A poly(ether-ester) copolymer for the preparation of nanocarriers with improved degradation and drug delivery kinetics

Mater Sci Eng C Mater Biol Appl. 2016 Feb:59:488-499. doi: 10.1016/j.msec.2015.10.054. Epub 2015 Oct 17.

Abstract

This paper reports the synthesis and the physicochemical, functional and biological characterisations of nanocarriers made of a novel di-block biodegradable poly(ether-ester) copolymer. This material presents tunable, fast biodegradation rates, but its products are less acidic than those of other biosorbable polymers like PLGA, thus presenting a better biocompatibility profile and the possibility to carry pH-sensitive payloads. A method for the production of monodisperse and spherical nanoparticles is proposed; drug delivery kinetics and blood protein adsorption were measured to evaluate the functional properties of these nanoparticles as drug carriers. The copolymer was labelled with a fluorescent dye for internalisation tests, and rhodamine B was used as a model cargo to study transport and release inside cultured cells. Biological tests demonstrated good cytocompatibility, significant cell internalisation and the possibility to vehiculate non-cell penetrating moieties into endothelial cells. Taken together, these results support the potential use of this nanoparticulate system for systemic administration of drugs.

Keywords: Biocompatibility; Biodegradable nanoparticles; Biodegradation; Drug delivery; Metoxy polyethyleneglycol-block-poly(ε-caprolactone-co-4-hydroxyvalerolactone).

MeSH terms

  • Adsorption
  • Animals
  • Blood Proteins / chemistry
  • Cell Line, Transformed
  • Drug Carriers* / chemistry
  • Drug Carriers* / pharmacokinetics
  • Drug Carriers* / pharmacology
  • Lactic Acid* / chemistry
  • Lactic Acid* / pharmacokinetics
  • Lactic Acid* / pharmacology
  • Materials Testing*
  • Mice
  • Nanoparticles / chemistry*
  • Polyglycolic Acid* / chemistry
  • Polyglycolic Acid* / pharmacokinetics
  • Polyglycolic Acid* / pharmacology
  • Polylactic Acid-Polyglycolic Acid Copolymer
  • Rhodamines* / chemistry
  • Rhodamines* / pharmacokinetics
  • Rhodamines* / pharmacology

Substances

  • Blood Proteins
  • Drug Carriers
  • Rhodamines
  • Polylactic Acid-Polyglycolic Acid Copolymer
  • Polyglycolic Acid
  • Lactic Acid
  • rhodamine B