超声波增强了黄素的生物可访问性和药理作用,在包括复合物中
Matheus X Oliveira1, Irisvan S Ribeiro2, Francisca Vanessa C Canafístula2
1Department of Organic and Inorganic Chemistry, Polymer Laboratory, Federal University of Ceará, UFC, Fortaleza, CE, Brazil; Department of Chemistry, Polymer Transport Phenomena Laboratory, University of Coimbra, U.C, Coimbra, Portugal.
通过超声波辅助的黄素与氧-β-环氧 (HP-β-CD) 的复合显著增强了黄素.
科学领域:
- 材料科学 材料科学 材料科学
- 制药技术 制药技术 制药技术
- 纳米技术 纳米技术
背景情况:
- 黄素具有较差的水溶性和较低的口服生物可用性,限制了其治疗应用.
- 环氧,特别是基-β-环氧 (HP-β-CD),被广泛用于改善难溶性药物的物理化学特性.
- 开发有效的黄素-HP-β-CD复合方法对于提高其输送和有效性至关重要.
研究的目的:
- 开发一种优化的方法,利用超声波辅助溶剂蒸发,与HP-β-CD复合黄素.
- 评估超声波参数对黄素-HP-β-CD复合物的复合效率和特征的影响.
- 评估优化复合物的增强性质,包括可溶性,稳定性,生物可访问性和生物活动.
主要方法:
- 库尔库-HP-β-CD复合物是使用溶剂蒸发与不同超声波时间 (5-15分钟) 结合使用的.
- 为了进行比较,在没有超声波的情况下准备了一个控制复合体.
- 描述包括产量,封装效率,载荷能力,颗粒大小分析,溶解度的确定,以及抗氧化剂,细胞相容性,抗菌性和生物可访问性属性的评估.
主要成果:
- 与非超声波控制相比,超声波显著提高了复合产量,封装效率和负载能力.
- 通过10分钟的超声波 (HP-CD/Cur10) 实现了最佳结果,产生了最高的封装效率,黄素加载,最小的颗粒大小和减少的黄素自氧化.
- HP-CD/Cur10的水溶性增加了360倍以上,增强了对MRSA的抗氧化和抗菌活性,改善了细胞相容性和优越的黄素生物可访问性.
- 在1:1 (mol/mol) 的HP-β-CD与黄素比率下,实现了高封装效率,减少了所需的环极素量.
结论:
- 超声辅助复合是一种有效和高效的方法,用于制备黄素-HP-β-CD复合物.
- 优化的HP-CD/Cur10配方显著克服了自由黄素的局限性,提供了更好的溶解性,稳定性和生物可用性.
- 这种先进的输送系统对制药和食品应用具有相当大的前景,可以方便口服黄素的使用.
更多相关视频
05:08Solubility of Hydrophobic Compounds in Aqueous Solution Using Combinations of Self-assembling Peptide and Amino Acid
Published on: September 20, 2017
08:39Magnetic and Thermal-sensitive PolyN-isopropylacrylamide-based Microgels for Magnetically Triggered Controlled Release
Published on: July 4, 2017
相关概念视频
Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry
Factors Influencing Drug Absorption: Physicochemical Parameters
Enhanced drug absorption can be achieved by reducing particle sizes and increasing surface areas, thereby facilitating...
Factors Influencing Bioavailability: First-Pass Elimination
Factors Influencing Drug Absorption: Pharmaceutical Parameters
Methods for Studying Drug Absorption: In situ
The Doluisio method involves perfusing a prepared segment of a rat's small intestine with a solution of radiolabeled drug and a non-absorbable marker. This helps to differentiate between absorbed and non-absorbed drug concentrations. The intestinal segment is connected at both ends using tubing and syringes,...
Methods for Studying Drug Absorption: In vitro
The diffusion cell method uses a two-compartment cell, including a donor compartment with the drug solution, which simulates the environment where the drug is applied, and a receptor compartment with a buffer solution, which simulates the environment...
