Nanosuspensions as carriers of active ingredients: Chemical composition, development methods, and their biological activities.

Nanosuspensions (NSps) are colloidal dispersions of particles that have the potential to solve the delivery problems of active ingredients associated with their low solubility in water or instability due to environmental factors. It is essential to consider their chemical composition and preparation methods because they directly influence drug loading, size, morphology, solubility, and stability; these characteristics of nanosuspensions influence the delivery and bioavailability of active ingredients. NSps provides high loading of drugs, protection against degrading agents, rapid dissolution, high particle stability, and high bioavailability of active ingredients across biological membranes. In addition, they provide lower toxicity compared to other nanocarriers, such as liposomes or polymeric nanoparticles, and can modify the pharmacokinetic profiles, thus improving their safety and efficacy. The present review aims to address all aspects related to the composition of NSps, the different methods for their production, and the main factors affecting their stability. Moreover, recent studies are described as carriers of active ingredients and their biological activities.

Formulation and characterisation of Azadirachta indica nanobiopesticides for ecofriendly control of wheat pest Tribolium castaneum and Rhyzopertha dominica.

This study aimed to formulate the green, sustainable, and ecofriendly nanobiopesticides of Azadirachta indica with enhanced pest control efficacy. Nanoprecipitation method was used for the development of nanobiopesticides. Optimisation was done by response surface methodology. Nanoformulations were characterised by zetasizer, scanning electron microscopy, energy dispersive x-ray spectroscopy, atomic force microscopy, and Fourier transform infrared spectroscopy. Pesticidal potential of nanosuspensions was evaluated by insecticide impregnated filter paper method. Optimised nanobiopesticide showed an average particle size of 275.8 ± 0.95 nm, polydispersity index (PDI) 0.351 ± 0.002, and zeta potential of -33 ± 0.90 mV. Nanobiopesticides exhibited significantly higher mortality rates of 86.81 ± 3.04 and 84.97 ± 2.83% against Tribolium castaneum and Ryzopertha dominica, respectively, as compared to their crude extract. Minor change in particle size from 275.8 ± 0.95 to 298.8 ± 1.00 nm and PDI from 0.351 ± 0.002 to 0.445 ± 0.02 were observed after 3 months of storage at 4 °C. Pesticidal efficacy of A. indica was significantly enhanced by the formulation of its nanobiopesticides.

Design and in vitro characterization of ivermectin nanocrystals liquid formulation based on a top-down approach.

The aim of this study was to develop ivermectin (IVM) nanosuspensions (NSs) to improve the dissolution rate of this poorly water-soluble drug. Different NSs combining different stabilizers, i.e. poloxamer 188 (P188), polysorbate 80 (T80), polyvinylpyrrolidone (PVP), and sodium lauryl sulfate (SLS), were prepared by high-pressure homogenization. The stabilizers were selected based on the saturation solubility and IVM stability within 72 h. The screening of formulations was performed by considering the drug content within the nanosize range. The best formulation (IVM:T80:PVP 1:0.5:0.5 wt%) was characterized in terms of the particle size distribution, morphology, crystallinity, drug content, and in vitro dissolution profile. This NS was also evaluated from a stability point of view, by conditioning samples at a constant temperature and relative humidity for six months. The fresh and conditioned best NSs Z-sizes were 174.6 and 215.7 nm, respectively; while both NSs showed low polydispersity indexes. The faster dissolution rate for the IVM NS was attributed to the presence of nanoparticles and changes to the crystal structure (i.e. amorphization) that further improved solubility. The best NS had a 4-fold faster initial dissolution rate than raw IVM, and is thus a promising formulation for the treatment of human and animal parasitic diseases.

Elucidating the influence of praziquantel nanosuspensions on the in vivo metabolism of Taenia crassiceps cysticerci.

The aim of this work was to develop nanosuspensions of praziquantel (PZQ) and to evaluate their influence on the energetic metabolism of cysticerci inoculated in BALB/c mice. We analyzed metabolic alterations of glycolytic pathways and the tricarboxylic acid cycle in the parasite. The nanosuspensions were prepared by precipitation and polyvinyl alcohol (PVA), poloxamer 188 (P188) and poloxamer 407 (P407) were used as stabilizers. Nanosuspension prepared with PVA had a particle size of 100nm, while P188- and P407-based nanosuspensions had particle sizes of 74nm and 285nm, respectively. The zeta potential was -8.1, -8.6, and -13.2 for the formulations stabilized with PVA, P188 and P407, respectively. Treatments of T. crassiceps cysticerci-infected mice resulted in an increase in glycolysis organic acids, and enhanced the partial reversion of the tricarboxylic acid cycle, the urea cycle and the production of ketonic bodies in the parasites when compared to the groups treated with conventional PZQ. These data suggest that PZQ nanosuspensions greatly modified the energetic metabolism of cysticerci in vivo. Moreover, the remarkable metabolic alterations produced by the stabilizers indicate that further studies on nanoformulations are required to find potentially suitable nanomedicines.