在增强药物输送的PEG改性石墨烯氧化物上对他莫西芬吸附的综合实验和DFT研究
Khaled Almansour1, Hashem O Alsaab2, Mahboubeh Pishnamazi3
1Department of Pharmaceutics, College of Pharmacy, University of Hail, Hail, Saudi Arabia.
概括
我们使用石墨烯氧化物-聚乙烯甘醇 (GO-PEG) 开发了一种对pH值敏感的tamoksifen (TAM) 纳米复合物,用于向乳腺癌治疗. 这种纳米平台增强了药物输送,克服了TAM耐药性,显示了改善治疗结果的希望.
科学领域:
- 生物材料科学 生物材料科学
- 纳米技术 纳米技术
- 计算化学计算化学
背景情况:
- 乳腺癌是导致死亡的主要原因,ER+瘤占~70%的病例.
- 标准内分泌疗法塔莫西芬 (TAM) 面临着一些挑战,包括溶解性差,生物可用性低以及获得的耐药性.
- 开发先进的药物输送系统对于提高乳腺癌治疗疗效至关重要.
研究的目的:
- 为了设计一个响应pH的纳米复合物,加载着tamoxifen的氧化石墨烯-聚乙烯甘醇 (TAM@GO-PEG).
- 为了增强药物负载,实现瘤选择性释放,并克服TAM抵抗.
- 使用计算方法研究纳米复合材料的结合相互作用和电子特性.
主要方法:
- GO-PEG纳米载体的合成和TAM的加载.
- 使用光谱 (FTIR,UV-Vis) 和显微 (TEM,XRD) 技术进行表征.
- 在不同的pH值下进行体外药物释放研究.
- 密度函数理论 (DFT) 模拟用于绑定能量和电子结构分析.
主要成果:
- 实现了高的药物加载效率 (DLE ≈80%) 和依赖pH的电荷逆转.
- 已证明瘤选择性TAM释放 (89.3%在pH 5.5下,相比61.1%在pH 7.4下).
- DFT揭示了强大的π-π堆叠和键相互作用,具有增强的稳定性和pH调节的释放.
结论:
- 纳米复合材料TAM@GO-PEG是一种有前途的纳米平台,用于针对性乳腺癌治疗.
- 该系统提供高药物负载,pH触发释放和可调节的电子特性.
- 综合实验和计算方法为设计下一代纳米疗法提供了一个强大的框架.
更多相关视频
相关概念视频
01:05Bioavailability Enhancement: Drug Stability Enhancement and GI Retention
200
Body:Improving a drug's stability in the gastrointestinal (GI) tract is paramount for enhancing its bioavailability and therapeutic effectiveness. Various strategies are employed to protect the drug from the harsh gastric milieu and to ensure its release and absorption at the desired site within the GI tract.Polymer coatings are one such method used to shield drugs from the stomach's acidic environment. By preventing premature drug release, these coatings improve the bioavailability of unstable...
200
01:16Methods for Studying Drug Absorption: In vitro
574
In vitro experiments are crucial for understanding the transport and absorption of drugs through biological materials. These studies employ varied methods such as the diffusion cell method, the everted sac technique, and the everted ring technique.
The diffusion cell method uses a two-compartment cell, including a donor compartment with the drug solution, which simulates the environment where the drug is applied, and a receptor compartment with a buffer solution, which simulates the environment...
The diffusion cell method uses a two-compartment cell, including a donor compartment with the drug solution, which simulates the environment where the drug is applied, and a receptor compartment with a buffer solution, which simulates the environment...
574
01:09Methods for Studying Drug Absorption: In situ
636
In situ experiments, such as the Doluisio method and Single-Pass Perfusion technique, provide critical insights into drug uptake by simulating in vivo conditions for drug absorption.
The Doluisio method involves perfusing a prepared segment of a rat's small intestine with a solution of radiolabeled drug and a non-absorbable marker. This helps to differentiate between absorbed and non-absorbed drug concentrations. The intestinal segment is connected at both ends using tubing and syringes,...
The Doluisio method involves perfusing a prepared segment of a rat's small intestine with a solution of radiolabeled drug and a non-absorbable marker. This helps to differentiate between absorbed and non-absorbed drug concentrations. The intestinal segment is connected at both ends using tubing and syringes,...
636
01:27Bioavailability Enhancement: Drug Permeability Enhancement
186
Body:After oral administration, poor permeability often limits the rate at which drugs are absorbed through the intestinal epithelium. Enhancing drug permeability is crucial for effective therapy, and several strategies have been developed to overcome this challenge.One effective strategy involves the use of lipid-based formulations. These formulations enhance dissolution and solubility, targeting physiological mechanisms to increase drug absorption. This includes stimulating bile salt...
186