Carbon dioxide-mediated generation of hybrid nanoparticles for improved bioavailability of protein kinase inhibitors.

ABSTRACT:

Purpose

A versatile methodology is demonstrated for improving dissolution kinetics, gastrointestinal (GI) absorption, and bioavailability of protein kinase inhibitors (PKIs).

Methods

The approach is based on nanoparticle precipitation by sub- or supercritical CO2 together with a matrix-forming polymer, incorporating surfactants either during or after nanoparticle formation. Notably, striking synergistic effects between hybrid PKI/polymer nanoparticles and surfactant added after particle formation is investigated.

Results

The hybrid nanoparticles, consisting of amorphous PKI embedded in a polymer matrix (also after 12 months), display dramatically increased release rate of nilotinib in both simulated gastric fluid and simulated intestinal fluid, particularly when surfa

SUBMITTER: Jesson G 

PROVIDER: S-EPMC3931930 | biostudies-literature | 2014 Mar

REPOSITORIES: biostudies-literature