基于微乳液的藜芦醇热敏水凝胶可用于阴道炎症的局部治疗

IF 4.3 4区 医学 Q1 PHARMACOLOGY & PHARMACY Journal of Drug Targeting Pub Date : 2024-04-01 Epub Date: 2024-02-12 DOI:10.1080/1061186X.2024.2310879
Jiaxin Liu, Liuqi Zhou, Huijing Cong, Jing Hu, Jingling Tang
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引用次数: 0

摘要

阴道炎是一种常见的妇科疾病。如果不及时治疗,有可能扩散到泌尿和生殖系统。在这项研究中,我们提出了一种负载白藜芦醇的微乳液型热敏水凝胶(Res-Me-Tsgel),并将其与壳聚糖水凝胶型 Res-Me-Cogel 进行了比较。我们制备的 Res-Me-Tsgel 在室温下是透明的液态溶液,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都具有卓越的持续释放特性。体外和体内研究都证实了 Res-Me-Cogel 和 Res-Me-Tsgel 极佳的生物安全性。大鼠经阴道服用这些制剂后,白藜芦醇可在阴道内长期存留。值得注意的是,由于给药后白藜芦醇流入阴道褶皱的情况有所改善,在给药后 24 小时,Res-Me-Tsgel 组的白藜芦醇保留率比 Res-Me-Cogel 组高约三倍。总之,这些研究结果突出表明,Res-Me-Tsgel 有可能成为治疗阴道炎症的一种有效方法。
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Resveratrol-loaded microemulsion based thermosensitive hydrogel for potential topical treatment of the vaginal inflammation.

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.

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来源期刊
CiteScore
9.10
自引率
0.00%
发文量
165
审稿时长
2 months
期刊介绍: Journal of Drug Targeting publishes papers and reviews on all aspects of drug delivery and targeting for molecular and macromolecular drugs including the design and characterization of carrier systems (whether colloidal, protein or polymeric) for both vitro and/or in vivo applications of these drugs. Papers are not restricted to drugs delivered by way of a carrier, but also include studies on molecular and macromolecular drugs that are designed to target specific cellular or extra-cellular molecules. As such the journal publishes results on the activity, delivery and targeting of therapeutic peptides/proteins and nucleic acids including genes/plasmid DNA, gene silencing nucleic acids (e.g. small interfering (si)RNA, antisense oligonucleotides, ribozymes, DNAzymes), as well as aptamers, mononucleotides and monoclonal antibodies and their conjugates. The diagnostic application of targeting technologies as well as targeted delivery of diagnostic and imaging agents also fall within the scope of the journal. In addition, papers are sought on self-regulating systems, systems responsive to their environment and to external stimuli and those that can produce programmed, pulsed and otherwise complex delivery patterns.
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