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Formulation of Diblock Polymeric Nanoparticles through Nanoprecipitation Technique
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Designed proteinoid polymers and nanoparticles encapsulating risperidone for enhanced antipsychotic activity.

L Lugasi1, I Grinberg1, S Rudnick-Glick1

  • 1Department of Chemistry, The Institute of Nanotechnology and Advanced Materials, Bar-Ilan University, 5290002, Ramat Gan, Israel.

Journal of Nanobiotechnology
|October 22, 2020
PubMed
Summary

New proteinoid nanoparticles effectively deliver risperidone (RSP), enhancing antipsychotic activity. This drug delivery system shows potential for improved efficacy and reduced side effects in patients.

Keywords:
Antipsychotic therapyDrug deliveryProteinoid nanoparticlesRisperidoneSelf-assembly

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Area of Science:

  • Nanotechnology
  • Materials Science
  • Pharmacology

Background:

  • Nanoparticles (NPs) can improve drug delivery across biological barriers like the blood-brain barrier (BBB).
  • Encapsulating drugs in NPs can overcome solubility issues, enhancing bioavailability and targeting.
  • Proteinoid NPs offer a novel system for improving drug efficacy, with risperidone (RSP) selected as a model antipsychotic.

Purpose of the Study:

  • To develop and characterize novel proteinoid nanoparticles for drug delivery.
  • To encapsulate risperidone (RSP) within proteinoid NPs for enhanced antipsychotic treatment.
  • To evaluate the efficacy and biodistribution of RSP-loaded proteinoid NPs.

Main Methods:

  • Synthesis of high molecular weight proteinoid polymers from L-amino acids and poly-L-lactic acid (PLLA).
  • Preparation of RSP-loaded proteinoid NPs via self-assembly, followed by PEGylation.
  • Characterization of NPs (size, drug loading, ζ-potential) and evaluation of cytotoxicity, biodistribution, and psychopharmacological effects.

Main Results:

  • Synthesized proteinoid polymers exhibited high molecular weight and low polydispersity.
  • PEGylated RSP-loaded NPs were successfully prepared and characterized.
  • Drug-loaded proteinoid NPs demonstrated significantly higher antipsychotic activity compared to free RSP.

Conclusions:

  • Proteinoid NPs effectively enhance the delivery of risperidone (RSP).
  • This NP system has the potential to increase drug efficacy.
  • Reduced dosage and side effects may be achievable with this novel drug delivery approach.