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5-Fluorouracil-Loaded BSA Nanoparticles: Formulation Optimization and In Vitro Release Study

机译:5-氟尿嘧啶负载的BSA纳米颗粒:配方优化和体外释放研究

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摘要

Over the past few decades, there has been considerable interest in developing protein nanoparticles as drug delivery devices. The underlying rationale is their exceptional characteristics, namely biodegradability and nonantigenicity. Herein, phase separation method was used to prepare 5-fluorouracil-loaded bovine serum albumin (BSA) nanoparticles. Drug release was tracked by continuous flow dialysis technique. Effect of process variables on loading efficiency of 5-fluorouracil was investigated and optimized through Taguchi’s M16 design with the amount of entrapped drug as response. Optimum condition was found to be 2 mg/mL of 5-fluorouracil, 3.7 mL of added ethanol, 176 µL of glutaraldehyde, drug–protein incubation time of 30 min, and pH of 8.4 for 200 mg of BSA in 2 mL drug solution. pH had the most noticeable effect on the amount of entrapped drug, but glutaraldehyde had the least. Mean diameter and zeta potential of fabricated nanoparticles under these conditions were 210 nm and −31.7 mV, respectively. Drug-loaded BSA nanoparticles suspension maintained constant release of drug for 20 h under experimental conditions, so this colloidal drug carrier is capable of releasing drug in a sustained manner.
机译:在过去的几十年中,人们对开发蛋白质纳米颗粒作为药物递送装置有相当大的兴趣。其基本原理是其卓越的特性,即可生物降解性和非抗原性。在此,使用相分离法制备负载5-氟尿嘧啶的牛血清白蛋白(BSA)纳米颗粒。通过连续流透析技术追踪药物释放。通过Taguchi的M16设计,以截留药物的量为响应,研究并优化了工艺变量对5-氟尿嘧啶负载效率的影响。发现最佳条件是2 mg药物溶液中200 mg BSA的最佳条件是2 mg / mL的5-氟尿嘧啶,3.7 mL的添加乙醇,176μL的戊二醛,药物-蛋白温育时间为30分钟,pH值为8.4。 pH对截留药物的影响最明显,而戊二醛影响最小。在这些条件下,制成的纳米颗粒的平均直径和Zeta电位分别为210 nm和-31.7 mV。在实验条件下,载有药物的BSA纳米颗粒悬浮液在20小时内保持药物的恒定释放,因此这种胶体药物载体能够持续释放药物。

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