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Fabrication and process investigation of vancomycin loaded silica xerogel/polymer core-shell composite nanoparticles for drug delivery

机译:载有万古霉素的硅胶干凝胶/聚合物核壳复合纳米粒子的制备及工艺研究

摘要

Biodegradable polymer-inorganic composites particles can provide significant advantages while avoiding the shortcomings of using polymer or inorganic particles alone as drug delivery vehicles. Most of the existing fabrication methods for polymer nanoparticles and silica xerogel nanoparticles are not applicable for composite nanoparticles. To overcome these difficulties, a novel gelation-emulsion method was successfully developed through the integration of sol-gel and modified double emulsion processes, in which gelation of the silica solution was enabled in nanodroplets generated in the modified emulsion process. Spherical vancomycin loaded silica xerogel/polymer core-shell composite nanoparticles with a tunable size and good drug encapsulation efficiency were fabricated through this novel method. By changing the process variables of the modified double emulsion process in terms of the second sonication time and PVA concentration, the average diameter of the composite nanoparticles could be adjusted in the range of 192-569 nm, with a maximum encapsulation efficiency up to 82.2%. With the introduction of silica xerogel as the primary core material by the sol-gel process, the prepared composite nanoparticles exhibited a higher encapsulation efficiency, lower burst drug release and longer drug complete release time than the polymer nanoparticles by 110%, 37.5% and 230%, respectively, enabling these composite nanoparticles to be better candidates for long-term sustained drug release applications. Formation mechanisms of the composite nanoparticles with respect to the second sonication time and PVA concentration were also discussed.
机译:可生物降解的聚合物-无机复合材料颗粒可提供显着的优势,同时避免了单独使用聚合物或无机颗粒作为药物输送载体的缺点。现有的用于聚合物纳米颗粒和二氧化硅干凝胶纳米颗粒的大多数制造方法不适用于复合纳米颗粒。为了克服这些困难,通过将溶胶-凝胶与改性双乳化工艺相结合,成功开发了一种新型的凝胶-乳化方法,其中在改性乳化工艺中产生的纳米液滴中能够使二氧化硅溶液发生凝胶化。通过这种新颖的方法,制备了球形可可霉素负载的二氧化硅干凝胶/聚合物核-壳复合纳米粒子,具有可调的尺寸和良好的药物包封效率。通过根据第二次超声处理时间和PVA浓度改变改性双乳液工艺的工艺变量,可以将复合纳米颗粒的平均直径调节在192-569 nm范围内,最大包封效率高达82.2% 。通过溶胶-凝胶工艺引入二氧化硅干凝胶作为主要核心材料,所制备的复合纳米颗粒与聚合物纳米颗粒相比,具有更高的包封效率,更低的突释药物释放和更长的药物完全释放时间,分别为110%,37.5%和230分别使这些复合纳米颗粒成为长期持续药物释放应用的更好候选者。还讨论了复合纳米粒子相对于第二次超声处理时间和PVA浓度的形成机理。

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