研究大麻素酸/环极地含复合物用于改善物理化学和生物性能
Chulhun Park1, Jieyu Zuo2, Myung-Chul Gil3,4
1College of Pharmacy, Jeju National University, Jeju 63243, Republic of Korea.
Pharmaceutics
|November 25, 2023
概括
这项研究通过使用环氧德克斯 (CD) 纳入复合物增强了大麻素酸 (THCA,CBDA) 的溶解性和稳定性. 优化的大麻素酸/M-β-CD复合体显示出改善的透性和优异的抗癌活性.
科学领域:
- 制药科学 制药科学
- 材料科学 材料科学 材料科学
- 生物化学 生化学
背景情况:
- 像THCA和CBDA这样的大麻素酸具有较差的溶解性和稳定性,限制了它们的治疗应用.
- 已知循环德克斯 (CDs) 能形成包容复合物,增强难溶性化合物的物理化学性质.
研究的目的:
- 通过形成环极 (CD) 纳入复合体,增强四大麻酸 (THCA) 和大麻酸 (CBDA) 的溶解性和稳定性.
- 优化大麻素酸/CD纳入复合物的制备和干燥方法.
- 评估优化复合体的物理化学和生物性能.
主要方法:
- 用五种类型的环极素 (α-CD,β-CD,γ-CD,HP-β-CD,M-β-CD) 进行了相位溶解性研究.
- 通过调整pH值和采用喷雾干燥,冷干燥和喷雾冷干燥技术来优化包含复杂的制备.
- 鉴定包括溶解度测定,DSC,FE-SEM,XRD和1H NMR光谱.
主要成果:
- 通过DSC,XRD和FE-SEM证实,大麻素酸/CD纳入复合体处于非晶状状态.
- 与大麻乙醇提取物相比,喷雾冷干燥的大麻素酸/M-β-CD纳入复合体显示出明显改善的透性.
- 在模拟生理条件下,大麻素酸/M-β-CD纳入复合体在7天内表现出增强的稳定性和对MCF-7乳腺癌细胞的优越抗癌活性.
结论:
- 循环德克斯含有复杂化,特别是使用喷雾结干燥的M-β-CD,有效地提高了大麻素酸的溶解性,稳定性和生物活性.
- 这些优化的CD纳入复合体代表了在大麻衍生产品中配制脂性大麻素的有希望的策略.
- 改进的物理化学和生物特性表明了先进药物递送系统的潜力.
相关概念视频
Factors Influencing Drug Absorption: Physicochemical Parameters
297
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...
297
Factors Influencing Drug Absorption: Pharmaceutical Parameters
134
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...
134
Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry
208
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...
208
Biopharmaceutics and Pharmacokinetics: Overview
2.0K
Understanding drugs, drug products, and their performance in pharmaceutical science is pivotal. Drugs, whether simple molecules or complex compounds, are designed to interact with the body's biological systems to diagnose, treat, or prevent diseases. Drug products include various delivery systems such as tablets, capsules, injections, and inhalers. The performance of these drug products is gauged by their ability to deliver the active ingredient to the desired site of action at the...
2.0K
Chemotherapy-Induced Nausea and Vomiting: Cannabinoids
285
Tetrahydrocannabinol (THC) is a phytocannabinoid that primarily interacts with the CB1 receptor, a type of G protein-coupled receptor (GPCR) predominantly in and around the chemoreceptor trigger zone (CTZ) and emetic center. THC also blocks the serotonin receptor activity in the dorsal vagal complex (DVC) by inhibiting serotonin release. THC exerts its anti-emetic effects through these interactions, which are beneficial for patients undergoing chemotherapy.
Two synthetic agonists of THC,...
Two synthetic agonists of THC,...
285
CNS Stimulants: Cocaine, Amphetamines and Cannabinoids
203
CNS stimulants, such as cocaine, amphetamines, and cannabinoids, have varying structures and mechanisms of action that lead to different therapeutic effects and side effects. Cocaine, with its molecular formula C17H21NO4, is a tropane alkaloid and a tertiary amino compound. It has two chemical forms: the hydrochloride salt and the "freebase." The former is in powder form, while the latter involves removing the hydrochloride salt to create a form that can be smoked. Cocaine exerts its...
203


