Pereira Amélia Aparecida Rocca, Aparecida José Vitor Melchiades, Ramalho Maria Eduarda, Ferreira Leonardo Miziara Barboza, Gremião Maria Palmira Daflon
Faculty of Pharmaceutical Science, UNESP-São Paulo State University, Rodovia Araraquara-Jaú, Km 01, Araraquara 14801-902, Brazil.
Pharmaceutics. 2024 Nov 21;16(12):1489. doi: 10.3390/pharmaceutics16121489.
: This study evaluated how the relative proportion of chitosan (CS) to the polyanions alginate (ALG) and hydroxypropyl-methylcellulose phthalate (HP) affects the colloidal properties of mesalazine (MSZ) nanosuspensions as a strategy to produce particles with specific characteristics. : Nanosuspensions were prepared using a bottom-up approach based on acid-base reactions and were modified with CS in a binary mixture with ALG or a ternary mixture with ALG and HP. The particle size, polydispersity index (PDI), zeta potential, morphology, and drug association efficiency were analyzed. : Higher proportions of CS relative to the polyanions resulted in smaller, less polydisperse particles. The zeta potential inversion was influenced by the relative proportion of CS in the system. These results were consistent over 30 days and pH exerted an influence on the magnitude of the observed effect. The optimized NS modified with binary CS/ALG blends had the following properties at pH 6.0: an average particle size of 324.9 nm, PDI of 0.5, and zeta potential of +40.8 mV; at pH 4.0, it had an average particle size of 310.4 nm, PDI of 0.4, and zeta potential of +43.6 mV. The optimized NS modified with ternary CS/ALG/HP had the following properties at pH 6.0: an average particle size of 316.7 nm, PDI of 0.5, and zeta potential of +33.9 mV; at pH 4.0, it had an average particle size of 363.5 nm, PDI of 0.6, and zeta potential of +33.9 mV. : CS-based polyelectrolyte complexes with ALG and ALG/HP offer an approach to modulating the properties of MSZ nanosuspensions, enabling the production of particles with tailored characteristics.
本研究评估了壳聚糖(CS)与聚阴离子海藻酸盐(ALG)和邻苯二甲酸羟丙基甲基纤维素(HP)的相对比例如何影响美沙拉嗪(MSZ)纳米混悬液的胶体性质,以此作为制备具有特定特性颗粒的一种策略。采用基于酸碱反应的自下而上方法制备纳米混悬液,并用CS与ALG的二元混合物或与ALG和HP的三元混合物进行改性。分析了粒径、多分散指数(PDI)、zeta电位、形态和药物结合效率。相对于聚阴离子,较高比例的CS导致颗粒更小、多分散性更低。系统中CS的相对比例影响zeta电位反转。这些结果在30天内保持一致,pH对观察到的效应大小有影响。用二元CS/ALG共混物改性的优化纳米混悬液在pH 6.0时具有以下性质:平均粒径324.9 nm,PDI为0.5,zeta电位为+40.8 mV;在pH 4.0时,平均粒径310.4 nm,PDI为0.4,zeta电位为+43.6 mV。用三元CS/ALG/HP改性的优化纳米混悬液在pH 6.0时具有以下性质:平均粒径316.7 nm,PDI为0.5,zeta电位为+33.9 mV;在pH 4.0时,平均粒径363.5 nm,PDI为0.6,zeta电位为+33.9 mV。基于CS的与ALG和ALG/HP的聚电解质复合物为调节MSZ纳米混悬液的性质提供了一种方法,能够制备具有定制特性的颗粒。