开发可调节的HLB聚胺酸-维生素E合物作为增强TPGS替代品,以改善溶解,生物安全和抗氧化
Chujuan Huang1,2, Yuanyuan Lin2, Guanglin Lu2
1Department of Pharmacology and Department of Gastroenterology of the Second Affiliated Hospital, Zhejiang University School of Medicine, Hangzhou 310058, China.
Langmuir : the ACS journal of surfaces and colloids
|July 10, 2025
概括
一种新的维生素E (VE) 和-多聚胺酸 (γ-PGA) 结合物,γ-PGAVE,比TPGS提供了更好的溶解和抗氧化能力. 这种生物相容的替代品对制药和食品应用具有前景.
科学领域:
- 聚合物化学 聚合物化学
- 材料科学 材料科学 材料科学
- 生物相容性材料 生物相容性材料
背景情况:
- d-α-托科法醇聚乙烯甘醇酸盐 (TPGS) 是FDA批准的溶解剂,容量有限,毒性高.
- 制药和其他行业需要更安全,更有效的溶解剂.
研究的目的:
- 为了合成和表征一种新型的两动物,g-PGAVE结合物,作为一种潜在的TPGS替代品.
- 评估γ-PGAVE的溶解能力,抗氧化活性和细胞毒性.
主要方法:
- 通过将α-托科菲罗尔 (维生素E) 化为γ-多聚胺酸骨干,合成γ-PGAVE合物.
- 通过控制 VE 接种率来调整水友性-脂友性平衡 (HLB) 和临界细胞度 (CMC).
- 评估溶解能力,抗氧化活性和体外细胞毒性.
主要成果:
- 根据VE接种比,γ-PGAVE合物表现出可调节的CMC (2.4-9.1μg/mL) 和HLB (4.45-13.39).
- 具有2.5% VE接种比率的γ-PGAVE (γ-PGAVE-2.5%) 显示出优越的水溶解能力.
- γ-PGAVE-2.5%的抗氧化能力与TPGS相比较,细胞毒性显著降低.
结论:
- 由于其增强的溶解和抗氧化特性,γ-PGAVE-2.5%是TPGS的一个有希望的生物相容替代品.
- 这种新型结合物具有作为食品添加剂,食补充剂,化品成分和制药辅助剂的应用潜力.
相关概念视频
01:22Phase II Reactions: Glutathione Conjugation and Mercapturic Acid Formation
386
Glutathione, a tripeptide made up of glutamate, cysteine, and glycine, is a critical player in the detoxification of drugs and xenobiotics via a process known as glutathione conjugation or mercapturic acid formation. This phase II biotransformation reaction involves the covalent binding of glutathione to a drug or its metabolite, enhancing the compound's water solubility and enabling its excretion.
Several distinctive characteristics distinguish glutathione conjugation from other phase II...
Several distinctive characteristics distinguish glutathione conjugation from other phase II...
386
01:14Drug Metabolism: Phase II Reactions
4.2K
Phase II reactions are essential for the detoxification and elimination of drugs from the body. These reactions involve the conjugation of parent drugs or their phase I metabolites with endogenous molecules, resulting in more hydrophilic drug conjugates. The primary conjugation reactions in this phase are sulfation and glucuronidation. Both sulfation and glucuronidation typically produce biologically inactive metabolites. However, in some cases involving prodrugs, active metabolites may be...
4.2K
01:16Drug Biotransformation: Overview
2.9K
Pharmaceutical substances known as xenobiotics are predominantly lipophilic and nonionized. This enables them to permeate lipid bilayers, such as cell membranes, and interact with intracellular target receptors. Lipophilic drugs have an advantage in crossing biological barriers and reaching their intended sites of action. However, lipophilic drugs often have a restricted capacity for renal expulsion or elimination from the body. When these drugs enter the kidneys and undergo glomerular...
2.9K
01:19Phase II Reactions: Sulfation and Conjugation with α-Amino Acids
435
Sulfation and α-amino acid conjugation are two critical biotransformation reactions in drug metabolism. Sulfation, a phase II biotransformation reaction, involves adding a polar sulfate group to a drug, enhancing its water solubility and promoting excretion. This process can either co-occur with or occur independently of glucuronidation. Nonmicrosomal sulfotransferase enzymes catalyze the process. The reaction involves 3'-phosphoadenosine-5'-phosphosulfate or PAPS coenzyme...
435
01:24Phase II Reactions: Glucuronidation
813
Glucuronidation, a pivotal phase II biotransformation process, involves the coupling of glucuronic acid to a drug or xenobiotic. Given its widespread occurrence and critical role in drug metabolism, it's considered the most crucial phase II reaction. It enhances the water solubility of substances, aiding their expulsion from the body. The driving force behind these reactions is a group of enzymes known as UDP-glucuronosyltransferases (UGTs). UGTs facilitate the transfer of a glucuronic acid...
813