Abstract
Osteoporosis, a systemic skeleton disease, can be prevented by increasing calcium levels in serum via administration of calcium salts. However, traditional calcium-based formulations have not appeared to be effective, hence the purpose of the present work has been to prepare and test in vitro/vivo a formulation able to gradually release calcium during transit over the GI tract, thus increasing bioavailability and reducing daily dose, and hence, side effects. Calcium controlled-release granules based on zeolite and Precirol® were prepared. In the best case, represented by granules sized 1.2 mm, containing 20% Precirol®, 19% zeolite, 60% calcium (granule), the release lasted ≈6 h. The release is controlled by diffusion of calcium ions through the aqueous channels forming within granules, once these come into contact with physiological fluids. Such a diffusion is hindered by the interaction of calcium ions with the negatively charged surface of the zeolite. Ovariectomy was used to make rats osteopenic. For in vivo studies, rats were divided into the following groups. Sham: not treated; ova: ovariectomized (ova); CaCl2 1.0 g: ova, treated with 1.0 g/die Ca2+; CaCl2 0.5 g: ova, treated with 0.5 g/die Ca2+; granule 1.0 g, or granule 0.5 g: ova, treated with granules equivalent to 1.0 g/die or 0.5 g/die Ca2+ in humans. Ca2+ amounts in femur bone and bone marrow, femur mechanical characteristics, and femur medullary canalicule diameter were measured and the same efficacy rank order was obtained: ova < CaCl2 0.5 g < CaCl2 1.0 g < granule 0.5 g ≈ granule 1.0 g ≈ sham. The results show promise of an effective prevention of osteoporosis, based on a controlled-rate administration of a calcium dose half that administered by the current therapy, with reduced side effects.
Highlights
Osteoporosis is a systemic skeleton disease, characterized by a reduction of bone mass and a deterioration of bone tissue microarchitecture, with consequent increase of frailty and liability to fracturing, mostly of hip bone, back bone, or wrist bone. [1,2,3]
Calcium transport via the paracellular route is not influenced by vitamin D, rather, it only depends on calcium solubility, chimo transit time over the intestine, and calcium paracellular permeability [8]
Negative charges are found on the surface of such silicates that bind the calcium positive ions via ionic exchange with the zeolite negative ions
Summary
Osteoporosis is a systemic skeleton disease, characterized by a reduction of bone mass and a deterioration of bone tissue microarchitecture, with consequent increase of frailty and liability to fracturing, mostly of hip bone, back bone, or wrist bone. [1,2,3]. To prevent osteoporosis, increasing serum calcium levels has been attempted by administering adequate calcium amounts [4,5,6]. The most common calcium supplements currently in use are carbonate, citrate, chloride, and gluconate calcium salts. Nutrients 2019, 11, 2467 calcium ion, release is only determined by the salt solubility in gastrointestinal fluids. Calcium supplements with or without vitamin D are useful, even essential, for those whose diet cannot include dairy products. Calcium is actively absorbed in duodenum and proximal jejunum via carriers, the synthesis of which is stimulated by vitamin D. It is absorbed passively via the paracellular route in the whole intestine, including, though minimally, the colon [7]. Calcium transport via the paracellular route is not influenced by vitamin D, rather, it only depends on calcium solubility, chimo transit time over the intestine, and calcium paracellular permeability [8]
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