含有tizanidine的内鼻三甲基基托桑涂层乳液作为治疗的脑向治疗:配方,优化和药物动力学评估
Mohammed H Elkomy1, Omnia M Hendawy2, Randa Mohammed Zaki3,4
1Department of Pharmaceutics, College of Pharmacy, Jouf University, 72341, Sakaka, Saudi Arabia.
Drug delivery and translational research
|December 12, 2024
概括
这项研究开发了鼻内提扎尼丁HCl (TZN) 乳液,以改善用于治疗的大脑输送. 与口服TZN相比,新配方显著提高了TZN在大脑和血中的生物可用性.
科学领域:
- 制药科学 制药科学
- 药物输送系统 药物输送系统
- 神经科学是一个神经科学.
背景情况:
- 口服的tizanidine HCl (TZN) 由于吸收不良,肝脏新陈代谢快速,血脑屏障透受限制,有效性有限.
- 水友性质和饮食依赖的吸收进一步使TZN的口服生物可用性和治疗有效性复杂化.
研究的目的:
- 开发用于鼻内注射的含有TZN的酸盐涂层乳液 (TZN-CTS-EMS).
- 绕过肝脏新陈代谢并提高TZN在大脑中的生物可用性.
主要方法:
- 使用薄膜水化技术制定了TZN-CTS-EMS.
- 用一个Box-Behnken实验设计来优化囊泡特征.
- 在体内进行了药理动力学研究和鼻子粘膜组织病理学评估.
主要成果:
- 优化的TZN-CTS-EMS显示了可取的特征:粒子大小为127.63nm,封装效率为67.36%和32.49mV的泽塔电位.
- 与鼻内TZN-CTS-EMS溶液相比,鼻内TZN-CTS-EMS的相对生物可用性显著提高:在血中达到191.9%,在大脑中达到459.3%.
- 组织病理学证实,鼻腔粘膜没有结构性损伤或毒性.
结论:
- 鼻内TZN-CTS-EMS提供了一个有前途的非侵入性策略,可以有效地将TZN传递给大脑组织.
- 这种方法可以提高TZN治疗性的安全性和药理效率.
相关概念视频
Spasmolytic Agents: Chemical Classification
857
Spasmolytic agents are drugs used to alleviate muscle spasms and spasticity. They can be categorized into different chemical groups based on their mechanisms of action. Centrally acting spasmolytics primarily affect the spinal cord, while others directly target skeletal muscle cells.
A major class of centrally acting spasmolytics is the α2-agonist, such as tizanidine. These drugs bind to α2-adrenoceptors, inhibiting the release of the excitatory neurotransmitter glutamate. They also...
A major class of centrally acting spasmolytics is the α2-agonist, such as tizanidine. These drugs bind to α2-adrenoceptors, inhibiting the release of the excitatory neurotransmitter glutamate. They also...
857
Centrally Acting Muscle Relaxants: Therapeutic Uses
624
Centrally acting muscle relaxants reduce muscle tone and tension by interfering with the postsynaptic reflexes in the central nervous system.
Centrally acting drugs are classified into spasmolytic and antispasmodic drugs. Spasmolytic drugs such as baclofen, diazepam, and tizanidine inhibit spinal motor neurons and decrease muscle tone. Spasmolytic drugs are administered for severe and chronic spasms due to multiple sclerosis, cerebral palsy, stroke, and spinal cord and muscle injuries. However,...
Centrally acting drugs are classified into spasmolytic and antispasmodic drugs. Spasmolytic drugs such as baclofen, diazepam, and tizanidine inhibit spinal motor neurons and decrease muscle tone. Spasmolytic drugs are administered for severe and chronic spasms due to multiple sclerosis, cerebral palsy, stroke, and spinal cord and muscle injuries. However,...
624
Drug Delivery: Miscellaneous Routes
320
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...
320
Drug Delivery: Parenteral Route
417
The parenteral route is a critical method of drug administration. It delivers compounds directly into the systemic circulation and bypasses the gastrointestinal tract. This approach is particularly advantageous for drugs that exhibit poor absorption or instability when administered orally.
There are three primary parenteral routes: intravenous (IV), intramuscular (IM), and subcutaneous (SC). The IV route introduces the drug directly into the bloodstream, ensuring immediate action. The IM route...
There are three primary parenteral routes: intravenous (IV), intramuscular (IM), and subcutaneous (SC). The IV route introduces the drug directly into the bloodstream, ensuring immediate action. The IM route...
417


