物理化学表征和在体外活性的多 (ε-卡普罗拉克) / 基酸无形固体分散的体外活性
Oroitz Sánchez-Aguinagalde1, Eva Sanchez-Rexach1, Yurena Polo2
1Department of Mining-Metallurgy Engineering and Materials Science, POLYMAT, Bilbao School of Engineering, University of the Basque Country (UPV/EHU), Plaza Ingeniero Torres Quevedo 1, 48013 Bilbao, Spain.
Polymers
|April 27, 2024
概括
菌酸 (MPA) 的无形固体分散在聚乙烯 (PCL) 中增强了药物的生物可用性. 这些系统在体外显示出有利的相互作用,良好的药物释放和潜在的抗癌活性.
科学领域:
- 材料科学 材料科学 材料科学
- 制药科学 制药科学
- 生物技术是生物技术.
背景情况:
- 菌酸 (MPA) 是一种免疫抑制药物,具有潜在的抗癌特性.
- 提高MPA等难溶性药物的生物可用性对于有效的治疗结果至关重要.
- 无形固体分散 (ASDs) 为提高药物的溶解性和生物可用性提供了一个有希望的策略.
研究的目的:
- 准备和描述在聚乙烯-烯酸盐 (PCL) 中基酸 (MPA) 的无形固体分散 (ASD).
- 调查MPA和PCL在ASD中的混合性和特定相互作用.
- 评估MPA-PCL ASDs的体外药物释放概况和初步抗癌疗效.
主要方法:
- 差分扫描热量计 (DSC) 用于通过玻璃过渡温度 (Tg) 和点压力来评估可混合性.
- 里埃变换红外光谱法 (FTIR) 用于分析特定的分子间相互作用.
- 在体外释放药物的研究,以量化MPA随时间的释放.
- 在体外细胞培养实验中评估抗癌活性.
主要成果:
- 通过DSC的负相互作用参数证实了MPA和PCL之间的有利的相互作用相互作用.
- FTIR分析支持PCL/MPA混合物中存在特定相互作用的存在.
- 实验室药物释放表明,在所有成分中,超过70%的MPA在第三天释放.
- 初步的细胞培养研究表明,当使用含有MPA的支架进行治疗时,癌细胞的减少.
结论:
- 在PCL中可以成功制备MPA的无形固体分散物,从而由于有利的相互作用而提高生物可用性.
- 开发的ASD表现出良好的体外药物释放特征.
- 含有MPA的PCL支架显示出抗癌应用的潜力,需要进一步调查.
相关概念视频
Factors Affecting Dissolution: Polymorphism, Amorphism and Pseudopolymorphism
301
Polymorphism refers to the existence of a drug substance in multiple crystalline forms, known as polymorphs. Recently, this term has been expanded to include solvates (forms containing a solvent), amorphous forms (non-crystalline forms), and desolvated solvates (forms from which the solvent has been removed).
Some polymorphic crystals possess lower aqueous solubility than their amorphous counterparts, leading to incomplete absorption. For instance, the oral suspension of Chloramphenicol, which...
Some polymorphic crystals possess lower aqueous solubility than their amorphous counterparts, leading to incomplete absorption. For instance, the oral suspension of Chloramphenicol, which...
301
Factors Influencing Drug Absorption: Pharmaceutical Parameters
133
Solid dosage forms such as tablets and capsules undergo rigorous manufacturing processes to ensure stability and effectiveness. Their dissolution and absorption properties are influenced significantly by the choice of excipients (inactive ingredients that serve various roles in the formulation), and the methodology applied during production. The manufacturing parameters, such as compression force and granulation techniques, significantly affect dissolution rates. Elevated compression forces...
133
Factors Influencing Drug Absorption: Physicochemical Parameters
268
The physicochemical characteristics of drugs play a crucial role in formulating stable and bioavailable drug products. The solubility of a drug, governed by the varying pH along the GI tract and its dissociation constant (pKa), is pivotal in determining its ionization state and absorption rate. Notably, weak acids and bases remain unionized and are absorbed more rapidly.
Enhanced drug absorption can be achieved by reducing particle sizes and increasing surface areas, thereby facilitating...
Enhanced drug absorption can be achieved by reducing particle sizes and increasing surface areas, thereby facilitating...
268
Factors Affecting Dissolution: Drug pKa, Lipophilicity and GI pH
1.3K
Drug absorption within the gastrointestinal (GI) tract is a complex process influenced by several critical factors, including the site pH, the drug's dissociation constant (pKa), and the drug's lipophilicity. The GI tract exhibits a pH gradient, with an acidic environment in the stomach and a more alkaline environment in the small intestine. This pH variation directly affects the ionization state of drugs.
A drug's pKa and the pH of the gastrointestinal (GI) tract play crucial roles...
A drug's pKa and the pH of the gastrointestinal (GI) tract play crucial roles...
1.3K
Polymer Classification: Crystallinity
2.8K
Unlike ionic or small covalent molecules, polymers do not form crystalline solids due to the diffusion limitations of their long-chain structures. However, polymers contain microscopic crystalline domains separated by amorphous domains.
Crystalline domains are the regions where polymer chains are aligned in an orderly manner and held together in proximity by intermolecular forces. For example, chains in the crystalline domains of polyethylene and nylon are bound together by van der Waals...
Crystalline domains are the regions where polymer chains are aligned in an orderly manner and held together in proximity by intermolecular forces. For example, chains in the crystalline domains of polyethylene and nylon are bound together by van der Waals...
2.8K
Factors Influencing Drug Absorption: Drug Dissolution
478
The pharmacokinetic journey of drugs from solid oral dosage forms into systemic circulation is multifaceted. It begins with disintegration, a prerequisite ensuring a solid dosage form's subdivision into minute particles. Dissolution occurs next as these granulated entities solubilize in gastrointestinal fluids. This solubilization is crucial for the succeeding stage, permeation, which describes the traversal of the drug across the intestinal membrane and its subsequent entry into the blood...
478


