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How to achieve high encapsulation efficiencies for macromolecular and sensitive apis in liposomes

Ullmann, Kirsten ORCID iD icon 1; Leneweit, Gero; Nirschl, Hermann 1
1 Institut für Mechanische Verfahrenstechnik und Mechanik (MVM), Karlsruher Institut für Technologie (KIT)

This research highlights the capacity of a newly introduced centrifugation process to form liposomes from water-in-fluorocarbon nano-emulsions stabilized with phospholipids to incorporate macromolecular and sensitive active pharmaceutical ingredients (API). The encapsulation efficiency of the produced liposomes, incorporating fluorescein-sodium, bovine serum albumin and fluorecein isothiocyanate dextran as model APIs, is determined by applying Vivaspin® centrifugation filtration and quantified by UV-Vis spectroscopy. It was found that higher densities of the fluorocarbons used as the hydrophobic phase enable a higher encapsulation efficiency and that an efficiency of up to 98% is possible depending on the used phospholipid. Among the engineering aspects of the process, a comparison between different membrane substances was performed. Efficiency increases with a higher phospholipid concentration but decreases with the addition of cholesterol. Due to the higher bending modulus, liposome formation is slowed down by cholesterol during liposome closure leading to a greater leakage of the model API. The encapsulation of bovine serum albumin and dextran, both investigated under different osmotic conditions, shows that an efflux negatively affects the encapsulation efficiency while an influx increases the stability. ... mehr

Verlagsausgabe §
DOI: 10.5445/IR/1000133848
Veröffentlicht am 14.06.2021
DOI: 10.3390/pharmaceutics13050691
Zitationen: 3
Web of Science
Zitationen: 2
Zitationen: 4
Cover der Publikation
Zugehörige Institution(en) am KIT Institut für Mechanische Verfahrenstechnik und Mechanik (MVM)
Publikationstyp Zeitschriftenaufsatz
Publikationsjahr 2021
Sprache Englisch
Identifikator ISSN: 1999-4923
KITopen-ID: 1000133848
Erschienen in Pharmaceutics
Verlag MDPI
Band 13
Heft 5
Seiten 691
Bemerkung zur Veröffentlichung Gefördert durch den KIT-Publikationsfonds
Schlagwörter encapsulation efficiency; liposomes; phospholipids; fluorocarbon; nano-emulsions; active pharmaceutical ingredients
Nachgewiesen in Dimensions
Web of Science
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