy, Harbin Medical University, Harbin, China.

出版信息

J Drug Target. 2024 Apr;32(4):404-412. doi: 10.1080/1061186X.2024.2310879. Epub 2024 Feb 12.

Abstract

BACKGROUND

Vaginal inflammation is a prevalent gynecological condition. If left untreated, it can potentially spread to the urinary and reproductive systems.

METHODS

In this study, we propose a resveratrol-loaded microemulsion-based thermosensitive hydrogel (Res-Me-Tsgel) and compare it with a chitosan hydrogel-based Res-Me-Cogel. We characterized the different characters of Res-Me-Tsgel. The safety of Res-Me-Tsgel was also evaluated in vitro and in vivo. Finally, we measured the retention of Res in the vagina after drug administration.

RESULTS

The Res-Me-Tsgel we prepared is a transparent liquid solution at room temperature that rapidly forms a gel at 37oC. Compared to Res solution and Res-Me, both Res-Me-Cogel and Res-Me-Tsgel demonstrate superior sustained release properties. Both in vitro and in vivo studies confirm the excellent biosafety profile of Res-Me-Cogel and Res-Me-Tsgel. Vaginal administration of these formulations in rats results in prolonged retention of resveratrol within the vagina. Notably, due to its improved flow into vaginal folds after administration, the retention of Resveratrol was approximately three times higher for the Res-Me-Tsgel group compared to the Res-Me-Cogel group at 24 h post-administration. Overall, these findings highlight the potential application of Res-Me-Tsgel as an effective means for vaginal inflammation.

CONCLUSIONS

We developed a novel micromulsion based thermosensitive hydrogel for the delivery of Res. The sustained release of Res and favorable vaginal retention from Res-Me-Tsgel make them promise as a potential candidate for local intravaginal therapy.

摘要

背景

阴道炎症是一种常见的妇科疾病。如果不加以治疗,它可能会扩散到泌尿系统和生殖系统。

方法

在这项研究中,我们提出了一种负载白藜芦醇的微乳基温敏水凝胶(Res-Me-Tsgel),并将其与壳聚糖水凝胶基 Res-Me-Cogel 进行了比较。我们对不同特性的 Res-Me-Tsgel 进行了表征。还在体外和体内评估了 Res-Me-Tsgel 的安全性。最后,测量了给药后 Res 在阴道中的保留情况。

结果

我们制备的 Res-Me-Tsgel 在室温下是一种透明的液体溶液,在 37°C 时迅速形成凝胶。与 Res 溶液和 Res-Me 相比,Res-Me-Cogel 和 Res-Me-Tsgel 都表现出更好的持续释放性能。体外和体内研究均证实了 Res-Me-Cogel 和 Res-Me-Tsgel 的优异生物安全性。这些制剂在大鼠阴道中的给药导致 Resveratrol 在阴道内的保留时间延长。值得注意的是,由于给药后其更容易进入阴道褶皱,与 Res-Me-Cogel 组相比,Res-Me-Tsgel 组在给药后 24 小时时 Resveratrol 的保留量约高 3 倍。总体而言,这些发现强调了 Res-Me-Tsgel 作为阴道炎症有效治疗方法的潜力。

结论

我们开发了一种用于输送 Res 的新型微乳基温敏水凝胶。Res 的持续释放和 Res-Me-Tsgel 从阴道中的良好保留使它们成为局部阴道内治疗的潜在候选药物。

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