基于环德的高分子深溶解剂 (CycloDES):一种用于输送难溶药物的载体
Gennaro Balenzano1, Giuseppe Francesco Racaniello1, Ilaria Arduino1
1Department of Pharmacy - Pharmaceutical Sciences, University of Bari "Aldo Moro", Via E. Orabona, 4, I-70125 Bari, Italy.
International journal of pharmaceutics
|October 26, 2023
概括
新的基于循环德的深溶解剂 (CycloDES) 显著提高了药物的溶解性和稳定性. 这些新型溶剂提供了一种有前途的方法,用于输送难溶性药物,改善口服生物利用性.
科学领域:
- 制药科学 制药科学
- 超分子化学 超分子化学
- 药物输送系统 药物输送系统
背景情况:
- 药物的溶解性差,特别是BCSII和IV类药物的溶解性差,仍然是制药开发中的一个重大挑战.
- 基-基-β-环德 (HPβCD) 以其复合能力而闻名,以改善药物溶解性.
- 深度浸泡溶剂 (DES) 为药物配方提供可调节的特性,但需要优化稳定性和有效性.
研究的目的:
- 开发和描述基于循环德克斯特林的新型高分子深层欧特溶剂 (CycloDES).
- 评估使用CycloDES的BCSII类药物的溶解和透增强.
- 与传统的DES相比,评估CycloDES在稀释后的稳定性.
主要方法:
- 基于HPβCD的DES (CycloDES) 的合成和物理化学表征.
- 在CycloDES中装载模型药物 (大麻二醇,印米他素,甲).
- 药物溶解性和透性增强的评估.
- 稀释研究比较CycloDES与标准的DES (葡萄糖胆化物).
主要成果:
- 赛克洛德斯 (CycloDES) 显示,研究BCS II类药物的可溶性至少提高了100倍.
- 赛克洛德斯表现出显著改善的抗稀释性,在添加水后保持高度的药物.
- 药物透受评估因素的影响,CycloDES显示出单独的HPβCD复杂化的潜力.
结论:
- 循环DES代表了一种新且有效的工具,用于提高难以溶解药物的溶解度 (BCS II 和 IV 类).
- 对稀释的增强稳定性使CycloDES成为用于药物输送应用的强大系统.
- 这种方法提供了一个潜在的策略,可以将固体药物转化为有利的液体配方,绕过溶解速率限制.
相关概念视频
Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry
209
Orally administered drugs primarily enter the systemic circulation via passive diffusion through the intestinal membranes. The drug's absorption is influenced by drug stability in the gastrointestinal GI tract, membrane permeability, the surface area available for absorption, luminal drug concentration, and residence time in the lumen. Drug permeability can be enhanced by adjusting the lipophilicity, polarity, or molecular size of the drug, promoting its passive transport across intestinal...
209
Drug Delivery: Overview
300
The selection of a drug's delivery route depends upon its physicochemical properties, including lipid or water solubility and ionization, as well as the therapeutic requirement, such as immediate or sustained effect. These routes can be divided into three primary categories: enteral, parenteral, and topical.
Enteral delivery involves administering drugs directly through swallowing, sublingual placement, or buccal application. Orally administered drugs predominantly navigate the...
Enteral delivery involves administering drugs directly through swallowing, sublingual placement, or buccal application. Orally administered drugs predominantly navigate the...
300
Factors Affecting Dissolution: Particle Size and Effective Surface Area
864
Dissolution kinetics, an essential aspect of oral drug delivery, is significantly influenced by the drug's particle size. According to the Noyes-Whitney dissolution model, the dissolution rate correlates directly with the drug's surface area. The larger the surface area, the higher the drug's solubility in water, leading to a faster drug dissolution rate. Reducing particle size increases the effective surface area, enhancing the dissolution process. Micronization and nanosizing are...
864
Factors Influencing Drug Absorption: Drug Dissolution
531
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...
531
Drug Delivery: Miscellaneous Routes
359
Drug delivery methods like oral inhalation, nasal sprays, transdermal patches, eye drops, intravitreal injection, and rectal administration provide localized effects with reduced toxicity.
Oral inhalation and nasal sprays swiftly transfer drugs across the respiratory epithelium's mucosal layer. Inhaled glucocorticoids and bronchodilators directly target lung conditions such as asthma, while fluticasone nasal spray mitigates allergic rhinitis.
Transdermal patches transport drugs...
Oral inhalation and nasal sprays swiftly transfer drugs across the respiratory epithelium's mucosal layer. Inhaled glucocorticoids and bronchodilators directly target lung conditions such as asthma, while fluticasone nasal spray mitigates allergic rhinitis.
Transdermal patches transport drugs...
359
Factors Affecting Dissolution: Polymorphism, Amorphism and Pseudopolymorphism
314
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...
314


