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【答案】应助回帖
(3) 考察不同PH值(PH=4.3、PH=5.6和PH=7.4)、不同载药率(9.53%、17.48%和26.37%)以及偶联配体对纳米粒释药性能的影响,并模拟人体内部环境进行释药行为的研究,分析每个阶段的释药机理,拟合五种常见药物模型的曲线方程并选择最佳释药模型。
(3) the influence of pH values (pH = 4.3, 5.6 and 7.4), drug loading rates (9.53%, 17.48%, and 26.37%), and the of coupling ligands on the drug release properties of nanoparticles were studied, and the internal environment release behavior of body was simulated, the release mechanism in different stage was analysed, the best drug delivery model was selected through fitting the curve equation model of five kinds of common drugs.
实验结果:(1)通过单因素考察和正交试验设计确定了制备三种载药纳米粒的最佳制备工艺,在最佳制备条件下制得的载药纳米粒载药率和包封率分别为26.9%,66.5%;27.4%,67.2%和30.3%,73.6%。纳米粒表面光滑圆整、分散性好,平均粒径分别为110nm、117nm和125nm,且粒径分布范围较窄;
Results: (1) the best fabrication process of three kinds of drug-loaded nanoparticles were determined through the investigation of single factor and orthogonal design, drug loading rates of the three kinds of drug-loaded nanoparticles obtained in the optimal preparation process were 26.9%, 27.4%, and 30.3%, respectively, while the encapsulation efficiency of that were 66.5%, 67.2%, and 73.6%. The average diameter of obtained nanoparticles were 110nm, 117nm, and 125 nm, respectively, with smooth and rounded morphology, good dispersion, and narrow particle size distribution.
(2) 用红外光谱(IR)表征纳米粒表面分子基团的变化,表明FA和HA分别通过酰胺键作用成功的偶联到了纳米粒表面。确定了FA和HA的最佳偶联工艺,在最佳偶联反应条件下FA和HA的偶联量分别为0.0237×10-3mol/g和0.0178×10-6mol/g。粒径分析表明FA偶联前后纳米粒粒径基本无变化,HA(Mr=300000)偶联后粒径由122.2nm增长到131.3nm,表明大分子量的HA对粒径变化影响较大。通过放大不同倍数的SEM照片可看出配体偶联后纳米粒分布均匀,分散性较好;
The change of molecular groups on nanoparticle surface were characterized by infrared spectroscopy (IR), the study results indicated that HA and FA groups were successfully coupled to the nanoparticles with the amide bonds. The coupling amount of FA and HA under the optimal process, which was decided in our experiment, were 0.0237 × 10-3mol/g and 0.0178 × 10 6 mol/g. The results of particle size analysis showed that the size of nanoparticles were same before and after the FA coupling, while the particles size increased from 122.2nm to 131.3nm with the HA(Mr=300000) coupling, which indicated that the high molecular weight HA has a great impact on particle size. The SEM photographs with different magnification showed the uniform distribution and good dispersion of ligand coupled nanoparticle
(3)纳米粒释药速率和累积释药量顺序为PH=4.3>PH=5.6>PH=7.4,且在一定PH范围内酸性越强释药速率和累计释放量越高,高载药率纳米粒在相同环境下的释药速率高于中、低载药率纳米粒,FA偶联后对纳米粒释药性能基本无影响,大分子的HA偶联到纳米粒表面后释药速率明显降低。靶向PLA载药纳米粒模拟体内环境释药表现出良好的缓释效果,拟合的FA/HA-PLA载药纳米粒的释药模型分别为InIn(1/(1-Q))=0.04633Int-1.03562和1-Q1/3=-0.01368t+1.04726。
Drug release rate and the cumulative amount of drug release of nanoparticles decreased with the increasing pH values(4.3, 5.6, and 7.4), and the stronger acidity within a certain pH range leads to a higher release rate and cumulative release, release rate of high drug loading nanoparticles is higher than that in middle and low drug loading nanoparticles in the same conditions, the influence of FA coupling on the drug release properties of nanoparticles was little, drug release rate was significantly reduced after macromolecular HA coupled to the surface of the nanoparticles. targeting PLA drug-loaded nanoparticles exhibited good controlled-release effect in simulated environment of body, the fitted FA and HA-PLA drug release model of the drug-loaded nanoparticles were ININ (1 / (1-Q)) = 0.04633 Int-1.03562 and 1-Q1 / 3 =-0.01368t +1.04726, respectively. |
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