curcumin and ethyl-cellulose

Co-encapsulation of retinoic acid (RA), curcumin and/or resveratrol into microparticles composed by alginic acid sodium and the ethyl cellulose + polyethylene glycol (EC + PEG) blend was proposed for the protection and co-delivery of these bioactive compounds. The final aim is to take benefit of combined therapeutic potential related to these molecules and use loaded microparticles obtained by spray-drying to improve the treatment of acute promyelocytic leukemia (APL). Alginic acid sodium-based emulsions were characterized regarding rheological properties (i.e. viscosity), stability and droplet size distribution. Biopolymer- and synthetic polymer-based microparticles loaded with RA, RA + curcumin, RA + resveratrol and RA + curcumin + resveratrol were produced with a product yield between 10 and 35 %. The obtained microparticles exhibited a variable form, a morphology that varied between a slightly and high rough surface and a mean diameter that ranged from 2.97 ± 0.04 and 88 ± 3 μm. Encapsulation efficiency was significantly influenced by the encapsulating agent(s) used in the microparticles formulations. The bioactive compounds that were co-encapsulated showed a similar release profile.

Topics: Alginic Acid; Curcumin; Drug Compounding; Emulsions; Particle Size; Resveratrol; Tretinoin

A simple and versatile strategy for controlled production of monodisperse ethyl cellulose (EC) microcapsules by a single-stage emulsification method has been developed. Monodisperse oil-in-water emulsions, obtained by a microfluidic device, are used as templates for preparing EC microcapsules. Oil-soluble ethyl acetate (EA) is miscible with water, so the interfacial mass transfer between EA and water occurs sufficiently, which leads to water molecules pass through the phase interface and diffuse into emulsion interior. Water molecules aggregate at the interface, and some merge into a large water drop in the central position of the emulsion. After evaporation of EA solvent, monodisperse EC microcapsules create large numbers of pits on the surface with a hollow structure. Curcumin is used as a model drug and embedded in the hollow structure. EC microcapsules have good, sustained drug release efficacy in a simulated intestinal environment, and the release process of EC microcapsules containing 6.14% drug-loaded capacity is fully consistent with the vitro drug release model. Such simple techniques for making EC microcapsules may open a window to the controlled preparation of other multifunctional microcapsules. Besides, it offers theoretical guidance for the study of EC microcapsules as drug carriers and expanding clinical application of curcumin.

Topics: Capsules; Cellulose; Curcumin; Delayed-Action Preparations; Emulsions; Particle Size; Water

We have developed an ethyl cellulose-based nanoparticulate system for encapsulation of sparingly soluble active pharmaceutical ingredients. Cannabidiol (CBD) and curcumin (CUR) were selected as model active ingredients. Using the nanoprecipitation method, nanoparticles ranged between 150 nm and 250 nm were obtained with an entrapment efficiency of >80%. It has been shown that incorporation of stabilizing lipids significantly reduced aggregation, increased the yield and the active ingredient-to-polymer ratio. In this study, we have explored the influence of process parameters on the extent of new particle core formation: chemical properties of the active ingredients, polymer concentrations, non-solvent addition rate, and the volume of the organic solvent for nanoparticle size control. The relationship between the particle radius [R] and the polymer concentration [Pol] was defined by R ∝ [Pol]

Topics: Cellulose; Curcumin; Drug Carriers; Keratinocytes; Lipids; Nanoparticles; Particle Size

In this work, sequential electrospinning was utilized to fabricate a multilayer film with ethylcellulose nanofibers as the outer layer and curcumin-loaded gelatin nanofibers as the inner layer. Field-emission scanning electronic microscopy observations showed that the outer and inner layers had a smooth surface and clear boundary. The hydrophobic outer layers decreased the water vapor permeability and improved the water contact resistance of the hydrophilic inner layer, and the intimate interactions of hydrogen bonds between two adjacent layers enhanced the thermal stability. The multilayer film exhibited a sustained release manner of the encapsulated curcumin for 96 h, compared to the burst release within 30 min from the gelatin film. In addition, the antioxidant activities of the released curcumin from the multilayer film were well retained within 96 h. These results suggested that the multilayer nanofibrous film fabricated by sequential electrospinning has potential applications in bioactive encapsulation and controlled release.

Topics: Cellulose; Curcumin; Delayed-Action Preparations; Gelatin; Hydrogen Bonding; Hydrophobic and Hydrophilic Interactions; Nanofibers; Water

The stable colloidal nano-dispersion of curcumin (CU) loaded zein-ethyl cellulose (ZN-EC) as three hydrophobic agent in water was prepared using two step antisolvent co-precipitation method. The EC coated NPs were prepared by adding EC in ethyl acetate to the ZN-CU NPs at a concentration ratio of 1: 3.5 w/v. The prepared colloidal suspension of ZN-EC showed high physical stability during storage time. The particle diameters and zeta potential values of ZN-CU and ZN-CU-EC colloidal suspensions were 140 ± 12 nm, 38 ± 2 mV and 179 ± 12 nm, 12 ± 2 mV, respectively. Based on Scanning electron microscopy (SEM) images, participation of EC on the surface of ZN-CU particles could reduce the sticky appearance of particles. Encapsulation efficiency of CU in NPs did not improve after precipitation of EC, but the stability of NPs against pH changes, increased and release rate of CU from NPs at different pH values (3-8) were significantly reduced in comparison of ZN-CU NPs. The EC coated NPs showed the excessive protection for CU antioxidant activity during storage. In conclusion, the prepared NPs, with high physical stability, have good potential for encapsulation and delivery of CU to colon region.

Topics: Cellulose; Curcumin; Drug Carriers; Hydrophobic and Hydrophilic Interactions; Nanoparticles; Particle Size; Water; Zein

The current study developed ethylcellulose (EC) based oleogels with the addition of a surface active ingredient (sorbitan monopalmitate, SP), in order to increase the active loading of curcumin by reducing lipid oxidation, improving curcumin solubility and chemical stability. With the increase in SP content, EC oleogels had more compact gel networks with evenly distributed smaller pores. Rheological analysis revealed that the gels had shear-thinning behavior, and higher concentration of SP contributed to the systems with higher viscosity. The inclusion of SP also worked to reinforce gel strength as determined by frequency sweep, creep recovery and textural analyses. EC oleogels with higher content of SP were capable to hold more liquid oil during centrifugation, and the T

Topics: Cellulose; Curcumin; Drug Stability; Hexoses; Oils; Organic Chemicals; Oxidation-Reduction; Peroxides; Rheology; Solubility; Surface-Active Agents; Ultraviolet Rays

Curcumin (CUR) demonstrates a variety of biological activities; however, the poor oral bioavailability limits its clinical application. The objective of this study was to develop and evaluate characteristics and bioavailability of hollow microspheres loading curcumin (CUR-HPs). CUR-HPs were prepared by solvent diffusion and evaporation method. The effect of viscosity of ethyl cellulose (EC), amount of EC, citric acid (CA) and CUR on physicochemical characteristics and in vitro release profile of CUR-HPs were evaluated. Scanning electron microscopy (SEM) showed microspheres had smooth surfaces with hollow structures. The yield of CUR-HPs was (96 ± 1.80) %. The floating rate at 24 h was (89.67 ± 4.91) % and the drug loading was (3.41 ± 0.21) %. Nearly 95% of CUR was released from the HPs at 24 h. In vitro release profiles of CUR-HPs fitted the Korsmeyer et al.'s equation and indicated that CUR was released through the combination of diffusion and erosion mechanisms. The bioavailability of CUR-HPs was 12-fold higher than that of CUR. The peak time was delayed for 7.5 h and peak concentration of CUR-HPs was 3.21 times than that of free CUR. The CUR-HPs might be a promising strategy to achieve sustained release and increase oral bioavailability of CUR.

Topics: Animals; Biological Availability; Cellulose; Citric Acid; Curcumin; Diffusion; Drug Carriers; Drug Liberation; Microspheres; Rats; Rats, Sprague-Dawley; Solvents

Bladder cancer is the second type of malignant carcinoma of the urinary tract. The treatment is time-consuming and requires maintenance doses of the drug for long period of time with important side effects. Curcumin has shown evident clinical advances in the treatment of cancer. The technology of microencapsulation and the use of mucoadhesive materials can contribute to modify the delivery and improve the bioavailability of curcumin.. The aim of this study was to design and characterize mucoadhesive microparticles containing curcumin using multivariate analysis and the spray-drying technique.. A factorial design 32+1 was employed to investigate the influence of gelatin, ethylcellulose, and curcumin on size, polydispersity index, drug content and entrapment efficiency. Microparticles were also evaluated by ATR-FTIR, X-ray diffraction, antioxidant activity, in-vitro release profile, exvivo mucoadhesion performance, and in-vitro cytotoxicity.. Microparticles showed non-uniform surface, mean diameter from 2.73 µm to 4.62 µm and polydispersity index from 0.72 to 1.09, according to the different combinations of the independent factors. These independent variables also had a significant effect on the drug content. The highest values of drug trapping efficiency were obtained with the highest concentration of curcumin and polymers. Formulations displayed slow drug release and important antioxidant activity. The good mucoadhesive performance of microparticles was assessed by the falling film technique. Moreover, the formulations did not display in vitro toxicity against Artemia salina and Fibroblasts LM(TK).. The design results were useful for developing of curcumin dosage form with good physicochemical characteristics and mucoadhesive properties for the bladder administration.

Topics: Adhesiveness; Animals; Antioxidants; Artemia; Benzothiazoles; Cell Survival; Cellulose; Curcumin; Drug Carriers; Drug Design; Drug Liberation; Fibroblasts; Gelatin; Microspheres; Mucous Membrane; Nanoparticles; Sulfonic Acids; Swine; Urinary Bladder

Curcumin-ethyl-cellulose (EC) sustained-release composite particles were prepared by using supercritical CO2 anti-solvent technology. With drug loading and yield of inclusion complex as evaluation indexes, on the basis of single factor tests, orthogonal experimental design was used to optimize the preparation process of curcumin-EC sustained-release composite particles. The experiments such as drug loading, yield, particle size distribution, electron microscope analysis (SEM) , infrared spectrum (IR), differential scanning calorimetry (DSC) and in vitro dissolution were used to analyze the optimal process combination. The orthogonal experimental optimization process conditions were set as follows: crystallization temperature 45 degrees C, crystallization pressure 10 MPa, curcumin concentration 8 g x L(-1), solvent flow rate 0.9 mL x min(-1), and CO2 velocity 4 L x min(-1). Under the optimal conditions, the average drug loading and yield of curcumin-EC sustained-release composite particles were 33.01% and 83.97%, and the average particle size of the particles was 20.632 μm. IR and DSC analysis showed that curcumin might complex with EC. The experiments of in vitro dissolution showed that curcumin-EC composite particles had good sustained-release effect. Curcumin-EC sustained-release composite particles can be prepared by supercritical CO2 anti-solvent technology.

Topics: Carbon Dioxide; Cellulose; Curcumin; Delayed-Action Preparations; Solubility; Solvents; Technology, Pharmaceutical

The work was aimed to validate the gastroretentive potential of microsponges via optimization of targeted floating curcumin microsponges for improved site specific absorption for gastric cancer Modified quasi emulsion solvent diffusion method was used to formulate microsponges using 3(2) full factorial design. The effect of different levels of ethyl cellulose and polyvinyl alcohol concentration, selected as independent variables was determined on the % entrapment efficiency, % buoyancy and % cumulative drug release. Modified rosette rise apparatus was used for in vitro release and the release data best fitted Higuchi's model and mechanism of drug release was diffusion (n). The optimized formulation (MS5) demonstrated favourable % entrapment efficiency (90.7 ± 1.7), % buoyancy (82.0 ± 2.0) and % cumulative drug release (85.2 ± 1.07) with maximum desirability factor of 0.816. SEM revealed spherical and porous microsponges. DSC confirmed molecular dispersion of the drug in the microsponges polymeric matrix. DRIFT revealed no chemical interaction between the drug and polymer used. The in vitro permeation of curcumin through gastric mucin gel layer affirmed the capability of microsponges to deliver drug across mucin r and reach the target site to treat gastric cancer. Anticancer oral dose of microsponges was calculated as 50mg by cytotoxicity assay in human cancer cell line KB. The pharmacokinetic evaluation of MS5 in rabbits revealed 10-fold increase in bioavailability as compared to native curcumin, demonstrated the superiority of microsponges over native curcumin as gastro retentive drug delivery system. This study presents a new approach based on floating ability of microsponges for treatment of gastric cancer.

Topics: Animals; Antineoplastic Agents, Phytogenic; Cell Survival; Cellulose; Curcumin; Delayed-Action Preparations; Drug Delivery Systems; Excipients; Gastric Mucins; Gastric Mucosa; Goats; Humans; KB Cells; Polymethacrylic Acids; Polyvinyl Alcohol; Rabbits; Sodium Chloride

Curcumin is known for its anti-inflammatory, antioxidative, and anticarcinogenic properties. However, the strong lipophilic compound is not easily applicable, neither in water, nor directly in o/w formulations. So far, loading of nano or micro scaled carriers has enabled only an uptake up to 30% of curcumin.. In the present article, curcumin was successfully encapsulated into two different safe and inexpensive polymers, ethyl cellulose and methyl cellulose blended ethyl cellulose with a loading capacity of ~ 46-48%. In addition, the in vitro skin penetration of the two curcumin encapsulated particular systems, which were applied each in three different formulations, an o/w, w/o lotion, and water suspension, was investigated on porcine ear skin using Laser scanning microscopy.. It was found that in comparison to water suspensions, o/w and w/o lotions enhanced, especially the follicular penetration of the encapsulated curcumin particles into porcine skin, whereas the w/o enhanced the penetration better than the o/w lotion. Furthermore, the application of ethyl cellulose blended with methyl cellulose improved the penetration of curcumin in all formulations.. High loaded encapsulated curcumin systems, prepared from a simple and highly efficient encapsulation system can be used to transport curcumin effectively into the skin.

Topics: Animals; Anti-Inflammatory Agents, Non-Steroidal; Capsules; Cellulose; Chemistry, Pharmaceutical; Curcumin; Drug Carriers; Ear, External; Hair Follicle; Methylcellulose; Microscopy, Confocal; Microscopy, Electron, Scanning; Microscopy, Electron, Transmission; Microspheres; Nanoparticles; Skin; Skin Cream; Swine; Water

The phytochemical curcumin possesses antioxidant activity; however, it becomes unstable after being exposed to light or heat or loses activity during storage. This is especially important when curcumin is applied to the skin within a cosmetic or pharmaceutical formulation, since sun exposure is unavoidable. This drawback can be directly addressed by encapsulation of curcumin in photo-stable nanospheres. Therefore, curcumin was encapsulated into nanoparticles consisting of ethyl cellulose and/or methyl cellulose. Nanoparticles were subjected to processing conditions commonly used in industry, for example, temperature and pressure and thus retained their morphology. Furthermore, sun exposure resulted in the protection of curcumin by nanoparticles, whereas non-encapsulated curcumin degraded completely. Determination of the radical protection factor resulted in similar antioxidant activity of encapsulated and non-encapsulated curcumin indicating that curcumin maintains its antioxidant activity. Application of lotions containing curcumin or curcumin nanoparticles to the skin and subsequent UVB-irradiation resulted in less radical formation compared to lotion application only. Moreover, radical formation was even less after nanoparticle application compared to free curcumin. Nanoencapsulation protects curcumin from photo degradation and can therefore prolong the antioxidant activity of curcumin.

Topics: Administration, Cutaneous; Animals; Antioxidants; Cellulose; Curcumin; Drug Stability; Drug Storage; Free Radical Scavengers; In Vitro Techniques; Methylcellulose; Nanoparticles; Photolysis; Pressure; Skin; Sunlight; Swine; Temperature; Time Factors; Ultraviolet Rays

The purpose of this research was to develop a matrix-type transdermal therapeutic system containing herbal drug, curcumin (CUR), with different ratios of hydrophilic (hydroxyl propyl methyl cellulose K4M [HPMC K4M]) and hydrophobic (ethyl cellulose [EC]) polymeric systems by the solvent evaporation technique. Different concentrations of oleic acid (OA) were used to enhance the transdermal permeation of CUR. The physicochemical compatibility of the drug and the polymers was also studied by differential scanning calorimetry (DSC) and infrared (IR) spectroscopy. The results suggested no physicochemical incompatibility between the drug and the polymers. Formulated transdermal films were physically evaluated with regard to drug content, tensile strength, folding endurance, thickness, and weight variation. All prepared formulations indicated good physical stability. In vitro permeation studies of formulations were performed by using Franz diffusion cells. The results followed Higuchi kinetics, and the mechanism of release was diffusion-mediated. Formulation prepared with hydrophilic polymer containing permeation enhancer showed best in vitro skin permeation through rat skin as compared with all other formulations. This formulation demonstrated good anti-inflammatory activity against carrageenan-induced oedema in Wistar albino rats similar to standard formulation.

Topics: Administration, Cutaneous; Animals; Anti-Inflammatory Agents, Non-Steroidal; Carrageenan; Cellulose; Curcumin; Delayed-Action Preparations; Drug Carriers; Drug Compounding; Drug Delivery Systems; Drug Design; Drug Evaluation, Preclinical; Drug Incompatibility; Drug Stability; Edema; Excipients; Hydrophobic and Hydrophilic Interactions; Hypromellose Derivatives; In Vitro Techniques; Kinetics; Methylcellulose; Permeability; Pharmaceutical Vehicles; Rats; Rats, Wistar; Skin; Skin Absorption; Tensile Strength