Department of Pharmaceutics, State Key Laboratory of Natural Medicines, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing 210009, China.
Department of Pharmaceutics, State Key Laboratory of Natural Medicines, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing 210009, China.
Eur J Pharm Biopharm. 2019 Apr;137:140-147. doi: 10.1016/j.ejpb.2019.02.021. Epub 2019 Feb 25.
The purpose of this study was to apply the phenomenon of liquid jet breakup to the preparation of sustained-release microspheres. The mechanisms of liquid jet breakup in different jet states were investigated and the single factor method was used to study the effect of each process parameter on the particle size and size distribution of microspheres. Meantime, the prepared microspheres were characterized by morphology, drug loading, encapsulation efficiency and in vitro release. The results indicated that the process of liquid jet breakup could have 5 different states. The laminar flow state dominated when the Reynolds number (Re) was low, and the prepared microspheres had larger particle sizes. When the Re was high, the turbulent state was dominant and the microspheres had smaller particle sizes. And during the transition state from the laminar flow to the turbulence, the microspheres had a wide particle size distribution. Different process parameters could affect the particle size and distribution of microspheres by changing the Re, surface tension coefficient and viscosity. The microspheres prepared by liquid jet breakup were smooth and round with the drug loading of 35% and the encapsulation efficiency of 88%. In addition, when the polymeric carrier materials were different, the microspheres could have various drug release models such as sustained release with a lag phase, sustained release with no lag phase, pulsed release and so on, which could be applied widespread in the future.
本研究旨在将液体射流分裂现象应用于缓释微球的制备中。研究了不同射流状态下液体射流分裂的机理，并采用单因素法研究了各工艺参数对微球粒径和粒径分布的影响。同时，对所制备的微球进行了形态、载药量、包封率和体外释放的表征。结果表明，液体射流分裂过程可分为 5 种不同状态。当雷诺数（Re）较低时，以层流状态为主，所制备的微球粒径较大。当 Re 较高时，以湍流状态为主，微球粒径较小。在从层流向湍流的过渡状态下，微球的粒径分布较宽。不同的工艺参数可以通过改变 Re、表面张力系数和粘度来影响微球的粒径和分布。通过液体射流分裂法制备的微球光滑圆润，载药量为 35%，包封率为 88%。此外，当聚合物载体材料不同时，微球可以具有不同的药物释放模型，如具有滞后期的持续释放、无滞后期的持续释放、脉冲释放等，这在未来具有广泛的应用前景。
