99mTc-labeled, tofacitinib citrate encapsulated chitosan microspheres loaded in situ gel formulations for intra-articular treatment of rheumatoid arthritis

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dc.authoridKarpuz, Merve/0000-0001-6681-2448
dc.contributor.authorKarpuz, Merve
dc.contributor.authorAydin, Husniye Hande
dc.contributor.authorOzgenc, Emre
dc.contributor.authorErel-Akbaba, Gulsah
dc.contributor.authorAtlihan-Gundogdu, Evren
dc.contributor.authorSenyigit, Zeynep
dc.date.accessioned2024-08-31T07:47:40Z
dc.date.available2024-08-31T07:47:40Z
dc.date.issued2024
dc.departmentEge Üniversitesien_US
dc.description.abstractInflammatory diseases including rheumatoid arthritis are major health problems. Although different techniques and drugs are clinically available for the diagnosis and therapy of the disease, novel approaches regarding radiolabeled drug delivery systems are researched. Hence, in the present study, it was aimed to design, prepare, and characterize (99)mTc-radiolabeled and tofacitinib citrate-encapsulated microsphere loaded poloxamer in situ gel formulations for the intra-articular treatment. Among nine different microsphere formulations, MS/TOFA-9 was chosen as the most proper one due to particle size, high encapsulation efficiency, and in vitro drug release behavior. Poloxamer 338 at a concentration of 15% was used to prepare in situ gel formulations. For intra-articular administration, microspheres were dispersed in an in situ gel containing 15% Poloxamer 338 and characterized in terms of gelation temperature, viscosity, rheological, mechanical, and spreadability properties. After the determination of the safe dose for MS/TOFA-9 and PLX-MS/TOFA-9 as 40 mu L/mL in the cell culture study performed on healthy cells, the high anti-inflammatory effects were due to significant cellular inhibition of fibroblasts. In the radiolabeling studies with (99)mTc, the optimum radiolabeling condition was determined as 200 ppm SnCl2 and 0.5 mg ascorbic acid, and both (99)mTc-MS/TOFA-9 and (99)mTc-PLX-MS/TOFA-9 exhibited high cellular binding capacity. In conclusion, although further in vivo experiments are required, PLX-MS/TOFA-9 was found to be a promising agent for intra-articular injection in rheumatoid arthritis.en_US
dc.description.sponsorshipTurkiye Bilimsel ve Teknolojik Arastirma Kurumu [119S639]en_US
dc.description.sponsorshipTurkiye Bilimsel ve Teknolojik Arastirma Kurumu, Grant/Award Number: 119S639en_US
dc.identifier.doi10.1002/ddr.22247
dc.identifier.issn0272-4391
dc.identifier.issn1098-2299
dc.identifier.issue5en_US
dc.identifier.pmid39138857en_US
dc.identifier.scopus2-s2.0-85201244963en_US
dc.identifier.scopusqualityQ2en_US
dc.identifier.urihttps://doi.org/10.1002/ddr.22247
dc.identifier.urihttps://hdl.handle.net/11454/104508
dc.identifier.volume85en_US
dc.identifier.wosWOS:001290849200001en_US
dc.identifier.wosqualityN/Aen_US
dc.indekslendigikaynakWeb of Scienceen_US
dc.indekslendigikaynakScopusen_US
dc.indekslendigikaynakPubMeden_US
dc.language.isoenen_US
dc.publisherWileyen_US
dc.relation.ispartofDrug Development Researchen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.rightsinfo:eu-repo/semantics/openAccessen_US
dc.snmz20240831_Uen_US
dc.subjectChitosan Microspheresen_US
dc.subjectIn Situ Gelsen_US
dc.subjectIntra-Articular Treatmenten_US
dc.subjectTechnetium-99men_US
dc.subjectTofacitinib Citrateen_US
dc.title99mTc-labeled, tofacitinib citrate encapsulated chitosan microspheres loaded in situ gel formulations for intra-articular treatment of rheumatoid arthritisen_US
dc.typeArticleen_US

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