Designed proteinoid polymers and nanoparticles encapsulating risperidone for enhanced antipsychotic activity
- PDF / 1,834,397 Bytes
- 16 Pages / 595.276 x 790.866 pts Page_size
- 84 Downloads / 122 Views
Journal of Nanobiotechnology Open Access
RESEARCH
Designed proteinoid polymers and nanoparticles encapsulating risperidone for enhanced antipsychotic activity L. Lugasi1, I. Grinberg1, S. Rudnick‑Glick1, E. Okun2, H. Einat3 and S. Margel1*
Abstract Background: Nanoparticles (NPs) incorporating drug formulations can be used to facilitate passage through biologi‑ cal barriers including the blood–brain barrier (BBB) and increase drug delivery and bioavailability. Hence, NP-based administration may enhance the efficiency of current antipsychotics. Encapsulation within NPs can resolve aqueous solubility problems that not only reduce permeability through the BBB but also affect targeting. The present study describes a new drug delivery system based on proteinoid NPs to explore the possibility of improving drug efficacy. Risperidone (RSP) is a commonly used atypical antipsychotic medication, and was therefore selected for encapsula‑ tion by proteinoid NPs. Results: Proteinoid polymers with high molecular weight and low polydispersity were synthesized from l-amino acids and poly-l-lactic acid (PLLA) by thermal step-growth polymerization mechanism. RSP-loaded proteinoid NPs were then prepared using a self-assembly process in the presence of RSP, followed by PEGylation. The optimal PEGylated RSP-loaded NPs were characterized in terms of diameter and size distribution, drug loading, ζ-potential, cytotoxicity, biodistribution, and psychopharmacological effects. The findings indicate significantly higher antipsy‑ chotic activity of drug-loaded proteinoid NPs compared to free RSP. Conclusions: Proteinoid NPs enhance RSP delivery and may potentially increase drug efficiency by reducing dosage and side effects. Keywords: Proteinoid nanoparticles, Self-assembly, Risperidone, Drug delivery, Antipsychotic therapy Background Mental disorders are cognitive behavioral or emotional patterns that cause significant distress and/or permanent impairment of personal functions [1]. They affect approximately 13% of the global population. Signs and symptoms vary, ranging from mild to moderate and even severe impairment. Triggers of mental disorders include genetics [2], biochemical processes in brain structure and development [3], environmental changes *Correspondence: [email protected] 1 Department of Chemistry, The Institute of Nanotechnology and Advanced Materials, Bar-Ilan University, 5290002 Ramat Gan, Israel Full list of author information is available at the end of the article
[4], traumatic life events [5], drug use, and lifestyle [6]. Treatment is disorder- and individual-specific and usually combines psychotherapy and medication. Antipsychotics (also called neuroleptics or major tranquilizers) are a class of medications that are primarily used in the treatment of psychoses, in particular schizophrenia and bipolar disorders [7]. Risperidone (RSP, Fig. 1) is considered as one of the most reliable and effective atypical (second generation) antipsychotic medications, and is widely used in the treatment of irritability associ
Data Loading...
