Famciclovir, the drug of choice for cold sores and recurrent genital herpes, shows poor oral bioavailability and is associated with numerous side effects. The present work emphasizes the possibility of transdermal application of famciclovir through a transferosome-loaded gelling system to localize the drug at the site of application with better penetrability, therapeutic effects, and comfort. Transferosome of famciclovir was prepared using tween 80, phospholipid, and cholesterol. To optimize the entrapment of the drug, and the vesicular size of the transferosomes, central composite design was employed. The optimized formulation was evaluated for physicochemical characteristics, surface morphology study, and degree of deformability. The optimized product was included in Carbopol 940 gelling system. The gel was evaluated for ex vivo permeation, skin irritation, drug deposition at various layers of skin, and histopathology study. The design optimization yielded an optimized product (FAMOPT) of nano-sized (339 nm) stable vesicle of transferosome of famciclovir. The surface morphology study revealed the formation of nanovesicles without aggregation. Compatibility between the drug and the excipients was established. The elasticity of the vesicles proved the resistance to leakage. Permeation of the drug was enhanced by 2.8 times. The gel was found to be nonirritating and non-sensitizing to the animal skin. The drug deposition at various layers of skin was remarkably improved indicating effective penetration of the drug. Histopathology study further proved that penetration of nano vesiculate drug through the deeper layers of the skin. Hence, the nano vesicular delivery of famciclovir can be a promising alternative to the conventional delivery of famciclovir with enhanced local and systemic action for the treatment of herpes.

Keywords: Famciclovir, transferosome, deformable vesicle, transdermal penetration, skin deposition