The College of Pharmacy discussed the PhD dissertation entitled “Diacerein Novasome as Transdermal Drug Delivery: Formulation, In vitro, Ex vivo Characterization, and In vivo Study” by Noor Yousif Fareed and the supervisor, Assistant Professor Dr. Hanan Jalal Kassab, at the Pharmaceutics Department.The study aimed to investigate the potential of novasomal carriers to enhance the transdermal permeation of diacerein as an alternative delivery system to the standard oral treatment, thereby eliminating the laxative effect.The thin-film hydration method was utilized to prepare diacerein-loaded novasomes. The selected formula was further investigated for its zeta potential and ex vivo permeation study of the rat’s skin, and the permeation parameters were compared to the niosomal dispersion and solution of the pure drug. The anti-inflammatory activity of Diacerein novasomes-based transdermal gel was compared with standard oral treatment in the management of osteoarthritis in an experimental animal model.The solid-state characterization studies revealed that diacerein was compatible with other excipients utilized in the study, and the drug molecules existed in an amorphous form encapsulated within the vesicles. The in vitro drug release study demonstrated a biphasic release property with an initial burst phase, followed by a sustained releasing phase over an 8-hour release period. The ex vivo drug permeation study through the rat’s skin for the selected formula F6 showed a significant increase in the amount of drug permeated and transdermal flux from F6 compared to niosomal dispersion and pure drug solution. Morphological studies revealed that both diacerein treatments significantly reduced joint swelling as compared to the untreated group. Also, the serum levels of Tumor Necrosis Factor Alpha and Interleukin-1 beta were significantly lower in both diacerein treatment groups as compared to the untreated group throughout the study. Both histological and radiological findings confirmed that transdermal Diacerein treatment protects against cartilage degradation, similar to oral treatment. In conclusion, novasomal carriers could be a promising delivery strategy to improve the transdermal delivery of diacerein. An in vivo animal study in a model of osteoarthritis showed that transdermal gels of diacerein succeeded in providing sufficient pharmacological activity to attenuate the disease. This could support its use as an alternative to the standard oral treatment to avoid side effects.
