Biodegradable pH-responsive alginate-poly (lactic-co-glycolic acid) nano/micro hydrogel matrices for oral delivery of silymarin

This study involves the development and characterization of a series of sodium alginate-based pH-responsive hydrogel microspheres encapsulating poly(D,L-lactic-co-glycolic acid) (PLGA) nanoparticles (NPs). The effect of the drying technique (air- or freeze-drying) on the size of the developed particles was determined. Swelling characteristics at different pH values, in vitro biodegradation and moisture contents of both air-dried and freeze-dried hydrogel particles were investigated. The effect of drying method on the morphology of the particles was also studied using SEM and AFM. Then, the developed alginate-PLGA particles were evaluated as potential carriers, through a new approach, to improve the dissolution, bioavailability and oral sustained release of silymarin, as a model of hydrophobic natural therapeutics. The used silymarin was isolated from the seeds of some native milk thistle (Silybum marianum) ecotypes of delta Egypt and was characterized with the aid of several analytical techniques including; H-1 NMR, UV and FTIR. The obtained data showed a considerable effect of the alginate content and the drying method onto the characteristics of the prepared particles. Also, the results demonstrated that the developed alginate-based hydrogel microparticles encapsulating silymarin-loaded PLGA NPs can be used as biodegradable carriers that can confer sustained oral release of silymarin in addition to enhancing its overall dissolution and oral bioavailability. (C) 2010 Elsevier Ltd. All rights reserved.