对于pH值敏感的液晶晶珠,设计用于口服的零序延长药物释放
Eliezer Y Goldmünz1, Abraham Aserin1, Ananya Pal2
1The Casali Center for Applied Chemistry, The Institute of Chemistry, The Hebrew University of Jerusalem, Edmond J. Safra Campus, Jerusalem 9190401, Israel.
International journal of pharmaceutics
|March 14, 2025
概括
这项研究提出了用于持续口服药物输送的新型利奥托普液晶 (LLC) 珠子. 这些响应pH的珠子控制药物释放,增强口服输送系统的有效性.
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:
- 热液晶 (LLCs) 提供了控制药物输送的潜力.
- 开发稳定和可调节的口服输送系统仍然是一个挑战.
研究的目的:
- 开发新的利奥特罗普液晶 (LLC) 珠子,用于持续的口服药物输送.
- 设计pH响应的LLC系统,以控制脂性药物的释放.
主要方法:
- 一种新的自下而上的制造工艺,用于造有控制直径的LLC珠子.
- 嵌入LLC珠子在一个凝-酸联合合剂中,以防止凝聚.
- 制定pH响应性LLCs以调节不同pH水平的药物释放.
- 装载Celecoxib (CLXB) 作为一种模型的脂性药物,以证明系统适用性.
- 利用小角度X射线衍射,NMR和EPR等技术研究药物释放机制.
主要成果:
- 开发的LLC珠子证明了对药物释放率的精确控制.
- 响应pH的系统有效地减弱了初始药物爆发,并在pH 6.4时增强释放.
- 切莱可西布 (CLXB) 释放显示了依赖于pH值的希古奇释放常数的增加.
- 在高pH下,CLXB的持续释放档案达到零级 (>10小时).
- 在脂友性化合物释放和LLC曲率变化之间观察到一种相互依赖的关系.
结论:
- 这种新的自下而上的制造方法可以有效地控制LLC珠子的特性.
- 响应pH的LLC系统对受控口服输送脂性药物充满希望.
- 了解药物释放和LLC结构之间的相互作用,可以提高配方设计,以提高药物的疗效.
相关概念视频
Factors Affecting Dissolution: Polymorphism, Amorphism and Pseudopolymorphism
276
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...
276
Factors Influencing Drug Absorption: Drug Dissolution
395
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...
395
Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry
164
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...
164
Factors Influencing Drug Absorption: Pharmaceutical Parameters
111
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...
111
Factors Affecting Dissolution: Particle Size and Effective Surface Area
658
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...
658
Factors Affecting Dissolution: Drug pKa, Lipophilicity and GI pH
908
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...
908


