Preparation of PLGA microparticles by an emulsion-extraction process using glycofurol as polymer solvent.
OBJECTIVE
To develop biodegradable poly(lactic-co-glycolic acid) (PLGA) microparticles prepared by an original emulsion-extraction process, with glycofurol, a nontoxic excipient, as polymer solvent.


METHODS
The preparation of microparticles consisted in dissolving polymer in glycofurol. This solution was emulsified in a vegetable oil, and then amphiphilic agent was added into the emulsion to extract glycofurol and lead to microparticle formation. Physicochemical studies were carried out, and an experimental design was prepared in order to elucidate the impact of the formulation composition on the microparticle characteristics. Finally, encapsulation tests were made with a model protein.


RESULTS
In a ternary diagram, a small feasibility area allowing particle formation was located. The resulting microparticles were spherical with a homogeneous, polymeric matrix structure. They exhibited a variable size from 3 to 15 microm, which was controlled by the different formulation parameters. Differential scanning calorimetry (DSC) analysis made it possible to detect their composition. Preliminary results showed that these particles were able to encapsulate a protein model, lysozyme.


CONCLUSIONS
This simple and convenient technique enabled us to obtain spherical, biodegradable microparticles from acceptable excipients. Moreover, the process conditions made possible the encapsulation of drugs, including proteins.
Aubert-Pouëssel
Anne
A
INSERM U646, Ingénierie de la Vectorisation Particulaire, IBT, 10 rue André Boquel, 49 100 Angers, France.
Venier-Julienne
Marie-Claire
MC
Saulnier
Patrick
P
Sergent
Michelle
M
Benoît
Jean-Pierre
JP
D004655:Emulsions; D019344:Lactic Acid / Q000138:chemical synthesis*; D008863:Microspheres; D010316:Particle Size; D011092:Polyethylene Glycols / Q000138:chemical synthesis*; D011100:Polyglycolic Acid / Q000138:chemical synthesis*; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011108:Polymers / Q000138:chemical synthesis*; D012997:Solvents / Q000138:chemical synthesis*
D004655:Emulsions; D011108:Polymers; D012997:Solvents; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid; D011092:Polyethylene Glycols; C018557:glycofurol