Itraconazole is a poorly soluble
drug which is used in the treatment of systemic
fungal infections. However, there is little reported literature about
itraconazole loaded delivery systems used for targeted delivery. Therefore, poly(butyl
cyanoacrylate)
nanospheres (PBCA-NSP) have been developed as a potential delivery system for transport of
itraconazole. One possible application of
itraconazole loaded PBCA-NSP could be to treat
cryptococcal meningitis. An oil-in-water (o/w)
emulsion solvent evaporation was performed for formulation generation. Manufacturing optimization was achieved using design of experiments (DoE) methodology. The average size of PBCA-NSPs varied between 60 and 80 nm. Encapsulation efficiency (EE (%)), absolute
drug loading (AL (%)) and release rate of
itraconazole from PBCA-NSP in vitro were measured by reversed phase high-performance liquid chromatography (RP-HPLC). EE of 87% could be achieved when the AL of 17.6% was intended. Lyophilization of
itraconazole loaded PBCA-NSP was needed to increase the stability of formulations, which was achieved by evaluating different
sugar cryoprotectants. In this study, PBCA-NSPs were successfully generated as a delivery system for
itraconazole providing a promising approach to improve the
therapy of
fungal infections of specific organs such as the brain
infection cryptococcal meningitis.