Abstract:
BACKGROUND:The objective of this study was to develop and evaluate a more effective mucoadhesive thiomer for buccal drug-delivery systems. METHODS:2-iminothiolane was covalently attached to a chitosan backbone. A preactivation step followed, mediated by 6,6´dithionicotinamide, thiol groups were modified by disulfide bonds formation. Mucoadhesion studies were performed on buccal mucosa. In addition, water-uptake capacity, disintegration, release and cytotoxicity studies were completed. RESULTS:The obtained chitosan-thiobutylamidine conjugate displayed 647.4 ± 85.23 µmol/g immobilized thiol groups. Due to the preactivation, approximately 60% of thiol groups were modified by formation of disulfide bonds. Chitosan-thiobutylamidine-mercaptonicotinamide displayed 1.8-fold higher stability and 1.6-fold higher mucoadhesive properties, respectively. The release study demonstrated a 1.4-fold more prolonged drug release compared with corresponding thiomers. CONCLUSION:According to these results, preactivated thiomers demonstrate an improved stability and increased mucoadhesive properties. Therefore, they seem to be advantageous for buccal administration over corresponding thiomers and chitosan.
journal_name
Future Med Chemjournal_title
Future medicinal chemistryauthors
Laffleur F,Shahnaz G,Islambulchilar Z,Bernkop-Schnürch Adoi
10.4155/fmc.13.33subject
Has Abstractpub_date
2013-04-01 00:00:00pages
511-22issue
5eissn
1756-8919issn
1756-8927journal_volume
5pub_type
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pub_type: 杂志文章
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pub_type: 杂志文章
doi:10.4155/fmc.13.190
更新日期:2014-02-01 00:00:00
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更新日期:2015-01-01 00:00:00
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更新日期:2014-01-01 00:00:00
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journal_title:Future medicinal chemistry
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更新日期:2010-09-01 00:00:00
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journal_title:Future medicinal chemistry
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更新日期:2017-04-01 00:00:00
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journal_title:Future medicinal chemistry
pub_type: 杂志文章,评审
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更新日期:2019-05-01 00:00:00
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journal_title:Future medicinal chemistry
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doi:10.4155/fmc-2016-0212
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journal_title:Future medicinal chemistry
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journal_title:Future medicinal chemistry
pub_type: 杂志文章,评审
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更新日期:2019-06-01 00:00:00