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

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  • Author(s): Shao Y;Shao Y; Jia YG; Shi C; Luo J; Zhu XX
  • Source:
    Biomacromolecules [Biomacromolecules] 2014 May 12; Vol. 15 (5), pp. 1837-44. Date of Electronic Publication: 2014 Apr 24.
  • Publication Type:
    Journal Article; Research Support, N.I.H., Extramural; Research Support, Non-U.S. Gov't
  • Language:
    English
  • Additional Information
    • Source:
      Publisher: American Chemical Society Country of Publication: United States NLM ID: 100892849 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1526-4602 (Electronic) Linking ISSN: 15257797 NLM ISO Abbreviation: Biomacromolecules Subsets: MEDLINE
    • Publication Information:
      Original Publication: Washington, DC : American Chemical Society, c2000-
    • Subject Terms:
      Temperature*; Antineoplastic Agents/*administration & dosage ; Cholic Acid/*chemistry ; Drug Carriers/*chemistry ; Ethylene Glycol/*chemistry ; Paclitaxel/*administration & dosage ; Polymers/*chemistry; Antineoplastic Agents/chemistry ; Antineoplastic Agents/pharmacology ; Cell Survival/drug effects ; Drug Carriers/administration & dosage ; Drug Carriers/chemical synthesis ; Drug Screening Assays, Antitumor ; Female ; Humans ; Hydrodynamics ; Inhibitory Concentration 50 ; Micelles ; Models, Molecular ; Molecular Structure ; Ovarian Neoplasms/pathology ; Paclitaxel/chemistry ; Paclitaxel/pharmacology ; Particle Size ; Polymers/administration & dosage ; Polymers/chemical synthesis ; Surface Properties ; Tumor Cells, Cultured
    • 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.
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    • Grant Information:
      R01 CA140449 United States CA NCI NIH HHS; R01CA140449 United States CA NCI NIH HHS
    • Accession Number:
      0 (Antineoplastic Agents)
      0 (Drug Carriers)
      0 (Micelles)
      0 (Polymers)
      FC72KVT52F (Ethylene Glycol)
      G1JO7801AE (Cholic Acid)
      P88XT4IS4D (Paclitaxel)
    • Publication Date:
      Date Created: 20140415 Date Completed: 20150310 Latest Revision: 20211021
    • Publication Date:
      20221213
    • Accession Number:
      PMC4020593
    • Accession Number:
      10.1021/bm5002262
    • Accession Number:
      24725005