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1.
The objective of this work was to develop a self-microemulsifying drug delivery system (SMEDDS) for improving oral absorption of poorly water-soluble drug, silymarin. The pseudo-ternary phase diagrams were constructed using ethyl linoleate, Cremophor EL, ethyl alcohol, and normal saline to identify the efficient self-microemulsification region. The particle size and its distribution of the resultant microemulsions were determined using dynamic light scattering. The optimal formulation with the best self-microemulsifying and solubilization ability consisted of 10% (w/w) of ethyl linoleate, 30% of Cremophor EL, and 60% of ethyl alcohol. The release of silymarin from SMEDDS was significantly faster than that from the commercial silymarin preparation hard capsule (Legalon®). The bioavailability results indicated that the oral absorption of silymarin SMEDDS was enhanced about 2.2-fold compared with the hard capsule in fasted dogs. It could be concluded that SMEDDS would be a promising drug delivery system for poorly water-soluble drugs by the oral route. 相似文献
2.
The purpose of this research work was to formulate and characterize self-micro emulsifying drug delivery system containing
exemestane. The solubility of exemestane was determined in various vehicles. Pseudo ternary phase diagram was used to evaluate
the micro-emulsification existence area. SMEDDS formulations were tested for micro-emulsifying properties, and the resultant
formulations loaded with exemestane (ME1, ME2, ME3, ME4 and ME5) were investigated for clarity, phase separation, globule
size and shape, zeta potential, effect of various diluents and dilutions, thermodynamic and thermal stability. From the results
it is concluded that increase in droplet size is proportional to the concentration of oil in SMEDDS formulation. Minor difference
in the droplet size and zeta potential was observed by varying the diluents (deionized water and 0.1 N HCl) and dilutions
(1:10, 1:50 and 1:100). Formulations, which were found to be thermodynamically stable (ME1, ME2, ME3 and ME4), were subjected
to stability studies as per International Conference on Harmonization (ICH) guidelines. No significant variations were observed
in the formulations over a period of 3 months at accelerated and long-term conditions. TEM photographs of microemulsions formulations
further conformed the spherical shape of globules. Among the various SMEDDS formulations, ME4 offer the advantages of good
clarity systems at high oil content and thus offer good solubilization of exemestane. Thus this study indicates that the SMEDDS
can be used as a potential drug carrier for dissolution enhancement of exemestane and other lipophilic drug(s). 相似文献
3.
Mohsin K 《AAPS PharmSciTech》2012,13(2):637-646
Lipid-based drug carriers are likely to have influence on bioavailability through enhanced solubilization of the drug in the gastrointestinal tract. The study was designed to investigate the lipid formulation digestibility in the simulated gastro intestinal media. Fenofibrate was formulated in representative Type II, IIIA, IIIB and IV self-emulsifying/microemulsifying lipid delivery systems (SEDDS and SMEDDS designed for oral administration) using various medium-chain glyceride components, non-ionic surfactants and cosolvents as excipients. Soybean oil was used only as an example of long-chain triglycerides to compare the effects of formulation with their counterparts. The formulations were subjected to in vitro digestion specifically to predict the fate of the drug in the gastro intestinal tract after exposure of the formulation to pancreatic enzymes and bile. In vitro digestion experiments were carried out using a pH-stat maintained at pH 7.5 for 30 min using intestinal fluids simulating the fed and fasted states. The digestion rate was faster and almost completed in Type II and IIIA systems. Most of the surfactants used in the studies are digestible. However, the high concentration of surfactant and/or cosolvent used in Type IIIB or IV systems lowered the rate of digestion. The digestion of medium-chain triglycerides was faster than long-chain triglycerides, but kept comparatively less drug in the post digestion products. Medium-chain mixed glycerides are good solvents for fenofibrate as rapidly digested but to improve fenofibrate concentration in post digestion products the use of long-chain mixed glycerides are suggested for further investigations.KEY WORDS: fenofibrate, in vitro lipolysis, lipid formulation classification system, self-emulsifying/microemulsifying drug delivery systems (SEDDS, SMEDDS) 相似文献
4.
Vijaykumar Nekkanti Pradeep Karatgi Raghavendra Prabhu Raviraj Pillai 《AAPS PharmSciTech》2010,11(1):9-17
Sparingly, water-soluble drugs such as candesartan cilexetil offer challenges in developing a drug product with adequate bioavailability.
The objective of the present study was to develop and characterize self-microemulsifying drug delivery system (SMEDDS) of
candesartan cilexetil for filling into hard gelatin capsules. Solubility of candesartan cilexetil was evaluated in various
nonaqueous careers that included oils, surfactants, and cosurfactants. Pseudoternary phase diagrams were constructed to identify
the self-microemulsification region. Four self-microemulsifying formulations were prepared using mixtures of oils, surfactants,
and cosurfactants in various proportions. The self-microemulsification properties, droplet size, and zeta potential of these
formulations were studied upon dilution with water. The optimized liquid SMEDDS formulation was converted into free flowing
powder by adsorbing onto a solid carrier for encapsulation. The dissolution characteristics of solid intermediates of SMEDDS
filled into hard gelatin capsules was investigated and compared with liquid formulation and commercial formulation to ascertain
the impact on self-emulsifying properties following conversion. The results indicated that solid intermediates showed comparable
rate and extent of drug dissolution in a discriminating dissolution medium as liquid SMEDDS indicating that the self-emulsifying
properties of SMEDDS were unaffected following conversion. Also, the rate and extent of drug dissolution for solid intermediates
was significantly higher than commercial tablet formulation. The results from this study demonstrate the potential use of
SMEDDS as a means of improving solubility, dissolution, and concomitantly the bioavailability. 相似文献
5.
Formation of core/shell nanoparticles with a lipid core and their application as a drug delivery system 总被引:1,自引:0,他引:1
A novel preparation method for core/shell nanoparticles with a drug-loaded lipid core was designed and characterized. The lipid core is composed of lecithin and a drug, and the polymeric shell is composed of Pluronics (poly(ethylene oxide)-poly (propylene oxide)-poly(ethylene oxide) triblock copolymer, F-127). For the formation of stabilized core/shell nanoparticles, freeze-drying was performed in the presence of trehalose used as a cryoprotectant. Cryogenic transmittance electron microscopy (cryo-TEM), differential scanning calorimetry (DSC), and a particle size analyzer were used to observe the formation of the stabilized core/shell nanoparticles. For the application of the core/shell nanoparticles as a drug carrier, paclitaxel, a potent anticancer drug, was loaded into the core/shell nanoparticles, and the drug loading amount and the drug release pattern were observed. 相似文献
6.
The objective of present investigation was to formulate self-microemulsifying drug delivery systems (SMEDDS) of tacrolimus
(FK 506), a poorly water soluble immunosuppressant that exhibits low and erratic bioavailability. Solubility of FK 506 in
various oils, surfactants cosurfactants and buffers was determined. Phase diagrams were constructed at different ratios of
surfactant/cosurfactant (K
m
) to determine microemulsion existence region. The effect of oil content, pH of aqueous phase, dilution, and incorporation
of drug on mean globule size of resulting microemulsions was studied. The optimized SMEDDS formulation was evaluated for in vitro dissolution profile in comparison to pure drug and marketed formulation (Pangraf capsules). The in vivo immunosuppressant activity of FK 506 SMEDDS was evaluated in comparison to Pangraf capsules. Area of o/w microemulsion region in phase diagram was increased with increase in K
m
. The SMEDDS yielded microemulsion with globule size less than 25 nm which was not affected by the pH of dilution medium.
The SMEDDS was robust to dilution and did not show any phase separation and drug precipitation even after 24 h. Optimized
SMEDDS exhibited superior in vitro dissolution profile as compared to pure drug and Pangraf capsules. Furthermore, FK 506 SMEDDS exhibited significantly higher
immunosuppressant activity in mice as compared to Pangraf capsules. 相似文献
7.
Oh KS Han SK Lee HS Koo HM Kim RS Lee KE Han SS Cho SH Yuk SH 《Biomacromolecules》2006,7(8):2362-2367
Core/shell nanoparticles with lipid core, were prepared and characterized as a sustained delivery system for protein. The lipid core is composed of protein-loaded lecithin and the polymeric shell is composed of Pluronics (poly(ethylene oxide)-poly(propylene oxide)-poly(ethylene oxide) triblock copolymer, F-127). Based on the preparation method in the previous report by us, the freeze-drying of protein-loaded lecithin was performed in the F-127 aqueous solution containing trehalose used as a cryoprotectant to form stabilized core/shell nanoparticles. Cryo-TEM (transmittance electron microscopy) and a particle size analyzer were used to observe the formation of stabilized core/shell nanoparticles. For the application of core/shell nanoparticles as a protein drug carrier, lysozyme and vascular endothelial growth factor (VEGF) were loaded into the core/shell nanoparticles by electrostatic interaction, and the drug release pattern was observed by manipulating the polymeric shell. 相似文献
8.
The objectives of this study were to develop and evaluate a novel self-emulsifying floating drug delivery system (SEFDDS)
that resulted in improved solubility, dissolution, and controlled release of the poorly water-soluble tetrahydrocurcumin (THC).
The formulations of liquid self-emulsifying drug delivery system (SEDDS; mixtures of Labrasol, Cremophor EL, Capryol 90, Labrafac
PG) were optimized by solubility assay and pseudo-ternary phase diagram analysis. The liquid SEDDS was mixed with adsorbent
(silicon dioxide), glyceryl behenate, pregelatinized starch, sodium starch glycolate, and microcrystalline cellulose and transformed
into pellets by the extrusion/spheronization technique. The resulting pellets with 22% liquid SEDDS had a uniform size and
good self-emulsification property. The microemulsions in aqueous media of different self-emulsifying floating pellet formulations
were in a particle size range of 25.9–32.5 nm. Use of different weight proportions of glyceryl behenate and sodium starch
glycolate in pellet formulations had different effects on the floating abilities and in vitro drug release. The optimum formulation (F2) had a floating efficiency of 93% at 6 h and provided a controlled release of THC
over an 8-h period. The release rate and extent of release of THC liquid SEDDS (80% within 2 h) and self-emulsifying floating
pellet formulation (80% within 8 h) were significantly higher than that of unformulated THC (only 30% within 8 h). The pellet
formulation was stable under intermediate and accelerated storage conditions for up to 6 months. Controlled release from this
novel SEFDDS can be a useful alternative for the strategic development of oral solid lipid-based formulations. 相似文献
9.
Polymeric micelles represent an effective delivery system for poorly water-soluble anticancer drugs. With small size (10–100 nm) and hydrophilic shell of PEG, polymeric micelles exhibit prolonged circulation time in the blood and enhanced tumor accumulation. In this review, the importance of rational design was highlighted by summarizing the recent progress on the development of micellar formulations. Emphasis is placed on the new strategies to enhance the drug/carrier interaction for improved drug-loading capacity. In addition, the micelle-forming drug-polymer conjugates are also discussed which have both drug-loading function and antitumor activity. 相似文献
10.
Oral Bioavailability Enhancement of Exemestane from Self-Microemulsifying Drug Delivery System (SMEDDS) 总被引:1,自引:0,他引:1
Ajeet K. Singh Akash Chaurasiya Anshumali Awasthi Gautam Mishra Dinesh Asati Roop K. Khar Rama Mukherjee 《AAPS PharmSciTech》2009,10(3):906-916
Limited aqueous solubility of exemestane leads to high variability in absorption after oral administration. To improve the solubility and bioavailability of exemestane, the self-microemulsifying drug delivery system (SMEDDS) was developed. SMEDDS comprises of isotropic mixture of natural or synthetic oil, surfactant, and cosurfactant, which, upon dilution with aqueous media, spontaneously form fine o/w microemulsion with less than 100 nm in droplet size. Solubility of exemestane were determined in various vehicles. Ternary phase diagrams were plotted to identify the efficient self-emulsification region. Dilution studies, droplet size, and zeta potential of the formulations were investigated. The release of exemestane from SMEDDS capsules was studied using USP dissolution apparatus in different dissolution media and compared the release of exemestane from a conventional tablet. Oral pharmacokinetic study was performed in female Wistar rats (n = 8) at the dose of 30 mg kg−1. The absorption of exemestane from SMEDDS form resulted in about 2.9-fold increase in bioavailability compared with the suspension. Our studies illustrated the potential use of SMEDDS for the delivery of hydrophobic compounds, such as exemestane by the oral route.Key words: bioavailability enhancement, exemestane, microemulsion, SMEDDS 相似文献
11.
Lipid nanoparticles based on solid matrix have emerged as potential drug carriers to improve gastrointestinal (GI) absorption and oral bioavailability of several drugs, especially lipophilic compounds. These formulations may also be used for sustained drug release. Solid lipid nanoparticle (SLN) and the newer generation lipid nanoparticle, nanostructured lipid carrier (NLC), have been studied for their capability as oral drug carriers. Biodegradable, biocompatible, and physiological lipids are generally used to prepare these nanoparticles. Hence, toxicity problems related with the polymeric nanoparticles can be minimized. Furthermore, stability of the formulations might increase than other liquid nano-carriers due to the solid matrix of these lipid nanoparticles. These nanoparticles can be produced by different formulation techniques. Scaling up of the production process from lab scale to industrial scale can be easily achieved. Reasonably high drug encapsulation efficiency of the nanoparticles was documented. Oral absorption and bioavailability of several drugs were improved after oral administration of the drug-loaded SLNs or NLCs. In this review, pros and cons, different formulation and characterization techniques, drug incorporation models, GI absorption and oral bioavailability enhancement mechanisms, stability and storage condition of the formulations, and recent advances in oral delivery of the lipid nanoparticles based on solid matrix will be discussed. 相似文献
12.
The purpose of this research was to develop and evaluate different preparations of sustained delivery systems, using Carbopols
as carriers, in the form of matrices and three-layer tablets with isosorbite mononitrate. Matrix tablets were prepared by
direct compression whereas three-layer tablets were prepared by compressing polymer barrier layers on both sides of the core
containing the drug. The findings of the study indicated that all systems demonstrated sustained release. The properties of
the polymer used and the structure of each formulation appear to considerably affect drug release and its release rate. The
three-layer formulations exhibit lower drug release compared to the matrices. This was due to the fact that the barrier-layers
hindered the penetration of liquid into the core and modified drug dissolution and release. The geometrical characteristics/structure
of the tablets as well as the weight/thickness of the barriers-layers considerably influence the rate of drug release and
the release mechanisms. Kinetic analysis of the data indicated that drug release from matrices was mainly attributed to Fickian
diffusion while three-layer tablets exhibited either anomalous diffusion or erosion/relaxation mechanisms. The advantage of
Carbopol formulations is that a range of release profiles can easily be obtained through variations in tablet structure and
thus Carbopols are appropriate carriers of oral sustained drug delivery systems for soluble drugs such as the isosorbite mononitrate. 相似文献
13.
14.
《Journal of liposome research》2013,23(1):53-79
AbstractThe characterization of two liposomal formulations of boronated DNA-interacting agents has been performed. It is shown that the two boronated drugs, WSA-Water Soluble Acridine and WSP-Water Soluble Phenantridine, can be encapsulated within unilamellar sterically stabilized liposomes with high drug-to-lipid ratios (up to 0.50:1 (mol:mol)), using transmembrane pH gradients. The steric stabilization of the liposomes was accomplished by the addition of DSPE-PEG(2000) (PEG-lipid) to DSPC/Cho lipid mixtures and the composition used was DSPC: Cho: DSPE-PEG 55:40:5 (moI%). The loading of the drugs resulted in drug precipitation in the liposomal aqueous core as observed by cryo-transmission electron microscopy (c-TEM). Moreover, it is shown that when pH gradients across the bilayer were used for remote loading of WSP or when ammonium sulfate gradients were used for remote loading of WSA, the formation of small bilayer fragments (discs) was induced. We present compelling evidence that the formation of discs is a consequence of precipitate growth in the liposomal interior. The precipitate growth causes some of the liposomes to rupture resulting in the above mentioned disc-formation and a substantial decrease in trapping efficiency. The in vitro stability of the drug loaded liposomes was excellent, both in buffer and in 25% human serum. For most of the formulations, the release of the drugs was below or around 10% after 24 hours at 37oC. Furthermore, the influence of initial internal pH and internal buffering capacity on release properties of WSA and WSP were investigated. It is shown that the release profiles of the drugs can be controlled, to a large extent, by varying the composition of the internal liposomal aqueous phase. 相似文献
15.
Phospholipid/cholesteryl ester microemulsions containing unesterified cholesterol: model systems for low density lipoproteins 总被引:2,自引:0,他引:2
As models for the effects of unesterified cholesterol (UC) on the lipid organization of low density lipoprotein (LDL), microemulsions containing either egg yolk phosphatidylcholine (EYPC) or dimyristoyl phosphatidylcholine (DMPC) as the surface component, cholesteryl oleate (CO) as the core component, and varying amounts of unesterified cholesterol were prepared by sonication. Gel filtration chromatography showed coelution of each of the lipid components, demonstrating the formation of well-defined microemulsion populations. Unesterified cholesterol incorporation into the microemulsions was proportional to the composition of the original mixture at low unesterified cholesterol compositions, but reached saturation at compositions of approximately 15 and 10 mol% unesterified cholesterol for EYPC/CO and DMPC/CO microemulsions, respectively. The Stokes' radius of the microemulsions was constant and similar to native LDL for initial compositions less than 15 mol% unesterified cholesterol, but increased at compositions above 15 mol%. In both EYPC/CO/UC and DMPC/CO/UC microemulsions, no significant changes were observed for the calorimetric or Van't Hoff enthalpy for the thermal transition of the core cholesteryl ester; however, increases in the transition temperature as a function of increasing unesterified cholesterol composition suggests that unesterified cholesterol has a stabilizing effect on the core transition. In DMPC/CO/UC microemulsions, the effect of unesterified cholesterol on the surface-located DMPC could be clearly observed as a broadening of the thermal transition of the acyl chains. These results demonstrate that unesterified cholesterol is located primarily in the surface of these protein-free lipid model systems for LDL. 相似文献
16.
The basic objective of this study was to explore the application of Gelucire 43/01 for the design of multi-unit floating systems
of a highly water-soluble drug diltiazem HCl. Diltiazem HCl-Gelucire 43/01 granules were prepared by melt granulation technique.
The granules were evaluated for in vitro and in vivo floating ability, surface topography, and in vitro drug release. Aging
effect on storage was vvaluated using scanning electron microscopy, hot stage polarizing microscopy (HSPM), differential scanning
calorimetry (DSC), and in vitro drug release. Granules were retained in stomach at least for 6 hours. Approximately 65% to
80% drug was released over 6 hours with initial fast release from the surface. Surface topography, HSPM, DSC study of the
aged samples showed phase transformation of Gelucire. The phase transformation also caused significant increase in drug release.
In conclusion, hydrophobic lipid, Gelucire 43/01, can be considered as an effective carrier for design of a multi-unit floating
drug delivery system of highly water-soluble drugs such as diltiazem HCl. 相似文献
17.
The pharmacokinetics (PK), biodistribution (BD), and therapeutic activity of pegylated liposomal doxorubicin formulations with different drug release rates were studied in an orthotopic 4T1 murine mammary carcinoma model. The focus of these experiments was to study the effects of different release rates on the accumulation of liposomal lipid and doxorubicin (DXR) into the tumor and cutaneous tissues of mice (skin and paws). These tissues were chosen because the clinical formulation of pegylated liposomal doxorubicin (Caelyx)/Doxi) causes mucocutaneous reactions such as palmar-plantar erythrodysesthesia (PPE). Liposomes with different doxorubicin (DXR) leakage rates were prepared by altering liposome fluidity through changing the fatty acyl chain length and/or degree of saturation of the phosphatidylcholine component of the liposome. Liposomes with fast, intermediate, and slow rates of drug release were studied. The plasma PK of the liposomal lipid was similar for all formulations, while the plasma PK of the DXR component was dependent on the liposome formulation. Liposomal lipid accumulated to similar levels in tumor and cutaneous tissues for all three formulations tested, while the liposomes with the slowest rates of DXR release produced the highest DXR concentrations in both cutaneous tissues and in tumor. Liposomes with the fastest drug release rates resulted in low DXR concentrations in cutaneous tissues and tumor. The formulation with intermediate release rates produced unexpected toxicity that was not related to the lipid content of the formulation. The liposomes with the slowest rate of drug leakage had the best therapeutic activity of the formulations tested. 相似文献
18.
Solubility of Drugs in Aqueous Polymeric Solution: Effect of Ovalbumin on Microencapsulation Process
Microencapsulation of water-soluble drugs using coacervation-phase separation method is very challenging, as these drugs partitioned
into the aqueous polymeric solution, resulting in poor drug entrapment. For evaluating the effect of ovalbumin on the microencapsulation
of drugs with different solubility, pseudoephedrine HCl, verapamil HCl, propranolol HCl, paracetamol, and curcuminoid were
used. In addition, drug mixtures comprising of paracetamol and pseudoephedrine HCl were also studied. The morphology, encapsulation
efficiency, particle size, and in vitro release profile were investigated. The results showed that the solubility of the drug determined the ratio of ovalbumin to
be used for successful microencapsulation. The optimum ratios of drug, ovalbumin, and gelatin for water-soluble (pseudoephedrine
HCl, verapamil HCl, and propranolol HCl), sparingly water-soluble (paracetamol), and water-insoluble (curcuminoid) drugs were
found to be 1:1:2, 2:3:5, and 1:3:4. As for the drug mixture, the optimum ratio of drug, ovalbumin, and gelatin was 2:3:5.
Encapsulated particles prepared at the optimum ratios showed high yield, drug loading, entrapment efficiency, and sustained
release profiles. The solubility of drug affected the particle size of the encapsulated particle. Highly soluble drugs resulted
in smaller particle size. In conclusion, addition of ovalbumin circumvented the partitioning effect, leading to the successful
microencapsulation of water-soluble drugs. 相似文献
19.
The aim of this study was to characterize the swelling and floating behaviors of gastroretentive drug delivery system (GRDDS) composed of hydroxyethyl cellulose (HEC) and sodium carboxymethyl cellulose (NaCMC) and to optimize HEC/NaCMC GRDDS to incorporate three model drugs with different solubilities (metformin, ciprofloxacin, and esomeprazole). Various ratios of NaCMC to HEC were formulated, and their swelling and floating behaviors were characterized. Influences of media containing various NaCl concentrations on the swelling and floating behaviors and drug solubility were also characterized. Finally, release profiles of the three model drugs from GRDDS formulation (F1-4) and formulation (F1-1) were examined. Results demonstrated when the GRDDS tablets were tested in simulated gastric solution, the degree of swelling at 6 h was decreased for each formulation that contained NaCMC in comparison to those in de-ionized water (DIW). Of note, floating duration was enhanced when in simulated gastric solution compared to DIW. Further, the hydration of tablets was found to be retarded as the NaCl concentration in the medium increased resulting in smaller gel layers and swelling sizes. Dissolution profiles of the three model drugs in media containing various concentrations of NaCl showed that the addition of NaCl to the media affected the solubility of the drugs, and also their gelling behaviors, resulting in different mechanisms for controlling a drug’s release. The release mechanism of the freely water-soluble drug, metformin, was mainly diffusion-controlled, while those of the water-soluble drug, ciprofloxacin, and the slightly water-soluble drug, esomeprazole, were mainly anomalous diffusion. Overall results showed that the developed GRDDS composed of HEC 250HHX and NaCMC of 450 cps possessed proper swelling extents and desired floating periods with sustained-release characteristics. 相似文献
20.
Katarzyna Szkudelska Leszek Nogowski Tomasz Szkudelski 《The Journal of steroid biochemistry and molecular biology》2009,113(1-2):17-24
Resveratrol is a naturally occurring diphenolic compound exerting numerous beneficial effects in the organism. The present study demonstrated its short-term, direct influence on lipogenesis, lipolysis and the antilipolytic action of insulin in freshly isolated rat adipocytes. In fat cells incubated for 90 min with 125 and 250 μM resveratrol (but not with 62.5 μM resveratrol), basal and insulin-induced lipogenesis from glucose was significantly reduced. The antilipogenic effect was accompanied by a significant diminution of CO2 release and enhanced production of lactate. The inhibition of glucose conversion to lipids found in the presence of resveratrol was not attenuated by activator of protein kinase C. However, acetate conversion to lipids appeared to be insensitive to resveratrol.In adipocytes incubated for 90 min with epinephrine, 10 and 100 μM resveratrol significantly enhanced lipolysis, especially at lower concentrations of the hormone. However, the lipolytic response to dibutyryl-cAMP, a direct activator of protein kinase A, was unchanged. Further studies demonstrated that, in cells stimulated with epinephrine, 1, 10 and 100 μM resveratrol significantly enhanced glycerol release despite the presence of insulin or H-89, an inhibitor of protein kinase A. The influence of resveratrol on epinephrine-induced lipolysis and on the antilipolytic action of insulin was not abated by the blocking of estrogen receptor and was accompanied by a significant (with the exception of 1 μM resveratrol in experiment with insulin) increase in cAMP in adipocytes. It was also revealed that resveratrol did not change the proportion between glycerol and fatty acids released from adipocytes exposed to epinephrine.Results of the present study revealed that resveratrol reduced glucose conversion to lipids in adipocytes, probably due to disturbed mitochondrial metabolism of the sugar. Moreover, resveratrol increased epinephrine-induced lipolysis. This effect was found also in the presence of insulin and resulted from the synergistic action of resveratrol and epinephrine. The obtained results provided evidence that resveratrol affects lipogenesis and lipolysis in adipocytes contributing to reduced lipid accumulation in these cells. 相似文献