Buspirone transdermal administration for menopausal syndromes, in vitro and in animal model studies.

Menopausal syndromes can seriously disturb the quality of women's life. In this work, we have investigated transdermal administration of buspirone, a 5-HT(1A) receptor agonist, for treatment of the major menopausal syndrome, hot flushes. To the best of our knowledge, this is the first time buspirone has been proposed for the treatment of hot flushes. We designed a buspirone transdermal system containing the drug in an ethosomal carrier. Pharmacokinetic data in rats following transdermal administration indicate that buspirone was present in plasma for 12 h, reaching a C(max) value of 120.07+/-86.97 ng/ml after 2 h. A F(rel) value of 0.89 was estimated for transdermal vs. oral buspirone. The effect of transdermal buspirone on hot flushes was evaluated in ovariectomized rats by monitoring tail skin temperature changes. Temperature alleviation (1.6+/-0.7 degrees C) to normal values was observed 3 h post-buspirone administration with the effect lasting for at least 3 h. Histological examination of the skin at the application site indicated that transdermal ethosomal buspirone is safe. The significant findings presented here encourage further studies with ethosomal buspirone transdermal system for treatment of menopausal syndromes.

Ibuprofen transdermal ethosomal gel: characterization and efficiency in animal models.

A new ibuprofen transdermal nanosystem, designed by using an ethosomal carrier, was characterized and tested for its pharmacokinetic profile and therapeutic effects in animal models. It was found that the ethosomal nanosystem contains unilamellar vesicles with a normal size distribution of about 200 nm. The drug applied transdermally from the ethosomal gel was present in plasma for a longer period of time as compared to the oral administration and showed a high relative bioavailability. Ibuprofen plasma concentration reached a Cmax of 74.11 +/- 18.52 microg/ml 2 hours post application on rat skin. The ibuprofen ethosomal gel had an efficient antipyretic effect in fevered rats. Animal body temperature decreased to normal value gradually with duration of action of at least 12 hours compared to only 7 hours after the oral treatment. The transdermal ibuprofen gel also induced an analgesic effect 30 minutes following its application lasting for at least 6 hours. Biochemical and clinical hematological analysis results of the blood taken from animals in all experimental groups and those of skin histological examination show that ibuprofen ethosomal gel is safe and does not irritate the skin. Data obtained in this work suggest that the designed ethosomal ibuprofen gel could be further investigated in humans for its antipyretic effect.