基于80的Tween自组合混合小胞增强瓦尔沙坦通过皮肤递送
Alaa Eldeen B Yassin1, Salam Massadeh2,3, Abdullah A Alshwaimi4
1College of Pharmacy, King Abdullah International Medical Research Center, King Saud Bin Abdulaziz University for Health Sciences, Riyadh 11481, Saudi Arabia.
Pharmaceuticals (Basel, Switzerland)
|January 23, 2024
概括
这项研究开发了瓦尔沙坦 (Val) 装载的混合微粒,用于通过皮肤输送. 优化的系统显著增强了通过皮肤的Val透,为高血压治疗提供了一个有前途的替代方案.
科学领域:
- 制药科学 制药科学
- 药物输送系统 药物输送系统
- 纳米技术纳米技术
背景情况:
- 瓦尔萨坦 (Val) 由于溶解度和溶解度低,其口服生物利用性较差.
- 通过皮肤输送提供了持续药物水平和减少副作用的潜力.
研究的目的:
- 优化混合细胞系统,以提高瓦尔萨坦的通过皮肤输送.
- 通过实现长期,均的药物水平来提高治疗效果.
主要方法:
- 通过薄膜水化和微相分离制备的瓦尔萨坦载混合.
- 优化表面活性剂类型和药物与表面活性剂的比率.
- 微粒大小,PDI,泽塔潜力和捕获效率 (EE) 的表征.
主要成果:
- 实现了高VAL捕获效率 (>90%) 和低颗粒电荷.
- 细胞大小在107.6至191.7nm之间,PDI值约为0.3.
- 配方F7显示显著的皮肤外流 (68.84±3.96μg/cm2/h),增强因子为16.57.
结论:
- 通过使用简单的方法,成功开发出可复制的瓦尔萨坦载混合细胞.
- 证明了广泛的通过皮肤递送,没有强烈的皮肤增强剂.
- 混合小粒显示了通过透皮途径改善瓦尔萨坦治疗的潜力.
相关概念视频
Modified-Release Drug Delivery Systems: Rate-Programmed II
Rate-programmed drug delivery systems release drugs in a controlled manner to maintain therapeutic levels. Three main designs include reservoir, matrix, and hybrid systems.Reservoir systems consist of a drug core enclosed within a membrane that controls drug release. In non-swelling reservoir systems, polymers like ethyl cellulose or polymethacrylates are used. These do not hydrate in aqueous media and control release through membrane thickness, porosity, or insolubility. This type includes...
Modified-Release Drug Delivery Systems: Overview
Modified-release dosage forms are designed to address the limitations of drugs with short biological half-lives. These forms maintain stable therapeutic drug concentrations over extended periods, reducing the need for frequent dosing. A consistent drug level helps minimize peak-trough fluctuations, which can reduce adverse effects, lower the risk of drug resistance, and improve overall treatment effectiveness.One common type of modified-release form is the extended-release (ER) formulation. ER...
Modified-Release Drug Delivery Systems: Bioavailability
Modified-release (MR) dosage forms are designed to extend drug release over time, thereby maintaining stable plasma concentrations and reducing dosing frequency. However, their bioavailability is typically below 100% due to incomplete drug release and presystemic metabolism, and limitations in drug permeability across the gastrointestinal epithelium, all of which can restrict the fraction of the drug reaching systemic circulation. Consequently, studying the in vivo bioavailability of MR...
Modified-Release Drug Delivery Systems: Rate-Programmed I
Rate-programmed drug delivery systems (DDS) are designed to release drugs at specific, controlled rates to maintain consistent therapeutic levels. These systems are categorized based on their release mechanisms, including dissolution-controlled DDS, diffusion-controlled DDS, and combined dissolution-diffusion-controlled DDS.In dissolution-controlled DDS, the release rate depends on the slow dissolution of the drug itself or the surrounding matrix. Drugs with inherently slow dissolution rates,...
Modified-Release Drug Delivery Systems: Site-Targeted
Site-targeted drug delivery systems enhance therapeutic efficacy while minimizing systemic toxicity and treatment costs. Unlike conventional methods, these systems ensure precise drug delivery, improving bioavailability and reducing side effects. Targeted drug delivery is classified into three levels. First-order targeting directs drugs to the capillary beds of specific organs or tissues. Second-order targets specific cell types, such as tumor cells, using receptor-mediated interactions.
Transdermal Drug Delivery Systems
Transdermal drug delivery systems (TDDS) enable the controlled release of drugs across the skin into systemic circulation. They are particularly advantageous for drugs with short half-lives or narrow therapeutic indices, as they maintain consistent plasma concentrations and reduce the risk of subtherapeutic or toxic levels.TDDS are categorized into monolithic, reservoir, and mixed systems. Monolithic systems embed the drug in a polymer matrix, where diffusion governs release. Reservoir systems...


