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Enhancement of transdermal delivery of phenylbutazone from liposomal gel formulations through deer skin
Author(s) -
JAYACHANDRA BABU R.,
RAVIS W. R.,
DURAN S. H.,
SCHUMACHER J.,
COX E.,
STAHL R.,
JONES K.,
JEAN LIN Y.J.,
PHILLIP LEE Y.H.,
PARSONS D. L.,
PORTMAN E. M.,
BROWN S. C. R.
Publication year - 2009
Publication title -
journal of veterinary pharmacology and therapeutics
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.527
H-Index - 60
eISSN - 1365-2885
pISSN - 0140-7783
DOI - 10.1111/j.1365-2885.2009.01060.x
Subject(s) - transdermal , phenylbutazone , pharmacology , chemistry , liposome , drug , bioavailability , penetration (warfare) , medicine , biochemistry , operations research , engineering
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 (μg/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 (μg/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.