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Chitosan-coated nanostructured lipid carriers of fenofibrate with enhanced oral bioavailability and efficacy.
Colloids and Surfaces B: Biointerfaces ( IF 5.8 ) Pub Date : 2020-08-26 , DOI: 10.1016/j.colsurfb.2020.111331
Yong-Chul Pyo 1 , Phuong Tran 1 , Dong-Hyun Kim 1 , Jeong-Sook Park 1
Affiliation  

Fenofibrate is frequently used to lower cholesterol levels in cardiovascular disease. Owing to its poor solubility and high gastrointestinal permeability, it is classified as a Biopharmaceutics Classification System class II compound. The aim of this study was to improve the solubility and bioavailability of fenofibrate by formulating it as fenofibrate-loaded nanostructured lipid carriers (FFB-NLCs) and coating it with a biodegradable polymer to allow controlled drug release. Chitosan-coated nanostructured lipid carriers (CF-NLCs) were prepared via an ultrasonication method using chitosan as the biodegradable polymer, stearic acid as the solid lipid, oleic acid as the liquid lipid, and Tween 80 as the surfactant. To study encapsulation efficiency and solubility conditions, stearic acid/oleic acid ratios were varied as 80/20, 70/30, 60/40, and 50/50 (mg/mg), by adjusting chitosan ratio. Chitosan is an adhesive polymer, coating the surface of the NLC to improve its bioavailability. All NLC formulations demonstrated a particle size of approximately 200 nm and a polydispersity index below 0.3. The encapsulation efficiencies of the NLC formulations were above 85%. For CF-NLCs, the solubility and encapsulation efficiency of fenofibrate were increased when compared with those of a commercial fenofibrate formulation. The pharmacokinetic and pharmacodynamic parameters of fenofibrate in the form of CF-NLCs were improved after oral administration. CF-NLCs can be used for allowing controlled release and improving the bioavailability and stability of fenofibrate.



中文翻译:

非诺贝特的壳聚糖涂层纳米结构脂质载体具有增强的口服生物利用度和功效。

非诺贝特常用于降低心血管疾病中的胆固醇水平。由于其较差的溶解度和较高的胃肠道通透性,它被归类为生物制药分类系统II类化合物。这项研究的目的是通过将非诺贝特配制为载有非诺贝特的纳米结构脂质载体(FFB-NLC)并用可生物降解的聚合物包衣以控制药物释放,从而提高非诺贝特的溶解度和生物利用度。通过壳聚糖作为生物可降解聚合物,硬脂酸作为固体脂质,油酸作为液体脂质,吐温80作为表面活性剂,通过超声方法制备了壳聚糖包覆的纳米结构脂质载体(CF-NLCs)。为了研究包封效率和溶解度条件,硬脂酸/油酸的比例分别为80 / 20、70 / 30、60 / 40,通过调节壳聚糖的比例为50/50(mg / mg)。壳聚糖是一种粘性聚合物,可覆盖NLC的表面以提高其生物利用度。所有NLC配方均显示出约200 nm的粒径和低于0.3的多分散指数。NLC制剂的包封效率高于85%。对于CF-NLC,与市售非诺贝特制剂相比,非诺贝特的溶解度和包封效率有所提高。口服后非诺贝特以CF-NLC形式的药代动力学和药效学参数得到改善。CF-NLC可用于控制释放并改善非诺贝特的生物利用度和稳定性。所有NLC配方均显示出约200 nm的粒径和低于0.3的多分散指数。NLC制剂的包封效率高于85%。对于CF-NLC,与市售非诺贝特制剂相比,非诺贝特的溶解度和包封效率有所提高。口服后非诺贝特以CF-NLC形式的药代动力学和药效学参数得到改善。CF-NLC可用于控制释放并改善非诺贝特的生物利用度和稳定性。所有NLC配方均显示出约200 nm的粒径和低于0.3的多分散指数。NLC制剂的包封效率高于85%。对于CF-NLC,与市售非诺贝特制剂相比,非诺贝特的溶解度和包封效率有所提高。口服后非诺贝特以CF-NLC形式的药代动力学和药效学参数得到改善。CF-NLC可用于控制释放并改善非诺贝特的生物利用度和稳定性。与市售非诺贝特制剂相比,非诺贝特的溶解度和包封效率提高了。口服后非诺贝特以CF-NLC形式的药代动力学和药效学参数得到改善。CF-NLC可用于控制释放并改善非诺贝特的生物利用度和稳定性。与市售非诺贝特制剂相比,非诺贝特的溶解度和包封效率提高。口服后非诺贝特以CF-NLC形式的药代动力学和药效学参数得到改善。CF-NLC可用于控制释放并改善非诺贝特的生物利用度和稳定性。

更新日期:2020-09-07
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