the Preparation and evaluation of Diacerein Novasomes transdermal HPMCK15M Gel Preparation and evaluation of Diacerein Novasomes transdermal HPMCK15M Gel

Abstract

 Abstract

Diacerein is an anthraquinone derivative used as a disease-modifying agent in the treatment of osteoarthritis.

Because of the laxative effect that is associated with the oral administration of diacerein, treatment is often

discontinued. The present study aims to prepare diacerein novasomes transdermal HPMCK15M Gel to

enhance drug permeation. The transdermal gel was prepared by hot-cold method in which the polymer is

dispersed in hot water while the prepared novasomal vesicles of diacerein were isolated by cold

centrifugation and dispersed in cold water. The prepared gel was evaluated for its drug content, pH,

spreadability, and in vitro drug release from the gel. The selected gel formula was further evaluated for its

release kinetic, rheological properties, and ex vivo permeation parameters. Results showed that the prepared

gels were clear and homogeneous, with a drug content from 92.86±3.1 to 99.89±0.18, pH value was 6.75-6.88,

and spreadability of 5.4±0.3to 9.1±0.8. The in vitro drug release kinetic was best fitted to the Higuchi model of

drug release with a Fiackian mechanism. Rheological evaluation of the selected gel formula displayed nonNewtonian pseudoplastic share thinning flow behavior. The ex vivo permeation study found that transdermal

flux was 60.349 ± 0.375 μg/cm2/h, the lag time was 2.8±0.1 and the permeability coefficient was 60.349*10-3

cm/hr. In conclusion, the prepared HPMCK15M transdermal gel at a concentration of 3% w/w was found to be

an appropriate vehicle for better transdermal delivery of diacerein from its novasomes.