Fabrication, optimisation and evaluation of cisplatin-loaded nanostructured carriers for improved urothelium permeability for intravesical administration

To design microemulsions as carriers to improve cisplatin permeation capability for intravesical administration.

The response surface methodology with factorial design was used to investigate and optimise the influence of the compositions e.g. capryol 90 and 5-pentanediol/transcutol mixture on the permeation accumulation amount and tissue deposition amount of cisplatin-loaded microemulsions. The in vitro permeation study and in vivo intravesical test were conducted to prove the effect of microemulsions.

The droplet size and the viscosity of all drug-loaded formulations ranged 235.8-309.3 nm and 550.8-861.7 cps, respectively. The permeation accumulation amounts significantly increased about 26-fold, by used microemulsion as carriers. In vivo study, the cisplatin deposition amount in bladder tissue significantly increased 4.1-fold (p < 0.05) and the penetration depth increased from 60 μm up 120 μm. The nanocarrier showed considerable thermodynamic stability.

The designed nanocarrier was considered to be a promising delivery system for cisplatin intravesical administration.