Buccal adhesive chitosan conjugate comprising pilocarpine for xerostomia.
Adhesives
/ chemical synthesis
Cell Line
Chitosan
/ chemical synthesis
Chromatography, High Pressure Liquid
Drug Carriers
/ chemistry
Drug Delivery Systems
Drug Liberation
Humans
Molecular Structure
Mouth Mucosa
Pilocarpine
/ administration & dosage
Protective Agents
/ chemistry
Rheology
Xerostomia
/ drug therapy
Mucoadhesion
Pilocarpine
Xerostomia
Journal
International journal of biological macromolecules
ISSN: 1879-0003
Titre abrégé: Int J Biol Macromol
Pays: Netherlands
ID NLM: 7909578
Informations de publication
Date de publication:
15 Aug 2019
15 Aug 2019
Historique:
received:
28
01
2019
revised:
27
05
2019
accepted:
30
05
2019
pubmed:
4
6
2019
medline:
18
12
2019
entrez:
4
6
2019
Statut:
ppublish
Résumé
Xerostomia is caused by different factors such as side effects of medication, radiotherapy by head and neck cancer as well as Sjögren syndrome. The goal was to synthesize novel preactivated chitosan conjugates and to design adhesive dosage forms comprising sialagogue pilocarpine. Unmodified chitosan (CH) was covalently linked to sulfhydryl possessing mercaptonicotinic acid (MNA) via amide bond formation. In a second step, preactivation occurred via disulfide bond establishment between sulfhydryl linked chitosan and preactivation ligand MNA. Mucoadhesive and mucoprotective properties were scrutinized on buccal mucosa. Safety assessment was performed on head and neck squamous cells. Histology assay was conducted on buccal tissue. Pilocarpine was scrutinized in terms of controlled release behavior. Novel preactivated CH was successfully synthesized and considered as not harmful to the cells at all. Furthermore, mucoadhesion was 1.3-fold improved in the presence of preactivated chitosan as compared to respective unmodified one. Pilocarpine exhibited a 3.1-fold controlled release in presence of novel synthesized chitosan as in comparison to unmodified CH. The novelty of this promising polymeric carrier lies in the synthesis procedure leading to a pronounced mucoadhesive, mucoprotecting and controlled release encouraging dosage form in the management of xerostomia.
Sections du résumé
BACKGROUND
BACKGROUND
Xerostomia is caused by different factors such as side effects of medication, radiotherapy by head and neck cancer as well as Sjögren syndrome.
AIM
OBJECTIVE
The goal was to synthesize novel preactivated chitosan conjugates and to design adhesive dosage forms comprising sialagogue pilocarpine.
METHODS
METHODS
Unmodified chitosan (CH) was covalently linked to sulfhydryl possessing mercaptonicotinic acid (MNA) via amide bond formation. In a second step, preactivation occurred via disulfide bond establishment between sulfhydryl linked chitosan and preactivation ligand MNA. Mucoadhesive and mucoprotective properties were scrutinized on buccal mucosa. Safety assessment was performed on head and neck squamous cells. Histology assay was conducted on buccal tissue. Pilocarpine was scrutinized in terms of controlled release behavior.
RESULTS
RESULTS
Novel preactivated CH was successfully synthesized and considered as not harmful to the cells at all. Furthermore, mucoadhesion was 1.3-fold improved in the presence of preactivated chitosan as compared to respective unmodified one. Pilocarpine exhibited a 3.1-fold controlled release in presence of novel synthesized chitosan as in comparison to unmodified CH.
CONCLUSION
CONCLUSIONS
The novelty of this promising polymeric carrier lies in the synthesis procedure leading to a pronounced mucoadhesive, mucoprotecting and controlled release encouraging dosage form in the management of xerostomia.
Identifiants
pubmed: 31158424
pii: S0141-8130(19)30711-1
doi: 10.1016/j.ijbiomac.2019.05.219
pii:
doi:
Substances chimiques
Adhesives
0
Drug Carriers
0
Protective Agents
0
Pilocarpine
01MI4Q9DI3
Chitosan
9012-76-4
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
1043-1051Informations de copyright
Copyright © 2019. Published by Elsevier B.V.