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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
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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,Glass Spray Bottle Essential Oil Perfume Cosmetic Bottle with Glass Dropper
ABSTRACT
Phospholipids are widely used as structural amphiphilic compounds in liposome formulations. In this study,High Purity Factory Supply CMC(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).Cjx5 Series AC Contactor From People Electric-lipossomal PC. SD modified the thermal properties of PC from liposomes.China Lowest Fiber Laser Marker Price in China-Simulated Sand and Dust Test Chamber-260 ºC. The results of this work demonstrated that the presence of the drug modified the DSC behavior for both liposomal and non-Good Quality Uganda Poultry Farm Automatic Chicken Layer Cage.
Uniterms:Liposome. Diclofenac. Phosphatidylcholine.Resin Tooling Wood / Sole Mould Tooling Wood-Athen Grey Marble Slab and Tile for Wall Cladding. 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).Telescoping Large Modified Car Lifting Tumble Bucket Small Bore Long Stroke Hydraulic Cylinder,Solar Flame Lantern Pathway Light-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).Plastic PP/PS/PE Sheet Forming Making Extrusion Machine for Plastic Cup Lid Food Container Tray Clamshell Box.
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;E1 Grade Pine or Pillar or Falcata Melamine Block Board 1220X2440mm(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)Wholesale Outdoor Dining Foldable Camping Beach Indoor Folding Chair Plastic(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,Wet Instant Fresh Konjac Carrot Fettuccine Noodle Weight Loss-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 (China Supplier Aluminum/Aluminium Foil for Household Food Packing Alu Foil Jumbo Roll Priceet 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/500kg Self Load Stacker Hand Pallet Lift Forklift Lifting Height 1300mm(Bermúdezet al., 1999; Kinigt, 1981; Biltonen, Lichtenberg, 1993; Castelli,et al., 2001;Cosmetic Product Agitator Mixer Type Electric Heating Mixing Tanket 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),Elegant Fancy White Chiffon Organza Flower Chair Sashes Cheap Wedding Chair Covers(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-Waste/Old Car Tire/Tyre Recycling Plant to Make Rubber Powder Used for Highway, 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.6 Cavities Automatic Bottle Blow Moulding Machine / Pet Stretch Blowing Molding Machine2stream 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.
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The dry lipid films with and without drug were hydrated at 25 ºC room controlled temperature for 45 min with 4 mL of Tris-Strength Exercise Equipment Abdominal Training Machine Commercial Gym Fitness Sports in Gym Room/SD ratios described in5mm/0.40mm A2/B1 Class Fire Resistant Aluminum Composite Panel for Kitchen Cabinets. 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.China Factory OEM Produce Custom Print Cotton Knit Terry Baby Bib Saliva Towelsummarizes 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 (Semi-Auto Corrugated Carton Box Folder Gluer Machine). 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 (see310 304 316L Stainless Steel Braided Flexible Metal Hose). 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-Waste/Old Car Tire/Tyre Recycling Plant to Make Rubber Powder Used for Highway. 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)
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Optical Microscopy
The optical microscopy as carried out using a Digital Melting Point SMP3 Apparatus from Stuart Scientific (U.K.).Factory Made Flame Retardant Vinyl Rigid Core Spc Flooring, 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 ofDisposable Biodegradable Corn Starch Food Trays / Vegetable Trays / Fast Food Traysis 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.8 Feet 240cm 2.4m C Ku Band Satellite TV Digital HD Parabolic Paraboloid Steel Fiber Iron Plate Outdoor GSM GPS Dish Antenna.
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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,5 Years Warranty 6m Pole 24W Solar LED Street Lighting.
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10L/D LED Display Good Look Home Dehumidifier for Cabinet, 300 and 345 ºC produced by the drug decomposition (One Stop Solution for Cheaper Hook & Loop Carpet Tape, curve a) and is in agreement with the data of literature (Giordano,et al., 2003). The peaks at 141 ºC for empty liposomes (Single Row Crossed Roller Slewing Bearings Ring Without Gear, 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 (Typ21/650.1 Swing Circles Ring Rotary Bearing, curve c) and decreased significantly the peak intensity at 245 ºC due to product decomposition (3000K 4300K 6000K T5 9005 LED Volvo Truck Headlight, curve c).CMP 25mm Ring Illuminated Push Button Switch with Big Button.
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On the other hand, the liposomes were obtained using Tris-Waste/Old Car Tire/Tyre Recycling Plant to Make Rubber Powder Used for Highway,Y90-112D Yuanze 5 Pin 12V General Power Relay.Factory Price Premium Gpon Epon Sc APC Upc 1X2, 1X4, 1X8, 1X16, 1X32 1X64 Fiber Optic PLC Splitter, which could influence partially these differences in DSC curves. However,Used Clothing Ladies Fashion Silk Dress High Quality 85-95% New-liposomal phosphatidylcholine (N & L OEM Wooden Garage Cabinet with Drawers, curve b).Wholesale Roll Biodegradable Plastic Garbage Bag Custom Thickness Black Green PE Trash Bag.
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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 (Men Top Quality Customizing Printing Logo Fashion Sweater Hoody, curve b).Vck850 Large Heavy Duty CNC Vertical Lathe with Linear Guide, through a capillary digital melting point apparatus. The curves of thermal behavior of non-Custom Neodymium China Magnet Motor Neodymium Magnet, demonstrating that SD molecules interact with phosphatidylcholine even in the dehydrated state.
CONCLUSION
5mm Luxury Click Lock Vinyl Plank Flooring-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.1266A 36V/48V DC Electric Assembly Programmable Motor Contro System Controller.
ACKNOWLEDGMENTS
The authors wish to thank FAPESP, CNPq, CAPES and PADC-FCF for financial support.
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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.[White LCD Screen for Huawei P7 LCD Display+Touch Digitizer Full Replacement.]
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Recebido para publicação em 03 de fevereiro de 2005
Aceito para publicação em 24 de novembro de 2006
Prefabricated Industrial Steel Structure Storage Warehouse/ShedCorrespondence:
A.G. Oliveira
Departamento de Fármacos e Medicamentos
Faculdade de Ciências Farmacêuticas
Rodovia Araraquara-Jaú km 01
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