Porous silicon oxide–PLGA composite microspheres for sustained ocular delivery of daunorubicin

A water-soluble anthracycline antibiotic drug (daunorubicin, DNR) was loaded into oxidized porous silicon (pSiO2) microparticles and then encapsulated with a layer of polymer (poly lactide-co-glycolide, PLGA) to investigate their synergistic effects in control of DNR release. Similarly fabricated PLGA–DNR microspheres without pSiO2, and pSiO2 microparticles without PLGA were used as control particles. The composite microparticles synthesized by a solid-in-oil-in-water emulsion method have mean diameters of 52.33 ± 16.37 μm for PLGA–pSiO2_21/40–DNR and the mean diameter of 49.31 ± 8.87 μm for PLGA–pSiO2_6/20–DNR. The mean size, 26.00 ± 8 μm, of PLGA–DNR was significantly smaller, compared with the other two (P < 0.0001). Optical microscopy revealed that PLGA–pSiO2–DNR microspheres contained multiple pSiO2 particles. In vitro release experiments determined that control PLGA–DNR microspheres completely released DNR within 38 days and control pSiO2–DNR microparticles (with no PLGA coating) released DNR within 14 days, while the PLGA–pSiO2–DNR microspheres released DNR for 74 days. Temporal release profiles of DNR from PLGA–pSiO2 composite particles indicated that both PLGA and pSiO2 contribute to the sustained release of the payload. The PLGA–pSiO2 composite displayed a more constant rate of DNR release than the pSiO2 control formulation, and displayed a significantly slower release of DNR than either the PLGA or pSiO2 formulations. We conclude that this system may be useful in managing unwanted ocular proliferation when formulated with antiproliferation compounds such as DNR.