Quercetin-loaded solid lipid nanoparticles for enhanced anti-helminthic activity

IF 5.2 2区 医学 Q1 PHARMACOLOGY & PHARMACY International Journal of Pharmaceutics Pub Date : 2025-03-15 Epub Date: 2025-01-31 DOI:10.1016/j.ijpharm.2025.125308
Sunidhi Sharma , Ruchika Thukral , Lachhman Das Singla , Neena Singla , Diptiman Choudhury
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Abstract

Quercetin, a naturally occurring flavonoid, exhibits various anti-carcinogenic, anti-viral, anti-inflammatory properties, and anti-helminthic properties. Still, a major portion of orally administered quercetin is metabolized in the intestine and only little amount get absorbed in the portal veins, attributing to its poor bioavailability. The lipid content of food increases the solubility, which inspired us to fabricate lipid-based nanoparticles that will be biocompatible, orally administrable, and enhance the effectiveness of quercetin in hosts. Quercetin-loaded solid lipid nanoparticles (SLN-Qt) are spherical-shaped, water-soluble in nature, and nanocarriers having a hydrodynamic size of 130.7 ± 42.0 nm showing a drug entrapment efficiency of 79.75 % with sustained drug release of 37.5 ± 1.5 % within the first 24 h at pH 6.4. The drug release was observed till 6 days with 93.7 ± 3.0 % of drug release at pH 7.4. These results suggest improved drug entrapment, high saturation solubility, and better drug distribution. The in-vivo analysis was performed in house rats (Rattus rattus), which were found infected with Syphacia muris, Aspicularis tetraptera, Hymenolepis diminuta, Hymenolepis nana, Cysticercus fasciolaris, Calodium hepaticum, and/ or Trichuris muris. SLN-Qt (200 mg/Kg) treatment showed a significant reduction of parasite egg counts (85.09 ± 15.00 %) of gastrointestinal helminths after 3-dose weekly treatment. Liver histology and biochemical analysis of blood plasma and liver homogenate showed no toxic effects of quercetin and SLN-Qt. Therefore, SLN-Qt presents a promising strategy for delivering poorly soluble drugs and could be a valuable tool in controlling parasitic infections and diseases.

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槲皮素负载固体脂质纳米颗粒增强抗蠕虫活性。
槲皮素是一种天然存在的类黄酮,具有多种抗癌、抗病毒、抗炎和抗蠕虫的特性。然而,口服槲皮素的大部分在肠道代谢,只有少量被门静脉吸收,这是由于它的生物利用度很差。食物的脂质含量增加了溶解度,这激发了我们制造基于脂质的纳米颗粒,这种纳米颗粒将具有生物相容性,可口服,并增强槲皮素在宿主体内的有效性。槲皮素负载的固体脂质纳米颗粒(SLN-Qt)为球形、水溶性纳米载体,其水动力学尺寸为130.7 ± 42.0 nm,在pH 6.4下的前24 h内,药物包封效率为79.75 %,药物持续释放率为37.5 ± 1.5 %。在pH 7.4下,药物释放率为93.7 ± 3.0 %,药物释放时间为6 d。这些结果表明,改进的药物包裹,高饱和溶解度,更好的药物分布。对家鼠(Rattus Rattus)进行体内分析,发现感染了鼠梅毒、四翅条虫、小膜绦虫、小膜绦虫、片膜绦虫、囊尾蚴、肝钙和(或)鼠滴虫。SLN-Qt(200 mg/Kg)处理后,每周给药3次,胃肠道蠕虫虫卵数显著减少(85.09 ± 15.00 %)。肝脏组织学和血浆及肝脏匀浆生化分析显示槲皮素和SLN-Qt无毒性作用。因此,SLN-Qt提供了一种很有前途的递送难溶性药物的策略,可能是控制寄生虫感染和疾病的有价值的工具。
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来源期刊
CiteScore
10.70
自引率
8.60%
发文量
951
审稿时长
72 days
期刊介绍: The International Journal of Pharmaceutics is the third most cited journal in the "Pharmacy & Pharmacology" category out of 366 journals, being the true home for pharmaceutical scientists concerned with the physical, chemical and biological properties of devices and delivery systems for drugs, vaccines and biologicals, including their design, manufacture and evaluation. This includes evaluation of the properties of drugs, excipients such as surfactants and polymers and novel materials. The journal has special sections on pharmaceutical nanotechnology and personalized medicines, and publishes research papers, reviews, commentaries and letters to the editor as well as special issues.
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