Water-Soluble Single-Chain Polymeric Nanoparticles for Highly Selective Cancer Chemotherapy

Chih Chia Cheng, Shan You Huang, Wen Lu Fan, Ai Wei Lee, Chih Wei Chiu, Duu Jong Lee, Juin Yih Lai

Research output: Contribution to journalArticlepeer-review

Abstract

Functionalized amphiphilic polymers consisting of hydrophilic poly(ethylene glycol) pendant groups and a hydrophobic poly(epichlorohydrin) backbone can spontaneously self-organize into single-chain polymeric nanoparticles (SCPNs) in water, without exhibiting concentration-dependent effects or requiring additional reactive additives or subsequent purification. These SCPNs can effectively encapsulate the anticancer drug doxorubicin and have a high drug-loading capacity, desirable particle size distribution, and excellent drug-entrapment stability in serum-containing media or buffer solutions at various pH values; these unique physical and biological properties will be crucial to the achievement of smart drug delivery nanocarriers based on functional micelles. Cytotoxicity assays confirmed that the drug-loaded SCPNs were not cytotoxic toward normal cells but were significantly cytotoxic toward tumor cells under normal physiological conditions. Our results suggest that the drug-loaded SCPNs exert selective, targeted cytotoxic effects in cancer cells, without affecting healthy cells. Importantly, cellular uptake and flow cytometric assays confirmed that the drug-loaded SCPNs effectively targeted and entered the tumor cells via endocytosis and subsequently effectively promoted apoptotic cell death. Thus, this SCPN system has the ability to improve the overall therapeutic efficacy and safety of cancer chemotherapy.

Original languageEnglish
Pages (from-to)474-484
Number of pages11
JournalACS Applied Polymer Materials
Volume3
Issue number1
DOIs
Publication statusPublished - Jan 8 2021

Keywords

  • amphiphilic polymers
  • drug delivery
  • select chemotherapy
  • spontaneous self-assembly
  • water-soluble single-chain polymeric nanoparticles

ASJC Scopus subject areas

  • Polymers and Plastics
  • Process Chemistry and Technology
  • Organic Chemistry

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