Proteinoid Nanocapsules as Drug Delivery System for Improving Antipsychotic Activity of Risperidone

Liroy Lugasi, Igor Grinberg, Rivka Sabag, Ravit Madar, Haim Einat, Shlomo Margel

Research output: Contribution to journalArticlepeer-review

9 Scopus citations

Abstract

Risperidone (RSP) is an atypical antipsychotic drug widely used to treat schizophrenia and bipolar disorder. Nanoparticles (NPs) are being developed as in vivo targeted drug delivery systems, which cross the blood-brain barrier and improve pharmacokinetics and drug effectiveness. Here, biodegradable proteinoids were synthesized by thermal step-growth polymerization from the amino acids l-glutamic acid, l-phenylalanine and l-histidine and poly (l-lactic acid). Proteinoid NPs containing RSP were then formed by self-assembly, overcoming the insolubility of the drug in water, followed by PEGylation (poly ethylene glycol (PEG) conjugation to increase the stability of the NPs in the aqueous continuous phase. These NPs are biodegradable owing to their peptide and ester moieties. They were characterized in terms of diameter, size distribution, drug loading, and long-term storage. Behavioral studies on mice found enhanced antipsychotic activity compared to free RSP.

Original languageEnglish
Article number4013
JournalMolecules
Volume25
Issue number17
DOIs
StatePublished - 1 Sep 2020
Externally publishedYes

Keywords

  • Drug delivery
  • Nanocapsules
  • Proteinoid nanoparticles
  • Risperidone
  • Self-assembly

ASJC Scopus subject areas

  • Analytical Chemistry
  • Chemistry (miscellaneous)
  • Molecular Medicine
  • Pharmaceutical Science
  • Drug Discovery
  • Physical and Theoretical Chemistry
  • Organic Chemistry

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