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Preparation and characterization of novel multi-core chitosan microspheres for stomach-specific delivery of hydrophilic antibiotics

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Abstract

Insufficient gastric mucosa drug concentration and short contact time were the main reason for the lack of eradication efficacy of Helicobacter pylori for peptic ulcer patients. Novel multi-core chitosan microspheres were prepared for stomach-specific delivery of hydrophilic antibiotics for the treatment of peptic ulcer. Chitosan microspheres with multiple Eudragit L100 cores were easily prepared by a new emulsification/coagulation encapsulating method. Swelling behaviors, surface amino groups and mucin absorption ability were investigated and the formulation that showed best mucoadhesive potential was adopted. The multi-core chitosan microspheres exhibited good mucoadhesiveness as well as controlled release manner for incorporated antibiotics in acidic environment. The release rate could be easily modulated with accumulative release ranging from 47.3 to 79.3% in 6 h. Accordingly, the multi-core chitosan microspheres could serve as a satisfactory vehicle for stomach-specific delivery of hydrophilic antibiotics.

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Acknowledgments

We gratefully acknowledge financial support from National novel drug R&D for the 11th five-year plan (2009ZX09503-026), a grant from National Basic Research Program of China (973 Program, 2009CB903300) and Youth academic leader Foundation of Sichuan province (09ZQ026-051).

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Authors and Affiliations

  1. Key Laboratory of Drug Targeting and Drug Delivery, Ministry of Education, West China School of Pharmacy, Sichuan University, No. 17, Block 3, Southern Renmin Road, Chengdu, 610041, Sichuan, People’s Republic of China

    Xi Zhu, Dan Zhou, Shan Guan, Peiwen Zhang, Zhirong Zhang & Yuan Huang

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  1. Xi Zhu
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  2. Dan Zhou
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  3. Shan Guan
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  4. Peiwen Zhang
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  5. Zhirong Zhang
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  6. Yuan Huang
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Correspondence to Yuan Huang.

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Zhu, X., Zhou, D., Guan, S. et al. Preparation and characterization of novel multi-core chitosan microspheres for stomach-specific delivery of hydrophilic antibiotics. J Mater Sci: Mater Med 23, 983–990 (2012). https://doi.org/10.1007/s10856-012-4567-9

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  • DOI: https://doi.org/10.1007/s10856-012-4567-9

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