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<p>Amisulpride effectively treats both positive and negative symptoms of schizophrenia. However, its poor aqueous solubility and low intestinal permeability limit oral bioavailability. This study developed chitosan-coated poly(lactic-co-glycolic acid) (PLGA) nanoparticles (NPs) encapsulating amisulpride for intranasal delivery, thereby enhancing solubility, permeability, and bioavailability. Amisulpride-loaded chitosan-coated PLGA NPs were prepared using the oil-in-water emulsion–solvent evaporation method. Formulations were optimized based on particle size (PS), zeta potential (ZP), polydispersity index (PDI), entrapment efficiency (EE%), and loading capacity (LC%). The optimized formulation was characterized by Fourier transform infrared spectroscopy (FTIR), scanning electron microscopy (SEM), thermogravimetric analysis (TGA), and X-ray diffraction (XRD). The solubility, stability, mucoadhesion, <i>in vitro</i> drug release, and cytotoxicity were also evaluated. The optimized formulation (F2) had a PS of 246.13 ± 2.28 nm, PDI of 0.14 ± 0.03, ZP of 41.04 ± 1.76 mV, EE% of 77.87, and LC% of 24.64. Encapsulating the drug in the NPs increased its solubility and the stability over three months showed no significant changes in the characteristics mentioned. F2 exhibited strong mucoadhesive properties and enhanced drug release at pH 5.5 and pH 7.4, with cumulative release of 77.41% at pH 7.4 and 92.17% at pH 5.5. Cytotoxicity testing confirmed biocompatibility across 0.75–10 mg/mL. Amisulpride chitosan-coated PLGA NPs demonstrated favourable physicochemical properties, solubility, stability, controlled drug release, and mucoadhesive profile with enhanced cell viability at specific concentrations across multiple epithelial cell lines compared with the drug solution and unloaded NPs. This work highlights the promising potential of Amisulpride Chitosan-coated PLGA NPs as an innovative intranasal nanocarrier for improved schizophrenia therapy.</p> Graphical Abstract <p></p>

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Formulation and Characterization of Amisulpride-Poly (Lactic-Co-Glycolic Acid) Nanoparticles Coated with Chitosan for Intranasal Delivery

  • 期刊论文

  • 发表日期：

    2026年3月23日

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  • Mai S. Khanfar,
  • Sumieh Y. Alaboud,
  • Raida W. Khalil,
  • Ruba S. Darweesh

摘要

Amisulpride effectively treats both positive and negative symptoms of schizophrenia. However, its poor aqueous solubility and low intestinal permeability limit oral bioavailability. This study developed chitosan-coated poly(lactic-co-glycolic acid) (PLGA) nanoparticles (NPs) encapsulating amisulpride for intranasal delivery, thereby enhancing solubility, permeability, and bioavailability. Amisulpride-loaded chitosan-coated PLGA NPs were prepared using the oil-in-water emulsion–solvent evaporation method. Formulations were optimized based on particle size (PS), zeta potential (ZP), polydispersity index (PDI), entrapment efficiency (EE%), and loading capacity (LC%). The optimized formulation was characterized by Fourier transform infrared spectroscopy (FTIR), scanning electron microscopy (SEM), thermogravimetric analysis (TGA), and X-ray diffraction (XRD). The solubility, stability, mucoadhesion, in vitro drug release, and cytotoxicity were also evaluated. The optimized formulation (F2) had a PS of 246.13 ± 2.28 nm, PDI of 0.14 ± 0.03, ZP of 41.04 ± 1.76 mV, EE% of 77.87, and LC% of 24.64. Encapsulating the drug in the NPs increased its solubility and the stability over three months showed no significant changes in the characteristics mentioned. F2 exhibited strong mucoadhesive properties and enhanced drug release at pH 5.5 and pH 7.4, with cumulative release of 77.41% at pH 7.4 and 92.17% at pH 5.5. Cytotoxicity testing confirmed biocompatibility across 0.75–10 mg/mL. Amisulpride chitosan-coated PLGA NPs demonstrated favourable physicochemical properties, solubility, stability, controlled drug release, and mucoadhesive profile with enhanced cell viability at specific concentrations across multiple epithelial cell lines compared with the drug solution and unloaded NPs. This work highlights the promising potential of Amisulpride Chitosan-coated PLGA NPs as an innovative intranasal nanocarrier for improved schizophrenia therapy.

Graphical Abstract