Design and Evaluation of Transdermal Delivery Systems for Cytisine
Two research approaches(using penetration enhancers individually and in combination)were employed to develop a transdermal drug delivery system of cytisine,with the aim of increasing the transdermal penetration of cytisine.In vitro permeation experiments were conducted using a horizontal double-chamber diffusion cell to evaluate the optimal approach for enhancing cytisine penetration.The preliminary investigation on the transdermal mechanisms involved in the optimal approach was carried out through in vitro release experiments and molecular simulation methods.The results demonstrated that geraniol,menthol,and their combination with isopropyl myristate exhibited a significant enhancement in permeability(P<0.05).Among them,the best enhancement was observed in a system with a combination of 5%geraniol and 5%isopropyl myristate as the enhancers,resulting in a 2.02 times increase in cumulative penetration amount at 24 h compared with the blank group.The in vitro release experiments and molecular simulation revealed that the best combination of penetration enhancers could promote the release of cytisine from patches and bind to skin action sites,thus increasing the penetration of cytisine.This combination is expected to be used as a promising method for cytisine permeation in future investigations.
cytisinepenetration enhancercombination of penetration enhancersin vitro penetrationpenetration promoting mechanismmolecular simulation