Alrumaihi Faris, Babiker Ali Yousif, Khan Arif
Department of Medical Laboratories, College of Applied Medical Sciences, Qassim University, Buraydah 51452, Saudi Arabia.
Department of Basic Health Sciences, College of Applied Medical Sciences, Qassim University, Buraydah 51452, Saudi Arabia.
Pharmaceuticals (Basel). 2025 Apr 15;18(4):574. doi: 10.3390/ph18040574.
[6]-Gingerol ([6]-G), a bioactive compound derived from Zingiber officinale (ginger), exhibits strong anticancer potential but is hindered by poor aqueous solubility and low bioavailability. This study aimed to develop and evaluate PEGylated liposomal [6]-G (6-G-Lip) to enhance its stability, bioavailability, and chemopreventive efficacy in benzo[a]pyrene (BaP)-induced lung carcinogenesis. 6-G-Lip was synthesized using a modified thin-film hydration technique and characterized for size, polydispersity index (PDI), zeta potential, encapsulation efficiency (EE%), and release kinetics. The chemopreventive effects were assessed in BaP-induced lung cancer in Swiss albino mice, with prophylactic 6-G-Lip administration from two weeks before BaP exposure through 21 weeks. Cancer biomarkers, antioxidant enzyme activity, reactive oxygen species (ROS) generation, induction of apoptosis, and histopathological alterations were analyzed. 6-G-Lip exhibited a particle size of 129.7 nm, a polydispersity index (PDI) of 0.16, a zeta potential of -18.2 mV, and an encapsulation efficiency (EE%) of 91%, ensuring stability and effective drug loading. The formulation exhibited a controlled release profile, with 26.5% and 47.5% of [6]-G released in PBS and serum, respectively, at 72 h. 6-G-Lip significantly lowered cancer biomarkers, restored antioxidant defenses (SOD: 5.60 U/min/mg protein; CAT: 166.66 μm HO/min/mg protein), reduced lipid peroxidation (MDA: 3.3 nm/min/mg protein), and induced apoptosis (42.2%), highlighting its chemopreventive efficacy. This study is the first to prepare, characterize, and evaluate PEGylated [6]-G-Lip for the chemoprevention of lung cancer. It modulates oxidative stress, restores biochemical homeostasis, and selectively induces apoptosis. These findings support 6-G-Lip as a promising nanotherapeutic strategy for cancer prevention.
[6]-姜辣素([6]-G)是一种从姜(姜科植物)中提取的生物活性化合物,具有很强的抗癌潜力,但因其水溶性差和生物利用度低而受到限制。本研究旨在开发并评估聚乙二醇化脂质体[6]-G(6-G-Lip),以提高其在苯并[a]芘(BaP)诱导的肺癌发生过程中的稳定性、生物利用度和化学预防效果。采用改良的薄膜水化技术合成6-G-Lip,并对其粒径、多分散指数(PDI)、zeta电位、包封率(EE%)和释放动力学进行表征。在瑞士白化小鼠BaP诱导的肺癌模型中评估化学预防效果,从BaP暴露前两周至21周预防性给予6-G-Lip。分析癌症生物标志物、抗氧化酶活性、活性氧(ROS)生成、凋亡诱导和组织病理学改变。6-G-Lip的粒径为129.7nm,多分散指数(PDI)为0.16,zeta电位为-18.2mV,包封率(EE%)为91%,确保了稳定性和有效的药物负载。该制剂呈现控释特性,在72小时时,[6]-G在PBS和血清中的释放率分别为26.5%和47.5%。6-G-Lip显著降低癌症生物标志物,恢复抗氧化防御(超氧化物歧化酶:5.60U/分钟/毫克蛋白;过氧化氢酶:166.66μm HO/分钟/毫克蛋白),减少脂质过氧化(丙二醛:3.3nm/分钟/毫克蛋白),并诱导凋亡(42.2%),突出了其化学预防效果。本研究首次制备、表征并评估了聚乙二醇化[6]-G-Lip用于肺癌的化学预防。它调节氧化应激,恢复生化稳态,并选择性诱导凋亡。这些发现支持6-G-Lip作为一种有前景的癌症预防纳米治疗策略。
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