Potential Application of A Synthetic Organo-funtionalized High Load Expandable Mica as A Drug Carrier for Controlled Release.

BACKGROUND: In this work the cytotoxicity and gastric and gastrointestinal resistance of a high-load synthetic expandable mica, Na-mica-4, is studied for the first time. The hydrophilic character of this clay mineral can be modified by ion exchange reaction between Na+ inorganic cations housed in the interlayer space, and surfactant molecules, resulting in the formation of an organophilic material. This adsorption capability of organic compounds makes them very useful for a wide range of applications, such as their use as drug carriers. Previous studies have shown the high adsorption capacity of organofunctionalized Na-mica-4 of different types of drugs. Objetive: To carry out initial trials aimed at testing the cytotoxicity of a synthetic organofunctional expandable mica and evaluating its resistance to gastric and gastrointestinal digestion. METHODS: A highly charged sodium mica (Na-mica-4) was synthesized and organofunctional by cationic exchange with an alkylamine, primary amine of 18 carbon atoms (C18-mica-4). Both were characterized by X-ray diffraction, field transmission electron microscopy, surface-specific analysis, differential scanning calorimetry, and thermal gravimetric analysis. In addition, screening cytotoxicity trials were conducted on the human intestinal cell line Caco-2 with C18-mica-4 (0-125 µg/ml). RESULTS: Only one of the endpoints evaluated (the reduction of tetrazolium MTS salt by dehydrogenase enzymes) showed a significant decrease in cellular viability after 48h at the highest concentration tested. C18-mica-4 shows structural resistance to both, gastric and gastrointestinal, digestion. CONCLUSION: A successful development of a functionalized mica has been made with a promising potential application as a carrier to the drug.

Synthetic high-charge organomica: effect of the layer charge and alkyl chain length on the structure of the adsorbed surfactants.

A family of organomicas was synthesized using synthetic swelling micas with high layer charge (Na(n)Si(8-n)Al(n)Mg(6)F(4)O(20)·XH(2)O, where n = 2, 3, and 4) exchanged with dodecylammonium and octadecylammonium cations. The molecular arrangement of the surfactant was elucidated on the basis on XRD patterns and DTA. The ordering conformation of the surfactant molecules into the interlayer space of micas was investigated by (13)C, (27)Al, and (29)Si MAS NMR. The arrangement of alkylammonium ions in these high-charge synthetic micas depends on the combined effects of the layer charge of the mica and the chain length of the cation. In the organomicas with dodecylammonium, a transition from a parallel layer to a bilayer-paraffin arrangement is observed when the layer charge of the mica increases. However, when octadecylammonium is the interlayer cation, the molecular arrangement of the surfactant was found to follow the bilayer-paraffin model for all values of layer charge. The amount of ordered conformation all-trans is directly proportional of layer charge.

Formation of organo-highly charged mica.

The interlayer space of the highly charged synthetic Na-Mica-4 can be modified by ion-exchange reactions involving the exchange of inorganic Na(+) cations by surfactant molecules, which results in the formation of an organophilic interlayer space. The swelling and structural properties of this highly charged mica upon intercalation with n-alkylammonium (RNH(3))(+) cations with varying alkyl chain lengths (R = C12, C14, C16, and C18) have been reported. The stability, fine structure, and evolution of gaseous species from alkylammonium Mica-4 are investigated in detail by conventional thermogravimetric analysis (TGA), Fourier transform infrared spectroscopy (FTIR), in situ X-ray diffraction (XRD), and solid-state nuclear magnetic resonance (MAS NMR) techniques. The results clearly show the total adsorption of n-alkylammonium cations in the interlayer space which expands as needed to accommodate intercalated surfactants. The surfactant packing is quite ordered at room temperature, mainly involving a paraffin-type bilayer with an all-trans conformation, in agreement with the high density of the organic compounds in the interlayer space. At temperatures above 160 °C, the surfactant molecules undergo a transformation that leads to a liquid-like conformation, which results in a more disordered phase and expansion of the interlayer space.