Diphenyl Diselenide-Loaded Nanocapsules: Preparation and Biological Distribution

Abstract

Over the past years, organoselenium compounds have been aimed as targets of interest in organic synthesis. Diphenyl diselenide [(PhSe)2] is an important example of this class showing several pharmacological properties. However, the poor water-solubility and its low oral bioavailability may be considered an obstruction for the clinical utility of this compound. For this reason, the use of nanocapsules is a prominent approach to increase the bioavailability of lipophylic molecules. This study aims to prepare diphenyl diselenide-loaded nanocapsules with two different concentrations, by interfacial deposition of the preformed polymer in order to develop a system to improve its oral bioavailability. The drug-loaded nanocapsules with 1.56 and 5 mg ml−1 and unloaded nanocapsule suspensions presented macroscopic homogeneous aspect, as well as submicronic sizes, low polydispersity, negative zeta potentials and slightly acid or neutral pH values. The biological tests of selenium distribution in different tissues of mice show a higher bioavailability of the (PhSe)2 nanocapsules when compared with the free (PhSe)2, both administered by per oral route at the dose of 50 mg/kg, showing a prominent influence of the nanocarries systems for biological properties of this organochalcogenium compound.

Free radical scavenging in vitro and biological activity of diphenyl diselenide-loaded nanocapsules: DPDS-NCS antioxidant and toxicological effects

“…13 In addition, our results established that DPDS-NCS in all tested doses did not present any significant effect on the GSH and GSSG levels in the brain and liver, indicating that even if the thiol groups of the compound are oxidized, normal levels can reestablished.…”

“…9,24 Additionally, DPDS-NCS was previously characterized as macroscopic homogeneous aspect, as well as submicronic sizes, low polydispersity indices, negative zeta potentials, and slightly acid or neutral pH values. 13 Giordani et al also demonstrated that nanoencapsulation improves the DPDS-NCS pharmacokinetics when compared to the free DPDS.…”

“…DPDS-NCS were prepared by dissolving DPDS in the organic solution during the preparation of the nanocapsules, according to the method described by Giordani et al 13 …”

“…The pH values were determined using a Digimed DM-20 calibrated potentiometer (Digimed, São Paulo, SP, Brazil). The encapsulation efficiency was determined by high-performance liquid chromatography as described by Giordani et al 13 animals Male adult swiss albino mice (25-30 g) were used. They were obtained from a local breeding colony.…”

“…12 Studies have shown that DPDS-loaded-nanocapsules (DPDS-NCS) have greater bioavailability than free DPDS in mice, which suggests an increase in drug absorption after nanoencapsulation. 13 However, DPDS-NCS antioxidant effects and the toxicity in mice remain unknown. Thus, the present study was designed to evaluate the antioxidant properties of DPDS-NCS against the generation of reactive oxygen or nitrogen species (ROS and RNS) in vitro and ex vivo and the biological effects following 72-hour exposure of DPDS-NCS exposure in mice.…”