Effect of stabilizers on encapsulation efficiency and release behavior of exenatide-loaded PLGA microsphere prepared by the W/O/W solvent evaporation method
作者： Heejun Park , Dong-Hyun Ha , Eun-Sol Ha , Jeong-Soo Kim , Min-Soo Kim
DOI: 10.3390/PHARMACEUTICS11120627
关键词:
摘要: The aim of this study was to investigate the effects various stabilizers on encapsulation efficiency and release exenatide-loaded PLGA (poly(lactic-co-glycolic acid)) microspheres prepared by water-in-oil-in-water (W/O/W) solvent evaporation (SE) method. It shown that affected exenatide stability in aqueous solutions, at water/dichloromethane interfaces, surfaces, or during freeze-thawing freeze-drying procedures. Sucrose predominantly reduces instability generated freeze-drying. Phenylalanine prevents destabilization water–dichloromethane (DCM) interface through decreased adsorption. Poloxamer 188 enhances solutions adsorption PLGA. Proline lysine decrease surfaces. Fourier transform infra-red spectroscopy (FT-IR) used find molecular interaction additives with Additives assessments were then added stepwise into inner outer water phase W/O/W double emulsion, using effect each stabilizer behavior correlated well assessment results, except for negative poloxamer 188. Particle size analysis laser diffractometry, scanning electron microscopy (SEM), vapor sorption analysis, differential calorimetry (DSC), circular dichroism (CD) also employed characterize microsphere. This demonstrated an adequate formulation can be obtained about peptide preformulation step. In addition, it help overcome problems cause a microsphere-manufacturing process sustained drug release.
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