Department of Drug Sciences, University of Pavia, Italy.
J Microencapsul. 2013;30(6):559-70. doi: 10.3109/02652048.2013.764938. Epub 2013 Apr 9.
The goal of the present work was to evaluate and discuss vibration nozzle microencapsulation (VNM) technology combined to lyophilization, for the microencapsulation of a hydrophilic model molecule into a hydrophilic polymer.
Fluorescein-loaded alginate microparticles prepared by VNM and emulsion phase inversion microencapsulation (EPIM) were lyophilized. Morphology, particle size distribution, lyophilized microspheres stability upon rehydration, drug loading and in vitro release were evaluated.
Well-formed microspheres were obtained by the VNM technique, with higher yields of production (93.3-100%) and smaller particle size (d50138.10-158.00) than the EPIM microspheres. Rehydration upon lyophilization occurred in 30 min maintaining microsphere physical integrity. Fluorescein release was always faster from the microspheres obtained by VNM (364 h) than from those obtained by EPIM (504 h).
The results suggest that VNM is a simple, easy to be scaled-up process suitable for the microencapsulation hydrophilic drugs.
本工作的目的是评估和讨论振动喷嘴微囊化(VNM)技术与冷冻干燥相结合,用于将亲水性模型分子包封到亲水性聚合物中。
通过 VNM 和乳液相转化微囊化(EPIM)制备载有荧光素的海藻酸钠微球,进行冷冻干燥。评估形态、粒径分布、复水时的冻干微球稳定性、载药量和体外释放。
通过 VNM 技术获得了形态良好的微球,具有更高的产率(93.3-100%)和更小的粒径(d50138.10-158.00)比 EPIM 微球。冷冻干燥后的复水在 30 分钟内完成,保持了微球的物理完整性。通过 VNM 获得的微球的荧光素释放始终比通过 EPIM 获得的微球快(364 h 比 504 h)。
结果表明,VNM 是一种简单、易于放大的适用于亲水性药物微囊化的方法。