Purpose <p>Olanzapine (OLZ), a potent antipsychotic for schizophrenia treatment, faces challenges due to low aqueous solubility and bioavailability, necessitating advanced drug targeting systems.</p> Methods <p>Lipid Polymer Hybrid Nanocarriers (LPHNPs) augment OLZ release, combining the sustained-release capability of a polymeric nucleus with the biocompatibility of a lipid periphery to mitigate hepatic first-pass metabolism and improve bioavailability.</p> Results <p>Using Central Composite Design (CCD) optimized, yielding nanoparticles with mean particle size 192.4 ± 2.55&#xa0;nm, polydispersity index (PDI) 0.226 ± 0.09, zeta potential -31.2 ± 2.05&#xa0;mV, and exceptional entrapment efficiency (96.40 ± 2.65%). Characterization via XRD, FTIR, DSC, confirmed OLZ’s amorphous dispersion within the lipid-polymer matrix, while TEM revealed spherical, homogeneous nanoparticles. In vitro dissolution revealed pH-invariant prolonged drug liberation (88.61% over 24&#xa0;h), fitting the first-order kinetics model. Accelerated stability studies (3&#xa0;months, 25&#xa0;°C/60% RH) showed minimal size distribution changes (203.9&#xa0;nm), PDI (0.326), and drug content (97.86%), underscoring robustness.</p> Conclusion <p>This work pioneers OLZ-LPHNPs as a stable, scalable nanocarrier system, offering enhanced therapeutic efficacy and reduced dosing frequency. The integration of CCD-based optimization and dual lipid-polymer architecture presents a promising strategy for hydrophobic drug delivery.</p>

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Engineered Dual-Component Lipid-Polymer Nanoparticles for Modified Olanzapine Release, Shelf-Life Assessment, and Elevated Bioavailability in Schizophrenia Therapy

  • Swati Raysing,
  • Aniket Chillarge,
  • Ujwal Katolkar,
  • Krunal Mali

摘要

Purpose

Olanzapine (OLZ), a potent antipsychotic for schizophrenia treatment, faces challenges due to low aqueous solubility and bioavailability, necessitating advanced drug targeting systems.

Methods

Lipid Polymer Hybrid Nanocarriers (LPHNPs) augment OLZ release, combining the sustained-release capability of a polymeric nucleus with the biocompatibility of a lipid periphery to mitigate hepatic first-pass metabolism and improve bioavailability.

Results

Using Central Composite Design (CCD) optimized, yielding nanoparticles with mean particle size 192.4 ± 2.55 nm, polydispersity index (PDI) 0.226 ± 0.09, zeta potential -31.2 ± 2.05 mV, and exceptional entrapment efficiency (96.40 ± 2.65%). Characterization via XRD, FTIR, DSC, confirmed OLZ’s amorphous dispersion within the lipid-polymer matrix, while TEM revealed spherical, homogeneous nanoparticles. In vitro dissolution revealed pH-invariant prolonged drug liberation (88.61% over 24 h), fitting the first-order kinetics model. Accelerated stability studies (3 months, 25 °C/60% RH) showed minimal size distribution changes (203.9 nm), PDI (0.326), and drug content (97.86%), underscoring robustness.

Conclusion

This work pioneers OLZ-LPHNPs as a stable, scalable nanocarrier system, offering enhanced therapeutic efficacy and reduced dosing frequency. The integration of CCD-based optimization and dual lipid-polymer architecture presents a promising strategy for hydrophobic drug delivery.