Enhanced Oral Bioavailability of Curcumin via a Solid Lipid-Based Self-Emulsifying Drug Delivery System Using a Spray-Drying Technique

Yan, Yongyong; Kim, Jung Ae; Kwak, Mi Kyung; Yoo, Bong Kyu; Yong, Chul Soon; Choi, Han‐Gon

doi:10.1248/bpb.34.1179

Cited by 99 publications

(56 citation statements)

References 29 publications

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“…12,14,15 Recently, several curcumin nanoformulations, such as polymer nanoparticles, selfassemblies, nanocrystal dispersions, nanoemulsions, lipid nanoparticles, and protein-based drug delivery systems, have shown improved solubility, stability, and bioavailability of the curcumin molecule. [14][15][16][17][18][19][20] Moreover, curcumin nanoformulations have demonstrated improved cellular uptake in cancer models that increases the chance of a positive therapeutic outcome. Curcumin nanoformulations have also exhibited superior in vitro anticancer responses compared with free curcumin due to sustained release of the active compound and the enhanced permeation and retention effects of nanoformulations.…”

Section: Introductionmentioning

confidence: 99%

Interaction of curcumin nanoformulations with human plasma proteins and erythrocytes

Yallapu¹,

Ebeling²,

Chauhan³

et al. 2011

IJN

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Background Recent studies report curcumin nanoformulation(s) based on polylactic- co -glycolic acid (PLGA), β-cyclodextrin, cellulose, nanogel, and dendrimers to have anticancer potential. However, no comparative data are currently available for the interaction of curcumin nanoformulations with blood proteins and erythrocytes. The objective of this study was to examine the interaction of curcumin nanoformulations with cancer cells, serum proteins, and human red blood cells, and to assess their potential application for in vivo preclinical and clinical studies. Methods The cellular uptake of curcumin nanoformulations was assessed by measuring curcumin levels in cancer cells using ultraviolet-visible spectrophotometry. Protein interaction studies were conducted using particle size analysis, zeta potential, and Western blot techniques. Curcumin nanoformulations were incubated with human red blood cells to evaluate their acute toxicity and hemocompatibility. Results Cellular uptake of curcumin nanoformulations by cancer cells demonstrated preferential uptake versus free curcumin. Particle sizes and zeta potentials of curucumin nanoformulations were varied after human serum albumin adsorption. A remarkable capacity of the dendrimer curcumin nanoformulation to bind to plasma protein was observed, while the other formulations showed minimal binding capacity. Dendrimer curcumin nanoformulations also showed higher toxicity to red blood cells compared with the other curcumin nanoformulations. Conclusion PLGA and nanogel curcumin nanoformulations appear to be very compatible with erythrocytes and have low serum protein binding characteristics, which suggests that they may be suitable for application in the treatment of malignancy. These findings advance our understanding of the characteristics of curcumin nanoformulations, a necessary component in harnessing and implementing improved in vivo effects of curcumin.

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Section: Introductionmentioning

confidence: 99%

Interaction of curcumin nanoformulations with human plasma proteins and erythrocytes

Yallapu¹,

Ebeling²,

Chauhan³

et al. 2011

IJN

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“…The droplet size after emulsification in aqueous medium is a critical factor in the SMEDDS formulation because a smaller globular size yields a larger interfacial surface area for drug absorption with excellent colloidal stability. 13) No change in the physical parameters such as droplet size and clarity was observed for test period in Labrafil M1944CS/ Kollidone EL formula (Table 1) and thus, Kollidone EL was selected as a surfactant. Previous literature revealed that DRN could be a potent P-glycoprotein (P-gp) substrate 14) and thus, we also expected that the incorporation of Kollidone EL in SMEDDS, a well-known P-gp inhibitor, might facilitate the intestinal absorption of the anti-arrhythmic agent, especially in the fasted state.…”

Section: Resultsmentioning

confidence: 99%

Reduced Food-Effect on Intestinal Absorption of Dronedarone by Self-microemulsifying Drug Delivery System (SMEDDS)

Han

Jung

Jang

et al. 2015

Biological & Pharmaceutical Bulletin

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The oral absorption of dronedarone (DRN), a benzofuran derivative with anti-arrhythmic activity, is significantly affected by food intake. The absolute bioavailability of the marketed product (Multaq ® , Sanofi, U.S.) was about 4% without food, but increased to 15% when administered with a high fat meal. Therefore, to reduce the food-effect on the intestinal absorption of DRN, a novel self-microemulsifying drug delivery system (SMEDDS) was formulated and the comparative in vivo absorption studies with the marketed product were carried out using male beagle dogs either in the fasted or fed state. The SMEDDS consisted of the drug, Labrafil M 1944CS, and Kolliphor EL in a weight ratio of 1 : 1 : 2, rapidly formed a fine oil-in-water emulsion with a droplet size less than 50 nm. An in vivo absorption study revealed that the area-under-curve (AUC 0-24 h ) and maximal plasma concentration (C max ) were 10.4-fold (p<0.05) and 8.6-fold (p<0.05) higher, respectively, after the marketed product was orally administered to beagles in the fed state when compared to those in the fasted state. This food-effect were remarkably alleviated by SMEDDS formulation, with AUC 0-24 h and C max 2.9-fold (p<0.05) and 2.6-fold (p<0.05) higher in the fed state when compared to the fasted state, by facilitating intestinal absorption of DRN in the fasted state. The results of this study suggest that SMEDDS may decrease the differences in oral absorption of DRN between the prandial states, improving therapeutic efficacy as well as patient compliance.Key words dronedarone; self-microemulsifying drug delivery system (SMEDDS); food-effect; oral absorption; solubilization Dronedarone (N-{2-butyl-3-[4-(3-dibutylaminopropoxy)benzoyl]benzofuran-5-yl}methane sulfonamide; DRN) is a benzofuran derivative with anti-arrhythmic properties belonging to all four Vaughan-Williams classes.1,2) This drug, commercialized under the trade name Multaq ® (Sanofi, U.S.), has been approved by the Food and Drug Administration (FDA) since 2009 in the tablet dosage form containing the hydrochloride salt of DRN (400 mg as base).3) In a clinical study, the antiarrhythmic agent effectively reduced cardiovascular hospitalization or death from any cause by 24.2% compared to the placebo group. 1) However, the oral administration of DRN has some problems such as extensive first-pass metabolism and food-effect on oral absorption.3) Although the original manufacturer (Sanofi, U.S.) formulated an oral dosage form (Multaq ® ) based on the solid dispersion (SD) system with a triblock copolymer of polypropylene glycol and polyethylene glycol to increase drug dissolution in the gastrointestinal (GI) tract, 4) the oral absorption of this biopharmaceutics classification system (BCS) ΙΙ compound is significantly affected by food intake. The absolute bioavailability (BA) of DRN is approximately 4% without food, which increased to approximately 15% when administered with a high fat meal.3) In this regard, Multaq ® tablets should be taken shortly after a meal to increase its intestinal abs...

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“…35) OA's status in this S-SEDDS was also investigated here. DSC curves of pure OA, mannitol, physical mixture and S-SEDDS were presented in Fig.…”

Section: )mentioning

confidence: 99%

Formulation and <i>in Vitro</i> Characterization of a Novel Solid Lipid-Based Drug Delivery System

Chu

Itagaki³

et al. 2014

CHEMICAL & PHARMACEUTICAL BULLETIN

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The liquid self-emulsifying drug delivery system (L-SEDDS), commonly used to deliver effective but poorly water-soluble oleanolic acid (OA), has many limitations such as high manufacturing costs, few choices of dosage forms, risk of leakage from hard gelatin capsules, low stability, limited portability, incompatibility with capsule materials, and relatively restricted storage conditions. Thus the main purpose of our study was to develop a promising solid lipid-based drug delivery system (S-SEDDS) for OA. The S-SEDDS, prepared from wet granulation with an optimized L-SEDDS formulation and mannitol, was characterized by particle size analysis, scanning electron microscopy, differential scanning calorimetry, and X-ray powder diffraction. Finally, the solubility of the OA-loaded S-SEDDS was compared with that of OA powder in the dissolution assay. Our new S-SEDDS for OA was developed from the optimum L-SEDDS with ethyl oleate (oil phase), Labrasol (surfactant), and Transcutol P (cosurfactant) at a volume ratio of 15 : 71 : 14 with 1.5% w/v OA and mannitol. The dissolution of OA was improved by 60% compared with that of the pure OA powder. All the problems associated with the L-SEDDS were resolved. The methodologies we developed for OA delivery could also be utilized for the delivery of other drugs with the S-SEDDS.

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Enhanced Oral Bioavailability of Curcumin via a Solid Lipid-Based Self-Emulsifying Drug Delivery System Using a Spray-Drying Technique

Cited by 99 publications

References 29 publications

Interaction of curcumin nanoformulations with human plasma proteins and erythrocytes

Interaction of curcumin nanoformulations with human plasma proteins and erythrocytes

Reduced Food-Effect on Intestinal Absorption of Dronedarone by Self-microemulsifying Drug Delivery System (SMEDDS)

Formulation and <i>in Vitro</i> Characterization of a Novel Solid Lipid-Based Drug Delivery System

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