Abstract
With the aim to develop alternative therapeutic tools for the treatment of resistant cancers, here we propose targeted Pluronic® P123/F127 mixed micelles (PMM) delivering niclosamide (NCL) as a repositioning strategy to treat multidrug resistant non-small lung cancer cell lines. To build multifunctional PMM for targeting and imaging, Pluronic® F127 was conjugated with biotin, while Pluronic® P123 was fluorescently tagged with rhodamine B, in both cases at one of the two hydroxyl end groups. This design intended to avoid any interference of rhodamine B on biotin exposition on PMM surface, which is a key fundamental for cell trafficking studies. Biotin-decorated PMM were internalized more efficiently than non-targeted PMM in A549 lung cancer cells, while very low internalization was found in NHI3T3 normal fibroblasts. Biotin-decorated PMM entrapped NCL with good efficiency, displayed sustained drug release in protein-rich media and improved cytotoxicity in A549 cells as compared to free NCL (P
| Original language | English |
|---|---|
| Pages (from-to) | 127-139 |
| Number of pages | 13 |
| Journal | International Journal of Pharmaceutics |
| Volume | 511 |
| Issue number | 1 |
| DOIs | |
| Publication status | Published - Sep 10 2016 |
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Keywords
- Lung cancer cells
- Micelle
- Multidrug resistance
- Niclosamide
- Pluronic
ASJC Scopus subject areas
- Pharmaceutical Science
Cite this
Biotin-targeted Pluronic® P123/F127 mixed micelles delivering niclosamide : A repositioning strategy to treat drug-resistant lung cancer cells. / Russo, Annapina; Pellosi, Diogo Silva; Pagliara, Valentina; Milone, Maria Rita; Pucci, Biagio; Caetano, Wilker; Hioka, Noboru; Budillon, Alfredo; Ungaro, Francesca; Russo, Giulia; Quaglia, Fabiana.
In: International Journal of Pharmaceutics, Vol. 511, No. 1, 10.09.2016, p. 127-139.Research output: Contribution to journal › Article
}
TY - JOUR
T1 - Biotin-targeted Pluronic® P123/F127 mixed micelles delivering niclosamide
T2 - A repositioning strategy to treat drug-resistant lung cancer cells
AU - Russo, Annapina
AU - Pellosi, Diogo Silva
AU - Pagliara, Valentina
AU - Milone, Maria Rita
AU - Pucci, Biagio
AU - Caetano, Wilker
AU - Hioka, Noboru
AU - Budillon, Alfredo
AU - Ungaro, Francesca
AU - Russo, Giulia
AU - Quaglia, Fabiana
PY - 2016/9/10
Y1 - 2016/9/10
N2 - With the aim to develop alternative therapeutic tools for the treatment of resistant cancers, here we propose targeted Pluronic® P123/F127 mixed micelles (PMM) delivering niclosamide (NCL) as a repositioning strategy to treat multidrug resistant non-small lung cancer cell lines. To build multifunctional PMM for targeting and imaging, Pluronic® F127 was conjugated with biotin, while Pluronic® P123 was fluorescently tagged with rhodamine B, in both cases at one of the two hydroxyl end groups. This design intended to avoid any interference of rhodamine B on biotin exposition on PMM surface, which is a key fundamental for cell trafficking studies. Biotin-decorated PMM were internalized more efficiently than non-targeted PMM in A549 lung cancer cells, while very low internalization was found in NHI3T3 normal fibroblasts. Biotin-decorated PMM entrapped NCL with good efficiency, displayed sustained drug release in protein-rich media and improved cytotoxicity in A549 cells as compared to free NCL (P
AB - With the aim to develop alternative therapeutic tools for the treatment of resistant cancers, here we propose targeted Pluronic® P123/F127 mixed micelles (PMM) delivering niclosamide (NCL) as a repositioning strategy to treat multidrug resistant non-small lung cancer cell lines. To build multifunctional PMM for targeting and imaging, Pluronic® F127 was conjugated with biotin, while Pluronic® P123 was fluorescently tagged with rhodamine B, in both cases at one of the two hydroxyl end groups. This design intended to avoid any interference of rhodamine B on biotin exposition on PMM surface, which is a key fundamental for cell trafficking studies. Biotin-decorated PMM were internalized more efficiently than non-targeted PMM in A549 lung cancer cells, while very low internalization was found in NHI3T3 normal fibroblasts. Biotin-decorated PMM entrapped NCL with good efficiency, displayed sustained drug release in protein-rich media and improved cytotoxicity in A549 cells as compared to free NCL (P
KW - Lung cancer cells
KW - Micelle
KW - Multidrug resistance
KW - Niclosamide
KW - Pluronic
UR - http://www.scopus.com/inward/record.url?scp=84978193827&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=84978193827&partnerID=8YFLogxK
U2 - 10.1016/j.ijpharm.2016.06.118
DO - 10.1016/j.ijpharm.2016.06.118
M3 - Article
AN - SCOPUS:84978193827
VL - 511
SP - 127
EP - 139
JO - International Journal of Pharmaceutics
JF - International Journal of Pharmaceutics
SN - 0378-5173
IS - 1
ER -