Process Evaluation of Sugar-Based Polymeric Colloidal Nanocarrier Formation

Abstract Several studies have demonstrated that sugar-based nanocarriers are recommended to develop drug delivery systems since they are biocompatible and biodegradable and might improve the therapeutic index of currently used drugs by reducing their toxicity and enhancing their bioavailability. Therewith, this work studied the processing conditions to formation of a sugar-based nanocarrier denominated polymeric colloidal nanocarriers (PCN). It reports the impact of emulsifiers types and concentration, salt concentration and copolymers addition on physical stability and particle size distribution of a maltodextin-based PCN. In order to define the most stable formulation to produce the maltodextrin nanocarriers, 13 PCN formulations were evaluated in respect to kinetic stability, particle size distribution and morphology. The results demonstrated that to have a stable sugar-based PCN in silicone for at least 3 days, it is necessary to work with Poloxamer 188 as a copolymer, SF 1540 surfactant in a concentration proportional to the solid content and a salt concentration of 0.4 %.摘要 已有多项研究表明，糖类基纳米载体（sugar-based nanocarriers）因具备良好的生物相容性与生物可降解性，且可通过降低现有药物的毒性、提升其生物利用度来改善药物治疗指数，因此被推荐用于开发药物递送系统。据此，本研究针对一种命名为聚合物胶体纳米载体（polymeric colloidal nanocarriers，PCN）的糖类基纳米载体的制备工艺条件展开了探究。本研究探讨了乳化剂种类与浓度、盐浓度以及共聚物添加量对麦芽糖糊精基聚合物胶体纳米载体的物理稳定性与粒径分布的影响。为确定制备麦芽糖糊精基纳米载体的最优稳定配方，本研究针对13组聚合物胶体纳米载体配方的动力学稳定性、粒径分布与形貌进行了评估。研究结果表明，若要使糖类基聚合物胶体纳米载体在有机硅介质中至少稳定保存3天，需采用泊洛沙姆188（Poloxamer 188）作为共聚单体、以与固含量成比例的浓度添加SF 1540表面活性剂，并将盐浓度控制为0.4%。