Doxorubicin-loaded galactose-conjugated poly(d,l-lactide-co-glycolide) nanoparticles as hepatocyte-targeting drug carrier

M Margarida Cardoso, Inês N. Peça, Cláudia D. Raposo, Krasimira Todorova Markova Petrova, Maria Teresa Barros, Rui Gardner, A. Bicho

Research output: Contribution to journalArticle

5 Citations (Scopus)

Abstract

The objective of this work is to produce doxorubicin-loaded galactose conjugated poly(D,L-lactide-coglycolide) (PLGA) nanoparticles (NPs) to be specifically recognised by human hepatoma cellular carcinoma (Hep G2) cells and assess NPs cytotoxicity. Doxorubicin-unloaded and doxorubicin-loaded galactose-conjugated PLGA NPs were prepared using an emulsion method and characterised for morphology, size, drug release behaviour, Hep G2 recognition and cell cytotoxicity. The produced doxorubicin-loaded PLGA-galactose conjugate nanoparticles (PLGA-GAL NPs) are spherical in shape with a size of 365 ± 74 nm, a drug encapsulation efficiency of 69% and released in a biphasic pattern with higher release rates at pH 5.
In vitro cell studies confirmed the specific interaction between the receptors of Hep G2 and the PLGA-GAL NPs. Cell cytotoxicity tests showed that unloaded NPs are non-toxic and that doxorubicin-loaded NPs caused a cellular viability decrease of around 80%, therefore representing a promising approach to
improve liver-specific drug delivery.
Original languageEnglish
Pages (from-to)315-322
Number of pages8
JournalJournal of Microencapsulation
Volume33
Issue number4
DOIs
Publication statusPublished - 18 May 2016

Fingerprint

galactose
Drug Carriers
Galactose
Nanoparticles
Doxorubicin
Hepatocytes
drugs
nanoparticles
Cytotoxicity
Hep G2 Cells
cells
dilactide
Drug Delivery Systems
Emulsions
Drug delivery
Encapsulation
viability
liver
Pharmaceutical Preparations
Liver

Keywords

  • Galactosylated PLGA
  • liver-specific nanoparticles
  • Hep G2 cells
  • asialoglycoprotein receptor (ASPGR)
  • doxorubicin delivery

Cite this

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title = "Doxorubicin-loaded galactose-conjugated poly(d,l-lactide-co-glycolide) nanoparticles as hepatocyte-targeting drug carrier",
abstract = "The objective of this work is to produce doxorubicin-loaded galactose conjugated poly(D,L-lactide-coglycolide) (PLGA) nanoparticles (NPs) to be specifically recognised by human hepatoma cellular carcinoma (Hep G2) cells and assess NPs cytotoxicity. Doxorubicin-unloaded and doxorubicin-loaded galactose-conjugated PLGA NPs were prepared using an emulsion method and characterised for morphology, size, drug release behaviour, Hep G2 recognition and cell cytotoxicity. The produced doxorubicin-loaded PLGA-galactose conjugate nanoparticles (PLGA-GAL NPs) are spherical in shape with a size of 365 ± 74 nm, a drug encapsulation efficiency of 69{\%} and released in a biphasic pattern with higher release rates at pH 5.In vitro cell studies confirmed the specific interaction between the receptors of Hep G2 and the PLGA-GAL NPs. Cell cytotoxicity tests showed that unloaded NPs are non-toxic and that doxorubicin-loaded NPs caused a cellular viability decrease of around 80{\%}, therefore representing a promising approach toimprove liver-specific drug delivery.",
keywords = "Galactosylated PLGA, liver-specific nanoparticles, Hep G2 cells, asialoglycoprotein receptor (ASPGR), doxorubicin delivery",
author = "Cardoso, {M Margarida} and Pe{\cc}a, {In{\^e}s N.} and Raposo, {Cl{\'a}udia D.} and Petrova, {Krasimira Todorova Markova} and Barros, {Maria Teresa} and Rui Gardner and A. Bicho",
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Doxorubicin-loaded galactose-conjugated poly(d,l-lactide-co-glycolide) nanoparticles as hepatocyte-targeting drug carrier. / Cardoso, M Margarida; Peça, Inês N.; Raposo, Cláudia D.; Petrova, Krasimira Todorova Markova; Barros, Maria Teresa; Gardner, Rui; Bicho, A.

In: Journal of Microencapsulation, Vol. 33, No. 4, 18.05.2016, p. 315-322.

Research output: Contribution to journalArticle

TY - JOUR

T1 - Doxorubicin-loaded galactose-conjugated poly(d,l-lactide-co-glycolide) nanoparticles as hepatocyte-targeting drug carrier

AU - Cardoso, M Margarida

AU - Peça, Inês N.

AU - Raposo, Cláudia D.

AU - Petrova, Krasimira Todorova Markova

AU - Barros, Maria Teresa

AU - Gardner, Rui

AU - Bicho, A.

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N2 - The objective of this work is to produce doxorubicin-loaded galactose conjugated poly(D,L-lactide-coglycolide) (PLGA) nanoparticles (NPs) to be specifically recognised by human hepatoma cellular carcinoma (Hep G2) cells and assess NPs cytotoxicity. Doxorubicin-unloaded and doxorubicin-loaded galactose-conjugated PLGA NPs were prepared using an emulsion method and characterised for morphology, size, drug release behaviour, Hep G2 recognition and cell cytotoxicity. The produced doxorubicin-loaded PLGA-galactose conjugate nanoparticles (PLGA-GAL NPs) are spherical in shape with a size of 365 ± 74 nm, a drug encapsulation efficiency of 69% and released in a biphasic pattern with higher release rates at pH 5.In vitro cell studies confirmed the specific interaction between the receptors of Hep G2 and the PLGA-GAL NPs. Cell cytotoxicity tests showed that unloaded NPs are non-toxic and that doxorubicin-loaded NPs caused a cellular viability decrease of around 80%, therefore representing a promising approach toimprove liver-specific drug delivery.

AB - The objective of this work is to produce doxorubicin-loaded galactose conjugated poly(D,L-lactide-coglycolide) (PLGA) nanoparticles (NPs) to be specifically recognised by human hepatoma cellular carcinoma (Hep G2) cells and assess NPs cytotoxicity. Doxorubicin-unloaded and doxorubicin-loaded galactose-conjugated PLGA NPs were prepared using an emulsion method and characterised for morphology, size, drug release behaviour, Hep G2 recognition and cell cytotoxicity. The produced doxorubicin-loaded PLGA-galactose conjugate nanoparticles (PLGA-GAL NPs) are spherical in shape with a size of 365 ± 74 nm, a drug encapsulation efficiency of 69% and released in a biphasic pattern with higher release rates at pH 5.In vitro cell studies confirmed the specific interaction between the receptors of Hep G2 and the PLGA-GAL NPs. Cell cytotoxicity tests showed that unloaded NPs are non-toxic and that doxorubicin-loaded NPs caused a cellular viability decrease of around 80%, therefore representing a promising approach toimprove liver-specific drug delivery.

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KW - liver-specific nanoparticles

KW - Hep G2 cells

KW - asialoglycoprotein receptor (ASPGR)

KW - doxorubicin delivery

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SN - 0265-2048

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