Preparation and characterization of salmon calcitonin-sodium triphosphate ionic complex for oral delivery.
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.
Lee
Hea Eun
HE
Department of Smart Foods and Drugs, Inje University, Gimhae, Gyeongnam 621-749, Republic of Korea.
Lee
Min Jung
MJ
Park
Cho Rong
CR
Kim
A Young
AY
Chun
Kyung Hwa
KH
Hwang
Hee Jin
HJ
Oh
Dong Ho
DH
Jeon
Sang Ok
SO
Kang
Jae Seon
JS
Jung
Tae Sung
TS
Choi
Guang Jin
GJ
Lee
Sangkil
S
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
D007477:Ions; D011122:Polyphosphates; C028815:salmon calcitonin; D002116:Calcitonin; C005692:triphosphoric acid