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Preparation and Characterization of Salmon Calcitonin–biotin Conjugates

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Abstract

This study was performed to prepare and characterize the biotinylated Salmon calcitonin (sCT) for oral delivery and evaluate the hypocalcemic effect of biotinylated-sCTs in rats. Biotinylated sCTs was characterized by using high performance liquid chromatography (HPLC) and MALDITOF-MS. The effect of biotinylation on permeability across Caco-2 cell monolayers was examined. Their hypocalcemic effect was determined in rats. Mono- and di-bio-sCTs were separated by reverse phase HPLC. The molecular weights of mono-bio-sCT and di-bio-sCT were determined to be 3,660.5 and 3,900.2 Da, respectively. The permeability of biotinylated-sCTs across Caco-2 cell monolayers was observed with a significant enhancement compared with sCT. Intrajejunal (ij) administration of mono-bio-sCT and di-bio-sCT resulted in sustained reduction in serum calcium levels, with a maximum reduction (% max(d)) of 21.6% and 30% after 4 h and 6 h of application, respectively. The biotin conjugation of sCT may be a promising strategy for increasing the oral bioavailability of sCT and achieving sustained calcium-lowering effects.

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Authors and Affiliations

  1. Department of Pharmaceutical Technology, Faculty of Pharmacy, Ataturk University, 25240, Erzurum, Turkey

    Meltem Cetin

  2. Drug Targeting Laboratory, College of Pharmacy, SungKyunKwan University, 300 Chonchon-dong, Jangan-ku, Suwon City, 440-746, Republic of Korea

    Yu Seok Youn & Kang Choon Lee

  3. Faculty of Pharmacy, Department of Pharmaceutical Technology, Hacettepe University, 06100, Ankara, Turkey

    Yilmaz Capan

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  1. Meltem Cetin
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  2. Yu Seok Youn
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Correspondence to Meltem Cetin.

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Cetin, M., Youn, Y.S., Capan, Y. et al. Preparation and Characterization of Salmon Calcitonin–biotin Conjugates. AAPS PharmSciTech 9, 1191–1197 (2008). https://doi.org/10.1208/s12249-008-9165-2

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