Student Research Committee, Faculty of Pharmacy, Mazandaran University of Medical Sciences, Sari, Iran.
Department of Pharmaceutics, Faculty of Pharmacy, Mazandaran University of Medical Sciences, Sari, Iran.
AAPS PharmSciTech. 2022 May 20;23(5):149. doi: 10.1208/s12249-022-02299-5.
The goal of this experimentation was to increase the cutaneous absorption of venlafaxine HCl (VFX) encapsulated in a niosome (venlasosme) produced by an ultrasonic approach. The impact of the cholesterol:surfactant (Chol:Surf) proportion was examined to modify the venlasosme properties. Photon correlation spectroscopy, powder X-ray diffraction (PXRD), SEM, DSC, and ATR-FTIR spectroscopy were utilized to investigate the solid-state and morphology of VFX in the venlasosme. The studies revealed that increasing the level of Chol in the venlasosme increased the size of the particles. Alterations in the Chol to surfactant ratios (when Chol decreased from 2.5 to 0%) caused the zeta potential enhancement from 7.37 ± 0.67 to 15.53 ± 1.47 mV. The venlasosme with the highest cholesterol concentration (2.5%) had the highest encapsulation efficiency (approximately 63%). PXRD results revealed that VFX in venlasosme was in the amorphous form. The levels of VFX in the cutaneous layers and the receiver compartment were higher for the venlasosme gel than for VFX simple gel in the cutaneous permeability study and showed no cutaneous irritancy in rats. Furthermore, the venlasosme gel demonstrated significant antinociceptive and anti-inflammatory responses when compared to the control groups (VFX simple gel and diclofenac gel). The topical administration of the venlasosme gel also considerably increased the tail-flick and hot-plate response time when compared to the VFX simple gel, control groups, and diclofenac gel (p < 0.05). These findings suggest that niosomes can improve VFX efficacy as an antinociceptive and anti-inflammatory substance by improving the medicaments delivery to the specified site.
本实验旨在提高包裹于超声法制备的尼森体中的盐酸文拉法辛（VFX）的经皮吸收。考察了胆固醇：表面活性剂（Chol:Surf）比例对改变尼森体性质的影响。利用光子相关光谱法、粉末 X 射线衍射（PXRD）、扫描电子显微镜（SEM）、差示扫描量热法（DSC）和衰减全反射傅里叶变换红外光谱（ATR-FTIR）研究了尼森体中 VFX 的固态和形态。研究表明，增加尼森体中 Chol 的含量会增加颗粒的粒径。改变 Chol 与表面活性剂的比例（Chol 从 2.5%降至 0%）会使 Zeta 电位从 7.37 ± 0.67 mV 增强至 15.53 ± 1.47 mV。胆固醇浓度最高（2.5%）的尼森体具有最高的包封效率（约 63%）。PXRD 结果表明，尼森体中的 VFX 处于无定形状态。在皮肤渗透研究中，与 VFX 简单凝胶相比，尼森体凝胶中 VFX 的皮肤层和接收室水平更高，且在大鼠中未表现出皮肤刺激性。此外，与对照组（VFX 简单凝胶和双氯芬酸钠凝胶）相比，尼森体凝胶表现出显著的镇痛和抗炎反应。与 VFX 简单凝胶、对照组和双氯芬酸钠凝胶相比，尼森体凝胶的局部给药还显著延长了尾巴摆动和热板的反应时间（p < 0.05）。这些发现表明，尼森体可以通过改善药物向指定部位的递送来提高 VFX 作为镇痛和抗炎物质的疗效。
