Purpose: To measure the extent of
solubility of the lipophilic drug, aceclofenac, in 13
oils as well as its in vitro permeability from these
oils in order to develop optimized topical microemulsion
and microemulsion-based gel for improved
bioavailability.
Methods: UV spectrophotometeric
method was used at the wavelength of 276 nm to measure
the dissolved quantity of aceclofenac in each of the
oils (almond oil, oleic acid, castor oil, paraffin oil,
cinnamon oil, clove oil, canola oil, sesame oil,
isopropyl myristate (ipm), sunflower oil, corn oil,
coconuts oil and eucalyptus oil) at 25 °C. The in-vitro
permeability of aceclofenac in each of these oils was
determined at 32 ± 0.5 °C using Franz diffusion cell
with phosphate buffer (pH 7.4) as medium with 0.45 µ
cellulose acetate membrane. The solubility and
permeability of aceclofenac were compared with the
hydroalcoholic solution of aceclofenac.
Results: The highest solubility
values of 9.153 and 8.560 mg/ml for aceclofenac were
obtained with almond oil and oleic acid, respectively (p
< 0.05). However the solubility and permeability of
aceclofenac in hydro-alcoholic solution were 150.65
mg/ml and 14.91± 0.05 µg/cm2/h, respectively.
Aceclofenac also showed higher permeability values
(1.45± 0.04 and 1.21 ± 0.06) in almond oil and oleic
acid, respectively, than in the other oils (p < 0.05).
Conclusion: These findings show that
almond oil and oleic acid are promising vehicles for
aceclofenac as its enhanced solubility and permeability
in these vehicles are suggestive of improved
bioavailability.
Keywords:
Aceclofenac, Almond oil, Solubility; Permeability, Oleic
acid, Bioavailability.