INFLUENCE OF OLEIC ACID ON THE IN VITRO PENETRATION OF DICLOFENAC SODIUM GEL

Abstract

Diclofenac sodium (DS) is a nonsteroidal
antiinflammatory drugs (NSAIDs), that inhibits
cyclooxygenase-2 enzyme (COX-2). It has first pass
metabolism by 40-50%, because of its short
biological half-life, the drug has to be given
frequently (Ganiswara, 2005). Dose of DS in gel is 1%
(Sweetman, 2007). In peroral use, it may cause the
risk of gastrointestinal bleeding, cardiovascular,
hypersensitivity reactions and disorders of the
central nervous (Katzung, 2002, Chuasuwan, et al.,
2008).
DS does not penetrate well through skin and cannot
reach the effective concentration at the site of
action after transdermal application (Mohammed,
2001; Ozguney, et al., 2006). DS partition coefficient
in n-octanol-buffer aqua (log P) was 1.1 (Chuasuwan,
2008). Lipophilic nature of the stratum corneum and
the hydrophilic nature of the underlying tissues
showed that the drug will penetrate the skin should
have an optimal balance between the lipophilic and
hydrophilic properties. In general, the skin is more
permeable to the material which has a partition
coefficient (P) in octanol-water between 10-1000
(Michniac-Kohn et al., 2005).
Oleic acid enhances the penetration of drugs into
the skin by increasing the fluidity of the stratum
corneum lipids through the establishment of
channels (water channels) (Fang , et al , 2003)
This study aimed to know the influence of Oleic
Acid (OA) in several concentrations (1%, 3% and
5%) as penetration enhancer on the in vitro
penetration of topical DS gel. Furthermore, the
physical properties of the topical preparation
(organoleptic, pH and viscosity), and DS penetration
percutaneously through rat skin . Then observed
that in spite of DS assay and penetrate through the
rat skin at certain intervals and observed by means
of HPLC.