Affiliations 

  • 1 Department of Pharmacy, Faculty of Medicine, University of Malaya, 50603, Kuala Lumpur, Malaysia
  • 2 Department of Chemical Engineering, National Taiwan University of Science and Technology, 43 Section 4, Keelung Road, Taipei, 10607, Taiwan
  • 3 Department of Pharmacology, Faculty of Medicine, University of Malaya, 50603, Kuala Lumpur, Malaysia
  • 4 Graduate Institute of Applied Science and Technology, National Taiwan University of Science and Technology, 43 Section 4, Keelung Road, Taipei, 10607, Taiwan
  • 5 Department of Materials Science and Chemistry, University of Hyogo, 2167 Shosha, Himeji, Hyogo, 671-2280, Japan
Macromol Biosci, 2016 06;16(6):882-95.
PMID: 26900760 DOI: 10.1002/mabi.201500435

Abstract

Previously synthesized amphiphilic diblock copolymers with pendant dendron moieties have been investigated for their potential use as drug carriers to improve the delivery of an anticancer drug to human breast cancer cells. Diblock copolymer (P71 D3 )-based micelles effectively encapsulate the doxorubicin (DOX) with a high drug-loading capacity (≈95%, 104 DOX molecules per micelle), which is approximately double the amount of drug loaded into the diblock copolymer (P296 D1 ) vesicles. DOX released from the resultant P71 D3 /DOX micelles is approximately 1.3-fold more abundant, at a tumoral acidic pH of 5.5 compared with a pH of 7.4. The P71 D3 /DOX micelles also enhance drug potency in breast cancer MDA-MB-231 cells due to their higher intracellular uptake, by approximately twofold, compared with the vesicular nanocarrier, and free DOX. Micellar nanocarriers are taken up by lysosomes via energy-dependent processes, followed by the release of DOX into the cytoplasm and subsequent translocation into the nucleus, where it exert its cytotoxic effect.

* Title and MeSH Headings from MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.