Comparative in-vitro and in-vivo evaluation of spherulites and cubosomes of Irinotecan for lung targeting.

AIMS

The present investigation aimed at the comparative evaluation of the developed nanocarriers, viz. spherulites and cubosomes for lung targeting.

MATERIALS AND METHODS

Both the spherulites and cubosomes were characterized for their entrapment efficiency, drug loading, size and zeta potential, in-vitro drug release profile, surface morphology, hemocompatibility, and in-vivo pharmacokinetic and lung biodistribution.

RESULTS AND CONCLUSIONS

The optimized batches of spherulites and cubosomes possessed high entrapment efficiency and drug loading with size around 200 nm, which is suitable for lung targeting. The zeta potential value for both the nanoformulations was found to be between -20 and -30 mv indicating the physical stability against aggregation. The SEM and TEM analysis revealed the presence of spherical and discrete particles in both the types of nanocarriers. Water channels were observed in case of cubosomes. Spherulites and cubosomes showed pH-dependent drug release with lower release at physiological pH while higher release at the pH of the tumor microenvironment. Both spherulites and cubosomes exhibited highly significant increase in the half-life and mean residence time in the plasma. The prepared nanoformulations were hemocompatible and had higher lung targeting potential compared to the plain drug solution.