Pb. Geraghty et al., THE IN-VITRO RELEASE OF SOME ANTIMUSCARINIC DRUGS FROM MONOOLEIN WATER LYOTROPIC LIQUID-CRYSTALLINE GELS/, Pharmaceutical research, 13(8), 1996, pp. 1265-1271
Purpose, To investigate the potential use of a monoolein/water lyotrop
ic liquid crystalline gel for the vaginal delivery of the antimuscarin
ic drags, propantheline bromide and oxybutynin hydrochloride to treat
urinary incontinence, using Myverol 18-99 as a commercially available
grade of monoolein. Methods, The influence of propantheline bromide an
d oxybutynin hydrochloride on the phase structure of Myverol 18-99/wat
er gels was investigated using polarising microscopy. The in-vitro rel
ease of the antimuscarinic drugs from Myverol 18-99/water gels was det
ermined and the release pattern interpreted with the aid of results fr
om swelling studies and partition coefficient determinations. Results,
Myverol 18-99 forms gels with lyotropic liquid crystalline structures
in the presence of water. The addition of propantheline bromide and o
xybutynin hydrochloride promoted the formation of gels with a lamellar
phase structure. The gels absorbed water at a rate inversely proporti
onal to their initial water content until they reached an equilibrium
water content of similar to 40% w/w whilst maintaining their physical
integrity. The release of the antimuscarinic drugs was sustained over
a period of similar to 18 hours and followed square root of time kinet
ics indicating that the rate of release was diffusion controlled. Conc
lusions. The in-vitro release behaviour of Myverol 18-99/water gels su
ggested that they are suitable carriers to deliver propantheline bromi
de or oxybutynin hydrochloride. The results of swelling studies indica
ted that a confined area, such as the vaginal cavity, would be a suita
ble site of administration.