姜黄素固体分散体原位凝胶用于局部治疗受损阴道细菌感染和改善阴道创伤愈合。

Curcumin solid dispersion-loaded in situ hydrogels for local treatment of injured vaginal bacterial infection and improvement of vaginal wound healing.

机构信息

Institute of Pharmacy, Pharmaceutical College of Henan University, Kaifeng, China.

Department of Pharmaceutical Sciences, Beijing Institute of Radiation Medicine, Beijing, China.

出版信息

J Pharm Pharmacol. 2019 Jul;71(7):1044-1054. doi: 10.1111/jphp.13088. Epub 2019 Mar 18.

Abstract

OBJECTIVES

Injured vaginal infection is detrimental to women. A curcumin hydrogel was studied for local treatment of injured vaginal infection.

METHODS

Curcumin solid dispersions (CSDs) were prepared from polyvinyl pyrrolidone and characterized by differential scanning calorimetry and an X-ray diffraction method. An in situ hydrogel CSD hydrogel (CSDG) was prepared with CSD/poloxamers and characterized. In vitro curcumin release and antibacterial effects of CSDs, CSDGs and curcumin were compared. The therapeutic effect of the CSDGs and Lincomycin/Lidocaine Gel was explored after intravaginal administration on the injured rat vaginal infection models.

KEY FINDINGS

Curcumin was amorphous in CSDs where curcumin rapidly released in simulated vaginal fluids. However, CSDGs showed sustained release. CSDGs quickly formed gels in the vagina. CSDGs showed high in vivo anti-Escherichia coli or Staphylococcus aureus effect though weak in vitro effect. The recovery of vaginal microenvironment and improvement of intravaginal Lactobacillus growth may be the major reason. Furthermore, CSDGs remarkably improved vaginal wound healing by alleviating inflammation and restoring vaginal epidermal tissues compared with the Lincomycin/Lidocaine Gel.

CONCLUSION

CSDGs are a promising topical formulation for local treatment of vaginal bacterial infection and improvement of vaginal wound healing.

摘要

目的

阴道损伤感染对女性有害。本研究旨在探讨姜黄素水凝胶对阴道损伤感染的局部治疗作用。

方法

采用聚乙烯吡咯烷酮制备姜黄素固体分散体(CSD),并通过差示扫描量热法和 X 射线衍射法进行表征。采用 CSD/泊洛沙姆制备原位水凝胶 CSD 水凝胶(CSDG),并对其进行表征。比较 CSD、CSDG 和姜黄素的体外累积释放和抗菌效果。通过阴道内给药,研究 CSDG 和林可霉素/利多卡因凝胶对损伤大鼠阴道感染模型的治疗效果。

主要发现

CSD 中姜黄素为无定形,在模拟阴道液中迅速释放姜黄素。然而,CSDG 则表现出持续释放。CSDG 在阴道中迅速形成凝胶。CSDG 在体内对大肠杆菌或金黄色葡萄球菌具有较高的抗菌效果,尽管体外效果较弱。恢复阴道微环境和增加阴道内乳杆菌生长可能是主要原因。此外,CSDG 可通过减轻炎症和恢复阴道表皮组织,显著改善阴道伤口愈合,优于林可霉素/利多卡因凝胶。

结论

CSDG 是一种有前途的局部治疗阴道细菌感染和改善阴道伤口愈合的局部给药制剂。

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