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1.
In Silico Pharmacol ; 12(2): 81, 2024.
Artículo en Inglés | MEDLINE | ID: mdl-39233909

RESUMEN

To evaluate the therapeutic potential of curcumin tagged cilostazol solid nano dispersion in wistar rat streptozotocin-nicotinamide-induced diabetic nephropathy. Cilostazol (CLT), a Phosphodiesterase (PDE) inhibitor has an inhibitory effect on reactive oxygen species (ROS), and Curcumin (Cur), an antioxidant, and anti-inflammatory, are water-soluble. Solid Nano dispersions were developed using the "Box-Behnken Design" and emulsion solvent evaporation procedure to improve the solubility and bioavailability. Streptozotocin (SPZ) and Nicotinamide (NA) caused diabetes in Wistar rats. DN developed 30-45 days after disease induction. All rat groups underwent histological, biochemical and pharmacokinetic evaluation. The optimized batch of Cilostazol Loaded Novel Curcumin Tagged Solid Nanodispersion (CLT-15 SND) estimated renal, lipid, and cytokine profiles better than the conventional batch. CLT-15 SND, given orally to diabetic rats for 45 days, significantly lowered fasting BGL and IL-6 levels and improved lipid and kidney-profile markers and body weight compared to plain Cilostazol Loaded Solid Nanodispersion (CLT-15 WC SND). CLT-15 SND treatment groups showed decreased blood glucose by 3.38 and 9.71 percent, increased body weight by 2.81 and 5.27 percent, improved Interleukin-6 (IL-6) by 21.36 and 18.36 percent, improved urine albumin levels by 5.67 and 14.19 percent and creatinine levels by 3.125 and 37.5 percent, improved serum urea by 30.48 percent, increased serum albumin by 2.59 and 11.18 percent, and decreased creatinine and 5.03 and 8.12 percent, respectively as compared to CLT-15 WC and MP treatment animal groups. CLT and Cur reduced IL-6, kidney, and lipid markers, demonstrating their renoprotective and pancreas-protective effects. CLT and Cur's inhibition may be the mechanism.

2.
Pestic Biochem Physiol ; 201: 105897, 2024 May.
Artículo en Inglés | MEDLINE | ID: mdl-38685223

RESUMEN

Solid nanodispersion (SND) is an important variety of nanopesticides which have been extensively studied in recent years. However, the key influencing factors for bioactivity enhancement of nanopesticides remain unclear, which not only limits the exploration of relevant mechanisms, but also hinders the precise design and development of nanopesticides. In this study, we explored the potential of SND in enhancing the bioactivity of nanopesticides, specifically focusing on abamectin SND prepared using a self-emulsifying-carrier solidifying technique combined with parameter optimization. Our formulation, consisting of 8% abamectin, 1% antioxidant BHT (2,6-di-tert-butyl-4-methylphenol), 12% complex surfactants, and 79% sodium benzoate, significantly increased the pseudo-solubility of abamectin by at least 3300 times and reduced its particle size to a mere 15 nm, much smaller than traditional emulsion in water (EW) and water-dispersible granule (WDG) forms. This reduction in particle size and increase in surface activity resulted in improved foliar adhesion and retention, enabling a more efficient application without the need for organic solvents. The inclusion of antioxidants also enhanced photostability compared to EW, and overall stability tests confirmed SND's resilience under various storage conditions. Bioactivity tests demonstrated a marked increase in toxicity against diamondback moths (Plutella xylostella L.) with abamectin SND, which exhibited 3.7 and 7.6 times greater efficacy compared to EW and WDG, respectively. These findings underscore the critical role of small particle size, high surface activity, and strong antioxidant properties in improving the performance and bioactivity of abamectin SND, highlighting its significance in the design and development of high-efficiency, eco-friendly nanopesticides and contributing valuably to sustainable agricultural practices.


Asunto(s)
Ivermectina , Ivermectina/análogos & derivados , Ivermectina/farmacología , Ivermectina/química , Animales , Insecticidas/farmacología , Insecticidas/química , Tamaño de la Partícula , Antioxidantes/farmacología , Antioxidantes/química , Nanopartículas/química , Mariposas Nocturnas/efectos de los fármacos , Tensoactivos/farmacología , Tensoactivos/química , Larva/efectos de los fármacos , Emulsiones
3.
Drug Discov Ther ; 14(6): 296-303, 2020.
Artículo en Inglés | MEDLINE | ID: mdl-33487621

RESUMEN

Oligo L-lactates (oligolactates) that have low molecular weights less than 2000 have been reported to inhibit tumor growth and extend the survival of experimental animals. Because oligolactates are scarcely soluble in water, they require a solvent or a solubilizing agent, such as a surfactant, to be dissolved in water. However, these agents are generally cytotoxic, an in vitro assay appropriate to evaluate the inhibitory effect on tumor growth has not been developed yet. Here, we prepared a solid nanodispersion of oligolactates using an oil-in-water emulsion solvent evaporation method to evaluate its tumor inhibitory activity in vitro without a solvent or surfactant. Polyol solutions containing polyvinyl alcohol (PVA) were used as a continuous phase. The formation of nanoparticles depended on the concentrations of polyol and PVA in the continuous phase. The nanoparticles with a particle size of approximately 100 nm were obtained using 10-15% PVA and 60% propylene glycol. The obtained aqueous nanodispersion of oligolactates inhibited the growth of B16-BL6 melanoma cells in vitro, whereas the medium alone did not affect tumor cell growth. Therefore, oligo(L-lactate) nanoparticles may be useful in the research and development of oligolactates as a remedy for cancer.


Asunto(s)
Antineoplásicos/administración & dosificación , Portadores de Fármacos/química , Lactatos/administración & dosificación , Melanoma/tratamiento farmacológico , Neoplasias Cutáneas/tratamiento farmacológico , Animales , Línea Celular Tumoral , Modelos Animales de Enfermedad , Composición de Medicamentos/métodos , Ensayos de Selección de Medicamentos Antitumorales , Emulsiones , Humanos , Melanoma/patología , Ratones , Nanopartículas/química , Tamaño de la Partícula , Polímeros/química , Alcohol Polivinílico/química , Neoplasias Cutáneas/patología
4.
Pest Manag Sci ; 75(2): 380-389, 2019 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-29923675

RESUMEN

BACKGROUND: Pesticide is an important agricultural necessity to control plant diseases and pests, ensuring safe production of food. However, the low efficacy, large dosage and high-frequency use of conventional pesticide formulation seriously induced food safety and ecological environment issues. In this research, lambda-cyhalothrin solid nanodispersion (LCSND) was developed by a self-dispersing method. RESULTS: The mean particle size of the lambda-cyhalothrin solid nanodispersion was 32.7 ± 1.1 nm. It exhibited excellent dispersibility, wettability and stability, especially the improved bioavailability compared to the commercial formulations. Notably, the solid nanodisperison had a small particle size and large specific surface area. The solid nanodispersion without organic solvents can minimize the environment pollution and overcome the instability characteristic of the liquid formulations. CONCLUSION: Therefore, lambda-cyhalothrin solid nanodispersion has broad application prospects in agricultural production and environmental protection. © 2018 Society of Chemical Industry.


Asunto(s)
Fungicidas Industriales/química , Insecticidas/química , Nanopartículas/química , Nitrilos/química , Tamaño de la Partícula , Control de Plagas/instrumentación , Piretrinas/química , Disponibilidad Biológica , Control de Insectos/instrumentación , Solubilidad , Humectabilidad
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