title: Preparation and characterization of salmon calcitonin-sodium triphosphate ionic complex for oral delivery.
abstract: Even though salmon calcitonin (sCT) has been known as a potent hypocalcemic agent, only injection or nasal spray products are available on the market. In order to develop oral delivery system of the agent, a novel sCT-sodium tripolyphosphate (STPP) ionic complex was fabricated and also characterized. For the optimization of the ionic complexation, the effect of incubation time and molar ratio between sCT and STPP was evaluated. Particle size of the ionic complex in aqueous media, SEM images, DSC, FT-IR, in vitro release test, stability within the simulated intestinal fluid, and hypocalcemic effect were evaluated. The optimal molar complexation ratio of sCT to STPP was ranged from 1:5 to 1:10 and the complexation efficiency was about 95%. The SEM image has shown that the freeze dried ionic complex has rough morphology in their surface and the particle size in PBS (pH 7.4) was about 220nm. The DSC and FT-IR results provided evidences for ionic interaction between -NH(2) groups and -P horizontal lineO groups of sCT and STPP, respectively. The sCT ionic complex has shown sustained sCT releasing characteristics for 3weeks. The sCT-STPP ionic complex was protective to enzymatic attack and in vivo animal data revealed that the present ionic complex would show continuous hypocalcemic effect. Conclusively, the present sCT-STPP ionic complex formulation thought to be a novel oral delivery candidate for the treatment of osteoporosis.
authors.affiliation: Department of Smart Foods and Drugs, Inje University, Gimhae, Gyeongnam 621-749, Republic of Korea.
authors.forename: Hea Eun
authors.initials: HE
authors.lastname: Lee
authors.forename: Min Jung
authors.initials: MJ
authors.lastname: Lee
authors.forename: Cho Rong
authors.initials: CR
authors.lastname: Park
authors.forename: A Young
authors.initials: AY
authors.lastname: Kim
authors.forename: Kyung Hwa
authors.initials: KH
authors.lastname: Chun
authors.forename: Hee Jin
authors.initials: HJ
authors.lastname: Hwang
authors.forename: Dong Ho
authors.initials: DH
authors.lastname: Oh
authors.forename: Sang Ok
authors.initials: SO
authors.lastname: Jeon
authors.forename: Jae Seon
authors.initials: JS
authors.lastname: Kang
authors.forename: Tae Sung
authors.initials: TS
authors.lastname: Jung
authors.forename: Guang Jin
authors.initials: GJ
authors.lastname: Choi
authors.forename: Sangkil
authors.initials: S
authors.lastname: Lee
mesh_terms: D000284:Administration, Oral; D000818:Animals; D002116:Calcitonin / Q000008:administration & dosage* / Q000737:chemistry* / Q000494:pharmacology; D002152:Calorimetry, Differential Scanning; D004355:Drug Stability; D006996:Hypocalcemia / Q000139:chemically induced*; D007477:Ions / Q000737:chemistry; D008297:Male; D010316:Particle Size; D011122:Polyphosphates / Q000737:chemistry*; D051381:Rats; D017207:Rats, Sprague-Dawley; D017550:Spectroscopy, Fourier Transform Infrared
chemical_list: D007477:Ions; D011122:Polyphosphates; C028815:salmon calcitonin; D002116:Calcitonin; C005692:triphosphoric acid