title: Optimization and evaluation of pluronic lecithin organogels as a transdermal delivery vehicle for sinomenine.
abstract: The purpose of the present study was to prepare and optimize sinomenine (SIN) pluronic lecithin organogels system (PLO), and to evaluate the permeability of the optimized PLO in vitro and in vivo. Box-Behnken design was used to optimize the PLO and the optimized formulation was pluronic F127 of 19.61%, lecithin of 3.60% and SIN of 1.27%. The formulation was evaluated its skin permeation and drug deposition both in vitro and in vivo compared with gel. Permeation and deposition studies of PLO were carried out with Franz diffusion cells in vitro and with microdialysis in vivo. In vitro studies, permeation rate (Jss) of SIN from PLO was 146.55 ± 2.93 μg/cm(2)/h, significantly higher than that of gel (120.39 μg/cm(2)/h) and the amount of SIN deposited in skin from the PLO was 10.08 ± 0.86 μg/cm(2), significantly larger than that from gel (6.01 ± 0.04 μg/cm(2)). In vivo skin microdialysis studies showed that the maximum concentration (Cmax) of SIN from PLO in "permeation study" and "drug-deposition study" were 150.27 ± 20.85 μg/ml and 67.95 μg/ml, respectively, both significantly higher than that of SIN from gel (29.66 and 6.73 μg/ml). The results recommend that PLO can be used as an advantageous transdermal delivery vehicle to enhance the permeation and skin deposition of SIN.
authors.affiliation: a School of Chinese Materia Medica, Guangzhou University of Chinese Medicine , Guangzhou , Guangdong , China.
authors.forename: Wenqiang
authors.initials: W
authors.lastname: Ba
authors.affiliation: a School of Chinese Materia Medica, Guangzhou University of Chinese Medicine , Guangzhou , Guangdong , China.
authors.forename: Zhou
authors.initials: Z
authors.lastname: Li
authors.affiliation: a School of Chinese Materia Medica, Guangzhou University of Chinese Medicine , Guangzhou , Guangdong , China.
authors.forename: Lisheng
authors.initials: L
authors.lastname: Wang
authors.affiliation: a School of Chinese Materia Medica, Guangzhou University of Chinese Medicine , Guangzhou , Guangdong , China.
authors.forename: Ding
authors.initials: D
authors.lastname: Wang
authors.affiliation: a School of Chinese Materia Medica, Guangzhou University of Chinese Medicine , Guangzhou , Guangdong , China.
authors.forename: Weiguo
authors.initials: W
authors.lastname: Liao
authors.affiliation: a School of Chinese Materia Medica, Guangzhou University of Chinese Medicine , Guangzhou , Guangdong , China.
authors.forename: Wentao
authors.initials: W
authors.lastname: Fan
authors.affiliation: a School of Chinese Materia Medica, Guangzhou University of Chinese Medicine , Guangzhou , Guangdong , China.
authors.forename: Yinai
authors.initials: Y
authors.lastname: Wu
authors.affiliation: a School of Chinese Materia Medica, Guangzhou University of Chinese Medicine , Guangzhou , Guangdong , China.
authors.forename: Fengyun
authors.initials: F
authors.lastname: Liao
authors.affiliation: a School of Chinese Materia Medica, Guangzhou University of Chinese Medicine , Guangzhou , Guangdong , China.
authors.forename: Jianye
authors.initials: J
authors.lastname: Yu
mesh_terms: D000279:Administration, Cutaneous; D000818:Animals; D018501:Antirheumatic Agents / Q000008:administration & dosage / Q000378:metabolism*; D016503:Drug Delivery Systems / Q000379:methods*; D004353:Drug Evaluation, Preclinical / Q000379:methods; D005782:Gels; D054709:Lecithins / Q000008:administration & dosage / Q000378:metabolism*; D008297:Male; D009019:Morphinans / Q000008:administration & dosage / Q000378:metabolism*; D009924:Organ Culture Techniques; D020442:Poloxamer / Q000008:administration & dosage / Q000378:metabolism*; D051381:Rats; D017207:Rats, Sprague-Dawley; D012869:Skin Absorption / Q000187:drug effects / Q000502:physiology*
chemical_list: D018501:Antirheumatic Agents; D005782:Gels; D054709:Lecithins; D009019:Morphinans; D020442:Poloxamer; C009271:sinomenine
keywords: Box–Behnken design; microdialysis; percutaneous permeation; pluronic lecithin organogels; sinomenine