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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 ; Giuliani, Anna Maria ; Guistini, Mauro and Schillén, Karin LU orcid (2019) In Journal of Colloid and Interface Science 540. p.593-601
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... (More)
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 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.


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organization
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type
Contribution to journal
publication status
published
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in
Journal of Colloid and Interface Science
volume
540
pages
9 pages
publisher
Elsevier
external identifiers
  • scopus:85060194638
  • pmid:30677613
ISSN
0021-9797
DOI
10.1016/j.jcis.2019.01.075
language
English
LU publication?
yes
id
b6ef3d92-6b6a-4305-8daf-d7d34cec6bfe
date added to LUP
2019-01-17 11:06:17
date last changed
2022-04-25 20:12:20
@article{b6ef3d92-6b6a-4305-8daf-d7d34cec6bfe,
  abstract     = {{Hypothesis<br/>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.<br/>Experiments<br/>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.<br/>Findings<br/>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.<br/><br/><br/>}},
  author       = {{Tasca, Elisamaria and Del Giudice, Alessandra and Galantini, Luciano and Giuliani, Anna Maria and Guistini, Mauro and Schillén, Karin}},
  issn         = {{0021-9797}},
  language     = {{eng}},
  pages        = {{593--601}},
  publisher    = {{Elsevier}},
  series       = {{Journal of Colloid and Interface Science}},
  title        = {{A fluorescence study of the loading and time stability of doxorubicin in sodium cholate/PEO-PPO-PEO triblock copolymer mixed micelles}},
  url          = {{http://dx.doi.org/10.1016/j.jcis.2019.01.075}},
  doi          = {{10.1016/j.jcis.2019.01.075}},
  volume       = {{540}},
  year         = {{2019}},
}