壳聚糖作为缓释纳米粒提高盐酸佐米曲坦的生物利用度和治疗效果的制备及评价

Wajid Ahmad, Jaza Quazi
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引用次数: 1

摘要

对壳聚糖进行疏水改性,合成了n -丁基壳聚糖(NBC)和n -月桂酰壳聚糖(NLC),并通过红外光谱、核磁共振、XRD对改性壳聚糖进行了表征,改性壳聚糖的取代度约为14%,溶解度变化较大。用离子化法和TPP交联进一步评价合成的n -酰基壳聚糖负载盐酸佐米曲坦作为纳米颗粒。负载盐酸佐米曲坦的纳米颗粒的平均粒径为150.7±3.3nm,载药量为24.80±1.1%,包封效率为54.96±3.8%,其zeta电位为正,与改性壳聚糖中酰基取代的体积增大直接相关,但zeta电位呈负相关。透射电镜和扫描电镜分析了纳米颗粒的球形结构。盐酸佐米曲坦在pH为1.2的盐酸缓冲液和pH为7.4的磷酸盐缓冲液中的体外释放表现出最符合Korsmeyer - peppas动力学的双相释放模式。羧化壳聚糖的缓释随酰基长度的增加而降低。本研究结果表明,疏水修饰的酰化壳聚糖可用于实现酰化修饰控制的缓释。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Formulation and Evaluation as Sustain Released Nanoparticles for Zolmitriptan Hydrochloride for the enhanced Bioavailability and Better Therapeutic Action by using Chitosan as a Permeation Enhancer
Chitosan was hydrophobically modified as N-Butyryl chitosan (NBC), N-Lauroyl chitosan (NLC) were synthesized and characterized by FTIR, NMR, XRD, modified chitosan were having about 14 % degree of substitution and varying solubility. Further evaluation of synthesized N-acyl chitosan to loaded Zolmitriptan HCl as nanoparticle by ionotropic method with cross linking by TPP. Average particle size, drug loading, entrapment efficiency and in-vitro mucoadhesion of Zolmitriptan HCl loaded nanoparticle was 150.7±3.3nm, 24.80±1.1% and 54.96±3.8% respectively, with positive zeta potential which were directly correlated with increases bulkiness of the acyl substitution in the modified chitosan except zeta potential was found inversely correlated. TEM and SEM imaging relieved spherical structure of nanoparticle. In vitro release of Zolmitriptan HCl in 1.2 pH HCl buffer and pH 7.4 phosphate buffer solutions showed biphasic release pattern best fitted with Korsmeyer’s-Peppas kinetics with fickian transport mechanism. Acylated chitosan showed sustained release reducing with increasing length of acyl group. Result of the present study showed that hydrophobically modified acylated chitosan can be useful for achieving sustained release controlled by acylation modification.
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