Fernández-Urrusuno R, Calvo P, Remuñán-López C, Vila-Jato J L, Alonso M J
Department Pharmaceutical Technology, School of Pharmacy, Santiago de Compostela, Spain.
Pharm Res. 1999 Oct;16(10):1576-81. doi: 10.1023/a:1018908705446.
To investigate the potential of chitosan nanoparticles as a system for improving the systemic absorption of insulin following nasal instillation.
Insulin-loaded chitosan nanoparticles were prepared by ionotropic gelation of chitosan with tripolyphosphate anions. They were characterized for their size and zeta potential by photon correlation spectroscopy and laser Doppler anemometry, respectively. Insulin loading and release was determined by the microBCA protein assay. The ability of chitosan nanoparticles to enhance the nasal absorption of insulin was investigated in a conscious rabbit model by monitoring the plasma glucose levels.
Chitosan nanoparticles had a size in the range of 300-400 nm, a positive surface charge and their insulin loading can be modulated reaching values up to 55% [insulin/nanoparticles (w/w): 55/100]. Insulin association was found to be highly mediated by an ionic interaction mechanism and its release in vitro occurred rapidly in sink conditions. Chitosan nanoparticles enhanced the nasal absorption of insulin to a greater extent than an aqueous solution of chitosan. The amount and molecular weight of chitosan did not have a significant effect on insulin response.
Chitosan nanoparticles are efficient vehicles for the transport of insulin through the nasal mucosa.
研究壳聚糖纳米粒作为一种改善滴鼻后胰岛素全身吸收的系统的潜力。
通过壳聚糖与三聚磷酸阴离子的离子凝胶化制备负载胰岛素的壳聚糖纳米粒。分别用光子相关光谱法和激光多普勒测速法对其大小和zeta电位进行表征。通过微量BCA蛋白测定法测定胰岛素的负载量和释放量。通过监测清醒兔模型中的血浆葡萄糖水平，研究壳聚糖纳米粒增强胰岛素鼻腔吸收的能力。
壳聚糖纳米粒大小在300 - 400 nm范围内，表面带正电荷，其胰岛素负载量可调节，最高可达55%[胰岛素/纳米粒（重量/重量）：55/100]。发现胰岛素结合主要由离子相互作用机制介导，其在体外的释放于漏槽条件下迅速发生。壳聚糖纳米粒比壳聚糖水溶液更能增强胰岛素的鼻腔吸收。壳聚糖的量和分子量对胰岛素反应没有显著影响。
壳聚糖纳米粒是胰岛素通过鼻黏膜转运的有效载体。
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