Abstract
Carbamazepine (CBZ) was incorporated into layered double hydroxides (LDH) to be used as a controlled drug system in solid tumors. CBZ has a formal charge of zero, so its incorporation in the anionic clay implies a challenge. Aiming to overcome this problem, CBZ was loaded into LDH with sodium cholate (SC), a surfactant with negative charge and, for comparison, without SC by the reconstruction method. Surprisingly, it was found that both resultant nanocomposites had similar CBZ encapsulation efficiency, around 75%, and the LDH-CBZ system without SC showed a better performance in relation to the release kinetics of CBZ in simulated body fluid (pH 7.4) and acetate buffer simulating the cellular cytoplasm (pH 4.8) than the system with SC. The CBZ dimensions were measured with Chem3D and, according to the basal spacing obtained from X-ray patterns, it can be arranged in the LDH-CBZ system as a monolayer with the long axis parallel to the LDH layers. Fourier transform infrared spectroscopy and solid state NMR measurements confirmed the presence of the drug, and thermogravimetric analyses showed an enhanced thermal stability for CBZ. These results have interesting implications since they increase the spectrum of LDH application as a controlled drug system to a large number of nonionic drugs, without the addition of other components.
Highlights
Carbamazepine (CBZ) was incorporated into layered double hydroxides (LDH) to be used as a controlled drug system in solid tumors
We propose the use of a drug with potential anticancer activity that is not currently used as cytotoxic, with the increase of its activity and its selectivity by incorporating it in an inorganic solid, taking advantage of the LDH capability to avoid drug action during circulation and enhanced tumor cell penetration by clathrin endocytosis
Were measured with Chem3D 18.0 (Perkin Elmer) and are shown in Fig. 2a; Fig. 2c shows the way that CBZ might be accommodated into the LDH, taking into account that no superficial drug appeared in the diffractogram
Summary
Carbamazepine (CBZ) was incorporated into layered double hydroxides (LDH) to be used as a controlled drug system in solid tumors. Even with the advances in the last decades, there is still ample room for improvement since it produces many side effects[2,3] Another serious obstacle for effective anticancer drugs is their low solubility in water and low bioavailability; most of them require a vehicle to be carried in the organism. The empty LDH, of the hydrotalcite type, is currently commercially available and it is used as antacid for the treatment of stomach d iseases[18] Another challenge for modern medicine in the field of chemotherapy is to find novel anticancer drugs. CBZ produces alterations in red blood cells[27]
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