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Gelatin nanofiber assisted zero order release of Amphotericin-B: A study with realistic drug loading for oral formulation
Materials Today Communications ( IF 3.8 ) Pub Date : 2020-01-22 , DOI: 10.1016/j.mtcomm.2020.100953
Mrunalini Gaydhane , Pankaj Choubey , Chandra S. Sharma , Saptarshi Majumdar

Oral administration of Amphotericin B (AmB) is abstained due to its poor bioavailability and high toxicity. Current intravenous lipid formulations are delivered as 3−5 mg AmB/kg of body weight, due to its dose dependent nephrotoxicity. In this work, we engineer the electrospun gelatin nanofibers to enable their use for controlled release of AmB in the form of oral tablets while focusing on loading realistic drug doses of AmB as per the clinical guidelines for the treatment of Visceral Leishmaniasis. A detailed study is carried out to understand the effect of different crosslinking strategies, drug concentrations, compressive loading (to form tablets) and additional protective layer of sodium alginate on release kinetics. Based on the outcome of these studies, we developed a systematic protocol to achieve the controlled release and minimizing the frequency of dosing in order to attain less toxicity at realistic body pH condition. The swelling and enzymatic degradation studies further infer the realistic stability of the tablet and its correlation with the in-vitro release kinetics of drug.



中文翻译:

明胶纳米纤维辅助两性霉素B的零级释放:口服制剂中具有实际载药量的研究

由于两性霉素B(AmB)的生物利用度差和高毒性,因此无法口服。由于其剂量依赖性肾毒性,目前的静脉脂质制剂以3-5 mg AmB / kg体重的形式提供。在这项工作中,我们设计了电纺明胶纳米纤维,使其能够以口服片剂的形式用于AmB的控释,同时根据临床内脏利什曼病的临床指南,着重于加载实际剂量的AmB。进行了详细的研究,以了解不同的交联策略,药物浓度,压缩负荷(以形成片剂)和藻酸钠附加保护层对释放动力学的影响。根据这些研究的结果,我们开发了一种系统的方案,以实现控释并最小化给药频率,从而在实际的人体pH条件下获得较小的毒性。溶胀和酶降解研究进一步推断了片剂的实际稳定性及其与片剂的相关性。药物的体外释放动力学。

更新日期:2020-01-22
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