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通过界面聚合法制备丝胶蛋白/聚氰基丙烯酸乙酯纳米球以增强非诺贝特的生物疗效:体外和体内研究

Sericin/Poly(ethylcyanoacrylate) Nanospheres by Interfacial Polymerization for Enhanced Bioefficacy of Fenofibrate: In Vitro and In Vivo Studies.

作者信息

Parisi Ortensia I, Fiorillo Marco, Scrivano Luca, Sinicropi Maria S, Dolce Vincenza, Iacopetta Domenico, Puoci Francesco, Cappello Anna R

机构信息

Department of Pharmacy, Health and Nutritional Sciences, and §Department of Informatics, Modeling, Electronics and Systems Engineering, University of Calabria , 87036 Rende (CS), Italy.

出版信息

Biomacromolecules. 2015 Oct 12;16(10):3126-33. doi: 10.1021/acs.biomac.5b00746. Epub 2015 Sep 17.

Abstract

Fenofibrate is a lipophilic drug used in hypercholesterolemia and hypertriglyceridemia as a lipid-regulating agent; however, it is characterized by poor water solubility and low dissolution rate, which result in a low oral bioavailability. In the present study, sericin/poly(ethylcyanoacrylate) nanospheres are synthesized by interfacial polymerization in aqueous media and investigated as a novel sericin-based delivery system for improved and enhanced oral bioefficacy of fenofibrate. The incorporation of sericin into the prepared cyanoacrylate nanoparticles and their spherical shape are confirmed by Lowry assay and scanning electron microscopy, respectively. Hydrophilic and mucoadhesive properties of the synthesized nanospheres are also evaluated. Finally, both in vitro release and in vivo studies are performed and the oral absorbable amount of fenofibrate is calculated to be higher than 70% when incorporated into the polymeric material, reducing the levels of total cholesterol (TC), triacylglycerols (TG), very low-density lipoproteins (VLDL), and low-density lipoproteins (LDL) compared to fenofibrate alone.

摘要

非诺贝特是一种亲脂性药物,作为一种脂质调节剂用于治疗高胆固醇血症和高甘油三酯血症;然而,它的特点是水溶性差和溶解速率低,这导致口服生物利用度低。在本研究中,通过界面聚合在水介质中合成了丝胶蛋白/聚(氰基丙烯酸乙酯)纳米球,并将其作为一种新型的基于丝胶蛋白的递送系统进行研究,以提高和增强非诺贝特的口服生物疗效。分别通过洛瑞法和扫描电子显微镜证实了丝胶蛋白掺入制备的氰基丙烯酸酯纳米颗粒及其球形形状。还评估了合成纳米球的亲水性和粘膜粘附性。最后,进行了体外释放和体内研究,结果表明,当非诺贝特掺入聚合物材料中时,其口服吸收量计算高于70%,与单独使用非诺贝特相比,可降低总胆固醇(TC)、三酰甘油(TG)、极低密度脂蛋白(VLDL)和低密度脂蛋白(LDL)的水平。

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