Surface-functionalized curcumin-loaded polymeric nanocapsules could block apomorphine-induced behavioral changes in rats

Pharmacol Rep. 2022 Feb;74(1):135-147. doi: 10.1007/s43440-021-00331-2. Epub 2021 Nov 5.

Abstract

Background: Surface functionalization enhances the properties and characteristics of polymeric nanocapsules (NCs) mainly due to the surface charge, surfactants, and polymer coating type. Curcumin (CUR) is a bioactive compound with several proven pharmacological properties and low bioavailability. This study aimed to develop anionic (poly-ɛ-caprolactone; PCL) and cationic (Eudragit® RS100 (EUD)) NCs prepared with sorbitan monostearate (Span 60®) or sorbitan monooleate (Span 80®), coated with d-α-tocopherol polyethylene glycol 1000 succinate (TPGS) and optimized using 23 factorial analysis. Subsequently, the biological activity was evaluated.

Methods: A two-level, three-factor design (polymer, Span type, and TPGS concentration) was used. The biological effects of CUR-loaded TPGS-coated cationic and anionic NCs were assessed in apomorphine-induced stereotyped behavior in rats.

Results: The type of polymer (anionic or cationic) and Span® had a factorial influence on the physical and chemical characteristics of NCs according to the changes in TPGS concentrations. Both cationic and anionic CUR-NCs could block apomorphine-induced behavioral changes.

Conclusions: The CUR-loaded TPGS-coated NCs proved to be a promising brain delivery system.

Keywords: Anionic; Cationic; Curcumin; Nanocapsules; TPGS.

MeSH terms

  • Animals
  • Apomorphine / pharmacology*
  • Behavior, Animal / drug effects*
  • Curcumin / pharmacology*
  • Dopamine Agonists / pharmacology
  • Enzyme Inhibitors
  • Hexoses / pharmacology
  • Nanocapsules / chemistry*
  • Plants, Medicinal
  • Rats
  • Stereotyped Behavior / drug effects*
  • Treatment Outcome
  • Vitamin E / pharmacology

Substances

  • Dopamine Agonists
  • Enzyme Inhibitors
  • Hexoses
  • Nanocapsules
  • sorbitan monooleate
  • Vitamin E
  • Curcumin
  • Apomorphine
  • sorbitan monostearate
  • tocophersolan