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Calcein release from DPPC liposomes by phospholipase A2 activity: Effect of cholesterol and amphipathic copolymers.
Soto-Arriaza, Marco; Cena Ahumada, Eduardo; Bonardd, Sebastián; Melendez, Jaime.
Afiliação
  • Soto-Arriaza M; Escuela de Química y Farmacia, Facultad de Medicina y Ciencia, Universidad San Sebastián, Santiago, Chile.
  • Cena Ahumada E; Instituto de Bioquímica y Microbiología, Facultad de Ciencias, Universidad Austral de Chile, Valdivia, Chile.
  • Bonardd S; Centro de Física de Materiales (CSIC, UPV/EHU)-Materials Physics Center (MPC), Donostia-San Sebastían, Spain.
  • Melendez J; Department of Polymers and Advanced Materials: Physics, Chemistry and Technology, University of the Basque Country UPV/EHU, Donostia-San Sebastian, Spain.
J Liposome Res ; : 1-13, 2024 Jun 07.
Article em En | MEDLINE | ID: mdl-38850012
ABSTRACT
In this study, we evaluated the impact of incorporating diblock and triblock amphiphilic copolymers, as well as cholesterol into DPPC liposomes on the release of a model molecule, calcein, mediated by exogenous phospholipase A2 activity. Our findings show that calcein release slows down in the presence of copolymers at low concentration, while at high concentration, the calcein release profile resembles that of the DPPC control. Additionally, calcein release mediated by exogenous PLA2 decreases as the amount of solubilized cholesterol increases, with a maximum between 18 mol% and 20 mol%. At concentrations higher than 24 mol%, no calcein release was observed. Studies conducted on HEK-293 and HeLa cells revealed that DPPC liposomes reduced viability by only 5% and 12%, respectively, after 3 hours of incubation, while DPPC liposome in presence of 33 mol% of Cholesterol reduced viability by approximately 11% and 23%, respectively, during the same incubation period. For formulations containing copolymers at low and high concentrations, cell viability decreased by approximately 20% and 40%, respectively, after 3 hours of incubation. Based on these preliminary results, we can conclude that the presence of amphiphilic copolymers at low concentration can be used in the design of new DPPC liposomes, and together with cholesterol, they can modulate liposome stabilization. The new formulations showed low cytotoxicity in HEK-293 cells, and it was observed that calcein release depended entirely on PLA2 activity and the presence of calcium ions.
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Texto completo: 1 Base de dados: MEDLINE Idioma: En Ano de publicação: 2024 Tipo de documento: Article

Texto completo: 1 Base de dados: MEDLINE Idioma: En Ano de publicação: 2024 Tipo de documento: Article