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藻类聚合物在两性霉素B纳米颗粒设计中的意义。

Significance of algal polymer in designing amphotericin B nanoparticles.

作者信息

Bhatia Saurabh, Kumar Vikash, Sharma Kiran, Nagpal Kalpana, Bera Tanmoy

机构信息

PDMCOP, Bahadurgarh, Haryana 124507, India.

Department of Pharmaceutical Sciences, Jamia Hamdard, New Delhi 110062, India.

出版信息

ScientificWorldJournal. 2014;2014:564573. doi: 10.1155/2014/564573. Epub 2014 Nov 12.

Abstract

Development of oral amphotericin B (AmB) loaded nanoparticles (NPs) demands a novel technique which reduces its toxicity and other associated problems. Packing of AmB in between two oppositely charged ions by polyelectrolyte complexation technique proved to be a successful strategy. We have developed a novel carrier system in form of polyelectrolyte complex of AmB by using chitosan (CS) and porphyran (POR) as two oppositely charged polymers with TPP as a crosslinking agent. Initially POR was isolated from Porphyra vietnamensis followed by the fact that its alkali induced safe reduction in molecular weight was achieved. Formulation was optimized using three-factor three-level (3(3)) central composite design. High concentration of POR in NPs was confirmed by sulfated polysaccharide (SP) assay. Degradation and dissolution studies suggested the stability of NPs over wide pH range. Hemolytic toxicity data suggested the safety of prepared formulation. In vivo and in vitro antifungal activity demonstrated the high antifungal potential of optimized formulation when compared with standard drug and marketed formulations. Throughout the study TPP addition did not cause any significant changes. Therefore, these experimental oral NPs may represent an interesting carrier system for the delivery of AmB.

摘要

口服两性霉素B(AmB)纳米颗粒(NPs)的研发需要一种能降低其毒性及其他相关问题的新技术。通过聚电解质络合技术将AmB包裹在两个带相反电荷的离子之间,已被证明是一种成功的策略。我们利用壳聚糖(CS)和紫菜聚糖(POR)作为两种带相反电荷的聚合物,并以三聚磷酸钠(TPP)作为交联剂,开发了一种新型的AmB聚电解质络合物载体系统。首先从越南紫菜中分离出POR,随后实现了其经碱诱导的分子量安全降低。使用三因素三水平(3(3))中心复合设计对配方进行了优化。通过硫酸化多糖(SP)测定法确认了纳米颗粒中POR的高浓度。降解和溶解研究表明纳米颗粒在较宽的pH范围内具有稳定性。溶血毒性数据表明所制备配方的安全性。体内和体外抗真菌活性表明,与标准药物和市售配方相比,优化后的配方具有较高的抗真菌潜力。在整个研究过程中,添加TPP未引起任何显著变化。因此,这些实验性口服纳米颗粒可能是一种用于递送AmB的有趣载体系统。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4636/4244925/dcd3a282339d/TSWJ2014-564573.001.jpg

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