title: A novel elastic liposome for skin delivery of papain and its application on hypertrophic scar.
abstract: This study aims to investigate the therapeutic effects of papain elastic liposomes (PEL) on hypertrophic scar through topical application. PEL were prepared using the reverse-phase evaporation method and optimized by response surface methodology. The transdermal absorption of optimized PEL was tested by vertical Franz diffusion cells in vitro. The effects of PEL were investigated in rabbit model of hypertrophic scar in vivo, histological analysis and scar-related proteins were detected to reveal potential scar repair mechanism. The best formulation of PEL had EE (43.8±1.4%), particle size (100.9±2.2nm), PDI (0.037±0.003), zeta potential (-26.3±1.3mV), and DI (21.9±3.1). PEL gave the cumulative amounts and steady state fluxes in the receiver solution of 381.9±32.4μg/cm2, 11.4±1.5μg/cm2/h, and showed drug deposition in skin of 19.1±3.2% after 24h. After topical application, the scar elevation index, microvascular density, and collagen fiber were significantly decreased with regular arrangement. The expressions of TGF-β1, P-Smad-3, P-NF-κB p65, and P-IKBa in hypertrophic scar were significantly down regulated in contrast with those in model group. PEL were proven as an excellent topical preparation for hypertrophic scar treatment.
authors.affiliation: College of Basic Medical, Nanjing University of Chinese Medicine, Nanjing 210023, China; Yunnan Baiyao Group Wuxi Pharmaceutical Co., Ltd., Wuxi 214028, China.
authors.forename: Yan-Yan
authors.initials: YY
authors.lastname: Chen
authors.affiliation: Yunnan Baiyao Group Wuxi Pharmaceutical Co., Ltd., Wuxi 214028, China; Yunnan Institute of Materia Medica, Yunnan 650111, China.
authors.forename: Ye-Hui
authors.initials: YH
authors.lastname: Lu
authors.affiliation: College of Basic Medical, Nanjing University of Chinese Medicine, Nanjing 210023, China.
authors.forename: Chun-Hua
authors.initials: CH
authors.lastname: Ma
authors.affiliation: College of Basic Medical, Nanjing University of Chinese Medicine, Nanjing 210023, China.
authors.forename: Wei-Wei
authors.initials: WW
authors.lastname: Tao
authors.affiliation: College of Basic Medical, Nanjing University of Chinese Medicine, Nanjing 210023, China; Yunnan Baiyao Group Wuxi Pharmaceutical Co., Ltd., Wuxi 214028, China.
authors.forename: Jing-Juan
authors.initials: JJ
authors.lastname: Zhu
authors.affiliation: College of Basic Medical, Nanjing University of Chinese Medicine, Nanjing 210023, China. Electronic address: zhangxutcm@gmail.com.
authors.forename: Xu
authors.initials: X
authors.lastname: Zhang
mesh_terms: D000818:Animals; D017439:Cicatrix, Hypertrophic / Q000188:drug therapy* / Q000378:metabolism; D016503:Drug Delivery Systems / Q000379:methods*; D004548:Elasticity; D008081:Liposomes; D008297:Male; D009924:Organ Culture Techniques; D010206:Papain / Q000008:administration & dosage* / Q000378:metabolism; D011817:Rabbits; D011897:Random Allocation; D051381:Rats; D017207:Rats, Sprague-Dawley; D012867:Skin / Q000187:drug effects* / Q000378:metabolism
chemical_list: D008081:Liposomes; D010206:Papain
keywords: Elastic liposomes; Hypertrophic scar; Papain; Transdermal absorption