Self-assembled fisetin-phospholipid complex: Fisetin-integrated phytosomes for effective delivery to breast cancer

被引：8
作者：
Talaat, Sara M. [1 ]
Elnaggar, Yosra S. R. [1 ,2 ]
El-Ganainy, Samar O. [3 ]
Gowayed, Mennatallah A. [3 ]
Allam, Maram [4 ]
Abdallah, Ossama Y. [1 ]
机构：
[1] Alexandria Univ, Fac Pharm, Dept Pharmaceut, Alexandria, Egypt
[2] Pharos Univ Alexandria, Fac Pharm & Drug Mfg, Int Publicat & Nanotechnol Ctr INCC, Dept Pharmaceut, Alexandria, Egypt
[3] Pharos Univ Alexandria, Fac Pharm, Dept Pharmacol & Therapeut, Alexandria, Egypt
[4] Alexandria Univ, Fac Med, Dept Pathol, Alexandria, Egypt
来源：
EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS | 2023年 / 189卷
关键词：
Fisetin; Phospholipid; Phytosomes; Breast cancer; Pharmacodynamics; DIETARY FLAVONOID FISETIN; CELL-CYCLE ARREST; IN-VITRO; ORAL BIOAVAILABILITY; POLYMERIC MICELLES; NANOPARTICLES; APOPTOSIS; DRUG; VIVO; OPTIMIZATION;
D O I：
10.1016/j.ejpb.2023.06.009
中图分类号：
R9 [药学];
学科分类号：
1007 ;
摘要：
Nowadays, fisetin (FIS) is extensively studied as potent anticancer surrogate with a multitarget actions against various types of cancers including breast cancer. However, its poor aqueous solubility handicapped its clinical utility. The current work endeavored, for the first time, to develop FIS phytosomes (FIS-PHY) for improving its physicochemical properties and subsequently its anticancer activity. Optimization of FIS- phytosomes involved different preparation techniques (Thin film hydration and ethanol injection) and different FIS: phospholipid molar ratios (1:1, 1:2, and 1:3). Complex formation was confirmed by complexation efficiency, infrared spectroscopy (IR), solubility studies and transmission electron microscope. The optimized FIS-PHY of 1:1 M ratio (PHY1) exhibited a nanometric particle size of 233.01 & PLUSMN; 9.46 nm with homogenous distribution (PDI = 0.27), negative zeta potential of - 29.41 mV, 100% complexation efficiency and controlled drug release over 24 h. Invitro cytotoxicity study showed 2.5-fold decrease in IC50 of PHY1 compared with free FIS. Also, pharmacodynamic studies confirmed the promoted cytotoxicity of PHY1 against breast cancer through modulating TGF-& beta;1/ MMP-9 molecular pathways of tumorigenesis. Overall, overcoming FIS drawbacks were successfully achieved through development of innovative biocompatible phytosomal system.
引用
收藏
页码：174 / 188
页数：15
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