Abstract
The intercalation of cetirizine into two types of layered double hydroxides, Zn/Al and Mg/Al, has been investigated by the ion exchange method to form CTZAN and CTMAN nanocomposites, respectively. The basal spacing of the nanocomposites were expanded to 31.9 Å for CTZAN and 31.2 Å for CTMAN, suggesting that cetirizine anion was intercalated into Layered double hydroxides (LDHs) and arranged in a tilted bilayer fashion. A Fourier transform infrared spectroscopy (FTIR) study supported the formation of both the nanocomposites, and the intercalated cetirizine is thermally more stable than its counterpart in free state. The loading of cetirizine in the nanocomposite was estimated to be about 57.2% for CTZAN and 60.7% CTMAN. The cetirizine release from the nanocomposites show sustained release manner and the release rate of cetirizine from CTZAN and CTMAN nanocomposites at pH 7.4 is remarkably lower than that at pH 4.8, presumably due to the different release mechanism. The inhibition of histamine release from RBL2H3 cells by the free cetirizine is higher than the intercalated cetirizine both in CTZAN and CTMAN nanocomposites. The viability in human Chang liver cells at 1000 μg/mL for CTZAN and CTMAN nanocomposites are 74.5 and 91.9%, respectively.
Highlights
Pharmaceutical science usually suffers from short time release of the active compounds in the body to maintain the therapeutic window
During ion-exchange nitrate anions, the d- spacing of inorganic layers, Zn/Al- and Mg/Al-Layered double hydroxides (LDHs), which are 9.01 and 8.2 Å, respectively was expanded for the host cetirizine anions
This result may be due to the small amount of cetirizine made available for the RBL-2H3 cells study from CTZAN and CTMAN nanocomposites, due to their controlled release property
Summary
Pharmaceutical science usually suffers from short time release of the active compounds in the body to maintain the therapeutic window. Sustained release of drug for more effective delivery systems have received intense attention in recent years from the pharmaceutical industry due to the advantages they offer over conventional forms [1]. LDH has 2-D, positively-charged layers which are produced from the isomorphous substitution of magnesium cations by trivalent cations in a brucite structure. Each hydroxide is bonded to three magnesium atoms, resulting in neutral layer structure. To neutralize the positive charge of LDH structure, counter anions are intercalated between the interlayers which give the hydrotalcite-like structure with the general formula M. Antihistamine drugs prevent histamine release by displacement from the receptor. Cetirizine dihydrochloride ((2-1-piperazinyl ethoxy) acetic acid) is one of a second-generation of antihistamines which can inhibit histamine release by blocking the H1 receptor. We report here the study of the effect of the resulting nanocomposites on the histamine release from RBL2H3 cells as well as their LDH counterparts, Zn/Al- and Mg/Al-LDH
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