title: Enhancement of transdermal delivery of phenylbutazone from liposomal gel formulations through deer skin.
abstract: Phenylbutazone (PBZ) is a nonsteroidal anti-inflammatory drug used in the treatment of chronic pain and arthritis. Topical and transdermal administration of PBZ would be beneficial in large animals in terms of minimizing gastro-intestinal ulcerations and other side effects, easy administration to legs and joints and minimizing the dose to reduce systemic toxicity of the drug. A topical liposomal preparation with different concentrations of a mono-substituted alkyl amide (MSA) and PBZ was formulated. The formulations were evaluated by in vitro skin-permeation kinetics through deer skin using Franz diffusion cells. By increasing drug loading from 1% to 5% w/w, the steady-state flux (microg/cm(2)/h) of PBZ was increased twofold (P < 0.001). Similarly, by increasing the MSA concentration from 0% to 4%, the steady-state flux (microg/cm(2)/h) of PBZ was increased twofold (P < 0.001). Overall, by increasing the drug load and the use of an appropriate amount of the penetration enhancer, the steady-state flux of PBZ through skin was increased fourfold (P < 0.001). MSA at both 2% and 4% w/w concentrations significantly increased the skin levels of PBZ as compared with control (P < 0.05). In conclusion, MSA served as an effective skin-penetration enhancer in the liposomal gel of PBZ for deer.
authors.affiliation: Department of Pharmacal Sciences, Harrison School of Pharmacy, Auburn University, Auburn, AL 36849, USA. rjbabu68@gmail.com
authors.forename: R
authors.initials: R
authors.lastname: Jayachandra Babu
authors.forename: W R
authors.initials: WR
authors.lastname: Ravis
authors.forename: S H
authors.initials: SH
authors.lastname: Duran
authors.forename: J
authors.initials: J
authors.lastname: Schumacher
authors.forename: E
authors.initials: E
authors.lastname: Cox
authors.forename: R
authors.initials: R
authors.lastname: Stahl
authors.forename: K
authors.initials: K
authors.lastname: Jones
authors.forename: Y-J
authors.initials: YJ
authors.lastname: Jean Lin
authors.forename: Y-H
authors.initials: YH
authors.lastname: Phillip Lee
authors.forename: D L
authors.initials: DL
authors.lastname: Parsons
authors.forename: E M
authors.initials: EM
authors.lastname: Portman
authors.forename: S C R
authors.initials: SC
authors.lastname: Brown
mesh_terms: D000279:Administration, Cutaneous; D000704:Analysis of Variance; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage* / Q000378:metabolism; D002851:Chromatography, High Pressure Liquid / Q000662:veterinary; D003670:Deer; D005782:Gels; D008081:Liposomes; D010653:Phenylbutazone / Q000008:administration & dosage* / Q000378:metabolism; D012869:Skin Absorption / Q000187:drug effects*
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D005782:Gels; D008081:Liposomes; D010653:Phenylbutazone