Warokar Amol S, Telange Darshan R, Dumbhare Bhawna S, Telrandhe Umesh B
Dadasaheb Balpande College of Pharmacy, Rashtrasant Tukadoji Maharaj Nagpur University, Nagpur, 440037, Maharashtra, India.
Datta Meghe College of Pharmacy, Datta Meghe Institute of Higher Education and Research (Deemed to Be University), Sawangi (Meghe), Wardha, 442004, Maharashtra, India.
AAPS PharmSciTech. 2025 Aug 8;26(7):208. doi: 10.1208/s12249-025-03204-6.
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 Phospholipon80G (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 (H-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, AUC 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.
植物脂质体,即磷脂复合物,是一种囊泡药物递送系统,旨在增强难溶性植物成分的生物药剂学性质和药代动力学。然而,植物脂质体的粘性会导致其聚集,表现出植物成分的低溶解度和差溶出度。因此,使用磷脂酰胆碱80G(PL80G)制备阿魏酸植物脂质体(FAP),并使用壳聚糖M-5P将其转化为固化植物脂质体(S-FAP)。对S-FAP进行了粒度、zeta电位、扫描电子显微镜(SEM)、傅里叶变换红外光谱(FT-IR)、差示扫描量热法(DSC)、粉末X射线衍射法(PXRD)、质子核磁共振(H-NMR)、粉末特性、溶解度和体外溶出度测试。S-FAP在磷脂的极性头部内提高了阿魏酸的包封率约82.08%。S-FAP的粒径约为335.96nm,多分散指数(PDI)约为0.20,zeta电位较高约为-55.3mV,表明其适合口服给药途径。物理分析证实了通过阿魏酸、PL80G和壳聚糖M-5P之间的弱分子间键合合成了FAP和S-FAP。粉末特性研究表明,与FAP相比,S-FAP改善了粉末的流动性。溶解度研究表明,与纯阿魏酸相比,S-FAP极大地提高了阿魏酸(约2倍)和FAP(约1.5倍)的溶解度。同样,与纯阿魏酸相比,S-FAP和FAP分别提高了约53%和约39%的溶出度,而纯阿魏酸的溶出度约为25%。药代动力学结果表明,与FAP和纯阿魏酸相比,S-FAP显著提高了Cmax、Tmax、AUC和MRT,表明阿魏酸的口服生物利用度提高。稳定性研究表明,优化后的S-FAP在不同pH条件下物理和化学性质稳定。研究结果表明,使用壳聚糖M-5P开发的S-FAP可作为一种预期的制剂方案,以改善阿魏酸的生物药剂学和药代动力学性质。