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      Formulation development and evaluation of gastroretentive floating beads with Brucea javanica oil using ionotropic gelation technology

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          Abstract

          In the present study, a gastric retention floating system for Brucea javanica oil, composed of alginate and carrageenan, was prepared using ionotropic gelation. Parameters for floatability, drug load, encapsulation efficiency, bead morphology, in vitro release, and in vivo gastric retention were evaluated. The optimized formulation via Box-Behnken design consisted of 1.7% alginate (W/V), 1.02% carrageenan (W/V), 1.4% CaCO 3 (W/V), and a gelling bath of pH 0.8. The alginate-carrageenan-Brucea javanica oil beads had a porous structure and exhibited up to 24 h of in vitro floatability with a load capacity of 45%-55% and an encapsulation efficiency of 70%-80%. A 6-h sustained release was observed in vitro. The beads had a prolonged gastric retention (> 60% at 6 h) in fasted rats, compared to non-floating beads (15% at 6 h), as measured by gamma scintigraphy with single-photon emission tomography/computed tomography (SPET/CT). In conclusion, the alginate-carrageenan-Brucea javanica oil system showed enhanced oil encapsulation efficiency, excellent floating and gastric retention abilities, and a favorable release behavior.

          Author and article information

          Journal
          CJNM
          Chinese Journal of Natural Medicines
          Elsevier
          1875-5364
          20 April 2018
          : 16
          : 4
          : 293-301
          Affiliations
          [1] 1Experiment Center for Teaching and Learning, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China
          [2] 2School of Pharmacy, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China
          Author notes
          * Corresponding author: WANG Bin, Tel: 86-21-51323123, Fax: 86-21-5132 2337, E-mail: annabel_cn@ 123456163.com ; ZHANG Tong, Tel: 86-21-51322318, Fax: 86-21-51322337, E-mail: zhangtdmj@ 123456hotmail.com .

          These authors have no conflict of interest to declare.

          Article
          S1875-5364(18)30059-1
          10.1016/S1875-5364(18)30059-1
          d699b9d3-4b6c-4a44-98f6-5cdbecbeda6e
          Copyright © 2018 China Pharmaceutical University. Published by Elsevier B.V. All rights reserved.
          History
          : 26 October 2017
          Funding
          Funded by: National Natural Science Foundation of China
          Award ID: 81303233
          Funded by: Foundation of Shanghai Science and Technology Committee
          Award ID: 13401900300
          Funded by: Shanghai Municipal Commission of Health and Family Planning
          Award ID: 20124074
          This work was supported by the National Natural Science Foundation of China (No. 81303233), Foundation of Shanghai Science and Technology Committee (No. 13401900300) and Shanghai Municipal Commission of Health and Family Planning (No. 20124074). Its contents are solely the responsibility of the authors.

          Medicine,Pharmaceutical chemistry,Pharmacology & Pharmaceutical medicine,Complementary & Alternative medicine
          Box-Behnken design, Brucea javanica oil,Simaroubaceae,Alginate-carrageenan beads,Gastric retention,SPET/CT

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