Galactosylated poly(ethylene glycol)-b-poly(l-lactide-co-ß-malic acid) block copolymer micelles for targeted drug delivery: preparation and in vitro characterization
Aili Suo1, Junmin Qian2, Yu Yao1, Wanggang Zhang31Department of Medical Oncology, First Affiliated Hospital of Medical School, Xi’an Jiaotong University, 2State Key Laboratory for Mechanical Behaviors of Materials, School of Materials Science and Engineering, Xi’an Jiaoto...
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Dove Medical Press
2010
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oai:doaj.org-article:fb636773afe54c6aa4bd4b75549ccf3d2021-12-02T02:10:26ZGalactosylated poly(ethylene glycol)-b-poly(l-lactide-co-ß-malic acid) block copolymer micelles for targeted drug delivery: preparation and in vitro characterization1176-91141178-2013https://doaj.org/article/fb636773afe54c6aa4bd4b75549ccf3d2010-11-01T00:00:00Zhttp://www.dovepress.com/galactosylated-polyethylene-glycol-b-polyl-lactide-co-szlig-malic-acid-a5721https://doaj.org/toc/1176-9114https://doaj.org/toc/1178-2013Aili Suo1, Junmin Qian2, Yu Yao1, Wanggang Zhang31Department of Medical Oncology, First Affiliated Hospital of Medical School, Xi’an Jiaotong University, 2State Key Laboratory for Mechanical Behaviors of Materials, School of Materials Science and Engineering, Xi’an Jiaotong University, 3Second Affiliated Hospital of Medical School Xi’an Jiaotong University, Xi’an, ChinaAbstract: Biodegradable galactosylated methoxy poly(ethylene glycol)/poly(l-lactide-co-β-malic acid) (Gal-PEG-b-PLMA) block copolymer micelles were successfully prepared by a solvent diffusion method, and could efficiently encapsulate doxorubicin. The Gal-PEG-b-PLMA micelles before and after doxorubicin loading were characterized by size, morphology, in vitro drug release, and in vitro cytotoxicity in HepG2 cells. Transmission electron microscopy and dynamic light scattering results showed that the empty and doxorubicin-loaded micelles were approximately spherical in shape and had mean sizes of about 72 nm and 85 nm, respectively. In vitro release behavior of doxorubicin from the micelles was pH-dependent, with obviously faster release rates at mildly acidic pH 4.5 and 5.5 compared with physiologic pH 7.4. Methylthiazoletetrazolium assay and flow cytometric analysis indicated that the doxorubicin-loaded galactosylated micelles exhibited a greater growth-inhibitory effect on HepG2 cells than the nongalactosylated doxorubicin-loaded micelles, and induced S phase cell cycle arrest. Confocal laser scanning microscope observations revealed that the galactosylated micelles could be efficiently internalized by HepG2 cells through receptor-mediated endocytosis. The results suggest that Gal-PEG-b-PLMA copolymer micelles are a promising carrier system for targeted drug delivery in cancer therapy.Keywords: polymer micelles, targeted drug delivery, doxorubicin, chemotherapy, hepatocellular carcinoma Aili SuoJunmin QianYu Yaoet alDove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2010, Iss default, Pp 1029-1038 (2010) |
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Medicine (General) R5-920 |
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Medicine (General) R5-920 Aili Suo Junmin Qian Yu Yao et al Galactosylated poly(ethylene glycol)-b-poly(l-lactide-co-ß-malic acid) block copolymer micelles for targeted drug delivery: preparation and in vitro characterization |
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Aili Suo1, Junmin Qian2, Yu Yao1, Wanggang Zhang31Department of Medical Oncology, First Affiliated Hospital of Medical School, Xi’an Jiaotong University, 2State Key Laboratory for Mechanical Behaviors of Materials, School of Materials Science and Engineering, Xi’an Jiaotong University, 3Second Affiliated Hospital of Medical School Xi’an Jiaotong University, Xi’an, ChinaAbstract: Biodegradable galactosylated methoxy poly(ethylene glycol)/poly(l-lactide-co-β-malic acid) (Gal-PEG-b-PLMA) block copolymer micelles were successfully prepared by a solvent diffusion method, and could efficiently encapsulate doxorubicin. The Gal-PEG-b-PLMA micelles before and after doxorubicin loading were characterized by size, morphology, in vitro drug release, and in vitro cytotoxicity in HepG2 cells. Transmission electron microscopy and dynamic light scattering results showed that the empty and doxorubicin-loaded micelles were approximately spherical in shape and had mean sizes of about 72 nm and 85 nm, respectively. In vitro release behavior of doxorubicin from the micelles was pH-dependent, with obviously faster release rates at mildly acidic pH 4.5 and 5.5 compared with physiologic pH 7.4. Methylthiazoletetrazolium assay and flow cytometric analysis indicated that the doxorubicin-loaded galactosylated micelles exhibited a greater growth-inhibitory effect on HepG2 cells than the nongalactosylated doxorubicin-loaded micelles, and induced S phase cell cycle arrest. Confocal laser scanning microscope observations revealed that the galactosylated micelles could be efficiently internalized by HepG2 cells through receptor-mediated endocytosis. The results suggest that Gal-PEG-b-PLMA copolymer micelles are a promising carrier system for targeted drug delivery in cancer therapy.Keywords: polymer micelles, targeted drug delivery, doxorubicin, chemotherapy, hepatocellular carcinoma |
| format |
article |
| author |
Aili Suo Junmin Qian Yu Yao et al |
| author_facet |
Aili Suo Junmin Qian Yu Yao et al |
| author_sort |
Aili Suo |
| title |
Galactosylated poly(ethylene glycol)-b-poly(l-lactide-co-ß-malic acid) block copolymer micelles for targeted drug delivery: preparation and in vitro characterization |
| title_short |
Galactosylated poly(ethylene glycol)-b-poly(l-lactide-co-ß-malic acid) block copolymer micelles for targeted drug delivery: preparation and in vitro characterization |
| title_full |
Galactosylated poly(ethylene glycol)-b-poly(l-lactide-co-ß-malic acid) block copolymer micelles for targeted drug delivery: preparation and in vitro characterization |
| title_fullStr |
Galactosylated poly(ethylene glycol)-b-poly(l-lactide-co-ß-malic acid) block copolymer micelles for targeted drug delivery: preparation and in vitro characterization |
| title_full_unstemmed |
Galactosylated poly(ethylene glycol)-b-poly(l-lactide-co-ß-malic acid) block copolymer micelles for targeted drug delivery: preparation and in vitro characterization |
| title_sort |
galactosylated poly(ethylene glycol)-b-poly(l-lactide-co-ß-malic acid) block copolymer micelles for targeted drug delivery: preparation and in vitro characterization |
| publisher |
Dove Medical Press |
| publishDate |
2010 |
| url |
https://doaj.org/article/fb636773afe54c6aa4bd4b75549ccf3d |
| work_keys_str_mv |
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