Liposomes Loaded with Cisplatin and Magnetic Nanoparticles: Physicochemical Characterization, Pharmacokinetics, and In-Vitro Efficacy

With the aim improving drug delivery, liposomes have been employed as carriers for chemotherapeutics achieving promising results; their co-encapsulation with magnetic nanoparticles is evaluated in this work. The objective of this study was to examine the physicochemical characteristics, the pharmaco...

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Main Authors: Alfonso Toro-Cordova, Mario Flores-Cruz, Jaime Santoyo-Salazar, Ernesto Carrillo-Nava, Rafael Jurado, Pavel A. Figueroa-Rodriguez, Pedro Lopez-Sanchez, Luis A. Medina, Patricia Garcia-Lopez
Format: Article
Language:English
Published: MDPI AG 2018-09-01
Series:Molecules
Subjects:
Online Access:http://www.mdpi.com/1420-3049/23/9/2272
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author Alfonso Toro-Cordova
Mario Flores-Cruz
Jaime Santoyo-Salazar
Ernesto Carrillo-Nava
Rafael Jurado
Pavel A. Figueroa-Rodriguez
Pedro Lopez-Sanchez
Luis A. Medina
Patricia Garcia-Lopez
author_facet Alfonso Toro-Cordova
Mario Flores-Cruz
Jaime Santoyo-Salazar
Ernesto Carrillo-Nava
Rafael Jurado
Pavel A. Figueroa-Rodriguez
Pedro Lopez-Sanchez
Luis A. Medina
Patricia Garcia-Lopez
author_sort Alfonso Toro-Cordova
collection DOAJ
description With the aim improving drug delivery, liposomes have been employed as carriers for chemotherapeutics achieving promising results; their co-encapsulation with magnetic nanoparticles is evaluated in this work. The objective of this study was to examine the physicochemical characteristics, the pharmacokinetic behaviour, and the efficacy of pegylated liposomes loaded with cisplatin and magnetic nanoparticles (magnetite) (Cis-MLs). Cis-MLs were prepared by a modified reverse-phase evaporation method. To characterize their physicochemical properties, an evaluation was made of particle size, ζ-potential, phospholipid and cholesterol concentration, phase transition temperature (Tm), the encapsulation efficiency of cisplatin and magnetite, and drug release profiles. Additionally, pharmacokinetic studies were conducted on normal Wistar rats, while apoptosis and the cytotoxic effect were assessed with HeLa cells. We present a method for simultaneously encapsulating cisplatin at the core and also embedding magnetite nanoparticles on the membrane of liposomes with a mean vesicular size of 104.4 ± 11.5 nm and a ζ-potential of −40.5 ± 0.8 mV, affording a stable formulation with a safe pharmacokinetic profile. These liposomes elicited a significant effect on cell viability and triggered apoptosis in HeLa cells.
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spelling doaj.art-16906d84a00d4b91af272270250b92b32022-12-22T02:24:17ZengMDPI AGMolecules1420-30492018-09-01239227210.3390/molecules23092272molecules23092272Liposomes Loaded with Cisplatin and Magnetic Nanoparticles: Physicochemical Characterization, Pharmacokinetics, and In-Vitro EfficacyAlfonso Toro-Cordova0Mario Flores-Cruz1Jaime Santoyo-Salazar2Ernesto Carrillo-Nava3Rafael Jurado4Pavel A. Figueroa-Rodriguez5Pedro Lopez-Sanchez6Luis A. Medina7Patricia Garcia-Lopez8Laboratorio de Farmacología, Subdirección de Investigación Básica, Instituto Nacional de Cancerología, 14080 CDMX, MexicoLaboratorio de Farmacología, Subdirección de Investigación Básica, Instituto Nacional de Cancerología, 14080 CDMX, MexicoDepartamento de Física, Centro de Investigacion y de Estudios Avanzados del Instituto Politécnico Nacional, CINVESTAV-IPN, Zacatenco, 07360 CDMX, MexicoLaboratorio de Biofisicoquímica, Departamento de Fisicoquímica, Facultad de Química, Universidad Nacional Autónoma de México, 014510 CDMX, MexicoLaboratorio de Farmacología, Subdirección de Investigación Básica, Instituto Nacional de Cancerología, 14080 CDMX, MexicoUnidad de Investigación Biomédica en Cáncer INCan-UNAM, Instituto Nacional de Cancerología, 14080 CDMX, MexicoSección de Estudios de Posgrado e Investigación, Escuela Superior de Medicina, Instituto Politécnico Nacional, 11340 CDMX, MexicoUnidad de Investigación Biomédica en Cáncer INCan-UNAM, Instituto Nacional de Cancerología, 14080 CDMX, MexicoLaboratorio de Farmacología, Subdirección de Investigación Básica, Instituto Nacional de Cancerología, 14080 CDMX, MexicoWith the aim improving drug delivery, liposomes have been employed as carriers for chemotherapeutics achieving promising results; their co-encapsulation with magnetic nanoparticles is evaluated in this work. The objective of this study was to examine the physicochemical characteristics, the pharmacokinetic behaviour, and the efficacy of pegylated liposomes loaded with cisplatin and magnetic nanoparticles (magnetite) (Cis-MLs). Cis-MLs were prepared by a modified reverse-phase evaporation method. To characterize their physicochemical properties, an evaluation was made of particle size, ζ-potential, phospholipid and cholesterol concentration, phase transition temperature (Tm), the encapsulation efficiency of cisplatin and magnetite, and drug release profiles. Additionally, pharmacokinetic studies were conducted on normal Wistar rats, while apoptosis and the cytotoxic effect were assessed with HeLa cells. We present a method for simultaneously encapsulating cisplatin at the core and also embedding magnetite nanoparticles on the membrane of liposomes with a mean vesicular size of 104.4 ± 11.5 nm and a ζ-potential of −40.5 ± 0.8 mV, affording a stable formulation with a safe pharmacokinetic profile. These liposomes elicited a significant effect on cell viability and triggered apoptosis in HeLa cells.http://www.mdpi.com/1420-3049/23/9/2272cancercisplatindrug deliverymagnetiteliposomes pharmacokinetics
spellingShingle Alfonso Toro-Cordova
Mario Flores-Cruz
Jaime Santoyo-Salazar
Ernesto Carrillo-Nava
Rafael Jurado
Pavel A. Figueroa-Rodriguez
Pedro Lopez-Sanchez
Luis A. Medina
Patricia Garcia-Lopez
Liposomes Loaded with Cisplatin and Magnetic Nanoparticles: Physicochemical Characterization, Pharmacokinetics, and In-Vitro Efficacy
Molecules
cancer
cisplatin
drug delivery
magnetite
liposomes pharmacokinetics
title Liposomes Loaded with Cisplatin and Magnetic Nanoparticles: Physicochemical Characterization, Pharmacokinetics, and In-Vitro Efficacy
title_full Liposomes Loaded with Cisplatin and Magnetic Nanoparticles: Physicochemical Characterization, Pharmacokinetics, and In-Vitro Efficacy
title_fullStr Liposomes Loaded with Cisplatin and Magnetic Nanoparticles: Physicochemical Characterization, Pharmacokinetics, and In-Vitro Efficacy
title_full_unstemmed Liposomes Loaded with Cisplatin and Magnetic Nanoparticles: Physicochemical Characterization, Pharmacokinetics, and In-Vitro Efficacy
title_short Liposomes Loaded with Cisplatin and Magnetic Nanoparticles: Physicochemical Characterization, Pharmacokinetics, and In-Vitro Efficacy
title_sort liposomes loaded with cisplatin and magnetic nanoparticles physicochemical characterization pharmacokinetics and in vitro efficacy
topic cancer
cisplatin
drug delivery
magnetite
liposomes pharmacokinetics
url http://www.mdpi.com/1420-3049/23/9/2272
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