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Saquinavir-Piperine Eutectic Mixture: Preparation, Characterization, and Dissolution Profile.

Cinira Fandaruff1, María Isabel Quirós-Fallas2,3, José Roberto Vega-Baudrit2

  • 1Instituto de Tecnologías Emergentes y Ciencias Aplicadas (ITECA), UNSAM-CONICET, Escuela de Ciencia y Tecnología, Laboratorio de Cristalografía Aplicada, Av. 25 de Mayo 1169, San Martín 1650, Provincia de Buenos Aires, Argentina.

Pharmaceutics
|October 28, 2023
PubMed
Summary

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Correction: Bahloul et al. Investigating the Wound-Healing Potential of a Nanoemulsion-Gel Formulation of <i>Pituranthos tortuosus</i> Essential Oil. <i>Gels</i> 2024, <i>10</i>, 155.

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This summary is machine-generated.

The dissolution rate of the anti-HIV drug saquinavir base (SQV) was improved by forming a eutectic mixture with piperine (PIP). This approach enhanced drug solubility and bioavailability, offering a promising strategy for improving SQV

Area of Science:

  • Pharmaceutical Sciences
  • Materials Science
  • Drug Delivery

Background:

  • Saquinavir base (SQV) exhibits poor water solubility and low absolute bioavailability, limiting its therapeutic efficacy.
  • Improving the dissolution rate of poorly soluble drugs is crucial for enhancing their oral absorption and bioavailability.

Purpose of the Study:

  • To enhance the dissolution rate and bioavailability of saquinavir base (SQV) through eutectic mixture formation.
  • To investigate the solid-state properties and dissolution behavior of SQV-piperine (PIP) eutectic systems.

Main Methods:

  • Screening of coformers using liquid-assisted grinding and differential scanning calorimetry (DSC).
  • Characterization of the eutectic system using DSC, powder X-ray diffraction (PXRD), small-angle X-ray scattering (SAXS), Fourier transform infrared spectroscopy (FT-IR), and scanning electron microscopy (SEM).
Keywords:
dissolution enhancementeutectic mixturespiperinepowder diffractionsaquinavirsmall-angle X-ray scatteringsolid-state characterization

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  • Evaluation of the dissolution profile of the eutectic mixture compared to pure SQV.

    • Main Results:

    • A eutectic system was successfully formed between SQV and piperine (PIP) at a molar ratio of 0.6:0.4.
    • SAXS analysis revealed changes in crystal structure within the eutectic mixture, despite PXRD showing no overall structural changes.
    • FT-IR confirmed no molecular interactions in the solid state.
    • The SQV-PIP eutectic mixture demonstrated a significantly improved dissolution rate, with 55% of SQV dissolved in 45 minutes compared to 42% for pure SQV.

    Conclusions:

    • Eutectic mixture formation with piperine (PIP) is an effective strategy to enhance the dissolution rate of saquinavir base (SQV).
    • The improved dissolution characteristics of the SQV-PIP eutectic system hold potential for improving the bioavailability of saquinavir.
    • This study highlights the utility of coformer selection and eutectic crystallization in optimizing the delivery of poorly soluble drugs.