Polymeric micelles with small lipophilic moieties for drug delivery

Colloids Surf B Biointerfaces. 2014 Apr 1:116:627-32. doi: 10.1016/j.colsurfb.2013.10.032. Epub 2013 Oct 30.

Abstract

The aim of this study was to develop a new polymeric micelle delivery system for antitumor drugs. An amphiphile of methoxypoly(ethylene glycol)-histidine-di(cinnamic acid) (PEGHC) with a small lipophilic moiety instead of a hydrophobic biodegradable polymer chain was synthesized and characterized. The PEGHC self-assembled into micelles. The critical micelle concentration (CMC) was tested. 9-Nitro-20(s)-camptothecin (9-NC) was used as a model drug for encapsulation. The size and morphology of both blank and 9-NC loaded micelles were characterized by dynamic light scattering (DLS) and transmission electron microscopy (TEM). The release profile of 9-NC loaded micelles was studied. HepG2 liver cancer cells were incubated with the drug-loaded micelles to investigate the in vitro anticancer efficiency. The results showed that the 9-NC loaded micelles exhibited high accumulated release rate (>85%) and efficient in vitro anticancer activity.

Keywords: 9-nitro-20(s)-camptothecin; Cellular uptake; Cytotoxicity; Drug delivery; Micelle.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology*
  • Camptothecin / analogs & derivatives*
  • Camptothecin / chemistry
  • Camptothecin / pharmacology
  • Cell Proliferation / drug effects
  • Cell Survival / drug effects
  • Dose-Response Relationship, Drug
  • Drug Delivery Systems*
  • Drug Screening Assays, Antitumor
  • Hep G2 Cells
  • Humans
  • Hydrophobic and Hydrophilic Interactions
  • Micelles
  • Molecular Structure
  • Polymers / chemical synthesis
  • Polymers / chemistry*
  • Structure-Activity Relationship

Substances

  • Antineoplastic Agents
  • Micelles
  • Polymers
  • rubitecan
  • Camptothecin