Preparation of amino acid copolymers/water-insoluble drug nanoparticles: Polymer properties and processing variables

초록

An increase in the surface area of drugs by reducing particle sizes from microns to nanometers has been known as an efficient method to improve the bioavailability, of water-insoluble drugs. To prevent drug nanoparticles from aggregation during the processes of drug formulation, a limited number of pharmaceutical inactive ingredients such as hydroxypropyl cellulose has been employed as stabilizers or dispersants. In this study, copolymers of hydrophilic and hydrophobic amino acids were synthesized by the ring opening polymerization of their N-carboxyanhydride monomers and evaluated as novel candidates to stabilize the nanoparticles of a water insoluble drug, naproxen. Naproxen nanoparticles stabilized by synthesized amino acid copolymers were successfully prepared in the size of 200 similar to 500 nm in 60 min by a wet comminution process. Particle size analysis showed that the effective stabilization performance of copolymers required the hydrophobic moiety content to be higher than 10 mol%. However, the molecular weight and morphology of copolymers was not the critical parameters in determining the particle size reduction. Their particle size was found to be stable up to 14 days without significant aggregation.

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