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1.
Biomed Pharmacother ; 164: 114943, 2023 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-37267634

RESUMEN

In the present study, 5-fluorouracil-loaded niosomal nanoparticles were successfully prepared and coated with chitosan and subsequently crosslinked by tripolyphosphate to form niosomal nanogels. The prepared niosomal formulations were fully characterized for their particle size, zeta potential, particle morphology, drug entrapment efficiency, and in vitro drug release profile. The prepared niosomal nanocarriers exhibited nanoscale particle sizes of 165.35 ± 2.75-322.85 ± 2.75 nm. Chitosan-coated and TPP-crosslinked niosomes exhibited a slightly decreased in particle size and a switch of zeta potential from negative to positive values. In addition, high yield percentage, drug encapsulation efficiency, and drug loading values of 92.11 ± 2.07 %, 66.59 ± 6.06, and 4.65 ± 0.5 were obtained for chitosan-coated formulations, respectively. Moreover, lowering the rate of 5-FU in vitro release was achieved within 72 h by using chitosan-coated formulations. All prepared formulations revealed hemocompatible properties in hemolysis assay with less than 5 % hemolysis percentage at their higher possible concentrations (500 µM and 1 mM). The cell viability by MTT assay showed higher anticancer activity against B16F10 cancerous cells and lower cytotoxicity toward NIH3T3 normal cells than control and pure 5-FU in the studied concentration range (10-100 µM). Investigating the cell migration inhibition properties of fabricated formulations revealed similar results with in vitro cell viability assay with a higher migration inhibition rate for B16F10 cells than NIH3T3 cells, controls, and free 5-FU.


Asunto(s)
Quitosano , Nanopartículas , Ratones , Animales , Nanogeles , Preparaciones de Acción Retardada , Portadores de Fármacos , Hemólisis , Células 3T3 NIH , Fluorouracilo/farmacología , Antimetabolitos , Concentración de Iones de Hidrógeno , Tamaño de la Partícula
2.
Curr Pharm Des ; 26(42): 5468-5487, 2020.
Artículo en Inglés | MEDLINE | ID: mdl-32851955

RESUMEN

Flavonoids are secondary metabolites that are widely distributed in plants. These phenolic compounds are classified into various subgroups based on their structures: flavones, flavonols, isoflavones, flavanones, and anthocyanins. They are known to perform various pharmacological actions like antioxidant, anti-inflammatory, anticancer, antimicrobial, antidiabetic and antiallergic, etc. Diabetes is a chronic progressive metabolic disorder that affects several biochemical pathways and leads to secondary complications such as neuropathy, retinopathy, nephropathy, and cardiomyopathy. Among them, the management of diabetic neuropathy is one of the major challenges for physicians as well as the pharmaceutical industries. Naturally occurring flavonoids are extensively used for the treatment of diabetes and its related complications due to their antioxidant properties. Moreover, flavonoids inhibit various pathways that are involved in the progression of diabetic neuropathy like the reduction of oxidative stress, decrease in glycogenolysis, increase glucose utilization, decrease in the formation of advanced glycation end products, and inhibition of the α-glucosidase enzyme. This review entails current updates on the therapeutic perspectives of flavonoids in the treatment of neuropathic pain. This manuscript explains the pathological aspects of neuropathic pain, the chemistry of flavonoids, and their application in amelioration of neuropathic pain through preclinical studies either alone or in combination with other therapeutic agents.


Asunto(s)
Diabetes Mellitus , Neuropatías Diabéticas , Antioxidantes/farmacología , Neuropatías Diabéticas/tratamiento farmacológico , Flavonoides/farmacología , Humanos , Hipoglucemiantes/farmacología , Hipoglucemiantes/uso terapéutico , Estrés Oxidativo
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