RESUMO
Curcumin (CUR) is one natural bioactive compound acknowledged for diverse therapeutic activities, but its use is hindered by its poor bioavailability, fast metabolism, and susceptibility to pH variations and light exposure. Thus, the encapsulation in poly(lactic-co-glycolic acid), or PLGA, has been successfully used to protect and enhance CUR absorption in the organism, making CUR-loaded PLGA nanoparticles (NPs) promising drug delivery systems. However, few studies have focused beyond CUR bioavailability, on the environmental variables involved in the encapsulation process, and whether they could help obtain NPs of superior performance. Our study evaluated pH (3.0 or 7.0), temperature (15 or 35 °C), light exposure, and inert atmosphere (N2) incidence in the encapsulation of CUR. The best outcome was at pH 3.0, 15 °C, without light incidence, and without N2 usage. This best nanoformulation showed NP size, zeta potential, and encapsulation efficiency (EE) of 297 nm, -21 mV, and 72%, respectively. Moreover, the CUR in vitro release at pH values 5.5 and 7.4 suggested different potential applications for these NPs, one of which was demonstrated by the effective inhibition of multiple bacteria (i.e., Gram-negative, Gram-positive, and multi-resistant) in the minimal inhibition concentration assay. Besides, statistical analyses confirmed a significant impact of temperature on the NP size; in addition, temperature, light, and N2 affected the EE of CUR. Thus, the selection and control of process variables resulted in higher CUR encapsulation and customizable outcomes, ultimately enabling more economical processes and providing future scale-up guidelines.
Assuntos
Curcumina , Nanopartículas , Curcumina/farmacologia , Curcumina/química , Copolímero de Ácido Poliláctico e Ácido Poliglicólico , Glicóis , Sistemas de Liberação de Medicamentos , Nanopartículas/química , Tamanho da Partícula , Portadores de Fármacos/químicaRESUMO
Curcumin (CUR) is a phenolic compound present in some herbs, including Curcuma longa Linn. (turmeric rhizome), with a high bioactive capacity and characteristic yellow color. It is mainly used as a spice, although it has been found that CUR has interesting pharmaceutical properties, acting as a natural antioxidant, anti-inflammatory, antimicrobial, and antitumoral agent. Nonetheless, CUR is a hydrophobic compound with low water solubility, poor chemical stability, and fast metabolism, limiting its use as a pharmacological compound. Smart drug delivery systems (DDS) have been used to overcome its low bioavailability and improve its stability. The current work overviews the literature from the past 10 years on the encapsulation of CUR in nanostructured systems, such as micelles, liposomes, niosomes, nanoemulsions, hydrogels, and nanocomplexes, emphasizing its use and ability in cancer therapy. The studies highlighted in this review have shown that these nanoformulations achieved higher solubility, improved tumor cytotoxicity, prolonged CUR release, and reduced side effects, among other interesting advantages.