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<p>Phytosomes, i.e., phospholipid complexes, are a vesicular drug delivery system engineered to enhance the biopharmaceutical and pharmacokinetics of poorly water-soluble phytoconstituents. However, the stickiness of the phytosomes causes their aggregation, showing low solubility and poor dissolution of phytoconstituents. Therefore, ferulic acid phytosomes (FAP) were prepared using Phospholipon<sup>®</sup>80G (PL80G) and converted into solidified phytosomes (S-FAPs) using COS M-5P. S-FAPs were tested employing particle size, zeta potential, scanning electron microscopy (SEM), Fourier transform infrared spectroscopy (FT-IR), differential scanning calorimetry (DSC), powder x-ray diffractometry (PXRD), proton nuclear magnetic resonance (<sup>1</sup>H-NMR), powder characteristics, solubility, and <i>in vitro</i> dissolution. S-FAPs enhanced the entrapment of FA ~ 82.08% within the polar head of phospholipids. The particle size ~ 335.96&#xa0;nm, PDI ~ 0.20, and high zeta potential ~ -55.3&#xa0;mV of S-FAPs suggest its suitability for the oral route. Physical analysis confirmed the synthesis of FAP and S-FAPs through weak intermolecular bonding among FA, PL80G and COS M-5P. Powder characteristics study indicated that S-FAPs improved the powder flow properties compared to FAPs. A solubility study indicated that S-FAPs drastically enhanced the solubility of FA (~ 2-fold) and FAPs (~ 1.5-fold) compared to pure FA. Likewise, S-FAPs and FAPs enhanced the dissolution by ~ 53% and ~ 39% compared to pure FA by ~ 25%. Pharmacokinetic results indicated that S-FAPs significantly enhanced the <i>Cmax</i><i>, </i><i>Tmax, AUC</i><sub><i>0-t</i></sub><i> a</i>nd <i>MRT</i> compared to FAPs and pure FA, suggesting enhanced oral bioavailability of FA. A stability study suggested optimized S-FAPs are physically and chemically stable under different pH conditions. Findings indicate that developed S-FAPs using COS M-5P could be used as an anticipated formulation scheme to ameliorate FA's biopharmaceutical and pharmacokinetic properties.</p> Graphical Abstract <p></p>

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Cab-O-Sil®M-5P Integrated Solidified Phytosomes: A Novel Strategy to Enhance the Solubility, In Vitro Dissolution and Pharmacokinetic Performance of Ferulic Acid

  • 期刊论文

  • 发表日期：

    2025年8月8日

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  • Amol S. Warokar,
  • Darshan R. Telange,
  • Bhawna S. Dumbhare,
  • Umesh B. Telrandhe

摘要

Phytosomes, i.e., phospholipid complexes, are a vesicular drug delivery system engineered to enhance the biopharmaceutical and pharmacokinetics of poorly water-soluble phytoconstituents. However, the stickiness of the phytosomes causes their aggregation, showing low solubility and poor dissolution of phytoconstituents. Therefore, ferulic acid phytosomes (FAP) were prepared using Phospholipon®80G (PL80G) and converted into solidified phytosomes (S-FAPs) using COS M-5P. S-FAPs were tested employing particle size, zeta potential, scanning electron microscopy (SEM), Fourier transform infrared spectroscopy (FT-IR), differential scanning calorimetry (DSC), powder x-ray diffractometry (PXRD), proton nuclear magnetic resonance (1H-NMR), powder characteristics, solubility, and in vitro dissolution. S-FAPs enhanced the entrapment of FA ~ 82.08% within the polar head of phospholipids. The particle size ~ 335.96 nm, PDI ~ 0.20, and high zeta potential ~ -55.3 mV of S-FAPs suggest its suitability for the oral route. Physical analysis confirmed the synthesis of FAP and S-FAPs through weak intermolecular bonding among FA, PL80G and COS M-5P. Powder characteristics study indicated that S-FAPs improved the powder flow properties compared to FAPs. A solubility study indicated that S-FAPs drastically enhanced the solubility of FA (~ 2-fold) and FAPs (~ 1.5-fold) compared to pure FA. Likewise, S-FAPs and FAPs enhanced the dissolution by ~ 53% and ~ 39% compared to pure FA by ~ 25%. Pharmacokinetic results indicated that S-FAPs significantly enhanced the Cmax, Tmax, AUC0-t and MRT compared to FAPs and pure FA, suggesting enhanced oral bioavailability of FA. A stability study suggested optimized S-FAPs are physically and chemically stable under different pH conditions. Findings indicate that developed S-FAPs using COS M-5P could be used as an anticipated formulation scheme to ameliorate FA's biopharmaceutical and pharmacokinetic properties.

Graphical Abstract