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Preparation And Characterization Of Salmon Calcitonin–biotin Conjugates

M. Çetin, Yu Seok Youn, Y. Capan, Kang Choon Lee
Published 2008 · Chemistry, Medicine

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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.
This paper references
Chitosan-PEG nanocapsules as new carriers for oral peptide delivery. Effect of chitosan pegylation degree.
C. Prego (2006)
Molecular and functional characterization of the intestinal Na+-dependent multivitamin transporter.
P. Prasad (1999)
Uptake, localization, and noncarboxylase roles of biotin.
J. Zempleni (2005)
Development and in vivo evaluation of an oral insulin-PEG delivery system.
P. Calceti (2004)
The Calcitonins: Physiology and Pharmacology
M. Azria (1989)
Oral Delivery of Mono-PEGylated sCT (Lys18) in Rats: Regional Difference in Stability and Hypocalcemic Effect
S. Mansoor (2005)
Exposure-response relationships and drug interactions of sirolimus
J. J. Zimmerman (2008)
Targeting the Sodium-Dependent Multivitamin Transporter (SMVT) for Improving the Oral Absorption Properties of a Retro-Inverso Tat Nonapeptide
S. Ramanathan (2004)
Degradation pathways, analytical characterization and formulation strategies of a peptide and a protein. Calcitonine and human growth hormone in comparison.
M. Cholewinski (1996)
Chromatographic separation and mass spectrometric identification of positional isomers of polyethylene glycol-modified growth hormone-releasing factor (1-29).
Y. Youn (2004)
New surface-modified lipid nanoparticles as delivery vehicles for salmon calcitonin.
M. Garcia-Fuentes (2005)
In Vivo Evaluation of an Oral Salmon Calcitonin-Delivery System Based on a Thiolated Chitosan Carrier Matrix
D. Guggi (2004)
Regional permeability of salmon calcitonin in isolated rat gastrointestinal tracts: Transport mechanism using Caco-2 cell monolayer
R. Shah (2008)
Improved intestinal delivery of salmon calcitonin by Lys18-amine specific PEGylation: stability, permeability, pharmacokinetic behavior and in vivo hypocalcemic efficacy.
Y. Youn (2006)
Emerging trends in oral delivery of peptide and protein drugs.
R. Mahato (2003)
Chitosan nanocapsules as carriers for oral peptide delivery: effect of chitosan molecular weight and type of salt on the in vitro behaviour and in vivo effectiveness.
C. Prego (2006)
Comparison of the in vitro apparent permeability and stability of opioid mimetic compounds with that of the native peptide.
Yasuko Koda (2007)
Pharmacokinetic disposition of polyethylene glycol-modified salmon calcitonins in rats.
S. Yoo (2000)
A carrier-mediated, Na+ gradient-dependent transport for biotin in human intestinal brush-border membrane vesicles.
H. Said (1987)
Utility of pharmacodynamic measures for assessing the oral bioavailability of peptides. 1. Administration of recombinant salmon calcitonin in rats.
P. Sinko (1995)
hypocalcemic effects in rats
K. C. Lee (2003)
Current challenges in non-invasive insulin delivery systems: a comparative review.
E. Khafagy (2007)
Potentiality of double liposomes containing salmon calcitonin as an oral dosage form.
Kenji Yamabe (2003)
Protection of salmon calcitonin breakdown with serine proteases by various ovomucoid species for oral drug delivery.
R. Shah (2004)
Effect of surfactants on the nasal absorption of insulin in rats
Hirai Shinichiro (1981)
Molecular mechanism of the intestinal biotin transport process.
N. Chatterjee (1999)
Targeted PEG-based bioconjugates enhance the cellular uptake and transport of a HIV-1 TAT nonapeptide.
S. Ramanathan (2001)
Preparation, characterization, and application of biotinylated and biotin-PEGylated glucagon-like peptide-1 analogues for enhanced oral delivery.
S. Chae (2008)
Pharmacokinetic and biodistribution properties of poly(ethylene glycol)-protein conjugates.
P. Caliceti (2003)
Synthesis, characterization, and pharmacokinetic studies of PEGylated glucagon-like peptide-1.
S. Lee (2005)
Enhanced intestinal absorption of salmon calcitonin (sCT) from proliposomes containing bile salts.
Keon-Hyoung Song (2005)
Monitoring of peptide acylation inside degrading PLGA microspheres by capillary electrophoresis and MALDI-TOF mass spectrometry.
D. Na (2003)
Reversible lipidization for the oral delivery of salmon calcitonin.
J. Wang (2003)
Biodegradable nanoparticles containing protein‐fatty acid complexes for oral delivery of salmon calcitonin
H. Yoo (2004)
Intranasal Delivery of PEGylated Salmon Calcitonins: Hypocalcemic Effects in Rats
K. C. Lee (2002)
Regional oral absorption, hepatic first-pass effect, and non-linear disposition of salmon calcitonin in beagle dogs.
Y. Hee Lee (2000)
Oral delivery of salmon calcitonin.
Y. H. Lee (2000)

This paper is referenced by
Developing oral formulations for protein and peptide drugs
A. Parry (2013)
Salmon calcitonin-loaded Eudragit® and Eudragit®-PLGA nanoparticles: in vitro and in vivo evaluation
M. Cetin (2012)
Permeation of Insulin, Calcitonin and Exenatide across Caco-2 Monolayers: Measurement Using a Rapid, 3-Day System
V. Gupta (2013)
Overcoming the intestinal barrier: A look into targeting approaches for improved oral drug delivery systems.
Yining Xu (2020)
Oral delivery of zoledronic acid by non-covalent conjugation with lysine-deoxycholic acid: In vitro characterization and in vivo anti-osteoporotic efficacy in ovariectomized rats.
Ok-cheol Jeon (2016)
Colonic absorption of salmon calcitonin using tetradecyl maltoside (TDM) as a permeation enhancer.
S. B. Petersen (2013)
Oral drug delivery systems using chemical conjugates or physical complexes.
T. A. Al-Hilal (2013)
Animal models for evaluation of oral delivery of biopharmaceuticals
Stine Harloff-Helleberg (2017)
Liposomes coated with thiolated chitosan enhance oral peptide delivery to rats☆
K. Gradauer (2013)
Transdermal Delivery of Salmon Calcitonin Using a Dissolving Microneedle Array: Characterization, Stability, and In vivo Pharmacodynamics.
L. Zhang (2020)
Title Safety and efficacy of sodium caprate in promoting oral drugabsorption : from in vitro to the clinic
S. Maher (2017)
Safety and efficacy of sodium caprate in promoting oral drug absorption: from in vitro to the clinic.
S. Maher (2009)
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