Use of hydrodynamic flow focusing for the generation of biodegradable camptothecin‐loaded polymer microspheres

Abstract

The present study was conducted to investigate the use of hydrodynamic flow focusing for the generation of biodegradable polymer microspheres encapsulating the anticancer drug camptothecin. Poly(D,L‐lactide‐co‐glycolide) (PLGA) and poly(L‐lactide) (PLA) were used as the matrix materials. Camptothecin was dissolved in the disperse phase and microspheres with a mean size between 2 and 3µm generated using hydrodynamic flow focusing. When up to 1 wt.% of the drug was added to PLA, the drug encapsulation efficiency was 64%. For PLGA, the drug encapsulation efficiency was between 39 and 46%. Drug release from PLA particles was rapid and complete within 6h, while drug release from PLGA particles showed no burst effect and followed a first order release profile. The encapsulated camptothecin stayed in its active lactone form, as shown by HPLC, and was able to exert cell toxic effects as shown by a cell viability assay. Hydrodynamic flow focusing is a promising tool for the preparation of drug‐releasing biodegradable microspheres typically made by solvent evaporation and/or solvent extraction, as indicated by the successful encapsulation of the anticancer drug camptothecin.