Effect of new Curcumin-containing nanostructured lipid dispersions on human keratinocytes proliferative responses (original) (raw)
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Nanoparticles containing curcuminoids (Curcuma longa): development of topical delivery formulation
Revista Brasileira de Farmacognosia, 2015
Solid lipid nanoparticles incorporating Curcuma longa L., Zingiberaceae, curcuminoids were produced by the hot melt emulsion method. A Box-Behnken factorial design was adopted to study the nanoparticles production at different levels of factors such as the percentage of curcuminoids, time of homogenization and surfactant ratio. The optimized nanoparticles were incorporated into hydrogels for stability, drug release and skin permeation tests. The average nanoparticle sizes were 210.4 nm; the zeta potential of −30.40 ± 4.16; the polydispersivity was 0.222 ± 0.125. The average encapsulation efficiency of curcumin and curcuminoids was 52.92 ± 5.41% and 48.39 ± 6.62%, respectively. Solid lipid nanocapsules were obtained with curcumin load varying from 14.2 to 33.6% and total curcuminoids load as high as 47.7%. The topical formulation containing SLN-Curcuminoids showed good spreadability and stability when subjected to mechanical stress test remained with characteristic color, showed no phase separation and no significant change in pH. As a result of slow release, the nanoparticles were able to avoid permeation or penetration in the pig ear epidermis/dermis during 18 h. The topical formulation is stable and can be used in further in vivo studies for the treatment of inflammatory reactions, in special for radiodermitis.
Drug development and industrial pharmacy, 2018
Tetrahydrocurcumin (THC) also referred to as "white curcumin", is a stable colourless hydrogenated product of curcumin with superior antioxidant and anti-inflammatory properties. Present study is an attempt to elevate the topical bioavailability of THC, post incorporation into a nano-carrier system with its final dosage as a hydrogel. Lipid nanoparticles of THC (THC-SLNs) prepared by microemulsification technique were ellipsoidal in shape (revealed in TEM) with a mean particle size of 96.6 nm and zeta potential of -22 mV. Total drug content and entrapment efficiency of THC-SLNs was 94.51% ± 2.15% and 69.56% ± 1.35%, respectively. DSC and X-Ray diffraction studies confirmed the formation of THC-SLNs. In vitro drug release studies showed the drug release from THC-SLNs gel to follow Higuchi's equation revealing a Fickian diffusion. Ex-vivo permeation studies indicated a 17 times (approximately) higher skin permeation of THC-SLNs gel as compared with the free THC gel. Skin...
Pharmaceutics
The external use of curcumin is rare, although it can be a valuable active ingredient in the treatment of certain inflammatory diseases. The aim of our experimental work was to formulate topical dosage forms containing curcumin for the treatment of atopic dermatitis. Curcumin has extremely poor solubility and bioavailability, so we have tried to increase it with the usage of self-emulsifying drug delivery systems. Creams and gels were formulated using penetration-enhancing surfactants and gelling agents. The release of the drug from the vehicle and its penetration through the membrane were determined using a Franz diffusion cell. An MTT cytotoxicity and in vitro antioxidant assays were performed on HaCaT cell line. The in vivo anti-inflammatory effect of the preparations was tested by measuring rat paw edema. In addition, we examined the degree of inflammation induced by UV radiation after pretreatment with the cream and the gel on rats. For the gels containing SNEDDS, the highest p...
Preparation of Lipid Nanoemulsions Incorporating Curcumin for Cancer Therapy
Journal of Nanotechnology, 2012
The aim of this study was to develop a new formulation of a curcumin lipid nanoemulsion having the smallest particle size, the highest loading, and a good physical stability for cancer chemotherapy. Curcumin lipid nanoemulsions were prepared by a modified thin-film hydration method followed by sonication. Soybean oil, hydrogenatedL-α-phosphatidylcholine from egg yolk, and cosurfactants were used to formulate the emulsions. The resultant nanoemulsions showed mean particle diameter of 47–55 nm, could incorporate 23–28 mg curcumin per 30 mL, and were stable in particle size for 60 days at 4°C. The cytotoxicity studies of curucumin solution and curcumin-loaded nanoemulsion using B16F10 and leukemic cell lines showed IC50values ranging from 3.5 to 30.1 and 22.2 to 53.7 μM, respectively. These results demonstrated the successful incorporation of curcumin into lipid nanoemulsion particles with small particle size, high loading capacity, good physical stability, and preserved cytotoxicity.
Pharmaceutics, 2019
Curcumin is a natural product with chemopreventive and other properties that are potentially useful in treating skin diseases, including psoriasis and melanoma. However, because of the excellent barrier function of the stratum corneum and the relatively high lipophilicity of curcumin (log P 3.6), skin delivery of curcumin is challenging. We used the principles of a Quality by Design (QbD) approach to develop nanoemulsion formulations containing biocompatible components, including Labrasol and Lecithin as surfactants and Transcutol and ethanol as cosurfactants, to enhance the skin delivery of curcumin. The nanoemulsions were characterised by cryo-SEM, Zeta potential, droplet size, pH, electrical conductivity (EC) and viscosity (η). Physicochemical long-term stability (6 months) was also investigated. The mean droplet sizes as determined by dynamic light scattering (DLS) were in the lower submicron range (20–50 nm) and the average Zeta potential values were low (range: −0.12 to −2.98 ...
Biomolecules
This work focuses on the development and evaluation of a dual nanostructured lipid carrier (NLC)/Carbopol®-based hydrogel system as a potential transporter for the topical delivery of curcumin to the skin. Two populations of different sized negatively charged NLCs (P1, 70–90 nm and P2, 300–350 nm) were prepared and characterized by means of dynamic light scattering. NLCs presented an ovoid platelet shape confirmed by transmission electron microscopy techniques. Curcumin NLC entrapment efficiency and release profiles were assessed by HPLC (high pressure liquid chromatography) and spectrophotometric methods. Preservation and enhancement of curcumin (CUR) antioxidant activity in NLCs (up to 7-fold) was established and cell viability assays on fibroblasts and keratinocytes indicated that CUR-NLCs are non-cytotoxic for concentrations up to 10 μM and exhibited a moderate anti-migration/proliferation effect (20% gap reduction). CUR-NLCs were then embedded in a Carbopol®-based hydrogel with...
Curcumin-Loaded Nanoemulsion for Better Cellular Permeation
Scientia Pharmaceutica
Curcumin nanoemulsion was prepared using coconut oil, Tween 80 (surfactant) and polyethylene glycol (co-solvent) with the addition of honey and glycerol as additives. The nanoemulsion was optimized and systematically characterized for transdermal delivery. Small particle size (15.92 nm), low polydispersity index (0.17) and slight acidic (pH 4.18) curcumin nanoemulsion was obtained without any chemical degradation based on the Fourier transform infrared (FTIR) spectrum. The incorporation of curcumin inside nanoglobul improved curcumin stability and skin permeability. Its high permeability can be seen from Nile dyed curcumin in different layers of skin through fluorescent imaging. The release kinetic of curcumin followed the Higuchi model, which explains why the skin permeation was a Fickian diffusion-controlled process because the Korsmeyer constant was proven to be 0.3 (<0.5). Nanoencapsulation slightly decreased the antioxidant capacity of curcumin for about 7.9% compared to its...
International journal of nanomedicine
From previous studies, it has been found that curcumin exhibits an anti-inflammatory activity and is being used for the treatment of skin disorders; however, it is hydrophobic and has weak penetrating ability, resulting in poor drug transport through the stratum corneum. The aim of this study was to develop liquid crystalline systems for topical administration of curcumin for the treatment of inflammation. These liquid crystalline systems were developed from oleic acid, polyoxypropylene (5) polyoxyethylene (20) cetyl alcohol, and water as the surfactant, oil phase, and aqueous phase, respectively. These systems were characterized, and polarized light microscopy showed anisotropy with lamellar mesophases (Formulation 1) and hexagonal mesophases (Formulations 2 and 3), which were confirmed by the peak ratio measured using small-angle X-ray scattering. In addition, rheological tests revealed that the formulations exhibited gel-like behavior (G'>G″), as evidenced by the increased...
Formulation and Physical Characterization of Curcumin Nanoparticle
2019
Objective: This study was conducted to formulate curcumin nanoparticles transdermal patches and to evaluate their physical characterization. Methods: Curcumin nanoparticles transdermal patches were formulated by the casting evaporation method. Transdermal patches were made using combinations of hydroxypropyl methylcellulose (HPMC) and ethyl cellulose (EC) at ratios of 4.5:1.5 for Formula 1 (F1), 4:1 for Formula 2 (F2), 3.5:1.5 for Formula 3 (F3), 3:2 for Formula 4 (F4), and 2.5:2.5 for Formula 5 (F5). Physical characterization evaluation (organoleptic properties, pH, weight uniformity, thickness uniformity, percent moisture content, and tensile strength) was then performed. The permeation of curcumin nanoparticles into the skin was evaluated using Franz diffusion cells. Results: Curcumin nanoparticles transdermal patches could be formulated by the casting evaporation method with the organoleptic properties characterized as smooth, dry, yellow in color, having menthol odor, and trans...