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首页> 外文期刊>Journal of Microencapsulation: Microcapsules Liposomes Nanoparticles Microcells Microspheres >High celecoxib-loaded nanoparticles prepared by a vibrating nozzle device
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High celecoxib-loaded nanoparticles prepared by a vibrating nozzle device

机译：通过振动喷嘴装置制备的载有高塞来昔布的纳米颗粒

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摘要

Drug delivery research has resulted in the availability of several enabling technologies for formulating poorly water-soluble compounds. In this study the vibrating nozzle device, originally used for encapsulation of drugs, cells and microorganisms, has been used to formulate nanoparticles (NP) with high loading capacity. Celecoxib was incorporated in NP of polylactic acid (PLA) and poly(lactic-co-glycolic acid) (PLGA) and the influence of polymers, initial drug:polymer ratio and stabilizer concentration on NP size and surface properties, entrapment efficiency, drug loading and in vitro release profile were investigated. NP were in the size range of 230-270 nm, with a polydispersity index less than 0.25 and a spherical shape. The highest celecoxib loading (13% w/w) was obtained at initial ratio celecoxib: Resomer RG 502 (PLA/PGA = 50/50) of 1:5 and 0.1 % w/w polyvinyl alcohol concentration. Thermal analysis and X-ray diffraction suggested that celecoxib was amorphous or molecularly dispersed in the polymeric matrix. The release profile exhibited an initial burst followed by sustained release. The freeze-dried NP could be completely dispersed on addition of lyoprotectants. The production of NP by the vibrating nozzle device is highly reproducible, time saving, can be performed under aseptic conditions and offers the possibility of scale-up.
机译：药物输送研究已导致可用于配制水溶性差的化合物的几种启用技术。在这项研究中，最初用于封装药物，细胞和微生物的振动喷嘴装置已用于配制具有高负载能力的纳米颗粒（NP）。塞来昔布被并入聚乳酸（PLA）和聚乳酸-乙醇酸共聚物（PLGA）的NP中，以及聚合物，初始药物：聚合物比率和稳定剂浓度对NP尺寸和表面性质，包封效率，载药量的影响和体外释放情况进行了调查。 NP的尺寸范围为230-270nm，多分散指数小于0.25且为球形。塞来昔布：Resomer RG 502（PLA / PGA = 50/50）的初始比例为1：5，聚乙烯醇浓度为0.1％w / w时，塞来昔布的最高负载量（13％w / w）获得了。热分析和X射线衍射表明塞来昔布是无定形的或分子分散在聚合物基质中。释放曲线表现出最初的爆发，随后是持续释放。加入冻干保护剂后，冻干的NP可以完全分散。通过振动喷嘴装置的NP的生产是高度可重复的，节省时间，可以在无菌条件下进行并且提供了放大的可能性。

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