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Purpose <p>Atorvastatin suffers from low oral bioavailability due to its poor solubility (BCS&#xa0;class II drug) and first-pass metabolism. Therefore, an approach of atorvastatin phospholipid&#xa0;complex and further its inclusion into a matrix dispersion was employed to&#xa0;improve the solubility and rate of solution of drug so that it can reach up to its full&#xa0;pharmacodynamic potential.</p> Methods <p>The, atorvastatin-phospholipid complex and matrix dispersion were prepared&#xa0;by solvent-evaporation technique using hydroxypropyl methyl cellulose (HPMC K 100M)&#xa0;and polyvinylpyrrolidone (PVP-K-30). Fourier transform infrared (FTIR), Nuclear&#xa0;magnetic resonance (NMR), Differential scanning calorimetry (DSC), Powder X-ray&#xa0;diffraction (PXRD), Scanning electron microscopy (SEM), and in-vitro drug release were&#xa0;performed to evaluate the performance of drug phospholipid complex and its matrix&#xa0;dispersion. Pharmacodynamic effects were evaluated in high fat diet induced rat models.</p> Results <p>Molecular docking confirmed the ability of atorvastatin to form complex with&#xa0;phospholipid. Results demonstrated a noteworthy increase in dissolution rates by drug phospholipid&#xa0;complex and its matrix dispersion as compared to marketed formulation due&#xa0;to the conversion of crystalline nature of drug into its amorphous form. In vivo&#xa0;pharmacodynamic studies also corroborated with the results of in vitro studies and&#xa0;demonstrated the significant decrease (P&lt;0.001) in triglyceride (103.195±3.197mg/dl),&#xa0;cholesterol (83.86± 3.76mg/dl), and low-density lipoprotein (86.41±3.85 mg/dl) and&#xa0;increase in high density lipoprotein (88.93±4.814mg/dl) levels.</p> Conclusion <p>This study greatly endorse that the implemented approach holds&#xa0;tremendous potential to enhance the dissolution and solubility profile of poorly aqueous&#xa0;soluble drugs like atorvastatin via its conversion to its amorphous form.</p> Graphical Abstract <p></p>

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Formulation and Development of HPMC-Based Matrix Dispersion of Atorvastatin-Phospholipid Complex for Attenuation of Hyperlipidaemic Activity in High Fat Diet Induced Rat Model

  • 期刊论文

  • 发表日期：

    2025年10月20日

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  • Durga Uniyal,
  • Sumit Durgapal,
  • Elphine Prabahar,
  • Lata Bisht,
  • Prashant Kumar,
  • Gauree Kukreti

摘要

Purpose

Atorvastatin suffers from low oral bioavailability due to its poor solubility (BCS class II drug) and first-pass metabolism. Therefore, an approach of atorvastatin phospholipid complex and further its inclusion into a matrix dispersion was employed to improve the solubility and rate of solution of drug so that it can reach up to its full pharmacodynamic potential.

Methods

The, atorvastatin-phospholipid complex and matrix dispersion were prepared by solvent-evaporation technique using hydroxypropyl methyl cellulose (HPMC K 100M) and polyvinylpyrrolidone (PVP-K-30). Fourier transform infrared (FTIR), Nuclear magnetic resonance (NMR), Differential scanning calorimetry (DSC), Powder X-ray diffraction (PXRD), Scanning electron microscopy (SEM), and in-vitro drug release were performed to evaluate the performance of drug phospholipid complex and its matrix dispersion. Pharmacodynamic effects were evaluated in high fat diet induced rat models.

Results

Molecular docking confirmed the ability of atorvastatin to form complex with phospholipid. Results demonstrated a noteworthy increase in dissolution rates by drug phospholipid complex and its matrix dispersion as compared to marketed formulation due to the conversion of crystalline nature of drug into its amorphous form. In vivo pharmacodynamic studies also corroborated with the results of in vitro studies and demonstrated the significant decrease (P<0.001) in triglyceride (103.195±3.197mg/dl), cholesterol (83.86± 3.76mg/dl), and low-density lipoprotein (86.41±3.85 mg/dl) and increase in high density lipoprotein (88.93±4.814mg/dl) levels.

Conclusion

This study greatly endorse that the implemented approach holds tremendous potential to enhance the dissolution and solubility profile of poorly aqueous soluble drugs like atorvastatin via its conversion to its amorphous form.

Graphical Abstract