Baicalein and hydroxypropyl-γ-cyclodextrin complex in poloxamer thermal sensitive hydrogel for vaginal administration.
The present study aimed to prepare a chemically and physically stable formulation of baicalein (Ba) in an in situ thermally sensitive hydrogel for vaginal administration. An inclusion complex of Ba and hydroxypropyl-γ-cyclodextrin (HP-γ-CD) was first developed to increase the stability and solubility of Ba in an aqueous solution. The formation of the Ba-HP-γ-CD complex was characterized by scanning electron microscopy (SEM), differential scanning calorimetry (DSC), and X-ray powder diffractometry (XRPD). Poloxamers 407, 188 (P407, P188), sodium alginate (SA), hydroxypropylmethylcellulose (HPMC), and benzalkonium bromide were mixed to obtain a hydrogel with an appropriate gelation temperature for vaginal use. Among the formulations examined, P407/Ba-HP-γ-CD/HPMC/P188/benzalkonium bromide (18/0.96/0.5/4.0/0.02%) represented the appropriate gelation temperature and acceptable drug release rate at the administration site. Release of Ba-HP-γ-CD from the poloxamer hydrogel followed Peppas equation, which suggests that it occurred through coupled corrosion-diffusion mechanism, and the corrosion-release curve showed that corrosion was the primary mode of release. In animal study, treatment by using Ba-HP-γ-CD thermosensitive hydrogel could produce a restoration of damaged tissues. Thermosensitive hydrogel formulation of the Ba-HP-γ-CD complex appears to be a promising treatment for cervicitis.
['Zhou|Qiuna|Q|', 'Zhong|Lin|L|', 'Wei|Xiaohui|X|', 'Dou|Wei|W|', 'Chou|Guixin|G|', 'Wang|Zhengtao|Z|']
D000282:Administration, Intravaginal D000464:Alginates D000818:Animals D000893:Anti-Inflammatory Agents D001548:Benzalkonium Compounds D001965:Bromides D002152:Calorimetry, Differential Scanning D002626:Chemistry, Pharmaceutical D004195:Disease Models, Animal D004337:Drug Carriers D004355:Drug Stability D005260:Female D044950:Flavanones D020723:Glucuronic Acid D006603:Hexuronic Acids D006801:Humans D020100:Hydrogels D065347:Hypromellose Derivatives D007700:Kinetics D008747:Methylcellulose D008855:Microscopy, Electron, Scanning D020442:Poloxamer D033362:Powder Diffraction D017207:Rats, Sprague-Dawley D012995:Solubility D013678:Technology, Pharmaceutical D013696:Temperature D002575:Uterine Cervicitis D014961:X-Ray Diffraction D047408:gamma-Cyclodextrins
Baicalein Hydroxypropyl-γ-cyclodextrin Thermosensitive Cervicitis Vaginal hydrogel