Effect of formulation variables on the properties of a new vesicular system of an anthraquinone derivative
Abstract
Drug delivery through the human skin is limited by the barrier function of the stratum corner. Several attempts have been investigated to enhance the transdermal permeation including vesicular structure. Diacerein is an anthraquinone derivative approved for osteoarthritis treatment. Owning to its oral side effects, transdermal delivery seems as an attractive approach. Vesicular carrier showed a promising results in enhancement of transdermal permeation. The present investigation aimed to screen the best surfactant and the optimum cholesterol-to-surfactant ratio needed for successfully entrapping the lipophilic investigated drug diacerein with the novasome. Diacerein novasomes has been successfully prepared by the thin film hydration method using different surfactant types. Also, Different cholesterol to span 60 ratio investigated. The vesicle size, PDI and EE% were determined for all of the prepared formulas. Results showed that span 60 as a surfactant gives the best results regarding entrapment efficiency owing to its unique physicochemical properties. A cholesterol to surfactant ratio of 1:4 gives superior entrapment efficiency. However, F1 needs further optimization by a suitable size reduction technique to produce a suitable a homogenous size distribution and an appropriate size range that is acceptable for transdermal delivery.
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