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通过聚合物纳米颗粒制剂提高没食子酸和槲皮素的生物利用度。

Improving gallic acid and quercetin bioavailability by polymeric nanoparticle formulation.

作者信息

Patil Poounima, Killedar Suresh

机构信息

Bharati Vidyapeeth College of Pharmacy, Kolhapur, India.

Ashokrao Mane College of Pharmacy, Peth-Vadgaon, India.

出版信息

Drug Dev Ind Pharm. 2021 Oct;47(10):1656-1663. doi: 10.1080/03639045.2022.2043353. Epub 2022 Feb 21.

Abstract

The anticancer activity and pharmacokinetic properties of encapsulated polyherbal nanoparticles (gallic acid (GA) and quercetin nanocomposite) and polyherbal extract (amla and pomegranate fruit peels) in normal and DMH-induced colorectal cancer in rats were examined in this work. In normal and DMH-induced rats, a pharmacokinetic study demonstrated that polyherbal nanoparticles had a typical sustained release profile with a fourfold increase in bioavailability when compared to polyherbal extract. Based on serum-concentration profiles of polyherbal nanoparticles and polyherbal extract following oral administration, the pharmacokinetic parameters for polyherbal nanoparticles and polyherbal extract were established using a single compartmental approach. This research suggests that encapsulating GA and quercetin in polymeric nanoparticles improves their oral bioavailability and anti-colon cancer efficacy. Polymeric nanoparticles could be a novel therapeutic possibility for carcinogenesis prevention.

摘要

本研究考察了包封的多草药纳米颗粒(没食子酸(GA)和槲皮素纳米复合材料)以及多草药提取物(印度醋栗和石榴果皮)在正常大鼠和二甲基肼诱导的大鼠结直肠癌中的抗癌活性和药代动力学特性。在正常大鼠和二甲基肼诱导的大鼠中,一项药代动力学研究表明,与多草药提取物相比,多草药纳米颗粒具有典型的缓释特征,生物利用度提高了四倍。基于口服给药后多草药纳米颗粒和多草药提取物的血清浓度曲线,采用单室模型方法确定了多草药纳米颗粒和多草药提取物的药代动力学参数。本研究表明,将GA和槲皮素包封在聚合物纳米颗粒中可提高其口服生物利用度和抗结肠癌疗效。聚合物纳米颗粒可能是预防癌症发生的一种新型治疗方法。

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