Regulation of Drug Release by Tuning Surface Textures of Biodegradable Polymer Microparticles

Abstract

Generally, size, uniformity, shape, and surface chemistry of biodegradable polymer particles will significantly affect the drug-release behavior in vitro and in vivo. In this study, uniform poly(d,l-lactic-co-glycolide) (PLGA) and PLGA-b-poly(ethylene glycol) (PLGA-b-PEG) microparticles with tunable surface textures were generated by combining the interfacial instabilities of emulsion droplet and polymer-blending strategy. Monodisperse emulsion droplets containing polymers were generated through the microfluidic flow-focusing technique. The removal of organic solvent from the droplets triggered the interfacial instabilities (spontaneous increase in interfacial area), leading to the formation of uniform polymer particles with textured surfaces. With the introduction of homopolymer PLGA to PLGA-b-PEG, the hydrophobicity of the polymer system was tailored, and a qualitatively different interfacial behavior of the emulsion droplets during solvent removal was observed. Uniform polymer particles with tunable surface roughness were thus generated by changing the ratio of PLGA-b-PEG in the polymer blends. More interestingly, surface textures of the particles determined the drug-loading efficiency and release kinetics of the encapsulated hydrophobic paclitaxel, which followed a diffusion-directed drug-release pattern. The polymer particles with different surface textures demonstrated good cell viability and biocompatibility, indicating the promising role of the particles in the fields of drug or gene delivery for tumor therapy, vaccines, biodiagnostics, and bioimaging.

Microfluidic assisted synthesis of PLGA drug delivery systems

“…14,60,61 However, the similar polymeric composition in a water immiscible or semimiscible solvent (DCM) produces droplets which need a further step to remove the solvent and produce MPs. 62 For example, change in the solvent from DCM to DMSO and also infusion with water droplets resulted in the sub-micron particles. Although they claimed the droplet-based microuidic produced nano-scale PLGA particles, the infusion of polymer mixture (water-miscible solvent) with water droplets produced NPs which the precipitation takes place within the droplets.…”

“…109 Hussein et al reported that surface texture is easily controllable using polymers with various hydrophobicity in a microuidics system. 62 They prepared PLGA 100k blend with PLGA 50k -b-PEG 5k /PLGA 100k or PLGA 10k -b-PEG 20k /PLGA 100k and PTX as a solution (10 mg mL À1 ) in DCM as a dispersed phase in the aqueous phase (5 mg mL À1 PVA) with varying ratios in a glass capillary. Results indicated that surface texture is controllable with the blend ratio and consequently it affects encapsulation efficiency and releases kinetics.…”

Surface Structures, Particles, and Fibers of Shape-Memory Polymers at Micro-/Nanoscale

“…Zhu and coworkers investigated the relationship between surface textures of polymer microparticles and their drug release property [72]. Poly(D,L-lactic-co-glycolide) (PLGA) and PLGA-b-poly(ethylene glycol) (PLGA-b-PEG) microparticles with uniform size and tunable surface structures were synthesized via the process combining the advantages of interfacial instabilities of emulsion droplet and polymerblending strategy utilizing microfluidic technology.…”

Multifunctional Magnetic Nanowires: Design, Fabrication, and Future Prospects as Cancer Therapeutics

“…Thus, NW morphology has a direct impact on drug loading capacity. Although NWs inherently have large surface areas, their surface area can be increased further by changing their morphology to include rough surfaces [93,94] or by synthesizing porous NWs [95,96]. Guo and co-workers achieved a high drug loading of 2000 mg/g using porous NW while Zhu and co-workers achieved a high drug loading capacity of 992.91 mg/g with their Co NW, which had a rough morphology.…”