Doxorubicin-loaded cholic acid-polyethyleneimine micelles for targeted delivery of antitumor drugs

Synthesis, characterization, and evaluation of their in vitro cytotoxicity

Muhammad Wahab Amjad, Mohd Cairul Iqbal Mohd Amin, Haliza Katas, Adeel Masood Butt

Research output: Contribution to journalArticle

18 Citations (Scopus)

Abstract

Doxorubicin-loaded micelles were prepared from a copolymer comprising cholic acid (CA) and polyethyleneimine (PEI) for the delivery of antitumor drugs. The CA-PEI copolymer was synthesized via pairing mediated by N,N'-dicyclohexylcarbodiimide and N-hydroxysuccinimide using dichloromethane as a solvent. Fourier transform infrared and nuclear magnetic resonance analyses were performed to verify the formation of an amide linkage between CA and PEI and doxorubicin localization into the copolymer. Dynamic light scattering and transmission electron microscopy studies revealed that the copolymer could self-assemble into micelles with a spherical morphology and an average diameter of <200 nm. The CA-PEI copolymer was also characterized by X-ray diffraction and differential scanning calorimetry. Doxorubicin-loaded micelles were prepared by dialysis method. A drug release study showed reduced drug release with escalating drug content. In a cytotoxicity assay using human colorectal adenocarcinoma (DLD-1) cells, the doxorubicin-loaded CA-PEI micelles exhibited better antitumor activity than that shown by doxorubicin. This is the first study on CA-PEI micelles as doxorubicin carriers, and this study demonstrated that they are promising candidates as carriers for sustained targeted antitumor drug delivery system.

Original languageEnglish
Pages (from-to)1-9
Number of pages9
JournalNanoscale Research Letters
Volume7
Issue number1
DOIs
Publication statusPublished - 2012

Fingerprint

Cholic Acid
Polyethyleneimine
Micelles
Cytotoxicity
Antineoplastic Agents
Doxorubicin
delivery
micelles
drugs
copolymers
Copolymers
acids
Acids
evaluation
synthesis
Pharmaceutical Preparations
Dicyclohexylcarbodiimide
dialysis
Dialysis
light transmission

Keywords

  • Cholic acid
  • Doxorubicin
  • Micelles
  • Nanoparticles
  • Polyethyleneimine

ASJC Scopus subject areas

  • Materials Science(all)
  • Condensed Matter Physics

Cite this

@article{7eef21e43c274e1eb9a52209fb4df5df,
title = "Doxorubicin-loaded cholic acid-polyethyleneimine micelles for targeted delivery of antitumor drugs: Synthesis, characterization, and evaluation of their in vitro cytotoxicity",
abstract = "Doxorubicin-loaded micelles were prepared from a copolymer comprising cholic acid (CA) and polyethyleneimine (PEI) for the delivery of antitumor drugs. The CA-PEI copolymer was synthesized via pairing mediated by N,N'-dicyclohexylcarbodiimide and N-hydroxysuccinimide using dichloromethane as a solvent. Fourier transform infrared and nuclear magnetic resonance analyses were performed to verify the formation of an amide linkage between CA and PEI and doxorubicin localization into the copolymer. Dynamic light scattering and transmission electron microscopy studies revealed that the copolymer could self-assemble into micelles with a spherical morphology and an average diameter of <200 nm. The CA-PEI copolymer was also characterized by X-ray diffraction and differential scanning calorimetry. Doxorubicin-loaded micelles were prepared by dialysis method. A drug release study showed reduced drug release with escalating drug content. In a cytotoxicity assay using human colorectal adenocarcinoma (DLD-1) cells, the doxorubicin-loaded CA-PEI micelles exhibited better antitumor activity than that shown by doxorubicin. This is the first study on CA-PEI micelles as doxorubicin carriers, and this study demonstrated that they are promising candidates as carriers for sustained targeted antitumor drug delivery system.",
keywords = "Cholic acid, Doxorubicin, Micelles, Nanoparticles, Polyethyleneimine",
author = "Amjad, {Muhammad Wahab} and {Mohd Amin}, {Mohd Cairul Iqbal} and Haliza Katas and Butt, {Adeel Masood}",
year = "2012",
doi = "10.1186/1556-276X-7-687",
language = "English",
volume = "7",
pages = "1--9",
journal = "Nanoscale Research Letters",
issn = "1931-7573",
publisher = "Springer New York",
number = "1",

}

TY - JOUR

T1 - Doxorubicin-loaded cholic acid-polyethyleneimine micelles for targeted delivery of antitumor drugs

T2 - Synthesis, characterization, and evaluation of their in vitro cytotoxicity

AU - Amjad, Muhammad Wahab

AU - Mohd Amin, Mohd Cairul Iqbal

AU - Katas, Haliza

AU - Butt, Adeel Masood

PY - 2012

Y1 - 2012

N2 - Doxorubicin-loaded micelles were prepared from a copolymer comprising cholic acid (CA) and polyethyleneimine (PEI) for the delivery of antitumor drugs. The CA-PEI copolymer was synthesized via pairing mediated by N,N'-dicyclohexylcarbodiimide and N-hydroxysuccinimide using dichloromethane as a solvent. Fourier transform infrared and nuclear magnetic resonance analyses were performed to verify the formation of an amide linkage between CA and PEI and doxorubicin localization into the copolymer. Dynamic light scattering and transmission electron microscopy studies revealed that the copolymer could self-assemble into micelles with a spherical morphology and an average diameter of <200 nm. The CA-PEI copolymer was also characterized by X-ray diffraction and differential scanning calorimetry. Doxorubicin-loaded micelles were prepared by dialysis method. A drug release study showed reduced drug release with escalating drug content. In a cytotoxicity assay using human colorectal adenocarcinoma (DLD-1) cells, the doxorubicin-loaded CA-PEI micelles exhibited better antitumor activity than that shown by doxorubicin. This is the first study on CA-PEI micelles as doxorubicin carriers, and this study demonstrated that they are promising candidates as carriers for sustained targeted antitumor drug delivery system.

AB - Doxorubicin-loaded micelles were prepared from a copolymer comprising cholic acid (CA) and polyethyleneimine (PEI) for the delivery of antitumor drugs. The CA-PEI copolymer was synthesized via pairing mediated by N,N'-dicyclohexylcarbodiimide and N-hydroxysuccinimide using dichloromethane as a solvent. Fourier transform infrared and nuclear magnetic resonance analyses were performed to verify the formation of an amide linkage between CA and PEI and doxorubicin localization into the copolymer. Dynamic light scattering and transmission electron microscopy studies revealed that the copolymer could self-assemble into micelles with a spherical morphology and an average diameter of <200 nm. The CA-PEI copolymer was also characterized by X-ray diffraction and differential scanning calorimetry. Doxorubicin-loaded micelles were prepared by dialysis method. A drug release study showed reduced drug release with escalating drug content. In a cytotoxicity assay using human colorectal adenocarcinoma (DLD-1) cells, the doxorubicin-loaded CA-PEI micelles exhibited better antitumor activity than that shown by doxorubicin. This is the first study on CA-PEI micelles as doxorubicin carriers, and this study demonstrated that they are promising candidates as carriers for sustained targeted antitumor drug delivery system.

KW - Cholic acid

KW - Doxorubicin

KW - Micelles

KW - Nanoparticles

KW - Polyethyleneimine

UR - http://www.scopus.com/inward/record.url?scp=84875350068&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=84875350068&partnerID=8YFLogxK

U2 - 10.1186/1556-276X-7-687

DO - 10.1186/1556-276X-7-687

M3 - Article

VL - 7

SP - 1

EP - 9

JO - Nanoscale Research Letters

JF - Nanoscale Research Letters

SN - 1931-7573

IS - 1

ER -