壳聚糖季铵盐包裹甲状旁腺激素相关肽制备纳米缓释颗粒

摘要 背景：小范围研究显示，低剂量、间歇性应用甲状旁腺激素相关肽能有效治疗绝经后妇女骨质疏松症。但其存在着易变性、半衰期短、价格昂贵等缺陷，因此研制应用缓释系统控制甲状旁腺激素相关肽的释放速度，提高其生物利用效率极为必要。 目的：制备一种新型纳米载药颗粒，探讨其对甲状旁腺激素相关肽的包封及体外释放特性。 方法：采用离子交联法制备壳聚糖季铵盐纳米载药颗粒，用傅里叶红外光谱、透射电镜等进行表征，检测纳米颗粒的包封及体外释放特性。 结果与结论：在常温磁力搅拌条件下，当壳聚糖季铵盐与三聚磷酸钠投药量为5︰1~2︰1时可形成纳米颗粒，粒径100~ 180 nm，为规则球形，甲状旁腺激素相关肽投药质量浓度越高时包封率增大但载药量有所减少，体外PBS溶液中纳米载药颗粒表现出缓慢释放特性。 关键词：壳聚糖；壳聚糖季铵盐；纳米粒子；甲状旁腺激素相关肽；体外释放 doi:10.3969/j.issn.1673-8225.2011.03.019

Quaternary ammonium salt chitosan nanoparticles encapsulate parathyroid hormone-related peptide nanoparticles

Abstract BACKGROUND: Small-scale studies have shown that low-dose, intermittent application of parathyroid hormone related peptide can effectively treat osteoporosis in postmenopausal women. But it is disadvantageous due to prone to degrade, short half-life and expensive cost, therefore it is necessary to modulate the release speed of parathyroid hormone related peptide using controlled-release system and to improve the biological efficiency. OBJECTIVE: To prepare a novel nanoparticles for carrying drugs, and to investigate encapsulation efficiency and in vitro release characteristics of parathyroid hormone-related peptide. METHODS: Quaternary ammonium salt of chitosan nanoparticles were prepared based on ionic gelation, and the characteristics were observed by fourier transform infrared spectroscopy and transmission electron microscopy, and the encapsulation efficiency and release characteristics in vitro of the nanoparticles were determined. RESULTS AND CONCLUSION: Chitosan quaternary ammonium salt and sodium tripolyphosphate were mixed to form the nanoparticles when the quantity of chitosan quaternary ammonium salt and sodium tripolyphosphate was 5:1-2:1 under stirring at room temperature. The nanoparticles size was about 100-180 nm, regular sphere. With the increase of the parathyroid hormone-related peptide concentration, the drug encapsulation efficiency increased but the loading capacity reduced. The drug-loading nanoparticles showed slow release characteristics in PBS solution in vitro.