title: Transdermal baicalin delivery using diethylene glycol monoethyl ether-mediated cubic phase gel.
abstract: This study investigated the transdermal permeability of baicalin, a hydrophobic and readily hydrolyzed drug, delivered by glyceryl monooleate (GMO)-based cubic phase gel (CPG) mediated with Transcotol(®) P (TP, diethylene glycol monoethyl ether). A range of CPGs was produced by varying GMO, water, and TP levels. Examination of their physicochemical properties revealed that the optically isotropic CPG showed higher viscosity than lamellar phase gels (LPG), and the baicalin cargo increased CPG viscosity. The GMO:TP ratio and water content also altered viscosity. CPG-mediated delivery increased baicalin's skin permeation, with 76.65- to 200.24-fold higher (p<0.05) transdermal flux than that of a Carbopol(®)-based hydrogel (HDG), and 6.72- to 17.55-fold (p<0.05) higher than that of LPG, with the same water content. Rat in vivo microdialysis showed that CPG produced sustained baicalin release, with superior pharmacokinetic parameters to those of HDG. Furthermore, cutaneous drug absorption was more efficient on rat abdominal skin, compared to that in the chest or scapular region. Effective fusion between the CPG lipid matrix and the stratum corneum may explain this enhancement of transdermal permeation. CPG containing TP therefore, achieved excellent transdermal drug delivery and good baicalin stability, indicating that this system represents a promising transdermal delivery vehicle.
authors.affiliation: Department of Pharmaceutical Sciences, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China.
authors.forename: Yongtai
authors.initials: Y
authors.lastname: Zhang
authors.affiliation: Department of Pharmaceutical Sciences, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China.
authors.forename: Kai
authors.initials: K
authors.lastname: Zhang
authors.affiliation: Department of Pharmaceutical Sciences, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China.
authors.forename: Teng
authors.initials: T
authors.lastname: Guo
authors.affiliation: Department of Pharmaceutical Sciences, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China.
authors.forename: Yuan
authors.initials: Y
authors.lastname: Li
authors.affiliation: Department of Pharmaceutical Sciences, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China.
authors.forename: Chunyun
authors.initials: C
authors.lastname: Zhu
authors.affiliation: Department of Pharmaceutical Sciences, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China. Electronic address: npfeng@hotmail.com.
authors.forename: Nianping
authors.initials: N
authors.lastname: Feng
mesh_terms: D000279:Administration, Cutaneous; D000818:Animals; D004355:Drug Stability; D005026:Ethylene Glycols / Q000008:administration & dosage* / Q000737:chemistry / Q000494:pharmacology; D005419:Flavonoids / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D005782:Gels; D005989:Glycerides / Q000008:administration & dosage* / Q000737:chemistry / Q000494:pharmacology; D066298:In Vitro Techniques; D008297:Male; D008819:Mice, Nude; D017551:Microdialysis; D017207:Rats, Sprague-Dawley; D012867:Skin / Q000378:metabolism; D012869:Skin Absorption
chemical_list: D005026:Ethylene Glycols; D005419:Flavonoids; D005782:Gels; D005989:Glycerides; C038044:baicalin; C010111:carbitol; C005953:monoolein
keywords: Cutaneous absorption; Liquid crystalline phase; Microdialysis; Monoglyceride; Permeability