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Formulation and Delivery - Chemical

(M1030-01-05) Novel Combination Approach to Enhance Solubility and Permeability of Pazopanib Using Phospholipid Complex and a Bioenhancer

Monday, October 21, 2024
10:30 AM – 11:30 AM MT

    Presenting Author(s)

  • Nishikant Ambadas Raut, Ph.D.

    Professor
    Rashtrasant Tukadoji Maharaj Nagpur University
    Nagpur, Maharashtra, India

    • Main Author(s)

  • RK

    Ruchita Kelwadkar

    M. Pharm Student
    Rashtrasant Tukadoji Maharaj Nagpur University
    Nagpur, Maharashtra, India

    • Co-Author(s)

  • YB

    Yogeshwary Bhongade

    Research Scholar
    Rashtrasant Tukadoji Maharaj Nagpur University
    Nagpur, Maharashtra, India

  • VD

    Vivek S. Dave, Ph.D.

    Associate Professor (Pharm. Sci.)
    St. John's University
    Rochester, New York, United States

Purpose: Poor aqueous solubility and dissolution rate are significant challenges in the formulation development of novel chemical entities, leading to diminished bioavailability. Phospholipid complexation presents a viable technique to enhance the solubility of BCS class II Active Pharmaceutical Ingredients (APIs), while bioenhancers are utilized to augment API permeability. This study aims to evaluate the synergistic effect of phospholipid complexation and the bioenhancer Quercetin on the solubility and permeability of Pazopanib.

Methods: The solvent evaporation method was employed to prepare the Pazopanib complex with Phospholipon 90H® (PPC), employing a Quality by Design (QbD) approach. Concurrent with phospholipid complexation, the bioenhancer Quercetin was incorporated to enhance permeability. Physical-chemical characterization of the developed complexes, Pazopanib-Phospholipon 90H® with and without Quercetin, was conducted using Fourier-transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), X-ray diffraction (XRD), and photomicroscopy. Functional evaluation encompassed apparent solubility, in vitro dissolution, and ex vivo permeability studies.

Results: The Pazopanib-Phospholipon 90H® complex (PPC) exhibited a six-fold increase in aqueous solubility, while PPC with Quercetin (PPQ) demonstrated a nine-fold increase. The cumulative % drug release of PPC displayed a 2.2-fold higher dissolution profile than pure Pazopanib, whereas PPQ exhibited a 4.7-fold increase compared to Pazopanib. Enhanced rate and extent of permeation were observed with a 2.3-fold increase in PPC and a significant 4.2-fold increase in permeation with PPQ.

Conclusion: The demonstrated enhancement in solubility and permeability of Pazopanib through the combined approach of phospholipid complexation and Quercetin represents a promising strategy to ameliorate its bioavailability.


In-Vitro dissolution study of Pazopanib, Pazopanib-Phospholipid complex, PPQ


Ex-vivo permeability study of Pazopanib, PPC & PPQ