title: Baicalein and hydroxypropyl-γ-cyclodextrin complex in poloxamer thermal sensitive hydrogel for vaginal administration.
abstract: 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.
authors.affiliation: The MOE Key Laboratory for Standardization of Chinese Medicines and the SATCM Key Laboratory for New Resources and Quality Evaluation of Chinese Medicines, Institute of Chinese Materia Medica, Shanghai University of Traditional Chinese Medicine, Shanghai 201210, China.
authors.forename: Qiuna
authors.initials: Q
authors.lastname: Zhou
authors.forename: Lin
authors.initials: L
authors.lastname: Zhong
authors.forename: Xiaohui
authors.initials: X
authors.lastname: Wei
authors.forename: Wei
authors.initials: W
authors.lastname: Dou
authors.forename: Guixin
authors.initials: G
authors.lastname: Chou
authors.forename: Zhengtao
authors.initials: Z
authors.lastname: Wang
mesh_terms: D000282:Administration, Intravaginal; D000464:Alginates / Q000737:chemistry; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000008:administration & dosage* / Q000737:chemistry; D001548:Benzalkonium Compounds / Q000737:chemistry; D001965:Bromides / Q000737:chemistry; D002152:Calorimetry, Differential Scanning; D002626:Chemistry, Pharmaceutical; D004195:Disease Models, Animal; D004337:Drug Carriers; D004355:Drug Stability; D005260:Female; D044950:Flavanones / Q000008:administration & dosage* / Q000737:chemistry; D020723:Glucuronic Acid / Q000737:chemistry; D006603:Hexuronic Acids / Q000737:chemistry; D006801:Humans; D020100:Hydrogels; D065347:Hypromellose Derivatives; D007700:Kinetics; D008747:Methylcellulose / Q000031:analogs & derivatives / Q000737:chemistry; D008855:Microscopy, Electron, Scanning; D020442:Poloxamer / Q000737:chemistry*; D033362:Powder Diffraction; D017207:Rats, Sprague-Dawley; D012995:Solubility; D013678:Technology, Pharmaceutical / Q000379:methods; D013696:Temperature; D002575:Uterine Cervicitis / Q000188:drug therapy / Q000473:pathology; D014961:X-Ray Diffraction; D047408:gamma-Cyclodextrins / Q000737:chemistry*
chemical_list: D000464:Alginates; D000893:Anti-Inflammatory Agents; D001548:Benzalkonium Compounds; D001965:Bromides; D004337:Drug Carriers; D044950:Flavanones; D006603:Hexuronic Acids; D020100:Hydrogels; D047408:gamma-Cyclodextrins; C479659:hydroxypropyl-gamma-cyclodextrin; D020442:Poloxamer; D065347:Hypromellose Derivatives; C006680:baicalein; D020723:Glucuronic Acid; D008747:Methylcellulose
keywords: Baicalein; Cervicitis; Hydroxypropyl-γ-cyclodextrin; Thermosensitive; Vaginal hydrogel