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Recuperating Biopharmaceutical Aspects of Amphotericin B and Paromomycin Using a Chitosan Functionalized Nanocarrier via Oral Route for Enhanced Anti-leishmanial Activity
Frontiers in Cellular and Infection Microbiology ( IF 5.7 ) Pub Date : 2020-09-09 , DOI: 10.3389/fcimb.2020.570573
Shabi Parvez 1 , Ganesh Yadagiri 1 , Archana Karole 1 , Om Prakash Singh 2 , Anurag Verma 3, 4 , Shyam Sundar 5 , Shyam Lal Mudavath 1
Affiliation  

The design and development of new pharmaceutical formulations for the existing anti-leishmanial is a new strategic alternate to improve efficacy and safety rather than new drug discovery. Herein hybrid solid lipid nanoparticles (SLN) have been engineered to direct the oral delivery of two anti-leishmanial drugs amphotericin B (AmB) and paromomycin (PM). The combinatorial nanocarriers consist of conventional SLN, antileishmanial drugs (AmB and PM) which have been functionalized with chitosan (Cs) grafted onto the external surface. The Cs-SLN have the mean particle size of 373.9 ± 1.41 nm, polydispersity index (PDI) of 0.342 ± 0.02 and the entrapment efficiency for AmB and PM was found to be 95.20 ± 3.19% and 89.45 ± 6.86 %, respectively. Characterization of SLN was performed by scanning electron microscopy and transmission electron microscopy. Complete internalization of the formulation was observed in Caco-2 cells. Cs-SLN has shown a controlled and slow drug release profile over a period of 72 h and was stable at gastrointestinal fluids, confirmed by simulated gastro-intestinal fluids study. Cs coating enhanced the mucoadhesive property of Cs-SLN. The in-vitro anti-leishmanial activity of Cs-SLN (1 μg/ml) has shown a maximum percentage of inhibition (92.35%) on intra-cellular amastigote growth of L. donovani.



中文翻译:

使用壳聚糖功能化的纳米载体通过口服途径恢复两性霉素B和巴龙霉素的生物制药方面,以增强抗利什曼活性

针对现有抗利什曼病毒药物的新药物制剂的设计和开发是提高功效和安全性的新战略替代方案,而不是新药开发。在本文中,已经设计了杂合固体脂质纳米颗粒(SLN)以指导两种抗利什曼病药物两性霉素B(AmB)和巴龙霉素(PM)的口服递送。组合的纳米载体由常规的SLN,抗疟疾药物(AmB和PM)组成,它们已经用接枝到外表面的壳聚糖(Cs)进行了功能化。Cs-SLN的平均粒径为373.9±1.41 nm,多分散指数(PDI)为0.342±0.02,AmB和PM的包封率分别为95.20±3.19%和89.45±6.86%。SLN的表征通过扫描电子显微镜和透射电子显微镜进行。在Caco-2细胞中观察到制剂完全内在化。通过模拟胃肠液研究证实,Cs-SLN在72小时内显示出受控且缓慢的药物释放曲线,并且在胃肠液中稳定。Cs涂层增强了Cs-SLN的粘膜粘附性能。体外 Cs-SLN的抗Leishmanial活性(1μg/ ml)已显示出最大抑制百分比(92.35%)对胞内鞭毛虫生长的抑制 多诺尼

更新日期:2020-10-16
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