Evaluation of in Vitro Release Profile and Local Retention of Estradiol Vaginal Thermosensitive Gel
FU Xu-dong1, WANG Shan-shan2, CHEN Hu-hai1
1.Department of Pharmacy, Wuhan General Hospital of PLA Area,Wuhan 430070,China; 2.Department of Pharmacy, Xiangyang No.1 People Hospital,Xiangyang 441200,China
Abstract��OBJECTIVE To examine the in vitro release profile and in vivo retention of estradiol vaginal thermosensitive gel (E2-VTG).METHODS E2-VTISG was prepared by cold dissolving method.The dynamic membrane dialysis method and HPLC-fluorometric method were used to determine the in vitro release characteristic of the estradiol vaginal thermosensitive gel.CRi Maestro was applied to evaluate the retention of E2-VTG in ICR mice with IR820 as the fluorescent marker. RESULTS Estradiol could be released slowly from the thermosensitive gel and the release profile was fitted with Higuchi equation. It was speculated that estradiol was mainly released through diffusion.NIR imaging and fluorescence quantitative analysis showed that thermosensitive gel could reside in vagina for at least 8 h. CONCLUSION Estradiol thermosensitive gel can prolong the drug residence time in vagina and sustain the drug release rate.
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FU Xu-dong, WANG Shan-shan, CHEN Hu-hai. Evaluation of in Vitro Release Profile and Local Retention of Estradiol Vaginal Thermosensitive Gel. Chinese Pharmaceutical Journal, 2017, 52(10): 852-856.
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2017, Vol. 52 
