氏脂纳米囊的配方:药物释放,透性,生物相容性和稳定性研究
Eva C Arrua1, Olga Hartwig2, Brigitta Loretz3
1Institute of Chemistry, IQUIR-CONICET, National Council Research, Suipacha 531, 2000 Rosario, Argentina.
International journal of pharmaceutics
|June 12, 2023
概括
新型脂质纳米囊改善了尼达的输送,用于查加斯病治疗. 这些纳米载体增强了药物的溶解性,透性和稳定性,为目前的疗法提供了一个有前途的替代方案.
科学领域:
- 制药纳米技术 制药纳米技术
- 药物输送系统 药物输送系统
- 查加斯病治疗方法 查加斯病治疗方法
背景情况:
- 尼达是查加斯病的主要治疗方法,但其溶解性差,副作用和慢性阶段有效性有限.
- 需要先进的尼达配方来提高治疗结果.
- 脂质纳米囊 (LNC) 为改善本兹尼达的药理动力学和药理动力学特征提供了一个潜在的解决方案.
研究的目的:
- 开发和描述带有尼达的脂质纳米囊 (LNC).
- 为了评估含本兹尼达LNC的可溶性,溶解率,稳定性和透性.
- 评估LNCs在改善查加斯病化疗方面的潜力.
主要方法:
- 用阶段逆转技术制备了封装本兹尼达的脂质纳米囊.
- 配方的特点是尺寸,多分散性指数,泽塔潜力,封装效率和药物负载.
- 在储存条件下评估稳定性,并在模拟的胃和肠液中研究药物释放.
- 通过肠表皮和粘液透进行了体外透性研究.
主要成果:
- 成功制备了三种LNC配方,尺寸为30,50和100纳米,表现出单模分布和近中性泽塔潜力.
- 实现了高封装效率 (83-92%) 和药物加载 (0.66-1.04%).
- LNCs在一年内表现出极好的稳定性,并且在模拟的胃液中保护了本兹尼达.
- 在模拟的肠液中观察到持续的药物释放,肠道透率增加了10倍,与粘素的相互作用减少.
- 在暴露于纳米配方时,上皮质完整性得到维持.
结论:
- 含有本津醇的LNC显著提高了药物的溶解性,溶解性和透性.
- LNCs为尼达提供了保护性和持续释放的平台.
- 这些纳米配方代表了一种有前途的策略,以提高本兹尼达化学疗法对查加斯病的安全性和有效性.
相关概念视频
01:20Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry
235
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...
235
01:23Factors Affecting Dissolution: Particle Size and Effective Surface Area
903
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...
903
01:28Factors Influencing Drug Absorption: Pharmaceutical Parameters
157
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...
157
01:27Factors Influencing Drug Absorption: Drug Dissolution
592
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...
592
01:22Factors Influencing Drug Absorption: Physicochemical Parameters
330
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...
330
01:23Factors Influencing Bioavailability: First-Pass Elimination
6.5K
When a drug is taken orally, it undergoes a journey starting from the gastrointestinal (GI) tract, passing through the portal vein, reaching the liver, and finally entering the systemic circulation. This process involves the absorption of the drug across the GI tract. The liver is the primary site for metabolizing the drug, with some metabolism also occurring in the gut wall. This journey significantly reduces the quantity of the drug that reaches the systemic circulation, a phenomenon known as...
6.5K