Publication: Exploration of hydrophobic modification degree of chitosan-based nanocomplexes on the oral delivery of enoxaparin
Issued Date
2013-09-27
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ISSN
18790720
09280987
09280987
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2-s2.0-84884514812
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Mahidol University
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SCOPUS
Bibliographic Citation
European Journal of Pharmaceutical Sciences. Vol.50, No.3-4 (2013), 263-271
Suggested Citation
Linlin Wang, Liang Li, Yujiao Sun, Ye Tian, Ying Li, Conghao Li, Varaporn B. Junyaprasert, Shirui Mao Exploration of hydrophobic modification degree of chitosan-based nanocomplexes on the oral delivery of enoxaparin. European Journal of Pharmaceutical Sciences. Vol.50, No.3-4 (2013), 263-271. doi:10.1016/j.ejps.2013.07.009 Retrieved from: https://repository.li.mahidol.ac.th/handle/20.500.14594/32730
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Title
Exploration of hydrophobic modification degree of chitosan-based nanocomplexes on the oral delivery of enoxaparin
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Abstract
The objective of this paper is to elucidate the influence of lipophilic modification degree of chitosan on the peroral absorption of enoxaparin. A series of novel chitosan grafted glyceryl monostearate (GM) copolymers with different GM substitution degree were synthesized and the successful synthesis was confirmed by1H NMR, FTIR and X-ray diffraction. Enoxaparin loaded nanocomplexes with different carriers were prepared by self-assembly process. Influence of GM substitution degree and chitosan molecular weight in the copolymer on the properties of the nanocomplexes was investigated. Morphology of the nanocomplexes was observed by atomic force microscopy. Mucoadhesive properties of the nanocomplexes were characterized using mucin particle method. Initially, mucoadhesion of the nanocomplexes increased with the increase of GM substitution degree and it started to decrease when the substitution degree was up to 18.6%. A good linear relationship between GM substitution degree and in vivo absorption of enoxaparin in fasted rats was established in the substitution degree range of 0-11.1%. In agreement with mucoadhesion data, further increasing GM substitution degree to 18.6% caused a decrease in oral absorption. In conclusion, oral bioavailability of enoxaparin can be enhanced by structure modification of the carriers and the bioavailability is hydrophobic modification degree dependent. © 2013 Elsevier B.V. All rights reserved.