Abstract
We have successfully prepared layered double hydroxide (LDH) nanomaterials containing calcium and aluminum ions in the framework (CaAl-LDH). The surface of CaAl-LDH was coated with enteric polymer, Eudragit®L 100 in order to protect nanomaterials from fast dissolution under gastric condition of pH 1.2. The X-ray diffraction patterns, Fourier transform infrared spectroscopy, scanning electron and transmission electron microscopy revealed that the pristine LDH was well prepared having hydrocalumite structure, and that the polymer effectively coated the surface of LDH without disturbing structure. From thermal analysis, it was determined that only a small amount (less than 1%) of polymer was coated on the LDH surface. Metal dissolution from LDH nanomaterials was significantly reduced upon Eudragit®L 100 coating at pH 1.2, 6.8 and 7.4, which simulates gastric, enteric and plasma conditions, respectively, and the dissolution effect was the most suppressed at pH 1.2. The LDH nanomaterials did not exhibit any significant cytotoxicity up to 1000 μg/mL and intracellular calcium concentration significantly increased in LDH-treated human intestinal cells. Pharmacokinetic study demonstrated absorption efficiency of Eudragit®L 100 coated LDH following oral administration to rats. Moreover, the LDH nanomaterials did not cause acute toxic effect in vivo. All the results suggest the great potential of CaAl-LDH nanomaterials as a calcium supplement.
Highlights
Along with the rapid development of nanotechnology in diverse industrial fields, nanomaterials have been widely applied to bio-related products, such as medicine, medical devices, pharmaceutics, personal care products, food etc. to endow a novel physicochemical property, to enhance functionality, bioactivity and bioavailability, and to effectively deliver bioactive molecules to target specific organs [1,2,3,4]
The crystal structure of pristine CaAl-layered double hydroxide (LDH) was confirmed with powder X-ray diffraction (XRD)
We demonstrated the potential of polymer-coated CaAl-LDH as a calcium supplement
Summary
Along with the rapid development of nanotechnology in diverse industrial fields, nanomaterials have been widely applied to bio-related products, such as medicine, medical devices, pharmaceutics, personal care products, food etc. to endow a novel physicochemical property, to enhance functionality, bioactivity and bioavailability, and to effectively deliver bioactive molecules to target specific organs [1,2,3,4]. As a potential candidate for calcium supplement nanomaterials, we developed layered double hydroxide (LDH) nanoparticle, a kind of layered mineral. Due to the diversity of exchangeable anions, intercalation capacity and biological inertness, LDHs have been explored as delivery nanovehicles for drugs and bioactive molecules [19,20]. LDHs have been reported to enhance cellular uptake rate as well as chemical/biological stability of intercalated biomolecules [21,22]. LDHs are expected to be dissolved into absorbable ions under gastric (pH~1.2) and small intestine (pH~6.8) conditions. Incorporation of bioactive molecules into calcium containing LDHs further enables the development of a dual functional system having both calcium supplement and delivery functions. The Eudragit®L 100 coating can protect LDH from acidic gastric conditions, and help to dissolve LDH in small intestine. Its cellular calcium uptake, pharmacokinetics and in vitro and in vivo toxicity were evaluated
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