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目的为避免传统制备壳聚糖微球过程中使用对人体具有刺激性和毒性的酸性溶剂及醛类交联剂,提高制剂鼻腔给药的生物相容性,本实验采用水溶性羧化壳聚糖为药物载体材料,通过乳化溶剂挥干法制备鼻用微球。方法以佐米曲普坦为模型药物,考察处方工艺因素的改变对载佐米曲普坦的羧化壳聚糖微球特性的影响,并筛选出微球的最佳处方和制备工艺,进而对微球的收率、粒径、外观、载药量、包封率以及释放行为等进行评价。结果所得微球呈球形,表面光滑,流动性较好,粒径分布较为均匀,平均粒径为(21.4±10.1)μm,载药量为5.67%,包封率为62.4%,体外释放研究表明微球具有一定的缓释作用。结论乳化溶剂挥干法制备羧化壳聚糖鼻用微球是可行的,可避免酸性溶剂及醛类毒性交联剂的使用。
OBJECTIVE To prevent the traditional preparation of chitosan microspheres using acidic solvents and aldehydes cross-linking agents that are irritating and toxic to human body and improve the biocompatibility of the nasal preparation, the water-soluble carboxylated chitosan Sugar as the drug carrier material, prepared by emulsifying the solvent swing dry nasal microspheres. Methods Zolmitriptan was used as a model drug to investigate the influence of prescription factors on the properties of carboxymethyl chitosan microspheres containing zolmitriptan. The optimum prescription and preparation process of microspheres were screened out The microspheres yield, particle size, appearance, drug loading, encapsulation efficiency and release behavior were evaluated. Results The microspheres were spherical, smooth and fluid with good particle size distribution. The mean diameter was (21.4 ± 10.1) μm, the drug loading was 5.67% and the entrapment efficiency was 62.4% Microspheres have a sustained release effect. Conclusion It is feasible to prepare carboxylated chitosan nasal microspheres by emulsification solvent evaporation method, which can avoid the use of acidic solvents and aldehyde toxic cross-linking agents.