开发含有cytarabine的响应pH的聚合水凝:一个体外和体外评估
Shaheer Khalid1, Sharjeel Adnan2, Asif Mahmood3,4
1Faculty of Pharmacy, The University of Lahore, Lahore, Pakistan.
Naunyn-Schmiedeberg's archives of pharmacology
|February 3, 2026
概括
在急性白血病治疗中,开发了一种新型的pH响应的聚合物水凝,用于控制的cytarabine输送. 这种生物相容的水凝确保了安全和向的药物释放,在白血病治疗中显示出有前途的结果.
科学领域:
- 生物材料科学 生物材料科学
- 药物输送系统 药物输送系统
- 聚合物化学 聚合物化学
背景情况:
- 急性白血病需要有效的化疗药物,如cytarabine.
- 细胞氨酸输送的挑战包括快速清除和全身毒性.
- 响应pH的水凝具有针对性和可控的药物释放的潜力.
研究的目的:
- 开发和优化一个响应pH的聚合物凝,用于控制的细胞氨酸输送.
- 评估水凝的物理化学特性,药物负载和释放动力学.
- 评估开发的水凝系统的安全性和生物相容性.
主要方法:
- 通过自由基聚合合成的聚合物凝合成,使用多酸F127,PEG-800和阿加.
- 与甲二烯胺的交叉连接.
- 描述包括细胞氨基酸负载,热分析,胀研究,形态学,FTIR和子体内毒性测试.
主要成果:
- 优化的水凝配方 (PPA12) 显示了增加的cytarabine负载,具有更高的聚合物/单体比和pH值.
- 在pH值7.4观察到出色的胀,促进药物释放.
- 在24小时内控制的细胞氨酸释放跟随零级动力学 (R2).
- FTIR证实了结构纠和水凝的形成.
- 毒性研究没有显示眼睛,口腔或皮肤毒性.
结论:
- 开发的pH响应的聚合物凝 (PPA12) 是生物相容和安全的.
- 它可以在特定的pH值下控制细胞氨基酸的输送.
- 这种水凝显示出作为向性白血病药物递送的载体的潜力.
相关概念视频
Equivalence: In Vitro and In Vivo Bioequivalence
234
Body:Bioequivalence studies are crucial in evaluating whether new drugs can match an approved one regarding pharmacological effects and clinical performance. These studies test if drugs, despite different dosage forms, share identical plasma concentration-time profiles. Three types of equivalence are central to these studies: chemical, pharmaceutical, and therapeutic. Chemical equivalence indicates that two or more drug products contain identical active ingredients in equal amounts.
234
Olefin Metathesis Polymerization: Ring-Opening Metathesis Polymerization (ROMP)
3.2K
Ring-opening metathesis polymerization or ROMP involves strained cycloalkenes as starting materials. The mechanism of ROMP proceeds by reacting cycloalkene with Grubbs catalyst to give metallacyclobutane intermediate which undergoes a ring-opening reaction to form new carbene. The new carbene reacts with another molecule of cycloalkene. Repetition of these steps leads to the formation of an unsaturated open-chain polymer product. All these steps are reversible, however, relieving the ring...
3.2K
Actin Polymerization
8.6K
Actin polymerization occurs through the head-to-tail association of binding sites on monomeric actin or G-actin to form filamentous or F-actin. The polymerization can be divided into three phases ̶ nucleation, elongation, and steady-state phase.
The nucleation phase involves forming a stable nucleus consisting of three actin monomers to form a new actin filament. Actin-binding proteins such as formins and Arp2/3 complex help filament growth post-nucleation. The Formins form straight...
The nucleation phase involves forming a stable nucleus consisting of three actin monomers to form a new actin filament. Actin-binding proteins such as formins and Arp2/3 complex help filament growth post-nucleation. The Formins form straight...
8.6K
In Vitro Drug Release Testing: Overview, Development and Validation
347
In vitro dissolution and drug release tests assess how quickly and how much of a drug is released from its dosage form into an aqueous medium under standardized laboratory conditions. These tests are essential tools in pharmaceutical development and quality assurance, offering insight into the drug's performance before clinical use.During formulation development, dissolution testing identifies incomplete or inconsistent drug release issues. It also supports decisions on selecting the optimal...
347
Impact Loading
701
Impact loading occurs when a moving object collides with a stationary structure, such as a rod with a uniform cross-sectional area fixed at one end. Under these conditions, the rod absorbs the kinetic energy from the striking object, leading to deformation and subsequent stress development. As the rod returns to its original position and reaches maximum stress, the absorbed energy, initially manifested as kinetic energy, transforms entirely into strain energy.
In cases of elastic deformation,...
In cases of elastic deformation,...
701
Drug Product Performance: In Vitro–In Vivo Correlation
278
In pharmaceutical development, it's crucial to establish a predictive in vitro–in vivo correlation (IVIVC) for two or more formulations to gain a comprehensive understanding of release properties. IVIVC reduces the need for costly in vivo studies and facilitates the establishment of meaningful dissolution specifications with significant cost savings and decreased regulatory burden. Furthermore, a meaningful IVIVC should predict Cmax and AUC within 20%, aligning with FDA guidance while...
278


