克韦尔/常规载荷PEG聚合物纳米颗粒的比较研究:可控药物释放及其生物活性
Renuka Mani1, Swethaa Viswaresh Babu1, Nishanth Murugesan1
1Department of Biochemistry, School of Bioscience, Periyar University, Salem, Tamil Nadu, India.
Journal of biochemical and molecular toxicology
|April 24, 2025
概括
像奎尔塞丁和鲁丁这样的黄类化合物被装入聚乙烯糖醇 (PEG) 聚合物纳米粒子 (NP) 中,以提高抗癌效果. 这些瑞/常规载荷的PEGNP显示出增强的抗氧化活性,并抑制了癌细胞的增殖.
科学领域:
- 纳米技术 纳米技术
- 药理学 药理学是指药理学的学科.
- 生物化学 生物化学
背景情况:
- 黄类化合物具有抗氧化和抗癌性质,但它们的治疗价值受到生物可用性差的限制.
- 传统的癌症化疗通常是无效的,需要新的治疗策略.
- 聚合物纳米粒子 (PEG NP) 提供了一个有前途的输送系统,以提高药物的生物可用性和循环时间.
研究的目的:
- 开发素/常规载荷的PEG聚合物纳米粒子 (Qu-PEG/Ru-PEGNP),以提高封装效率和持续的药物释放.
- 评估这些纳米配方的抗癌潜力和抗氧化活性.
- 研究纳米封装对癌细胞内细胞内活性氧物种 (ROS) 生成的作用.
主要方法:
- 使用UV-Vis光谱学,FTIR,NMR,XRD和SEM合成和表征奎思/常规载荷的PEGNP.
- 在pH 7.4的24小时内进行体外药物释放研究.
- 对KB癌细胞的抗氧化活性和体外细胞研究的评估,包括增殖抑制和细胞内ROS生成.
主要成果:
- 成功合成和特征Qu-PEG/Ru-PEGNP与增强封装和持续释放奎尔和鲁丁超过24小时.
- 与免费药物相比,聚合物纳米配方表现出优异的抗氧化活性,并有效抑制KB细胞增殖.
- Qu-PEG NPs和Ru-PEG NPs显著增加了癌细胞中的细胞内ROS生成.
结论:
- 在PEGNP中封装奎尔塞丁和鲁丁有效地准瘤微环境,增强药物的疗效.
- 含有黄胺的聚合物纳米颗粒显示出作为治疗癌症的治疗剂的巨大潜力.
- 这种方法为开发具有改善治疗结果的新型抗癌治疗提供了有前途的战略.
相关概念视频
Pharmaceutical Alternatives: Polymorphic Form-Related and Particle Size-Related Therapeutic Nonequivalence
Changes in polymorphic forms can significantly influence the bioavailability of poorly soluble drugs. Although the FDA defines pharmaceutical equivalence based on having the same active ingredient, dosage form, and route of administration, it does not automatically disqualify products with different polymorphic forms. This means two products with different polymorphs can still be deemed pharmaceutically equivalent. However, polymorphic differences can affect properties like wettability,...
Modified-Release Drug Delivery Systems: Influencing Factors
Modified-release drug delivery systems are designed to optimize the therapeutic effect of drugs by minimizing side effects, reducing the dosage required, and controlling drug release to align with pharmacokinetic and pharmacodynamic needs. The system depends on two key factors: the drug's release from the formulation and its movement through the body to the target site. Unlike conventional dosage forms, where absorption is the limiting step, the rate of drug release is the key determinant in...
Modified-Release Drug Delivery Systems: Bioavailability
Modified-release (MR) dosage forms are designed to extend drug release over time, thereby maintaining stable plasma concentrations and reducing dosing frequency. However, their bioavailability is typically below 100% due to incomplete drug release and presystemic metabolism, and limitations in drug permeability across the gastrointestinal epithelium, all of which can restrict the fraction of the drug reaching systemic circulation. Consequently, studying the in vivo bioavailability of MR...
Modified-Release Drug Delivery Systems: Drug Release Characteristics
Drug release from modified-release dosage forms is designed to achieve specific therapeutic effects by controlling the rate and extent of drug release. The classification of these drug release systems is based on key pharmacokinetic assumptions: drug disposition follows first-order kinetics, drug release is the rate-limiting step in absorption, and the released drug is rapidly and completely absorbed.There are four major models of drug release patterns. The first model is the slow zero-order...
Modified-Release Drug Delivery Systems: Site-Targeted
Site-targeted drug delivery systems enhance therapeutic efficacy while minimizing systemic toxicity and treatment costs. Unlike conventional methods, these systems ensure precise drug delivery, improving bioavailability and reducing side effects. Targeted drug delivery is classified into three levels. First-order targeting directs drugs to the capillary beds of specific organs or tissues. Second-order targets specific cell types, such as tumor cells, using receptor-mediated interactions.
Site-Targeted Drug Delivery Systems: Polymeric Carriers
Polymeric carriers enhance targeted drug delivery by increasing efficacy while minimizing off-target effects. These carriers comprise a biodegradable polymeric backbone integrated with functional elements that enable targeting, improve physicochemical properties, and regulate drug release.Targeting MechanismsThe targeting ability of polymeric carriers is mediated by a homing device, which is a molecular recognition component designed to selectively bind to specific tissues or cells. Monoclonal...


