Hypothesis: Doxorubicin hydrochloride (DX) is one of the most powerful anticancer agents though its clinical use is impaired by severe undesired side effects. DX encapsulation in nanocarrier systems has been introduced as a mean to reduce its toxicity. Micelles of the nonionic triblock copolymers of poly(ethylene oxide) (PEO) and poly(propylene oxide) (PPO) (PEO-PPO-PEO), are very promising carrier systems. The positive charge of DX confines the drug to the hydrophilic corona region of the micelles. The use of mixed micelles of PEO-PPO-PEO copolymers and a negatively charged bile salt should favour the solubilization of DX in the apolar core region of the micelles. Experiments: We studied the DX uptake in the micellar systems formed by sodium cholate (NaC) and the PEO 100 PPO 65 PEO 100 (F127) copolymer, prepared with different mole ratios (MR = n NaC /n F127 ) in the range 0 ÷ 1. The systems were characterized by small angle X-ray scattering (SAXS) and dynamic light scattering (DLS); DX encapsulation was followed by steady-state and time-resolved fluorescence spectroscopy. Findings: The successful solubilization of DX in the host micellar systems did not affect their structure, as evidenced by both SAXS and DLS data. In the presence of NaC, DX experiences a more apolar environment as indicated by its characteristic fluorescent behaviour. The almost complete uptake of the drug occurred shortly after the sample preparation; however, time resolved fluorescence revealed a slow partition of DX between corona and core regions of the micelles. DX degradation in the mixed micellar systems was markedly reduced relative to aqueous DX solutions. © 2019 Elsevier Inc. Experiments We studied the DX uptake in the micellar systems formed by sodium cholate (NaC) and the PEO100PPO65PEO100 (F127) copolymer, prepared with different mole ratios (MR= nNaC/nF127) in the range 0÷1. The systems were characterized by small angle X-ray scattering (SAXS) and dynamic light scattering (DLS); DX encapsulation was followed by steady-state and time-resolved fluorescence spectroscopy. Findings The successful solubilization of DX in the host micellar systems did not affect their structure, as evidenced by both SAXS and DLS data. In the presence of NaC, DX experiences a more apolar environment as indicated by its characteristic fluorescent behaviour. The almost complete uptake of the drug occurred shortly after the sample preparation; however, time resolved fluorescence revealed a slow partition of DX between corona and core regions of the micelles. DX degradation in the mixed micellar systems was markedly reduced relative to aqueous DX solutions.

A fluorescence study of the loading and time stability of doxorubicin in sodium cholate/PEO-PPO-PEO triblock copolymer mixed micelles / Tasca, Elisamaria; Del Giudice, Alessandra; Galantini, Luciano; Schillén, Karin; Giuliani, Anna Maria; Giustini, Mauro. - In: JOURNAL OF COLLOID AND INTERFACE SCIENCE. - ISSN 0021-9797. - 540:(2019), pp. 593-601. [10.1016/j.jcis.2019.01.075]

A fluorescence study of the loading and time stability of doxorubicin in sodium cholate/PEO-PPO-PEO triblock copolymer mixed micelles

Tasca, Elisamaria;Del Giudice, Alessandra;Galantini, Luciano;Giustini, Mauro
2019

Abstract

Hypothesis: Doxorubicin hydrochloride (DX) is one of the most powerful anticancer agents though its clinical use is impaired by severe undesired side effects. DX encapsulation in nanocarrier systems has been introduced as a mean to reduce its toxicity. Micelles of the nonionic triblock copolymers of poly(ethylene oxide) (PEO) and poly(propylene oxide) (PPO) (PEO-PPO-PEO), are very promising carrier systems. The positive charge of DX confines the drug to the hydrophilic corona region of the micelles. The use of mixed micelles of PEO-PPO-PEO copolymers and a negatively charged bile salt should favour the solubilization of DX in the apolar core region of the micelles. Experiments: We studied the DX uptake in the micellar systems formed by sodium cholate (NaC) and the PEO 100 PPO 65 PEO 100 (F127) copolymer, prepared with different mole ratios (MR = n NaC /n F127 ) in the range 0 ÷ 1. The systems were characterized by small angle X-ray scattering (SAXS) and dynamic light scattering (DLS); DX encapsulation was followed by steady-state and time-resolved fluorescence spectroscopy. Findings: The successful solubilization of DX in the host micellar systems did not affect their structure, as evidenced by both SAXS and DLS data. In the presence of NaC, DX experiences a more apolar environment as indicated by its characteristic fluorescent behaviour. The almost complete uptake of the drug occurred shortly after the sample preparation; however, time resolved fluorescence revealed a slow partition of DX between corona and core regions of the micelles. DX degradation in the mixed micellar systems was markedly reduced relative to aqueous DX solutions. © 2019 Elsevier Inc. Experiments We studied the DX uptake in the micellar systems formed by sodium cholate (NaC) and the PEO100PPO65PEO100 (F127) copolymer, prepared with different mole ratios (MR= nNaC/nF127) in the range 0÷1. The systems were characterized by small angle X-ray scattering (SAXS) and dynamic light scattering (DLS); DX encapsulation was followed by steady-state and time-resolved fluorescence spectroscopy. Findings The successful solubilization of DX in the host micellar systems did not affect their structure, as evidenced by both SAXS and DLS data. In the presence of NaC, DX experiences a more apolar environment as indicated by its characteristic fluorescent behaviour. The almost complete uptake of the drug occurred shortly after the sample preparation; however, time resolved fluorescence revealed a slow partition of DX between corona and core regions of the micelles. DX degradation in the mixed micellar systems was markedly reduced relative to aqueous DX solutions.
fluorescence; doxorubicin; pluronics bile salts; dynamic light scattering; small angle X-ray; scattering drug-delivery
01 Pubblicazione su rivista::01a Articolo in rivista
A fluorescence study of the loading and time stability of doxorubicin in sodium cholate/PEO-PPO-PEO triblock copolymer mixed micelles / Tasca, Elisamaria; Del Giudice, Alessandra; Galantini, Luciano; Schillén, Karin; Giuliani, Anna Maria; Giustini, Mauro. - In: JOURNAL OF COLLOID AND INTERFACE SCIENCE. - ISSN 0021-9797. - 540:(2019), pp. 593-601. [10.1016/j.jcis.2019.01.075]
File allegati a questo prodotto
File Dimensione Formato  
Tasca_Fluorescence-study_2019.pdf

solo gestori archivio

Note: https://linkinghub.elsevier.com/retrieve/pii/S0021979719300864
Tipologia: Versione editoriale (versione pubblicata con il layout dell'editore)
Licenza: Tutti i diritti riservati (All rights reserved)
Dimensione 2.07 MB
Formato Adobe PDF
2.07 MB Adobe PDF   Visualizza/Apri   Richiedi una copia

I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.

Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11573/1216535
Citazioni
  • ???jsp.display-item.citation.pmc??? 2
  • Scopus 20
  • ???jsp.display-item.citation.isi??? 18
social impact