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<p>The present work focuses on preparation of Lurasidone hydrochloride encapsulated lipid polymeric hybrid nanoparticles to achieve improved and enhanced delivery and uptake of Lurasidone. In 2010, U.S. Food and Drug Administration authorized Lurasidone hydrochloride, an atypical antipsychotic, for the treating schizophrenia. It functions as an antagonist at serotonin 5HT2A and dopamine (D2) receptors. The drug’s bioavailability drops to roughly 19% as a result of its high first pass metabolism. The goal of this work is to create lipid polymeric hybrid nanoparticles of Lurasidone that were loaded with Lurasidone hydrochloride to improve medication delivery. The modified single-step nanoprecipitation self-assembly process was used to create the Lurasidone lipid polymer hybrid nanoparticles (LUR-LPHN). In this method the organic phase which contained the drug (lurasidone) and polymer (polylactic acid) was mixed with the aqueous phase containing the lipid at constant stirring. With polydispersity index (PDI) 0.085 and, mean particle size 135.9&#xa0;nm, the nanoparticles were found to have a zeta potential (ZP) that ranged from − 27.1 mV. Drug loading was 12.08%±0.13 and the drug entrapment efficiency (EE%) was observed to be 97.89%±0.95. Transmission electron microscopy (TEM) has been done in order to confirm particle size, Fourier Transform Infrared spectroscopy (FTIR) and Differential calorimetry (DSC) studies have been conducted to find encapsulation of drug in the nanoparticles. Antioxidant activity of LUR-LPHN was determined via 2,2Diphenyl-1-picrylhydrazyl assay (DPPH) and Ferric Reducing Antioxidant Power assay (FRAP). In-vitro release profile for 72&#xa0;h has been examined in phosphate buffer saline pH 7.4 and simulated nasal fluid pH 5.5, and the release of 81.75 ± 0.88% and 83.85 ± 1.07% was observed respectively. The neuroblastoma cell line (neuro 2a cell line) was used to test in vitro cytotoxicity by using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay (MTT). Results indicated that cells which were treated by nanoparticles had higher viability (99.3%) compared to cells treated with Lurasidone hydrochloride aqueous solution. In Vitro Inflammatory Cytokines analysis was done on Tumour necrosis factor (TNF α), Interleukins (IL10) and Interleukins (IL 4) ELISA kits. Further the cellular uptake studies were done and lipid polymer hybrid nanoparticles of Lurasidone, showed enhanced cellular uptake as compared to aqueous drug solution.</p>

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Development and Evaluation of Lurasidone Hydrochloride Loaded Lipid Polymer Hybrid Nanoparticles: An In Vitro Study on Neuroblastoma Cells

  • 期刊论文

  • 发表日期：

    2026年4月28日

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  • Nikita Arora,
  • Shweta Dang

摘要

The present work focuses on preparation of Lurasidone hydrochloride encapsulated lipid polymeric hybrid nanoparticles to achieve improved and enhanced delivery and uptake of Lurasidone. In 2010, U.S. Food and Drug Administration authorized Lurasidone hydrochloride, an atypical antipsychotic, for the treating schizophrenia. It functions as an antagonist at serotonin 5HT2A and dopamine (D2) receptors. The drug’s bioavailability drops to roughly 19% as a result of its high first pass metabolism. The goal of this work is to create lipid polymeric hybrid nanoparticles of Lurasidone that were loaded with Lurasidone hydrochloride to improve medication delivery. The modified single-step nanoprecipitation self-assembly process was used to create the Lurasidone lipid polymer hybrid nanoparticles (LUR-LPHN). In this method the organic phase which contained the drug (lurasidone) and polymer (polylactic acid) was mixed with the aqueous phase containing the lipid at constant stirring. With polydispersity index (PDI) 0.085 and, mean particle size 135.9 nm, the nanoparticles were found to have a zeta potential (ZP) that ranged from − 27.1 mV. Drug loading was 12.08%±0.13 and the drug entrapment efficiency (EE%) was observed to be 97.89%±0.95. Transmission electron microscopy (TEM) has been done in order to confirm particle size, Fourier Transform Infrared spectroscopy (FTIR) and Differential calorimetry (DSC) studies have been conducted to find encapsulation of drug in the nanoparticles. Antioxidant activity of LUR-LPHN was determined via 2,2Diphenyl-1-picrylhydrazyl assay (DPPH) and Ferric Reducing Antioxidant Power assay (FRAP). In-vitro release profile for 72 h has been examined in phosphate buffer saline pH 7.4 and simulated nasal fluid pH 5.5, and the release of 81.75 ± 0.88% and 83.85 ± 1.07% was observed respectively. The neuroblastoma cell line (neuro 2a cell line) was used to test in vitro cytotoxicity by using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay (MTT). Results indicated that cells which were treated by nanoparticles had higher viability (99.3%) compared to cells treated with Lurasidone hydrochloride aqueous solution. In Vitro Inflammatory Cytokines analysis was done on Tumour necrosis factor (TNF α), Interleukins (IL10) and Interleukins (IL 4) ELISA kits. Further the cellular uptake studies were done and lipid polymer hybrid nanoparticles of Lurasidone, showed enhanced cellular uptake as compared to aqueous drug solution.