PMID- 29630934 OWN - NLM STAT- MEDLINE DCOM- 20180926 LR - 20181202 IS - 1873-3476 (Electronic) IS - 0378-5173 (Linking) VI - 544 IP - 1 DP - 2018 Jun 10 TI - Microparticle preparation by a propylene carbonate emulsification-extraction method. PG - 213-221 LID - S0378-5173(18)30209-6 [pii] LID - 10.1016/j.ijpharm.2018.03.062 [doi] AB - 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 microm. 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  degrees 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. CI - Copyright (c) 2018 Elsevier B.V. All rights reserved. FAU - Grizic, Daris AU - Grizic D AD - Department of Pharmaceutics, Institute of Pharmacy, University of Bonn, Gerhard-Domagk-Str. 3, 53121 Bonn, Germany. Electronic address: daris.grizic@uni-bonn.de. FAU - Lamprecht, Alf AU - Lamprecht A AD - Department of Pharmaceutics, Institute of Pharmacy, University of Bonn, Gerhard-Domagk-Str. 3, 53121 Bonn, Germany; PEPITE (EA4267), University of Burgundy/Franche-Comte, Besancon, France. Electronic address: alf.lamprecht@uni-bonn.de. LA - eng PT - Journal Article DEP - 20180406 PL - Netherlands TA - Int J Pharm JT - International journal of pharmaceutics JID - 7804127 RN - 0 (Emulsions) RN - 0 (Polysorbates) RN - 0 (Solvents) RN - 1SIA8062RS (Polylactic Acid-Polyglycolic Acid Copolymer) RN - 26009-03-0 (Polyglycolic Acid) RN - 33X04XA5AT (Lactic Acid) RN - 8D08K3S51E (propylene carbonate) RN - T75W9911L6 (Propane) SB - IM MH - Drug Compounding MH - Emulsions MH - Lactic Acid/*chemistry MH - Polyglycolic Acid/*chemistry MH - Polylactic Acid-Polyglycolic Acid Copolymer MH - Polysorbates/*chemistry MH - Propane/*analogs & derivatives/chemistry MH - Solvents/*chemistry OTO - NOTNLM OT - Enhanced solvent extraction OT - Microparticles OT - PLGA OT - Propylene carbonate EDAT- 2018/04/10 06:00 MHDA- 2018/09/27 06:00 CRDT- 2018/04/10 06:00 PHST- 2018/01/12 00:00 [received] PHST- 2018/03/16 00:00 [revised] PHST- 2018/03/31 00:00 [accepted] PHST- 2018/04/10 06:00 [pubmed] PHST- 2018/09/27 06:00 [medline] PHST- 2018/04/10 06:00 [entrez] AID - S0378-5173(18)30209-6 [pii] AID - 10.1016/j.ijpharm.2018.03.062 [doi] PST - ppublish SO - Int J Pharm. 2018 Jun 10;544(1):213-221. doi: 10.1016/j.ijpharm.2018.03.062. Epub 2018 Apr 6.