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Negatively charged poly(lactic-co-glycolic acid) (PLGA) microspheres encapsulated with hydrophilic drugs have been successfully prepared by a solid-in-oil-in-water (s/o/w) solvent evaporation method in the presence of anionic surfactants, sodium dodecyl sulfate (SDS), and dioctyl sodium sulfosuccinate (DSS), and nonionic surfactant polyvinyl alcohol (PVA). The effects of microencapsulation methods, surfactants types, and surfactant concentrations on the properties of microspheres were studied. Amoxicillin (AMX) was chosen as a hydrophilic model drug, and its encapsulation efficiency (EE) and in vitro release profiles were measured. The s/o/w method achieved higher EE of 40% in PLGA microspheres using surfactant SDS compared with the conventional water-in-oil-in-water (w/o/w) method (about 2%). Triphasic release profiles were observed for all PLGA microspheres (s/o/w) with slight drug burst, a slow diffusion-controlled release within the period of about 7 days and followed by the degradation-controlled sustained release for further 30 days. Smaller particle size and surface charge were achieved for s/o/w method than w/o/w method using the same anionic surfactants, and smooth surface and less porous interior matrix. The s/o/w method effectively encapsulated AMX into anionic PLGA microspheres using anionic surfactants, and these negatively charged PLGA microspheres represented an attractive approach for the controlled release of hydrophilic drugs.

Original publication

DOI

10.1002/jps.21612

Type

Journal article

Journal

J Pharm Sci

Publication Date

07/2009

Volume

98

Pages

2377 - 2389

Keywords

Amoxicillin, Anti-Bacterial Agents, Drug Carriers, Drug Combinations, Drug Compounding, Isatin, Lactic Acid, Microscopy, Electron, Scanning, Microspheres, Particle Size, Polyglycolic Acid, Polylactic Acid-Polyglycolic Acid Copolymer, Polyvinyl Alcohol, Pyridines, Sodium Dodecyl Sulfate, Spectrometry, X-Ray Emission, Static Electricity, Succinates, Surface-Active Agents, Transition Temperature