title: Ethosomes for skin delivery of ropivacaine: preparation, characterization and ex vivo penetration properties.
abstract: Ropivacaine, a novel long-acting local anesthetic, has been proved to own superior advantage. However, Naropin® Injection, the applied form in clinic, can cause patient non-convenience. The purpose of this study was to formulate ropivacaine (RPV) in ethosomes and evaluate the potential of ethosome formulation in delivering RPV transdermally. The RPV-loaded ethosomes were prepared with thin-film dispersion technique and the formulation was characterized in terms of size, zeta potential, differential scanning calorimetry (DSC) analysis and X-ray diffraction (XRD) study. The results showed that the optimized RPV-ethosomes displayed a typical lipid bilayer structure with a narrow size distribution of 73.86 ± 2.40 nm and drug loading of 8.27 ± 0.37%, EE of 68.92 ± 0.29%. The results of DSC and XRD study indicated that RPV was in amorphous state when encapsulated into ethosomes. Furthermore, the results of ex vivo permeation study proved that RPV-ethosomes could promote the permeability in a high-efficient, rapid way (349.0 ± 11.5 μg cm(-2) at 12 h and 178.8 ± 7.1 μg cm(-2) at 0.5 h). The outcomes of histopathology study forecasted that the interaction between ethosomes and skin could loosen the tight conjugation of corneocyte layers and weaken the permeation barrier. In conclusion, RPV-ethosomes could be a promising delivery system to encapsulate RPV and deliver RPV for transdermal administration.
authors.affiliation: a Department of Pharmaceutics, College of Pharmacy , Shandong University , Jinan , China .
authors.forename: Yingjie
authors.initials: Y
authors.lastname: Zhai
authors.affiliation: a Department of Pharmaceutics, College of Pharmacy , Shandong University , Jinan , China .
authors.forename: Rui
authors.initials: R
authors.lastname: Xu
authors.affiliation: b Department of Orthopedics, Changhai Hospital , Second Military Medical University , Shanghai , China , and.
authors.forename: Yi
authors.initials: Y
authors.lastname: Wang
authors.affiliation: c Department of Pharmacy, Changhai Hospital , Second Military Medical University , Shanghai , China.
authors.forename: Jiyong
authors.initials: J
authors.lastname: Liu
authors.affiliation: b Department of Orthopedics, Changhai Hospital , Second Military Medical University , Shanghai , China , and.
authors.forename: Zimin
authors.initials: Z
authors.lastname: Wang
authors.affiliation: a Department of Pharmaceutics, College of Pharmacy , Shandong University , Jinan , China .
authors.forename: Guangxi
authors.initials: G
authors.lastname: Zhai
mesh_terms: D000279:Administration, Cutaneous; D000577:Amides / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics*; D000818:Animals; D004337:Drug Carriers / Q000008:administration & dosage* / Q000138:chemical synthesis* / Q000737:chemistry; D008081:Liposomes; D010316:Particle Size; D051381:Rats; D000077212:Ropivacaine; D012867:Skin / Q000378:metabolism* / Q000473:pathology; D012869:Skin Absorption; D013499:Surface Properties
chemical_list: D000577:Amides; D004337:Drug Carriers; D008081:Liposomes; D000077212:Ropivacaine
keywords: Ethosomes; ropivacaine; transdermal delivery; vesicle–skin interaction