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用于关节腔内应用载有双氯芬酸钠的聚合物纳米颗粒的水凝胶制剂。

Hydrogel Formulation for Intra-Articular Application of Diclofenac Sodium-Loaded Polymeric Nanoparticles.

作者信息

Küçüktürkmen Berrin, Öz Umut Can, Bozkir Asuman

机构信息

Ankara University, Faculty Of Pharmacy, Department Of Pharmaceutical Technology, Ankara, Turkey.

出版信息

Turk J Pharm Sci. 2017 Apr;14(1):56-64. doi: 10.4274/tjps.84803. Epub 2017 Apr 15.

Abstract

OBJECTIVES

The world's population is getting older and the number of people suffering from arthritis is a major problem according to World Health Organization's data. In this respect, the need for more efficient treatment for arthritis becomes an urgent issue. In this research, nanoparticle bearing in situ gelling hydrogel formulation was developed for prolonged local delivery of diclofenac sodium (DS).

MATERIALS AND METHODS

Emulsion-solvent evaporation technique was used for the preparation of nanoparticles. Particle size, encapsulation efficiency, morphology, and drug release profile of DS loaded biodegradable nanoparticles as well as gel viscosity and gelation time of gelling hydrogel formulations were optimized to increase the time interval between each dose application for enhanced patience compliance.

RESULTS

The spherical nanoparticles with a mean particle diameter of 168 nm was obtained and confirmed by both transmission electron microscope and atomic force microscope. Different types of surfactants were tested in the first emulsification step of nanoparticle production process and Arlacel-C significantly increased the encapsulation efficiency to 89.7%. Thirty days prolonged release of DS was achieved by using the combined formulation of polymeric nanoparticles and hydrogel prepared by using poloxomer 407 and chitosan.

CONCLUSION

Local administration of DS with this novel delivery system could be considered of having potential to minimize side effects associated with decreased amount of drug in dosage form compared to conventional oral dose.

摘要

目的

根据世界卫生组织的数据,全球人口正在老龄化,患有关节炎的人数是一个重大问题。在这方面,对关节炎更有效治疗方法的需求成为一个紧迫问题。在本研究中,开发了负载纳米颗粒的原位凝胶化水凝胶制剂,用于双氯芬酸钠(DS)的延长局部递送。

材料与方法

采用乳液-溶剂蒸发技术制备纳米颗粒。对负载DS的可生物降解纳米颗粒的粒径、包封率、形态和药物释放曲线以及凝胶化水凝胶制剂的凝胶粘度和凝胶化时间进行了优化,以增加每次给药之间的时间间隔,提高患者依从性。

结果

通过透射电子显微镜和原子力显微镜获得并确认了平均粒径为168nm的球形纳米颗粒。在纳米颗粒生产过程的第一次乳化步骤中测试了不同类型的表面活性剂,Arlacel-C显著提高了包封率至89.7%。通过使用由泊洛沙姆407和壳聚糖制备的聚合物纳米颗粒和水凝胶的组合制剂,实现了DS的30天延长释放。

结论

与传统口服剂量相比,使用这种新型给药系统局部给药DS有可能将与剂型中药物量减少相关的副作用降至最低。

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