6533b851fe1ef96bd12a8e74

RESEARCH PRODUCT

Microparticle preparation by a propylene carbonate emulsification-extraction method

Daris GrizićAlf LamprechtAlf Lamprecht

subject

Drug CompoundingPolysorbatesPharmaceutical Science02 engineering and technology010402 general chemistry01 natural sciencesPropanechemistry.chemical_compoundHydrolysisPolylactic Acid-Polyglycolic Acid CopolymerLactic AcidMicroparticleLow toxicityExtraction (chemistry)021001 nanoscience & nanotechnology0104 chemical sciencesSolventPLGAchemistryChemical engineeringPropylene carbonateSolventsEmulsionsExtraction methods0210 nano-technologyPolyglycolic Acid

description

Abstract The use of various harmful organic solvents for microparticle formulations is still widespread. Here, an alternative low toxicity solvent (propylene carbonate; PC) is proposed for the preparation of poly(lactic-co-glycolic-acid) (PLGA) microparticles. Based on the classical emulsification-solvent extraction methodology, the use of PC offers the unique advantage of an additional solvent extraction step using hydrolytic solvent cleavage during microparticle preparation. Spherical, rough-surfaced microparticles were obtained with a volume median diameter range from 20 to 60 µm. The residual PC content has been identified to be the major factor for the solidification hindrance, leading to polymeric Tg shifting due to a plasticizing effect. When applying the enhanced PC extraction step, the residual PC content was lowered from 8.8% to 2.7% and subsequently Tg values shifted from 8.2 to 37.7 °C. Additionally, the hydrolytic solvent cleavage confirmed to have no impact on the PLGA stability. This method presents a significant advancement towards replacing of conventional solvents in the microparticle preparation due to more efficient solvent extraction.

yearjournalcountryeditionlanguage
2018-06-01International Journal of Pharmaceutics
https://doi.org/10.1016/j.ijpharm.2018.03.062