Chitosan-based buccal mucoadhesive patches to enhance the systemic bioavailability of tizanidine

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dc.authorid0000-0001-9290-2404
dc.contributor.authorArpa, Muhammet Davut
dc.contributor.authorÜstündağ Okur, Neslihan
dc.contributor.authorGök, Mehmet Koray
dc.contributor.authorÖzgümüş, Saadet
dc.contributor.authorCevher, Erdal
dc.date.accessioned2023-07-21T07:14:16Z
dc.date.available2023-07-21T07:14:16Z
dc.date.issued2023
dc.departmentİstanbul Medipol Üniversitesi, Eczacılık Fakültesi, Eczacılık Teknolojisi Bölümü, Farmasötik Teknoloji Ana Bilim Dalı
dc.description.abstractTizanidine hydrochloride (TZN) is a muscle relaxant used to treat a variety of disorders such as painful muscle spasms and chronic spasticity. TZN has low oral bioavailability due to extensive first-pass metabolism and is used orally at a dose of 6–24 mg per day. In the present study, buccal patches were prepared by solvent casting method using chitosan glutamate (Chi-Glu) and novel chitosan azelate (Chi-Aze) which was synthesised in-house for the first time, to enhance the bioavailability of TZN by bypassing first-pass metabolism. The characterisation, mucoadhesion and drug release studies were performed. Chi-Aze patches retained their integrity longer in the buccal medium and showed higher ex vivo drug permeability compared to that prepared with Chi-Glu. In vivo studies revealed that buccal formulation fabricated with Chi-Aze (3%) showed approx 3 times more bioavailability than the orally administered commercial product. Results of the studies indicate that Chi-Aze, prepared by conjugation of chitosan and a fatty acid, the patch formulation is a promising buccal mucoadhesive system due to the physical stability in buccal medium, the good mucoadhesiveness and the high TZN bioavailability. Moreover, Chi-Aze patch might be an alternative to oral formulations of TZN to reduce the dose and frequency of drug administration.
dc.description.sponsorshipPrimex EHFen_US
dc.identifier.citationArpa, M. D., Üstündağ Okur, N., Gök, M. K., Özgümüş, S. ve Cevher, E. (2023). Chitosan-based buccal mucoadhesive patches to enhance the systemic bioavailability of tizanidine. International Journal of Pharmaceutics, 642. https://dx.doi.org/10.1016/j.ijpharm.2023.123168
dc.identifier.doi10.1016/j.ijpharm.2023.123168
dc.identifier.issn0378-5173
dc.identifier.issn1873-3476
dc.identifier.pmid37356512
dc.identifier.scopus2-s2.0-85163418157
dc.identifier.scopusqualityQ1
dc.identifier.urihttps://dx.doi.org/10.1016/j.ijpharm.2023.123168
dc.identifier.urihttps://hdl.handle.net/20.500.12511/11233
dc.identifier.volume642
dc.identifier.wos001024632000001en_US
dc.identifier.wosqualityQ1
dc.indekslendigikaynakWeb of Science
dc.indekslendigikaynakScopus
dc.indekslendigikaynakPubMed
dc.institutionauthorArpa, Muhammet Davut
dc.language.isoen
dc.publisherElsevier B.V.
dc.relation.ispartofInternational Journal of Pharmaceuticsen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanı
dc.relation.tubitakinfo:eu-repo/grantAgreement/TUBITAK/SOBAG/217S257
dc.rightsinfo:eu-repo/semantics/embargoedAccess
dc.subjectAzelaic Acid
dc.subjectBioavailability
dc.subjectBuccal Patch
dc.subjectChitosan
dc.subjectMucoadhesion
dc.subjectTizanidine
dc.titleChitosan-based buccal mucoadhesive patches to enhance the systemic bioavailability of tizanidine
dc.typeArticle

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