Effect of microemulsion formulation on biodistribution of Tc-99m-Aprotinin in acute pancreatitis models induced rats

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dc.authorid0000-0002-3210-3747
dc.contributor.authorİlem Özdemir, Derya
dc.contributor.authorÜstündağ Okur, Neslihan
dc.contributor.authorAy Şenyiğit, Zeynep
dc.contributor.authorOruç, Nevin
dc.contributor.authorAşıkoğlu, Makbule
dc.contributor.authorÖzütemiz, Ömer
dc.contributor.authorKarasulu Yeşim, Hatice
dc.date.accessioned10.07.201910:49:13
dc.date.accessioned2019-07-10T19:51:52Z
dc.date.available10.07.201910:49:13
dc.date.available2019-07-10T19:51:52Z
dc.date.issued2016
dc.departmentİstanbul Medipol Üniversitesi, Eczacılık Fakültesi, Eczacılık Teknolojisi Bölümü, Farmasötik Teknoloji Ana Bilim Dalı
dc.descriptionWOS: 000388750400045
dc.descriptionPubMed ID: 26923781
dc.description.abstractBackground: Aprotinin is a monomeric globular polypeptide, which derived from bovine lung tissue and theoretically attractive molecule in ameliorating the effects of acute pancreatitis. Acute pancreatitis is an inflammatory condition of the pancreas that is painful and at times deadly. Over the following two decades Aprotinin therapeutic potential on pancreatitis is proven experimentally, its clinical therapeutic success is limited due to low targeting to pancreas. Objective: The aim of this study was to evaluate the biodistribution of Technetium-(99m)(Tc-99m)Aprotinin solution (Tc-99m-Aprotinin-S) and Tc-99m-Aprotinin loaded microemulsion, which was prepared for the aim of treatment for acute pancreatitis. Method: Aprotinin was radiolabeled with Tc-99m. Radiochemical purity was determined with radioactive thin layer chromatography studies. Tc-99m-Aprotinin-S and Tc-99m-Aprotinin loaded microemulsion (Tc-99m-Aprotinin-M) was administered to acute edematous, severe necrotizing pancreatitis and air pouch model induced rats. Tissue distribution of Aprotinin was investigated with gamma scintigraphy and biodistribution studies. Results: Aprotinin was radiolabeled by Tc-99m with high radiochemical purity (95.430 +/- 0.946%). The complex was found to be stable at room temperature up to 6 h. Animal studies have shown that similar to that of other small proteins Aprotinin is accumulated primarily in the kidney. The scintigraphy and biodistribution studies showed that, while i. v. administration of (99m)TcAprotinin-S distributed mostly in kidneys and bladder, Tc-99m-Aprotinin-M, with droplet size of 64.550 +/- 3.217 nm, has high uptake in liver, spleen and pancreas. Conclusion: This might be concluding that microemulsions may be suggested as promising formulations for selectively targeting Aprotinin to pancreas inflammation.
dc.description.sponsorshipScientific and Technological Research Council of Turkey (Tubitak) [108S083]; T.R. Prime Ministry State Planning Organization Foundation [09DPT001]en_US
dc.description.sponsorshipThe authors declare no conflict of interest. The authors alone are responsible for the content and writing of the article. This study was supported by The Scientific and Technological Research Council of Turkey (Tubitak 108S083). The authors also thank to the T.R. Prime Ministry State Planning Organization Foundation (Project Number: 09DPT001).en_US
dc.identifier.citationİlem Özdemir, D., Üstündağ Okur, N., Ay Şenyiğit, Z., Oruç, N., Aşıkoğlu, M., Özütemiz, Ö. ve Karasulu, H. Y. (2016). Effect of microemulsion formulation on biodistribution of Tc-99m-Aprotinin in acute pancreatitis models induced rats. Drug Delivery, 23(8), 3055-3062. https://dx.doi.org/10.3109/10717544.2016.1145306
dc.identifier.doi10.3109/10717544.2016.1145306
dc.identifier.endpage3062
dc.identifier.issn1071-7544
dc.identifier.issn1521-0464
dc.identifier.issue8
dc.identifier.scopusqualityQ2
dc.identifier.startpage3055
dc.identifier.urihttps://dx.doi.org/10.3109/10717544.2016.1145306
dc.identifier.urihttps://hdl.handle.net/20.500.12511/2298
dc.identifier.volume23
dc.identifier.wosqualityQ1
dc.indekslendigikaynakWeb of Science
dc.indekslendigikaynakScopus
dc.indekslendigikaynakPubMed
dc.language.isoen
dc.publisherTaylor & Francis
dc.relation.ispartofDrug Deliveryen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanı
dc.rightsinfo:eu-repo/semantics/openAccess
dc.subjectAprotinin
dc.subjectBiodistribution
dc.subjectMicroemulsion
dc.subjectPancreatitis
dc.subjectRadiolabeled Aprotinin
dc.titleEffect of microemulsion formulation on biodistribution of Tc-99m-Aprotinin in acute pancreatitis models induced rats
dc.typeArticle

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