Noscapine, recently identified as anticancer due to its microtubule-modulating properties. It is presently in Phase I/II clinical trials. The therapeutic efficacy of
noscapine has been established in several xenograft models. Its pharmacokinetic limitations such as low bioavailability and high ED50 impede development of clinically relevant treatment regimens. Here we present design, synthesis, in vitro and in vivo characterization of sterically stabilized
gelatin microassemblies of
noscapine (SSGMS) for targeting human
non-small cell lung cancer A549 cells. The average size of the sterically stabilized
gelatin microassemblies of
noscapine, SSGMS was 10.0±5.1 μm in comparison to
noscapine-loaded
gelatin microassemblies, GMS that was 8.3±5.5 μm. The
noscapine entrapment efficiency of SSGMS and GMS was 23.99±4.5% and 24.23±2.6%, respectively. Prepared microassemblies were spherical in shape and did not show any
drug and
polymer interaction as examined by FTIR, DSC and PXRD. In vitro release data indicated that SSGMS and GMS follow first-order release kinetics and exhibited an initial burst followed by slow release of the
drug. In vitro cytotoxicity evaluated using A549 cells showed a low IC50 value of SSGMS (15.5 μM) compared to GMS (30.1 μM) and free
noscapine (47.2 μM). The SSGMS can facilitate a sustained
therapeutic effect in terms of prolonged release of
noscapine as evident by
caspase-3 activity in A549 cells. Concomitantly, pharmacokinetic and biodistribution analysis showed that SSGMS increased the plasma half-life of
noscapine by ~9.57-fold with an accumulation of ~48%
drug in the lungs. Our data provides evidence for the potential usefulness of SSGMS for
noscapine delivery in
lung cancer.