Mb. Brown et al., An in vitro investigation into the effect of glycosaminoglycans on the skin partitioning and deposition of NSAIDs, INT J PHARM, 225(1-2), 2001, pp. 113-121
Recently, Solaraze gel (Bioglan, Herts, UK) a topical hyaluronan (HA)/dicto
fenac formulation for the treatment of actinic keratosis has received regul
atory approval in the US, Canada and Europe for the treatment of actinic ke
ratosis. However, a mechanism of action to explain the topical delivery pro
perties of HA remains to be elucidated. Thus, the aim of this study was to
compare the effect of HA with other glycosaminoglycans (chondroitin sulphat
e (CS), heparin (HP)) and pharmaceutically relevant polysaccharides (sodium
carboxymethyl cellulose and pectin) on the dermal partitioning and percuta
neous penetration of diclofenac and ibuprofen. The studies demonstrated tha
t HA significantly enhanced the partitioning of both diclofenac and ibuprof
en into human skin when compared to an aqueous control, pectin and carboxym
ethylcellulose (P < 0.01). Although the HA vehicle increased the partitioni
ng of both drugs compared to the effects of the other glycosaminoglycans, C
S and HP, this difference was not significant (P > 0.05). However, the resu
lts from the Franz cell diffusion studies showed that HA (1% w/w) significa
ntly enhanced the amount of drug localising within the skin when compared t
o all of the other polysaccharides (P < 0.05). The results suggest that the
use of HA as a vehicle excipient offers potential advantages in the dermal
delivery and localisation of drugs. (C) 2001 Elsevier Science B.V. All rig
hts reserved.