title: HIImesophase as a drug delivery system for topical application of methyl salicylate.
abstract: The main objective of this study was to develop reversed hexagonal (HII) mesophase for transdermal delivery of methyl salicylate. The formulation was prepared, characterized and evaluated for its skin penetration in vitro and skin retention in vivo. Preliminary pharmacodynamics and skin irritation were also investigated. The formulation was identified as hexagonal structure. In vitro study exhibited that HIImesophase enhanced the skin permeation by delivering 2.61 times more methyl salicylate than the commercially available cream. Meanwhile, HIImesophase presented higher bioavailability as AUC(0-24)and AUC(0-∞)were 32.894μg·mL-1and 32.935μg·mL-1respectively, while the cream were 12.791μg·mL-1and 12.970μg·mL-1. Preliminary pharmacodynamics studies demonstrated that HIImesophase possessed anti-inflammatory and analgesic effects for inhibiting paw edema, granuloma and pain. MeSa HIImesophase showed no skin irritation on the normal rat skin. Thus, HIImesophase was considered as an effective delivery system for MeSa.
authors.affiliation: Department of Pharmacy, Anhui University of Chinese Medicine, Hefei, Anhui 230012, China.
authors.forename: Xin
authors.initials: X
authors.lastname: Liang
authors.affiliation: Department of Pharmacy, Anhui University of Chinese Medicine, Hefei, Anhui 230012, China.
authors.forename: Yu-Lin
authors.initials: YL
authors.lastname: Chen
authors.affiliation: Department of Pharmacy, Anhui University of Chinese Medicine, Hefei, Anhui 230012, China.
authors.forename: Xiao-Jing
authors.initials: XJ
authors.lastname: Jiang
authors.affiliation: Department of Pharmacy, Anhui University of Chinese Medicine, Hefei, Anhui 230012, China.
authors.forename: Sheng-Mei
authors.initials: SM
authors.lastname: Wang
authors.affiliation: Center for Drug Delivery System, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China.
authors.forename: Ji-Wen
authors.initials: JW
authors.lastname: Zhang
authors.affiliation: Department of Pharmacy, Anhui University of Chinese Medicine, Hefei, Anhui 230012, China; Institute of Pharmaceutics, Anhui Academy of Chinese Medicine, Hefei, Anhui 230012, China; Key Laboratory of Xin'an Medicine, Ministry of Education, Hefei, Anhui 230012, China. Electronic address: guishy0520@126.com.
authors.forename: Shuang-Ying
authors.initials: SY
authors.lastname: Gui
mesh_terms: D000279:Administration, Cutaneous; D000700:Analgesics / Q000008:administration & dosage* / Q000097:blood / Q000493:pharmacokinetics / Q000627:therapeutic use; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000008:administration & dosage* / Q000097:blood / Q000493:pharmacokinetics / Q000627:therapeutic use; D001682:Biological Availability; D016503:Drug Delivery Systems; D004487:Edema / Q000188:drug therapy; D005233:Fatty Alcohols / Q000737:chemistry; D005260:Female; D050866:Liquid Crystals / Q000737:chemistry*; D008297:Male; D051379:Mice; D010146:Pain / Q000188:drug therapy; D017208:Rats, Wistar; D012459:Salicylates / Q000008:administration & dosage* / Q000097:blood / Q000493:pharmacokinetics / Q000627:therapeutic use; D012867:Skin / Q000187:drug effects / Q000378:metabolism; D012869:Skin Absorption; D023422:Skin Irritancy Tests
chemical_list: D000700:Analgesics; D000893:Anti-Inflammatory Agents; D005233:Fatty Alcohols; D012459:Salicylates; C508873:3,7,11,15-tetramethyl-1,2,3-hexadecanetriol; C033069:methyl salicylate
keywords: H(II) mesophase; Liquid crystalline; Methyl salicylate; Methyl salicylate (PubChem CID:3018525); Phytantriol (PubChem CID:4133); Salicylate acid (PubChem CID:338); Transdermal delivery