柏柏林HCl和迪亚塞林加载的双输送转基因组:使用Box-Behnken设计的配方和优化
Siddharth Singh1, Rajendra Awasthi1
1Department of Pharmaceutical Sciences, School of Health Sciences & Technology, UPES, Dehradun, Uttarakhand, India.
ADMET & DMPK
|August 2, 2024
概括
这项研究开发了优化转移体,用于局部输送柏柏林化和白素,证明了它们对有效的牛皮管理的潜力. 该配方显示出高的捕获效率和皮肤透能力.
科学领域:
- 药理学 药理学是指药理学的学科.
- 材料科学 材料科学 材料科学
- 皮肤病学 皮肤病学
背景情况:
- 柏柏林通过减少TNF-α和IL-12等促炎细胞因子,表现出抗炎性质.
- 迪亚赛林通过降低TNF-α和IL-12的产量来有效治疗牛皮.
- 柏柏林的水溶性较差限制了其治疗效果.
研究的目的:
- 开发和优化转基因组,以增强柏柏林HCl和迪亚塞林的局部输送.
- 为了评估牛皮管理的优化配方的抗炎潜力.
- 评估开发的转基因组合的皮肤透和稳定性.
主要方法:
- 用薄膜水化方法制备封装柏柏林化和迪亚塞林的转基因.
- 使用Box-Behnken设计进行了配方优化,使用不同的脂胆,边缘激活剂和超声波循环.
- 特性包括颗粒大小,捕获效率,多分散性指数,泽塔潜力,可变形性,抗氧化活性,体外释放和ex-vivo皮肤透研究.
主要成果:
- 优化的转移酶体实现了110.90±2.8nm的颗粒大小,具有高的捕获效率 (89.50±1.5%的柏柏林HCl,91.23±1.8%的迪亚塞林).
- 观察到药物释放量很高 (82.093±0.81%的柏柏林HCl,85.02±3.81%的迪亚塞林) 和显著的皮肤透 (柏柏林HCl的皮肤间流量为0.0224μg cm−2h−1,迪亚塞林的皮肤间流量为0.0462μg cm−2h−1).
- 拉曼分析证实了皮肤透,配方在3个月内表现出良好的稳定性,在小鼠中没有观察到皮肤刺激.
结论:
- 优化的转基因组提供了一个有效的系统,用于局部输送柏柏林酸盐和迪亚塞林.
- 这种配方有望通过增强的透皮药物输送来有效管理牛皮.
- 这项研究强调了转移体在克服可溶性问题和改善难溶性药物的治疗结果方面的潜力.
更多相关视频
07:53Encapsulation of Cancer Therapeutic Agent Dacarbazine Using Nanostructured Lipid Carrier
Published on: April 26, 2016
11.1K
10:53Anionic Polymerization of an Amphiphilic Copolymer for Preparation of Block Copolymer Micelles Stabilized by π-π Stacking Interactions
Published on: October 10, 2016
14.0K
相关概念视频
Factors Influencing Drug Absorption: Pharmaceutical Parameters
125
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...
125
Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry
191
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...
191
