In vitroevaluation of antioxidant and neuroprotective effects of curcumin loaded in Pluronic micelles

Abstract

Curcumin is a polyphenolic substance with attractive pharmacological activities (e.g. antioxidant, anti-inflammatory, anticancer). Incorporation of curcumin in polymeric micelles could overcome the problems associated with its instability and low aqueous solubility. The aim of this study was to load curcumin in polymeric micelles based on Pluronic Ò P 123 or Pluronic Ò F 127 triblock copolymers and evaluate the antioxidant and neuroprotective effects after micellization. The micelles were prepared and loaded with curcumin by applying the dissolution method. Higher encapsulation efficiency was observed in the micelles formulated with Pluronic Ò P 123. These micelles were characterized with small size and narrow size distribution. The effects of micellar curcumin were investigated in two in vitro models. First, the capacity of micellar curcumin to inhibit iron/ascorbic acid-induced lipid peroxidation in rat liver microsomes was evaluated. Micellar curcumin and free drug showed similar inhibition of lipid peroxidation. Second, micellar curcumin and free curcumin showed protective potential in a model of 6-hydroxydopamine induced neurotoxicity in rat brain synaptosomes. The results from both methods indicated preservation of antioxidant and neuroprotective activity of curcumin in micelles. The small micellar size, high loading capacity and preservation of antioxidant activity of curcumin into Pluronic micelles, suggested their further evaluation as a curcumin delivery system.

Microfluidic Processing Approach to Controlling Drug Delivery Properties of Curcumin-Loaded Block Copolymer Nanoparticles

“…33,35,36 In response to these challenges, numerous researchers have investigated CUR encapsulation in the hydrophobic cores of block copolymer PNPs. [36][37][38][39][40][41][42][43][44][45][46][47][48][49][50][51][52][53][54][55] These studies have shown that CUR encapsulation promotes improved aqueous dispersion, increased chemical stability, and more sustained release compared to free CUR. In vivo studies have additionally shown that CURloaded PNPs (CUR-PNPs) show enhanced bioavailability, improved distribution in the body, and promising antitumor activity compared to the unencapsulated drug.…”

“…In response to these challenges, numerous researchers have investigated CUR encapsulation in the hydrophobic cores of block copolymer PNPs. − These studies have shown that CUR encapsulation promotes improved aqueous dispersion, increased chemical stability, and more sustained release compared to free CUR. In vivo studies have additionally shown that CUR-loaded PNPs (CUR-PNPs) show enhanced bioavailability, improved distribution in the body, and promising antitumor activity compared to the unencapsulated drug. ,, CUR-PNPs are typically prepared using conventional self-assembly approaches, such as nanoprecipitation, thin film hydration, or dialysis, in which intermolecular forces alone are responsible for the size, structure, and drug delivery properties of the resulting colloids.…”

Encapsulation of Quercetin in a Mixed Nanomicellar System to Enhance its Cytotoxicity against Breast Cancer Cells

“…The average hydrodynamic size of mixed micelles was found to be 22.1 nm with an acceptable value of polydispersity index (PDI) of 0.2, indicating a narrow size distribution of prepared nanomicelles. The surface charge of mixed nanomicelles, measured by zeta potential analysis, was –7.63 ± 0.56 mV, which is in the range of the surface charge of Pluronic micelles 42.…”

Encapsulation of Quercetin in Tri-Block-Copolymer/Tween 80 Mixed Nanomicelles to Enhance its Cytotoxicity Against Breast Cancer Cells

“…The average hydrodynamic size of mixed micelles was measured to be 22.1 nm with acceptable value of polydispersity index (PDI) of 0.2, indicating a narrow size distribution of prepared nanomicelles. The surface charge of mixed nanomicelles, measured by zeta potential analysis, was -7.63 ± 0.56 mV, which is in the range of surface charge of pluronic micelles [17].…”

“…One of the best ways to enhance the water solubility and chemical stability of quercetin is its encapsulation into polymeric micelles [12]. Generally, encapsulation of hydrophobic drugs by polymeric micelles has been preferred as an e cient drug delivery system against many diseases [13][14][15][16][17].…”