Block and random copolymers bearing cholic acid and oligo(ethylene glycol) pendant groups: Aggregation, thermosensitivity, and drug loading

Yu Shao, Yong Guang Jia, Changying Shi, Juntao Luo, X. X. Zhu

Research output: Contribution to journalArticle

34 Citations (Scopus)

Abstract

A series of block and random copolymers consisting of oligo(ethylene glycol) and cholic acid pendant groups were synthesized via ring-opening metathesis polymerization of their norbornene derivatives. These block and random copolymers were designed to have similar molecular weights and comonomer ratios; both types of copolymers showed thermosensitivity in aqueous solutions with similar cloud points. The copolymers self-assembled into micelles in water as shown by dynamic light scattering and transmission electron microscopy. The hydrodynamic diameter of the micelles formed by the block copolymer is much larger and exhibited a broad and gradual shrinkage from 20 to 54 °C below its cloud point, while the micelles formed by the random copolymers are smaller in size but exhibited some swelling in the same temperature range. Based on in vitro drug release studies, 78% and 24% paclitaxel (PTX) were released in 24 h from micelles self-assembled by the block and random copolymers, respectively. PTX-loaded micelles formed by the block and random copolymers exhibited apparent antitumor efficacy toward the ovarian cancer cells with a particularly low half-maximal inhibitory concentration (IC50) of 27.4 and 40.2 ng/mL, respectively. Cholic acid-based micelles show promise as a versatile and potent platform for cancer chemotherapy.

Original languageEnglish (US)
Pages (from-to)1837-1844
Number of pages8
JournalBiomacromolecules
Volume15
Issue number5
DOIs
StatePublished - May 12 2014
Externally publishedYes

Fingerprint

Bearings (structural)
Cholic Acid
Ethylene Glycol
Ethylene glycol
Micelles
Agglomeration
Copolymers
Acids
Pharmaceutical Preparations
Paclitaxel
Chemotherapy
Ring opening polymerization
Dynamic light scattering
Light transmission
Block copolymers
Swelling
Hydrodynamics
Molecular weight
Cells
Transmission electron microscopy

ASJC Scopus subject areas

  • Bioengineering
  • Materials Chemistry
  • Polymers and Plastics
  • Biomaterials

Cite this

Block and random copolymers bearing cholic acid and oligo(ethylene glycol) pendant groups : Aggregation, thermosensitivity, and drug loading. / Shao, Yu; Jia, Yong Guang; Shi, Changying; Luo, Juntao; Zhu, X. X.

In: Biomacromolecules, Vol. 15, No. 5, 12.05.2014, p. 1837-1844.

Research output: Contribution to journalArticle

Shao, Yu ; Jia, Yong Guang ; Shi, Changying ; Luo, Juntao ; Zhu, X. X. / Block and random copolymers bearing cholic acid and oligo(ethylene glycol) pendant groups : Aggregation, thermosensitivity, and drug loading. In: Biomacromolecules. 2014 ; Vol. 15, No. 5. pp. 1837-1844.
@article{967b8dda24834cd6a0ddfae0e08fba7c,
title = "Block and random copolymers bearing cholic acid and oligo(ethylene glycol) pendant groups: Aggregation, thermosensitivity, and drug loading",
abstract = "A series of block and random copolymers consisting of oligo(ethylene glycol) and cholic acid pendant groups were synthesized via ring-opening metathesis polymerization of their norbornene derivatives. These block and random copolymers were designed to have similar molecular weights and comonomer ratios; both types of copolymers showed thermosensitivity in aqueous solutions with similar cloud points. The copolymers self-assembled into micelles in water as shown by dynamic light scattering and transmission electron microscopy. The hydrodynamic diameter of the micelles formed by the block copolymer is much larger and exhibited a broad and gradual shrinkage from 20 to 54 °C below its cloud point, while the micelles formed by the random copolymers are smaller in size but exhibited some swelling in the same temperature range. Based on in vitro drug release studies, 78{\%} and 24{\%} paclitaxel (PTX) were released in 24 h from micelles self-assembled by the block and random copolymers, respectively. PTX-loaded micelles formed by the block and random copolymers exhibited apparent antitumor efficacy toward the ovarian cancer cells with a particularly low half-maximal inhibitory concentration (IC50) of 27.4 and 40.2 ng/mL, respectively. Cholic acid-based micelles show promise as a versatile and potent platform for cancer chemotherapy.",
author = "Yu Shao and Jia, {Yong Guang} and Changying Shi and Juntao Luo and Zhu, {X. X.}",
year = "2014",
month = "5",
day = "12",
doi = "10.1021/bm5002262",
language = "English (US)",
volume = "15",
pages = "1837--1844",
journal = "Biomacromolecules",
issn = "1525-7797",
publisher = "American Chemical Society",
number = "5",

}

TY - JOUR

T1 - Block and random copolymers bearing cholic acid and oligo(ethylene glycol) pendant groups

T2 - Aggregation, thermosensitivity, and drug loading

AU - Shao, Yu

AU - Jia, Yong Guang

AU - Shi, Changying

AU - Luo, Juntao

AU - Zhu, X. X.

PY - 2014/5/12

Y1 - 2014/5/12

N2 - A series of block and random copolymers consisting of oligo(ethylene glycol) and cholic acid pendant groups were synthesized via ring-opening metathesis polymerization of their norbornene derivatives. These block and random copolymers were designed to have similar molecular weights and comonomer ratios; both types of copolymers showed thermosensitivity in aqueous solutions with similar cloud points. The copolymers self-assembled into micelles in water as shown by dynamic light scattering and transmission electron microscopy. The hydrodynamic diameter of the micelles formed by the block copolymer is much larger and exhibited a broad and gradual shrinkage from 20 to 54 °C below its cloud point, while the micelles formed by the random copolymers are smaller in size but exhibited some swelling in the same temperature range. Based on in vitro drug release studies, 78% and 24% paclitaxel (PTX) were released in 24 h from micelles self-assembled by the block and random copolymers, respectively. PTX-loaded micelles formed by the block and random copolymers exhibited apparent antitumor efficacy toward the ovarian cancer cells with a particularly low half-maximal inhibitory concentration (IC50) of 27.4 and 40.2 ng/mL, respectively. Cholic acid-based micelles show promise as a versatile and potent platform for cancer chemotherapy.

AB - A series of block and random copolymers consisting of oligo(ethylene glycol) and cholic acid pendant groups were synthesized via ring-opening metathesis polymerization of their norbornene derivatives. These block and random copolymers were designed to have similar molecular weights and comonomer ratios; both types of copolymers showed thermosensitivity in aqueous solutions with similar cloud points. The copolymers self-assembled into micelles in water as shown by dynamic light scattering and transmission electron microscopy. The hydrodynamic diameter of the micelles formed by the block copolymer is much larger and exhibited a broad and gradual shrinkage from 20 to 54 °C below its cloud point, while the micelles formed by the random copolymers are smaller in size but exhibited some swelling in the same temperature range. Based on in vitro drug release studies, 78% and 24% paclitaxel (PTX) were released in 24 h from micelles self-assembled by the block and random copolymers, respectively. PTX-loaded micelles formed by the block and random copolymers exhibited apparent antitumor efficacy toward the ovarian cancer cells with a particularly low half-maximal inhibitory concentration (IC50) of 27.4 and 40.2 ng/mL, respectively. Cholic acid-based micelles show promise as a versatile and potent platform for cancer chemotherapy.

UR - http://www.scopus.com/inward/record.url?scp=84900464943&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=84900464943&partnerID=8YFLogxK

U2 - 10.1021/bm5002262

DO - 10.1021/bm5002262

M3 - Article

C2 - 24725005

AN - SCOPUS:84900464943

VL - 15

SP - 1837

EP - 1844

JO - Biomacromolecules

JF - Biomacromolecules

SN - 1525-7797

IS - 5

ER -