聚烯丙基胺盐酸盐纳米粒制备工艺的研究与制剂学的初步评价  

Preparation of poly(allylamine)hydrochloride nanoparticles and preliminary evaluation of pharmaceutics

作　　者：熊峰 苏峰 鲁胜男 曹俊如 储晓琴[1] 何广卫 XIONG Feng;SU Feng;LU Sheng-nan;CAO Jun-ru;CHU Xiao-qin;HE Guang-wei(Anhui University of Chinese Medicine,Hefei 230012;Hefei Industrial Pharmaceutical Institute Co.,Ltd.,Hefei 230088;China Pharmaceutical University,Nanjing 211198;Anhui Medical University,Hefei 230032)

机构地区：[1]安徽中医药大学,合肥230012 [2]合肥医工医药股份有限公司,合肥230088 [3]中国药科大学,南京211198 [4]安徽医科大学,合肥230032

出　　处：《中南药学》2022年第12期2804-2812,共9页Central South Pharmacy

摘　　要：目的以纳米粒粒径及粒度分布为主要考察指标研究聚烯丙基胺盐酸盐(PAH)纳米粒制备方法,并对制剂学进行初步评价。方法分别采用涡旋振荡法、微流控技术制备纳米粒,通过调节磷酸盐(PBS)的浓度、PBS种类、微流控各通道的流速比等优化纳米粒制备方法;马尔文粒度电位仪测定粒径、多分散系数(PDI)、Zeta电位,以姜黄素作为模型药物制备载药纳米粒,采用超速离心法分离载药纳米粒和游离药物,以紫外分光光度法测定载药纳米粒的包封率。结果采用微流控技术在PBS浓度为6 mmol·L^(-1),流速比为36∶8∶36条件下可获得较优粒径,其粒径为(127.7±1.92)nm,PDI为(0.126±0.00),Zeta电位为(28.4±1.02)mV,包封率为(85.1±0.09)%,载药量为(30.3±3.9)%。此外,PAH载药纳米粒具有缓释性能。结论微流控技术制备的PAH纳米粒工艺简便、参数可控,制备出的载药纳米粒粒径较小,粒度分布良好,具有优良的载药与包封特性。Objective To study the preparation of poly(allylamine)hydrochloride(PAH)nanoparticles with nanoparticle size and particle size distribution as the main indicators and to evaluate the pharmaceutics.Methods The nanoparticles were prepared by vortex oscillation and microfluidics respectively.The nanoparticles were optimized by adjusting the concentration and type of phosphate and the flow rate ratio of each channel of microfluidics.The particle size,polydispersity coefficient(PDI)and Zeta potential were determined by Malvern particle size potentiometry.Curcumin was used as a model drug to prepare drug-loaded nanoparticles.Drug-loaded nanoparticles and free drugs were separated by ultracentrifugation,and the encapsulation efficiency of drug-loaded nanoparticles was determined by UV spectrophotometry.Results A superior particle size of(127.7±1.92)nm,a PDI of(0.126±0.00),a Zeta potential of(28.4±1.02)mV,an encapsulation efficiency of(85.1±0.09)%and a drug loading capacity of(30.3±3.9)%were obtained with microfluidics at a PBS concentration of 6 mmol·L^(-1)and a flow rate ratio of 36∶8∶36.In addition,the PAH drug-loaded nanoparticles exhibited sustained release properties.Conclusion The PAH nanoparticles by microfluidics are simply prepared,with controllable parameters.The prepared drug-loaded nanoparticles have excellent drug loading,encapsulation properties,small particle size and good particle size distribution.

关 键 词：聚烯丙基胺盐酸盐 微流控 纳米粒 姜黄素 包封率 载药量 

分 类 号：R943[医药卫生—药剂学]