Polymeric micelles of poly(2-ethyl-2-oxazoline)-block-poly(ε-caprolactone) copolymer as a carrier for paclitaxel

Sang Cheon Lee, Chulhee Kim, Ick Chan Kwon, Hesson Chung, Seo Young Jeong

Research output: Contribution to journalArticle

217 Citations (Scopus)

Abstract

Polymeric micelles based on amphiphilic block copolymers of poly(2-ethyl-2-oxazoline) (PEtOz) and poly(ε-caprolactone) (PCL) were prepared in an aqueous phase. The loading of paclitaxel into PEtOz-PCL micelles was confirmed by 1H-NMR spectra. Paclitaxel was efficiently loaded into PEtOz-PCL micelles using dialysis method, and the loading content of paclitaxel in micelles was in the range 0.5-7.6 wt.% depending on the block composition of block copolymers, organic solvent used in the dialysis, and feed weight ratio of paclitaxel to block copolymer. The higher the content of hydrophobic block in the block copolymers, the higher the loading efficiency of micelles for paclitaxel. When acetonitrile was used as solvent, a higher drug loading efficiency was obtained than with THF. The loading efficiency decreased with increasing feed weight ratio of paclitaxel to block copolymer from 0.1:1 to 0.2:1. The hydrodynamic diameters of paclitaxel-loaded micelles were in the range 18.3-23.4 nm with narrow size distribution. The hemolysis test of PEtOz-PCL performed in vitro indicated that the toxicity of PEtOz-PCLs to lipid membrane was not significant compared with Tween 80, and was comparable to that observed with Cremophore EL. The proliferation inhibition activity of paclitaxel-loaded micelles for KB human epidermoid carcinoma cells was also evaluated in vitro. Paclitaxel-entrapped polymeric micelles exhibited comparable activity to that observed with Cremophore EL-based paclitaxel formulations in inhibiting the growth of KB cells.

Original languageEnglish
Pages (from-to)437-446
Number of pages10
JournalJournal of Controlled Release
Volume89
Issue number3
DOIs
Publication statusPublished - 2003 May 20
Externally publishedYes

Fingerprint

Micelles
Paclitaxel
Dialysis
poly(2-ethyl-2-oxazoline)
polycaprolactone
KB Cells
Weights and Measures
Polysorbates
Hydrodynamics
Membrane Lipids
Hemolysis
Squamous Cell Carcinoma

Keywords

  • Amphiphilic block copolymers
  • Cell growth inhibition
  • Hemolysis
  • Paclitaxel
  • Poly(2-ethyl-2-oxazoline)
  • Polymeric micelles

ASJC Scopus subject areas

  • Pharmaceutical Science

Cite this

Polymeric micelles of poly(2-ethyl-2-oxazoline)-block-poly(ε-caprolactone) copolymer as a carrier for paclitaxel. / Lee, Sang Cheon; Kim, Chulhee; Kwon, Ick Chan; Chung, Hesson; Jeong, Seo Young.

In: Journal of Controlled Release, Vol. 89, No. 3, 20.05.2003, p. 437-446.

Research output: Contribution to journalArticle

Lee, Sang Cheon ; Kim, Chulhee ; Kwon, Ick Chan ; Chung, Hesson ; Jeong, Seo Young. / Polymeric micelles of poly(2-ethyl-2-oxazoline)-block-poly(ε-caprolactone) copolymer as a carrier for paclitaxel. In: Journal of Controlled Release. 2003 ; Vol. 89, No. 3. pp. 437-446.
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abstract = "Polymeric micelles based on amphiphilic block copolymers of poly(2-ethyl-2-oxazoline) (PEtOz) and poly(ε-caprolactone) (PCL) were prepared in an aqueous phase. The loading of paclitaxel into PEtOz-PCL micelles was confirmed by 1H-NMR spectra. Paclitaxel was efficiently loaded into PEtOz-PCL micelles using dialysis method, and the loading content of paclitaxel in micelles was in the range 0.5-7.6 wt.{\%} depending on the block composition of block copolymers, organic solvent used in the dialysis, and feed weight ratio of paclitaxel to block copolymer. The higher the content of hydrophobic block in the block copolymers, the higher the loading efficiency of micelles for paclitaxel. When acetonitrile was used as solvent, a higher drug loading efficiency was obtained than with THF. The loading efficiency decreased with increasing feed weight ratio of paclitaxel to block copolymer from 0.1:1 to 0.2:1. The hydrodynamic diameters of paclitaxel-loaded micelles were in the range 18.3-23.4 nm with narrow size distribution. The hemolysis test of PEtOz-PCL performed in vitro indicated that the toxicity of PEtOz-PCLs to lipid membrane was not significant compared with Tween 80, and was comparable to that observed with Cremophore EL. The proliferation inhibition activity of paclitaxel-loaded micelles for KB human epidermoid carcinoma cells was also evaluated in vitro. Paclitaxel-entrapped polymeric micelles exhibited comparable activity to that observed with Cremophore EL-based paclitaxel formulations in inhibiting the growth of KB cells.",
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