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Enteric-coated sustained-release nanoparticles by coaxial electrospray: preparation, characterization, and in vitro evaluation

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Abstract

Enteric-coated formulations can delay the release of drugs until they have passed through the stomach. However, high concentration of drugs caused by rapidly released in the small intestine leads to the intestinal damage, and frequent administration would increase the probability of missing medication and reduce the patient compliance. To solve the above-mentioned problems, aspirin-loaded enteric-coated sustained-release nanoparticles with core–shell structure were prepared via one-step method using coaxial electrospray in this study. Eudragit L100-55 as pH-sensitive polymer and Eudragit RS as sustained-release polymer were used for the outer coating and inner core of the nanoparticles, respectively. The maximum loading capacity of nanoparticles was 23.66 % by changing the flow rate ratio of outer/inner solutions, and the entrapment efficiency was nearly 100 %. Nanoparticles with core–shell structure were observed via fluorescence microscope and transmission electron microscope. And pH-sensitive and sustained drug release profiles were observed in the media with different pH values (1.2 and 6.8). In addition, mild cytotoxicity in vitro was detected, and the nanoparticles could be taken up by Caco-2 cells within 1.0 h in cellular uptake study. These results indicate that prepared enteric-coated sustained-release nanoparticles would be a more safety and effective carrier for oral drug delivery.

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Acknowledgments

The authors acknowledge the financial assistance provided by National Natural Science Foundation of China (31200713); International Science and Technology Cooperation Base Construction of Chongqing (CSTC 201110005), Chongqing University Postgraduates’ Innovative Team Building Project (201105A1001).

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Authors and Affiliations

  1. Key Laboratory of Biorheological Science and Technology, Ministry of Education, College of Bioengineering, Chongqing University, Chongqing, 400030, China

    Shilei Hao, Bochu Wang, Yazhou Wang & Yingqian Xu

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  1. Shilei Hao
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  2. Bochu Wang
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  3. Yazhou Wang
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  4. Yingqian Xu
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Correspondence to Bochu Wang.

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Hao, S., Wang, B., Wang, Y. et al. Enteric-coated sustained-release nanoparticles by coaxial electrospray: preparation, characterization, and in vitro evaluation. J Nanopart Res 16, 2204 (2014). https://doi.org/10.1007/s11051-013-2204-2

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