Highly lipophilic pluronics-conjugated polyamidoamine dendrimer nanocarriers as potential delivery system for hydrophobic drugs

Mater Sci Eng C Mater Biol Appl. 2017 Jan 1;70(Pt 2):992-999. doi: 10.1016/j.msec.2016.03.073. Epub 2016 Mar 26.

Abstract

In the study, four kinds of pluronics (P123, F68, F127 and F108) with varying hydrophilic-lipophilic balance (HLB) values were modified and conjugated on 4th generation of polyamidoamine dendrimer (PAMAM). The obtained results from FT-IR, 1H NMR and GPC showed that the pluronics effectively conjugated on the dendrimer. The molecular weight of four PAMAM G4.0-Pluronics and its morphologies are in range of 200.15-377.14kDa and around 60-180nm in diameter by TEM, respectively. Loading efficiency and release of hydrophobic fluorouracil (5-FU) anticancer drug were evaluated by HPLC; Interesting that the dendrimer nanocarrier was conjugated with the highly lipophilic pluronic P123 (G4.0-P123) exhibiting a higher drug loading efficiency (up to 76.25%) in comparison with another pluronics. Live/dead fibroblast cell staining assay mentioned that all conjugated nanocarriers are highly biocompatible. The drug-loaded nanocarriers also indicated a highly anti-proliferative activity against MCF-7 breast cancer cell. The obtained results demonstrated a great potential of the highly lipophilic pluronics-conjugated nanocarriers in hydrophobic drugs delivery for biomedical applications.

Keywords: 5-FU; Delivery; Lipophilic pluronic; Nanocarrier; Polyamidoamine dendrimer.

MeSH terms

  • Animals
  • Antineoplastic Agents / pharmacology
  • Cell Death / drug effects
  • Chromatography, Gel
  • Dendrimers / chemical synthesis
  • Dendrimers / chemistry*
  • Drug Carriers / chemistry*
  • Drug Delivery Systems*
  • Drug Liberation
  • Fluorouracil / pharmacology*
  • Humans
  • Hydrophobic and Hydrophilic Interactions*
  • Lipids / chemistry
  • MCF-7 Cells
  • Mice
  • Nanoparticles / chemistry*
  • Nanoparticles / ultrastructure
  • Nylons / chemical synthesis
  • Nylons / chemistry
  • Poloxamer / chemical synthesis
  • Poloxamer / chemistry*
  • Polyamines / chemical synthesis
  • Polyamines / chemistry*
  • Spectroscopy, Fourier Transform Infrared

Substances

  • Antineoplastic Agents
  • Dendrimers
  • Drug Carriers
  • Lipids
  • Nylons
  • PAMAM-G4
  • Poly(amidoamine)
  • Polyamines
  • Poloxamer
  • Fluorouracil