Abstract
BackgroundNanoparticles (NPs) incorporating drug formulations can be used to facilitate passage through biological 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 encapsulation by proteinoid NPs.ResultsProteinoid 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 antipsychotic activity of drug-loaded proteinoid NPs compared to free RSP.ConclusionsProteinoid NPs enhance RSP delivery and may potentially increase drug efficiency by reducing dosage and side effects.
Highlights
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
Prot.2/RSP presented smaller diameter compared to Prot.1/RSP of 86 ± 3 nm (DLS, Fig. 2g and Table 2) and 82 ± 2 nm. These results show that both methods for measuring NP diameter provide similar results; commonly, the diameters measured from the cryo-TEM were the same or slightly lower than those obtained by the dynamic light scattering (DLS)
In this study, a new drug delivery system was investigated for the antipsychotic drug RSP
Summary
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. Risperidone (RSP) is a commonly used atypical antipsychotic medication, and was selected for encapsula‐ tion by proteinoid NPs. Mental disorders are cognitive behavioral or emotional patterns that cause significant distress and/or permanent impairment of personal functions [1]. 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. 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 associated with autism and both positive (e.g., hallucinations or delusions) and negative (e.g., emotional withdrawal or loss of speech) symptoms of schizophrenia and bipolar disorders [8,9,10].
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