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Fabrication and in vitro/in vivo characterization of Eudragit enteric nanoparticles loaded with indomethacin

Xingrong Wang, Mufang Wang, Qi Wang, Ye Yuan, Qiulian Hao, Yanping Bi, Yujing He, Jing Zhao, and Jifu Hao

College of Pharmacy, Shandong First Medical University & Shandong Academy of Medical Science, Taian, People’s Republic of China

 

E-mail: Yz.xyd@163.com

Received: 24 May 2021  Accepted: 5 October 2021

Abstract:

The purpose of this study was to tailor and evaluate indomethacin-loaded Eudragit L 100–55 enteric nanoparticles (IDM@NPs). Nanoprecipitation approach was used to fabricate IDM@NPs, and the formulation was optimized by a central composite design (CCD). The physicochemical properties of IDM@NPs were characterized by FTIR, XRD and DSC, respectively. Furthermore, in situ intestinal perfusion, in vivo pharmacokinetic analysis and pharmacodynamics experiments were performed. The obtained IDM@NPs were in spherical shape. The results of FITC, XRD and DSC indicated that no molecular interaction occurred and no crystal drug present in the nanoparticles. The in vitro release confirmed the pH-sensitive released profiles of IDM@NPs. The Cmax and AUC of IDM@NPs were about 1.24-fold and 1.39-fold greater than those of given coarse IDM group. In addition, the therapeutic activity illustrated that IDM@NPs have the similar anti-inflammatory and analgesic effects as compared with IDM suspensions, while there were no statistical differences between the high- and low-dose group of IDM@NPs. The present study demonstrated the enteric nanoparticles could be used as potential therapeutic platforms for oral delivery of IDM.

Keywords: Indomethacin; Eudragit L 100–55; Enteric nanoparticles

Full paper is available at www.springerlink.com.

DOI: 10.1007/s11696-021-01921-3

 

Chemical Papers 76 (2) 1119–1133 (2022)

Wednesday, April 24, 2024

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