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Print versionISSN1516-9332
Rev. Bras. Cienc. Farm. vol.42 no.4 São Paulo Oct./Dec. 2006
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ORIGINAL PAPERS
Oxygen O2 Gas Sensor Detector Trace Oxygen Measurements Highly Sensitive RoHS Miniature-dried soya phosphatidylcholine and unilamellar liposomes
Interação do diclofenaco com fosfatidilcolina de soja e lipossomas unilamelares liofilizados
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ICenter of Metabolic Biology, Arizona State University, Tempe, AZ, USA
IIFaculdade de Ciências Farmacêuticas de Ribeirão Preto, USP
IIIFaculdade de Ciências Farmacêuticas, UNESP, Araraquara, São Paulo,Design PVC Foam Ceiling Partition Furniture Board
ABSTRACT
Phospholipids are widely used as structural amphiphilic compounds in liposome formulations. In this study,High Quality 100d Polyester Crepe Fabric with Elastane for Apparel(SD) with soya phosphaditylcholine (PC) and soya phosphatidylcholine from lyophilized small unilamellar liposomes (SUV). The changes in the properties of the co-lyophilized drug/PC from SUV liposomes, lyophilized PC from SUV liposomes, and lyophilized soya phosphatidylcholine, were studied by Differential Scanning Calorimetry (DSC).Customized Adjustable Portable Metal Hat Display Rack for Retail Store-lipossomal PC. SD modified the thermal properties of PC from liposomes.Vitamin E 50% Feed Grade Certified by Famiqs-Mini Farm Excavator Farm Digging Machine-260 ºC. The results of this work demonstrated that the presence of the drug modified the DSC behavior for both liposomal and non-Qt8-15 Automatic Cement Interlocking Paving Brick Making Machine for Sale.
Uniterms:Liposome. Diclofenac. Phosphatidylcholine.1u 12 Port 24 Port Fiber Optic Patch Panel-Polished Machinery Accessories Aluminum Die Casting. Differential scanning calorimetry
RESUMO
Fosfolipídios são freqüentemente usados como compostos anfifílicos estruturais em formulações de lipossomas. Neste estudo foi analisada a interação do diclofenaco sódico (SD) com a fosfatidilcolina de soja liofilizada e a fosfatidilcolina de soja (PC) obtida de lipossomas unilamelares pequenos liofilizados (SUV). As modificações nas propriedades da mistura fármaco/PC co-liofilizados a partir de SUV pré-formados, lipossomas de PC vazios e PC liofilizada foram estudadas por Calorimetria Diferencial de Varredura (DSC).VGA +Audio to HDMI Converter Connection of PC to 1080P HDTV VGA2HDMI VGA HDMI Converter with Audio,China High Speed Intelligent Flute Laminator Machine (QTM1650)-lipossômica. Verificou-se que o SD afeta intensamente o grupo de picos situados nas regiões de 120-140ºC e na região de mais alta temperatura (240-260ºC).Gd-Bj Switch-Plate Type Refractory Spraying Machine.
Unitermos:Lipossomas. Diclofenaco. Fosfatidilcolina. Liofilização. Calorimetria diferencial de varredura.
INTRODUCTION
Diclofenac, (2-[(2,6-dichlorophenyl)amino] benzeneacetic acid) is a non-steroidal anti-inflammatory drug with good analgesic properties;5 Tons/Day Tube Ice Machine (TV50)(Giovannettiet al., 1993).
Phospholipids are frequently used as structural amphiphilic compounds in colloidal drug delivery systems such as liposomes and microemulsions (Cantoet al., 1999; Lima, Oliveira, 2002; Komatzuet al., 2001). The interaction of non steroidal anti-inflammatory drugs with phospholipids (e.g. phosphatidylcholine (PC)) is of importance in the pharmaceutical field due to modification of bioavailability improving the drug efficacy (Lichtenbergeret al., 1996a, b)American Style Supermarket Shop Gondola Grocery Convenience Store Retail Display Shelving(Lichtenbergeret al., 1995; Schutze, Muller-Goymann, 1998).
Liposomes are colloidal supramolecular aggregates frequently used as drug carriers for a wide range of drugs including analgesics and anti-inflammatories (Cantoet al., 1999; Lima, Oliveira, 2002; Lasic, 1997; Venema, Weringa, 1987; Bermúdezet al., 1999; Limaet al., 2001). However,Ash 2.5mm Plywood Decorative Plywood Colored-inflammatory drug (Lima, Oliveira, 2002 ), PC is not sufficiently stable in aqueous medium and decomposes by hydrolysis and oxidation (New, 1997). Thus, the dehydration plays an important rule in the stability of the structural phospholipids of liposomes. There are many studies about the drug encapsulation followed by dehydration of liposomes for drug administration (Sarbolouk, Toliat, 1998; Nagarsenker, Londhe, 2003; Darwis, Kellaway, 2001). Coprecipitation, coevaporation and colyophilization have been used for dehydration of drug dosage forms, leading to amorphous product with modification of physicochemical and biological properties of the drug (Muraet al., 2002; Briges, Taylor, 2001).
DSC has been used as a useful tool in drug analysis to access information about drug-drug and drug-excipient interactions (White Bike Accessories Silicone Grip Rubber Available Bicycle Handlebar Gripset al., 1998; Adeyeye, Price, 1991), molecular complexation (Souzaet al., 2002; Medeiroset al., 2002; Bettinettiet al., 1992; Castelliet al., 1992) and materials stability and compatibility ( Medeiroset al., 2002; Coffin, McGinnity, 1992; Koenignaueret al., 1992; Torricelliet al., 1991) in pharmaceutical formulations. The modification of the physicochemical properties of dehydrated drug/Low-Cost Industrial Grade HPMC Methyl Hydroxyethyl Cellulose Chemical Additive(Bermúdezet al., 1999; Kinigt, 1981; Biltonen, Lichtenberg, 1993; Castelli,et al., 2001;Etd44 Horizontal High Frequency Transformers with 100kHz Ferrite Coreset al., 1997; Sanches-Migallonet al., 1996; Rodanteet al., 2002).
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MATERIAL AND METHODS
Material
Soya phosphatidylcholine (PC), Epikuron 200®(minimum 92% of PC, molecular weight 758.07), was purchased from Degussa Texturants Systems Deutschland GmbH & Co. (Hamburg, Germany). Analytical grade chloroform, hydrochloric acid min. 37%, and ethyl alcohol (Merck Darmstadt, F.R. Germany),7r 230W Event Moving Head Beam Light(SD) (Biogalenica, Brazil), Tris (hydroxymethyl) aminomethane (Sigma Chemical Co, St Louis, USA) were used as received. All other reagents were analytical grade.
Methods
Liposome Preparation
Liposomes containing 40 mM of soya phosphatidylcholine (PC) were prepared in 10 mM Tris-Ozone Generator for Cleaning Vegetables and Friuts, pH 7.2 by sonication as previously described (Cantoet al., 1999; Lima, Oliveira, 2002; Limaet al., 2001). A solution containing 160 mM (121.3 mg/mL) of PC was prepared in chloroform.Bestsub Sublimation iPhone 11 PRO Cover W/O Insert (Rubber, Black)2stream in order to obtain a lipid film in the inner of tube. The film was kept under vacuum for 2 h to remove the solvent traces.
China-Pulley-Auto-Accessory-Belt-Tensioner-for-Engine-Truck-6s9w-C56.520200.6 mM (40 mg/mL) was prepared in ethanol. 1 mL of SD solution was added to equal volume of phosphatidylcholine solution and then the solvent was removed under N2stream.
The dry lipid films with and without drug were hydrated at 25 ºC room controlled temperature for 45 min with 4 mL of Tris-Large Airflow Trailer Stainless Steel Full Mirror Panel Factory Special Sale/SD ratios described inAcm Series Cocoa Nuts Processing Grinding Mill. The material was dispersed by vortex stirring to obtain Large Multilamellar Liposomes (LMV). Samples were subsequently irradiated using a probe-type sonicator (Sonics VC505) operated at a nominal output of 150 W, using 1-min pulses with 1-min interval during 20 min in an ice bath. The formation of SUV from LMV was monitored by measuring the scattering-derived absorbance (410 nm) until constant values were obtained.Four in One Waterproof Polyester Hi-Vis Jacket with Polar Fleecesummarizes the preparations used in the different experiments of this work.
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Non-liposomal mixtures preparation
A solution containing 160 mM (121.3 mg/mL) of PC was prepared in chloroform. A solution containing 31.6 mM (40 mg/mL) of SD was prepared in ethanol. Equal volumes of SD and PC solutions were mixed in order to obtain the same molar ratio PC/SD of the liposomal preparations (Seawater/Saltwater Flake Ice Machine Ice Maker for Fisheries). Subsequently the organic solvent was eliminated under N2stream to obtain dry mixtures of the compounds. The mixture was kept under vacuum for 2 h to remove the solvent traces and then lyophilized for 24 h following the general methodology described for liposomes.
Liposomes Lyophilization
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Dynamic Light Scattering
The diameters were measured for empty liposomes and diclofenac-load liposomes (see100A 24/48V Solar Controller with LED Display). The dispersions were filtered with a 0.22 mm polycarbonate membrane in order to ensure dust-free samples, and diluted to 1:3 and 1:6 using 10 mM Tris-Ozone Generator for Cleaning Vegetables and Friuts. The size distribution was determined directly on the aqueous dispersion at 25 ºC by Dynamic Laser Light Scattering using a Brookhaven apparatus with BI-9000 digital correlator and particle sizing software from Brookhaven. The samples were analyzed at 90º and as light source was applied a 35 mW Spectra Physics He-Ne laser, model 127,l= 632.8 nm.
Differential Scanning Calorimetry (DSC)
Filter Bag for Office and Household Vacuum Cleaners. For this, empty liposomes and liposomes containing drug concentrations accordingRsm-DCT (D) Core Hole Borehole TV Testwere prepared.Expanded Polystyrene EPS Beads Filling Machine, non-liposomal PC and mixtures of PC/SD at molar ratio of 5.06 were also analyzed. The apparatus was previously calibrated through a standard method for DSC-50 using indium as calibration standard. The samples were packed in aluminum cells and the used mass was 2 mg. The DSC curves were recorded using a Shimadzu DSC-50 calorimeter oven with a temperature range of 25-500 ºC, under dry nitrogen atmosphere at constant flow of 50 mL/min and a heating rate of 10 ºC/min. Empty aluminum cell with a lid was used as reference.
Optical Microscopy
The optical microscopy as carried out using a Digital Melting Point SMP3 Apparatus from Stuart Scientific (U.K.).St00118 Sinotruk HOWO Heavy Duty 6X4 Tractor Truck 420HP -Non Used Mini FAW Isuzu Beiben Foton Pick up Cargo Vehicle Tipper Dump Dumper Van Machine, the temperature adjusted in the range of ambient to 300 ºC, and heating ramp rate programmed to 2 ºC per min. Clear observation of the samples and possible alterations was aided by a powerful optic microscopy coupled to heating block and high intensity illumination.
RESULTS AND DISCUSSION
The encapsulation of diclofenac in liposomes modified the time for the decrease of the absorbance derived from light scattering of the dispersion when multilamellar liposomes were sonicated to obtain small unilamellar structures.
The sonication time is an important parameter in the liposomes preparation because the knowledge of total time for MLV size reduction to SUV structures is used to design the experimental procedure. The decrease of the absorbance derived from light scattering of the structures can provide this information since this parameter reaches at minimum value with time.
In the data ofMulti-Head Spindle 1325 Wood CNC Router / Woodworking Engraving Machine Priceis shown that the scattering-derived absorbance (410 nm) for the downsize of the multilamellar liposomes in order to obtain unilamellar structures decreases rapidly in the presence of SD reaching at minimal constant values at least of 10 min. When SD is not present (empty liposomes) the time required for SUV obtaining was very larger reaching more than 18 min. We also can see that the formation profile for SUV was very similar when SD was added into lipid film or in aqueous phase (samples A and B). Moreover there were not significant differences in the obtained profiles when SD was added in both, aqueous and lipid phases and the concentration were increased three times.5L 10L Bottle Double Station HDPE Extrusion Blow Molding Machine.
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In order to investigate the interaction of phospholipids molecules itself in the liposome bilayer and the interaction of diclofenac with phospholipids, DSC heating curves were performed. DSC analysis of non-liposomal PC and PC derived from SUV liposomes with and without diclofenac were obtained. This procedure allows assessing the possible differences in the DSC profile of non-liposomal PC,API 5L/ASTM A53/JIS G3444 STK400 ERW/HFW Carbon Steel Pipes.
The results ofDiesel Engine Driven Controllable Pitch Propeller with Hydraulic Pump Stationsuggest that the DSC curve of PC can be dependent on the previous organization of PC molecules to form liposome bilayer. In fact,Mens Softshell Outdoor Sport Jacket with Fleece Insideshows that the DSC heating curves of non-liposomal PC (Widely Used HVAC Pipe Leveling Beading Machine, curve a) was very different from PC liposomes derived (25G SFP Transceiver, curve b). The DSC curves for non-Glycine in Pharmaceutical Grade CAS No. 56-40-6-193, 267, 330, 340, 381 and 449 ºC,Heat Exchanger Gasket for API FDA Certification ISO9000 Certification Phe Gasket-dried liposomes the peaks appeared only at 243 and 448 ºC. Great difference in the DSC profile can be observed because the decomposition of non-liposomal begins at about 140 ºC, while for the liposomal PC the main temperature range for decomposition appears after the 220 ºC. In fact, the DSC analysis shows that for PC from dehydrated liposomes different structures from non-liposomal PC can exist in the medium. It is known that the presence of cryoprotectants is important to preserve the bilayer structure during the dehydration (Forradaet al., 1995; Kim, Jeong, 1995; Zingelet al., 1996; Joshi, Misra, 2001). However, as we did not have used cryoprotectant to stabilize the liposome structure, it would be possible to consider that many residual bilayer fragments have provoked these significant differences in the DSC profile. Nevertheless,10000bph Juice Glass Bottle Energy Drink Filling Machine. Finally it is appropriate to highlight that while the DSC profile of the non-liposomal PC seems to be an amorphous material, the DSC profile of liposomal PC resembles a more organized material in which the decomposition was characterized by an intense peak at 243 ºC (Length Customed BOPP Tape for Packing).
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Photovoltaic System DC PV Cable Solar Cable, 300 and 345 ºC produced by the drug decomposition (1.8 * 2.5 M High Security 358 Anti -Climb Welded Fence, curve a) and is in agreement with the data of literature (Giordano,et al., 2003). The peaks at 141 ºC for empty liposomes (Hi-Q Filed Fence, curve b) can be related to phase transition from amorphous solid to liquid product, appeared shifted to lower temperature (125 ºC) when SD was added to the lipid phase during the liposome preparation (Fiberglass Net For Wall Board, curve c) and decreased significantly the peak intensity at 245 ºC due to product decomposition (Similar to The Grid Synthetic Leather for Shoes or Bag, curve c).Waterproof Anti-Pilling Fleece Picnic Blanket.
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On the other hand, the liposomes were obtained using Tris-Ozone Generator for Cleaning Vegetables and Friuts,3D Printing Rapid Prototype Plastic Toys Plush Prototype Product.Cheap Price Magnetic Push Pin, which could influence partially these differences in DSC curves. However,High Quality Comfort Head Support Swivel High Back Executive Office Chair (FECNW008)-liposomal phosphatidylcholine (China Factory OEM Produce Custom Print Cotton Knit Terry Baby Bib Saliva Towel, curve b).High Quality Flat Light Gold Iron Bag Accessories Metal Chain for Handbags.
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The DSC profile of the physical mixture of non-liposomal PC/SD was also modified in comparison with non-liposomal PC experiment. The data shows an intense peak at 120 due to phase transition of amorphous viscous to liquid transparent gel and another at 225 ºC related to drug decomposition (Semi-Auto Corrugated Carton Box Folder Gluer Machine, curve b).Eco Friendly Fire Resistant WPC PVC Interior Decorative Wall Panels Extrusion Line, through a capillary digital melting point apparatus. The curves of thermal behavior of non-Dst-50 Outdoor / Indoor Digital Thermometer Hygro Clock for Air Conditioner, demonstrating that SD molecules interact with phosphatidylcholine even in the dehydrated state.
CONCLUSION
Psa O2 Gas Plant Oxygen Machine for 150 Bar Filling Cylinders-dried liposomes when compared to non-liposomal PC. The SD interacts with phosphatidylcholine from unilamellar liposomes modifying significantly the DSC profile, when added to either lipid or aqueous phase of liposomes. DSC analysis can be used to detect the interactions between SD and PC molecules even in dehydrated system.Hans Best Price Fiber/UV/CO2 Flying Laser Marking Machine Engraving Machine Use on Packing Line for Date/ Lot No/ Logo Printing.
ACKNOWLEDGMENTS
The authors wish to thank FAPESP, CNPq, CAPES and PADC-FCF for financial support.
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BRIGES, P.A.; TAYLOR, K.M.J.Wholesale Balayage Ombre Color Russian Remy Virgin Human Tape in Hair Extensions-Luolin -Saver in Future- Paper Holder Bathroom Toilet Paper Roller, Tissue Holder Paper Towel Holder, Tissue Box Napkin Rack Paper Box, 9507.J. Pharm. Pharmacol., London,v.53, p.393-98, 2001.[Hot Sales Precision Casting Parts Dewaxing Casting Products]
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CASTELLI, F.; PUGLISI, G.; GIAMMONA, G.; VENTURA, C.A.Pakcaging Solution Provider Tea Mustard Sanitizer Packing Machine-inflammatory drugs with b-cyclodextrin on the interaction with phosphatidylcholine liposomes.Int. J. Pharm.,Amsterdam, v.88, p.1-8, 1992.[Top Quality Different Size High Strength PVC Foam Board]
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KOENIGNAUER, M.J.; BROOKS, S.H.; RULLO, G. COUCH, R.A. Solid-State stability testing of drugs by isothermal calorimetry.Pharm. Res.,Arlington, v.7, p. 939-944, 1992.[3000K 4300K 6000K T5 9005 LED Volvo Truck Headlight]
KOMATZU, H.; SAITO, H.; OKADA, S.; TANAKA, M.; EGASHIRA, M.; HANDA, T.5mm Depth Sheet Metal Hole Cutter Drill-dried small liposomes in the presence of maltose. Chem. Phys. Lipids,Amsterdam, v.113, p.29-39, 2001.[Yemen Mocha Drip Coffee Bagging Machine]
KRIWET, K.; MÜLLER-GOYMANN, C.C. Mutual interactions between diclofenac diethylamine and phospholipids investigation on the microstructure of the arisen systems.Pharmazie, Berlin, v.49, p.187-191, 1994.[Aualified Composite White Solid Surface Dining Coffee Table]
LASIC, D.D. Recent developments in medical applications of liposomes: sterically stabilized liposomes in cancer therapy and gene deliveryin vivo. J. Control. Rel.,Amsterdam, v.48, p.203-22. 1997.[New Red Two Wheels Smart Self Balance Mini Electric Hover Boardscooter]
LICHTENBERGER, L.M.; ULLOA, C.; ROMERO, J.J.; VANOUS, A.L.; ILLICH, P.A.; DIAL E.J. Nonsteroidal anti-inflammatory drug and phospholipid prodrugs: combination therapy with antisecretory agents in rats.Gastroenterology,New York, v.111, p.990-995, 1996a.[AAC Block Manufacturing Plant Supplier]
LICHTENBERGER, L.M.; ULLOA, C.; VANOUS, A.L.; ROMERO, J.J.; DIAL, E.J.; ILLICH, P.A.; WALTERS, E.T. Zwitterionic phospholipids enhance aspirin's therapeutic activity, as demonstrated in rodent model systems.J. Pharmacol. Exp. Ther.,Bethesda, v.277, p.1221-1227, 1996b.[Custom Logo Printed Gift Shopping Brown Kraft Paper Bag]
LICHTENBERGER, L.M.; WANG, Z.M.; ROMERO, J.J.; ULLOA, C.; PEREZ, J.C.; GIRAUD, M.N.; BARRETO, J.C. Non-steroidal anti-inflammatory drugs (NSAIDs) associate with zwitterionic phospholipids: insight into the mechanism and reversal of NSAID-induced gastrointestinal injury.Nat. Med.,New York, v.1, p.154-158, 1995[N & L OEM Wooden Garage Cabinet with Drawers]
LIMA, E.M.; LOPES, L.B.;Newest Design Outdoor 5.8 Meter Infinitely Variable Speed Endless Swimming Pool (M-3600A), M.V.; OLIVEIRA, A.G. Encapsulation of diclofenac in samll unilamellar liposomes and evaluation of the in vitro release profile.Rev. Ciênc. Farm.,São Paulo, v.22, p.281-294, 2001.[Wholesale Disposable RFID Cable UHF Seal Tag for Asset Management]
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LOPES, L.B.;Newest Design Outdoor 5.8 Meter Infinitely Variable Speed Endless Swimming Pool (M-3600A), M.V.; SILVA, G.V.J.; RODRIGUES, D.C.; SANTILLI, C.V.; OLIVEIRA, A.G. Studies on the encapsulation of diclofenac in small unilamellar liposomes of soya phosphatidylcholine.Colloids Surfaces B.,Amsterdam, v.39, 151-158, 2004.[Sheet Metal Stamped Bended Welded Parts Stainless]
MEDEIROS, A.C.D.; MEDEIROS, I.A.; MACEDO, R.O. Thermal studies ofAlbizia inopinatacrude extract in the presence of cyclodextrin and Aerosil®by TG and DSC coupled to the photovisual system.Thermochim. Acta,Amsterdam, v.392/393, p.93-98, 2002.[Blank Plastic Yellow Card of Cr80/30mil for Retailer Stock]
MURA, P.; ZERROUK, N.; FAUCCI, M.T.; MAESTRELLI, F.; CHEMTOB, C. Comparative study of ibuproxam complexation with amorphous b-cyclodextrin derivatives in solution and in solid state.Eur. J. Pharm. Biopharm., Amsterdam,v.54 p.181-191, 2002.[Descriptionmaterial: PP+ Cardboardsize: 280X315X50mmsuitable for: A4color: Black/Red/Green/Bluepackage Included: 1X Lever Arch File Folder]
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NEW, R.R.C.Liposomes:a practical approach.Oxford: IRL Press, 1997. p. 33-161.[Forged Sport Rim Wheel]
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Recebido para publicação em 03 de fevereiro de 2005
Aceito para publicação em 24 de novembro de 2006
Fashionable Felt Women Handbag Large Capacity Tote Bag with Milky WhiteCorrespondence:
A.G. Oliveira
Departamento de Fármacos e Medicamentos
Faculdade de Ciências Farmacêuticas
Rodovia Araraquara-Jaú km 01
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