Novel albendazole–chitosan nanoparticles for intestinal absorption enhancement and hepatic targeting improvement in rats

Abstract

To improve the treatment of helminthiasis, filariasis, and colorectal cancer, albendazole-associated chitosan nanoparticles (ABZ-CS-NPs) were prepared using the emulsion crosslinking volatile technique with contained sodium tripolyphosphate as the crosslinking agent and Poloxamer 188 as the auxiliary solvent. The structural characteristics of the NPs were determined using X-ray diffraction to analyze the interaction between CS and the drug. The NPs were then evaluated in terms of their physicochemical characteristics, drug release behavior, in vivo pharmacokinetic parameters, and biodistribution in animal studies. ABZ-loaded NPs with a uniformly spherical particle sizes (157.8 ± 2.82 nm) showed efficient drug loading, encapsulated efficiency, and high physical stability. The drug release from ABZ-CS-NPs was extended over several periods. Kinetic models were then fitted to determine the release mechanisms. ABZ and its metabolite albendazole sulfoxide (ABZSX) were analyzed in rats with mebendazole as the internal standard using reversed-phase high-performance liquid chromatography. Compared with the ABZ suspension groups, the relative bioavailability values of ABZ and ABZSX were 146.05 and 222.15%, respectively. In addition, the plasma concentration versus time curve is consistent with that of the two compartment models in the plasma concentration versus time curve. The results indicate that the ABZ-loaded NPs are promising novel ABZ candidates for passive diffusion in the treatment of hydatid cysts in the liver via oral administration.

Chitosan-based nanodelivery systems applied to the development of novel triclabendazole formulations

“…In Table 1 are shown the summary of the characteristics of the loaded and unloaded NCs and NEs, including the association efficiency and loading capacity. The association efficiency values determined correspond well with those measured in previous studies using chitosan-tripolyphosphate nanoparticles that lied in the range of 79.57 ± 0.96% and 13.38 ± 0.44% for the loading capacity [37].…”

Solid Polymeric Nanoparticles of Albendazole: Synthesis, Physico-Chemical Characterization and Biological Activity

“…Marslin et al reported in 2017 the preparation of ABZ-loaded solid lipid nanoparticles (SLN) which induced the slow release of the drug over a 24 h time period in phosphate buffer (pH = 7.4) reaching an 82% cumulative drug release [15]. Another study was published by Liu et al in 2013 regarding the synthesis of ABZ-loaded chitosan nanoparticles which were tested in acidic, slightly acid and neutral environments, respectively; the chitosan-nanoparticles revealed a similar behavior to our nanoformulations with the drug's highest dissolution in acid medium and a sustained release of the drug following encapsulation [69]. Similar results were also reported by Panwar et al in 2010 who prepared ABZ-loaded liposomes which revealed the sustained release of the drug over a 4.5 h period in slightly acid phosphate buffer (pH = 5.6) [70].…”

Study on Optimization of Wet Milling Process for the Development of Albendazole Containing Nanosuspension with Improved Dissolution

“…1). Our goal was to prepare ABZ nanocrystals with size distribution parameters similar to those, produced by novel modified variant of the so-called emulsion crosslinking volatile method [33,34].…”