caa a22 4500 445312998 CHVBK 20180317142636.0 cr unu---uuuuu 170323e20110301xx s 000 0 eng 10.1007/s11095-010-0304-6 doi (NATIONALLICENCE)springer-10.1007/s11095-010-0304-6 Microsphere Preparation Using the Untoxic Solvent Glycofurol [Elektronische Daten] [Daniela Allhenn, Alf Lamprecht] ABSTRACT: Purpose: At laboratory scale, the most widely applied methods in therapeutic microencapsulation are based on emulsification using organic solvents. Here, glycofurol was proposed as non-toxic solvent to circumvent these inconveniences using a quasi-emulsion extraction method for the preparation of poly (lactide-co-glycolide) microspheres. Methods: Matrix polymer and lipophilic drug were dissolved in glycofurol, building the internal phase, and emulsified under stirring into various external phases before microspheres could be obtained and characterized for their pharmacotechnical properties. Results: Microspheres were spherical with particle diameters around 100 to 200μm and also showed a monomodal particle size distribution. The internal sponge-like structure was related to an incomplete glycofurol extraction (residual content: 16.9% ± 1.6% of total particle mass), which is, however, no toxicological drawback. The encapsulation rate of several model compounds increased with rising partition coefficient (Ibuprofen: 1.9% ± 0.6%, Ritonavir: 11.2% ± 0.4%, Lopinavir: 14.0% ± 2.2%, Sudan III: 28.3% ± 0.4%) due to the decreasing solubility in the external phase. In-vitro release kinetics were varying from a complete release after 4h for Ritonavir to 3weeks for Sudan III. Conclusion: This new method was confirmed to be suitable for the preparation of microspheres with the use of a non-toxic solvent and to allow for the entrapment of lipophilic actives and their controlled release. Springer Science+Business Media, LLC, 2010 glycofurol nationallicence microencapsulation nationallicence microspheres nationallicence quasi emulsion nationallicence solvent extraction nationallicence Allhenn Daniela Institute of Pharmacy, Laboratory of Pharmaceutical Engineering, University of Bonn, Gerhard-Domagk-Str. 3, 53121, Bonn, Germany aut Lamprecht Alf Laboratory of Pharmaceutical Engineering, University of Franche-Comté, Besançon, France aut Pharmaceutical Research Springer US; http://www.springer-ny.com 28/3(2011-03-01), 563-571 0724-8741 28:3<563 2011 28 11095 https://doi.org/10.1007/s11095-010-0304-6 text/html Onlinezugriff via DOI 1 research-article jats NATIONALLICENCE 856 40 https://doi.org/10.1007/s11095-010-0304-6 text/html Onlinezugriff via DOI NATIONALLICENCE 700 1- Allhenn Daniela Institute of Pharmacy, Laboratory of Pharmaceutical Engineering, University of Bonn, Gerhard-Domagk-Str. 3, 53121, Bonn, Germany aut NATIONALLICENCE 700 1- Lamprecht Alf Laboratory of Pharmaceutical Engineering, University of Franche-Comté, Besançon, France aut NATIONALLICENCE 773 0- Pharmaceutical Research Springer US; http://www.springer-ny.com 28/3(2011-03-01), 563-571 0724-8741 28:3<563 2011 28 11095 Metadata rights reserved Springer special CC-BY-NC licence nationallicence BK010053 XK010053 XK010000 NATIONALLICENCE NATIONALLICENCE NL-springer