基于壳聚糖的胡桃醌纳米载药体系的构建及性能评价
Construction and Performance Evaluation of Juglone Nano Drug Delivery System Based on Chitosan

本实验拟构建基于壳聚糖的胡桃醌纳米载药体系并进行制备工艺优化。以胡桃醌的载药量和包封率为评价指标，采用不同的配比、pH值和醋酸浓度作为单因素实验的考察因素，分析不同水平的试验因素对胡桃醌纳米载体载药量和包封率的影响，依此来确定试验因素的重要程度和水平的设置梯度；以响应面试验优化胡桃醌纳米载体的制备工艺，采用紫外可见分光光度计(UV-vis)、扫描电镜(SEM)评价胡桃醌纳米载药体系的结构性能。结果表明，当TPP:Cts = 1:5，醋酸浓度 = 2%，pH = 7，Jug:Cts = 1:5时，胡桃醌纳米载药体系的载药量和包封率最佳，其中载药量最高可达到12.8%，包封率可达到87.9%。以此条件制备的Jug-Cts-NPs纳米载体呈海绵状，孔道分布密集，有利于药物的吸附载带，具有较好的外观形态，且48 h内累积释放量最高达79.1%，具有较好的体外释放性能。
In this study, a Juglone nano drug delivery system based on Chitosan was constructed and the preparation process was optimized. The dose ratio of TPP:Cts and Jug:Cts, pH value and acetate concentration were used as the investigation factors of single factor experiment to analyze the influence of different levels of experimental factors on the drug-loading rate and encapsulation rate of Juglone nanoloaded microspheres. Based on this, the importance degree of experimental factors and the setting gradient of the level were determined to optimize the preparation process of the Juglone nanocarrier by Box-behnken Design. Ultraviolet-visible spectrophotometer (UV-Vis) and scanning electron microscope (SEM) were used to evaluate the structure and properties of the Juglone nano-carrier system. According to the analysis of the overall experimental study, when TPP:Cts = 1:5, acetate concentration = 2%, pH = 7, Jug:Cts = 1:5, the drug loading capacity and encapsulation rate of Juglone nano drug delivery system are the best, in which the maximum drug-loading rate could reach 12.8% and encapsulation rate could reach 87.9%. The conditions were spongy with dense pore distribution, which was favorable for the adsorption of drugs. The microspheres had good appearance and shape, and the highest cumulative release within 48 h reached 79.1%, which showed good in vitro release performance.