title: Transdermal evaporation delivery system of praziquantel for schistosomiasis japonicum chemotherapy.
abstract: A transdermal evaporation delivery system (TEDS) of praziquantel (PZQ) was developed by selecting ethylene glycol monophenyl ether as a nonvolatile component solvent and ethanol as a volatile component solvent to control efficiently the transmission and morbidity of the global schistosomiasis, providing a convenient administration system of PZQ for both humans and domestic animals. The solubility of PZQ in TEDS was more than 400 mg/mL when the ethanol concentration was 50% (w/w) in the solvent mixture at 32 °C, enabling to adapt requirements for the treatment of schistosomiasis. The highest serum drug concentration reached 35.93 µg/mL after transdermal administration of TEDS of PZQ in rabbits, being 6.3-fold higher than that after oral administration at the same dose. The TEDS of PZQ achieved treatment efficacy with the worm reduction of 100% when it was applied in the experimental treatment of Schistosoma japonicum in rabbits. The TEDS of PZQ that provides passive and nonocclusive delivery, having the inexpensive cost, low skin irritation rates, and precise dose of administration, should find application in the transmission control and chemotherapy of global schistosomiasis.
authors.affiliation: Department of Chemistry, College of Science, Huazhong Agricultural University, Wuhan 430070, PR China.
authors.forename: Lei
authors.initials: L
authors.lastname: Wang
authors.forename: Xinsheng
authors.initials: X
authors.lastname: Zheng
authors.forename: Yan
authors.initials: Y
authors.lastname: Fang
authors.forename: Yi
authors.initials: Y
authors.lastname: Wang
authors.forename: Cunzheng
authors.initials: C
authors.lastname: Duan
authors.forename: Baoan
authors.initials: B
authors.lastname: Yao
mesh_terms: D000279:Administration, Cutaneous; D000284:Administration, Oral; D000818:Animals; D000871:Anthelmintics / Q000008:administration & dosage* / Q000097:blood / Q000737:chemistry / Q000493:pharmacokinetics; D001682:Biological Availability; D002626:Chemistry, Pharmaceutical; D004195:Disease Models, Animal; D004339:Drug Compounding; D016503:Drug Delivery Systems; D000431:Ethanol / Q000737:chemistry*; D005026:Ethylene Glycols / Q000737:chemistry*; D010539:Permeability; D011223:Praziquantel / Q000008:administration & dosage* / Q000097:blood / Q000737:chemistry / Q000493:pharmacokinetics; D011817:Rabbits; D012554:Schistosomiasis japonica / Q000188:drug therapy*; D012867:Skin / Q000378:metabolism; D012869:Skin Absorption; D012995:Solubility; D012997:Solvents / Q000737:chemistry*; D013678:Technology, Pharmaceutical / Q000379:methods; D013696:Temperature; D014835:Volatilization
chemical_list: D000871:Anthelmintics; D005026:Ethylene Glycols; D012997:Solvents; D000431:Ethanol; D011223:Praziquantel; C005398:phenoxyethanol