Chen Fu, Zhang Zhi-Rong, Huang Yuan
Key Laboratory of Drug Targeting of Ministry of Education, West China School of Pharmacy, Sichuan University, No. 17, Block 3, Southern Renmin Road, Chengdu 610041, PR China.
Int J Pharm. 2007 May 4;336(1):166-73. doi: 10.1016/j.ijpharm.2006.11.027. Epub 2006 Nov 12.
N-Trimethyl chitosan chloride (TMC) nanoparticles were prepared by ionic crosslinking of TMC with tripolyphosphate (TPP). Two model proteins with different pI values, bovine serum albumin (BSA, pI=4.8) and bovine hemoglobin (BHb, pI=6.8), were used to investigate the loading and release features of the TMC nanoparticles. TMC samples with different degrees of quaternization were synthesized to evaluate its influence on the physicochemical properties and release profiles of the nanoparticles. Sodium alginate was used to modify the TMC nanoparticles to reduce burst release. The results indicated that the TMC nanoparticles had a high loading efficiency (95%) for BSA but a low one (30%) for BHb. The particle size and zeta potential were significantly affected by the BSA concentration but not by the BHb concentration. Nanoparticles of TMC with a lower degree of quaternization showed an increase in particle size, a decrease in zeta potential and a slower drug-release profile. As for the alginate-modified nanoparticles, a smaller size and lower zeta potential were observed and the burst release of BSA was reduced. These studies demonstrated that TMC nanoparticles are potential protein carriers, and that their physicochemical properties and release profile could be optimized by means of various modifications.
通过氯化N-三甲基壳聚糖(TMC)与三聚磷酸钠(TPP)进行离子交联制备了TMC纳米颗粒。使用两种具有不同pI值的模型蛋白,即牛血清白蛋白(BSA,pI = 4.8)和牛血红蛋白(BHb,pI = 6.8),来研究TMC纳米颗粒的负载和释放特性。合成了具有不同季铵化程度的TMC样品,以评估其对纳米颗粒理化性质和释放曲线的影响。使用海藻酸钠对TMC纳米颗粒进行改性以减少突释。结果表明,TMC纳米颗粒对BSA具有较高的负载效率(95%),但对BHb的负载效率较低(30%)。粒径和zeta电位受BSA浓度的显著影响,但不受BHb浓度的影响。季铵化程度较低的TMC纳米颗粒粒径增大,zeta电位降低,药物释放曲线较慢。对于海藻酸钠改性的纳米颗粒,观察到粒径较小且zeta电位较低,并且BSA的突释减少。这些研究表明,TMC纳米颗粒是潜在的蛋白质载体,并且可以通过各种改性方法优化其理化性质和释放曲线。