甘油脂单油酸酯和甘油脂单硬脂酸酯的二元混合物，用于磁响应热响应局部药物递送系统。
Binary blend of glyceryl monooleate and glyceryl monostearate for magnetically induced thermo-responsive local drug delivery system.
机构信息
College of Pharmacy & Health Sciences, Drake University, Des Moines, Iowa, 50311, USA.
出版信息
Pharm Res. 2013 Dec;30(12):3214-24. doi: 10.1007/s11095-013-1230-1. Epub 2013 Oct 25.
PURPOSE
To develop a novel monoglycerides-based thermal-sensitive drug delivery system, specifically for local intracavitary chemotherapy.
METHODS
Lipid matrices containing mixtures of glyceryl monooleate (GMO) and glyceryl monostearate (GMS) were evaluated for their potential application as magnetically induced thermo-responsive local drug delivery systems using a poorly water-soluble model drug, nifedipine (NF). Oleic acid-modified iron oxide (OA-Fe3O4) nanoparticles were embedded into the GMO-GMS matrix for remote activation of the drug release using an alternating magnetic field (AMF).
RESULTS
The crystallization behavior of binary blends of GMO and GMS as characterized by DSC did show temperature dependent phase transition. GMO-GMS (75:25 wt%) blend showed a melting (T m ) and crystallization (T c ) points at 42°C and 37°C, respectively indicating the potential of the matrix to act as an 'on-demand' drug release. The matrix released only 35% of the loaded drug slowly in 10 days at 37°C whereas 96% release was obtained at 42°C. A concentration of 0.5% OA-Fe3O4 heated the matrix to 42.3 and 45.5°C within 5 min and 10 min of AMF exposure, respectively.
CONCLUSIONS
The in vitro NF release profiles form the monoglycerides matrix containing 0.5% OA-Fe3O4 nanoparticles after AMF activation confirmed the thermo-responsive nature of the matrix that could provide pulsatile drug release 'on-demand'.
目的
开发一种新型的基于单甘油脂的热敏药物传递系统，专门用于局部腔内化疗。
方法
评估含有甘油单油酸酯（GMO）和甘油单硬脂酸酯（GMS）混合物的脂质基质作为磁诱导热敏局部药物传递系统的潜在应用，使用一种难溶于水的模型药物硝苯地平（NF）。将油酸修饰的氧化铁（OA-Fe3O4）纳米粒子嵌入 GMO-GMS 基质中，以便通过交变磁场（AMF）远程激活药物释放。
结果
通过 DSC 对 GMO 和 GMS 的二元混合物的结晶行为进行了表征，结果表明其具有温度依赖性的相转变。GMO-GMS（75:25wt%）混合物在 42°C 和 37°C 处分别表现出熔融（Tm）和结晶（Tc）点，表明该基质具有作为“按需”药物释放的潜力。该基质在 37°C 下仅以缓慢的速度在 10 天内释放 35%的负载药物，而在 42°C 下则释放 96%的药物。浓度为 0.5%的 OA-Fe3O4 在 5 分钟和 10 分钟内分别将基质加热至 42.3°C 和 45.5°C。
结论
在 AMF 激活后，含有 0.5%OA-Fe3O4 纳米粒子的单甘油脂基质中的 NF 体外释放曲线证实了基质的热敏性质，这种性质可以按需提供脉冲式药物释放。
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