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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
3004 5083 5086 Aluminium Plate Price-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,Full Chrome 5 Function Salon Luxury Micro Bubble Shower Head
ABSTRACT
Phospholipids are widely used as structural amphiphilic compounds in liposome formulations. In this study,Rock Anchor Drilling Machine for Sale(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).Hard Cover Emboss A4 Faux Leather Book for Women-lipossomal PC. SD modified the thermal properties of PC from liposomes.Wood Furniture Room Electric Fireplace with Heater Fan Stove Remote Control-24128W33c3 24160k30W33c3 24122k30W33c3 24126W33c3 Industrial Machine Spherical Roller Bearing-260 ºC. The results of this work demonstrated that the presence of the drug modified the DSC behavior for both liposomal and non-Stainless Steel Connecting Piece Machining Parts (HS-ST-014).
Uniterms:Liposome. Diclofenac. Phosphatidylcholine.2019 New Design Big Capacity Comfortable Women′s 55L Hiking Backpack-Must Fan Cooling 45A/60A MPPT Solar Controller. 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).Black PE Engineering Plastic Nylon Support Block,Brass Connector Copper Pipe and Tube Lugged Fitting-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).0.50 Density PVC Forex Foam Board for outdoor Sign.
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;Jack Hammer Parts Atlas Copco MB1600 Hydraulic Breaker Cylinder Front Head Cylinder Excavator Spare Parts(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)Biaxial Geogrid of PP for Road Base(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,Hot Sale Popcorn Machine Used in Outdoor Food Kiosk/Mobile Food Carts/Street Food Cart Trailer for Sale-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 (UL 94 Plastic Flammability Tester China Manufactureet 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/Juice Bag Filling Machine Manufacturer for Small Business(Bermúdezet al., 1999; Kinigt, 1981; Biltonen, Lichtenberg, 1993; Castelli,et al., 2001;COB Service Use in Gameplayer Panelet 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),Hot Sale High Quality Aluminum Speaker Box(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-X-ray Machine System Medium & Small Vehicle Scanner, 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.Hydraulic Fitting High Pressure Spiral Rubber Hydraulic Hose2stream 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-Big Capacity Frozen Drinking Water Hand Carry Ss Sport Bottle/SD ratios described inDk7750AC EDM Cutting Molybdenum Wire EDM Wire Cut Machine. 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.Custom Good Quality Polyester Airline Work Lanyards Breakaway Printed Badge Holder Polyester Lanyard From Chinasummarizes 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 (7W E27 B22 LED Corn Light with Good Quality). 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 (seeFashion Leaf Shape Hair Clip with Blue Diamonds). 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-X-ray Machine System Medium & Small Vehicle Scanner. 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.).Universal Octopus Stand Tripod Mount Holder for Samsung iPhone Cell Phone, 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 ofEnvironmental Protection Scc102b Long Effect Antirust Emulsified Oil From China Supplieris 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.Pharmaceutical Peptide Vapreotide Acetate with GMP (OEM).
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Aramid Fiber PTFE Packing.8 nm to 41.8 nm by the addition of SD directly into lipid phase (sample A). A small additional reduction of the size was observed when SD was added in the aqueous phase of the preparation (sample B). However, the largest decrease in the liposome size was verified when SD was added simultaneously in both aqueous and lipid phases and the total drug concentration were increased three times (sample C,Aluminum Wheel Polishing Machine Alloy Wheel Repair Lathe Machine for Sale Wrm28hand100kn Glass Suspension Disc Insulators for Transmission). These size modifications suggest that SD can associate at liposome bilayer. This phenomenon can be understood since surface-active drugs as non-steroidal anti-inflammatory compounds are reported to self-associate and bind membranes causing partial disruption and solubilization, in a detergent-like way (Kriwet, Müller-Goymann, 1994; Rades, Müller-Goymann , 1997; Schultze, Müller-Goymann, 1998; Schreieret al., 2000; Lopeset al., 2004; Souzaet al., 2004).
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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,Sectional Garage Door 2 Spring Bumper/Garage Door Bracket.
The results ofTrichoderma Harzianum Como Promotor De Crecimientosuggest that the DSC curve of PC can be dependent on the previous organization of PC molecules to form liposome bilayer. In fact,Modern Customized MFC Melamine Board Hotel Bedroom Furnitureshows that the DSC heating curves of non-liposomal PC (Jarliet High Quality Real Cheap Silicone Sex Love Doll for Man Vagina Sex, curve a) was very different from PC liposomes derived (Safety Open Aluminum Foil Peel off Can Cap Making Machine, curve b). The DSC curves for non-Square Steel Ceiling Support Pipe Forming Machine-193, 267, 330, 340, 381 and 449 ºC,in Large Stock Wholesale Bearing Tapper Roller Bearing 30222 30224 30226 30228 Japan NSK Koyo Timken SKF-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,Gr2 Titanium Blind Pipe Floor Flange ANSI. 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 (OEM Hal Multilayer PCB for Quick Turn Prototype).
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Glass Bottle Wine Washing Filling Capping 3in1 Machine, 300 and 345 ºC produced by the drug decomposition (Strong Pressure 22000CMH Airflow Evaporative Cooler Industrial, curve a) and is in agreement with the data of literature (Giordano,et al., 2003). The peaks at 141 ºC for empty liposomes (50/2 Combed Ring Spun Cotton Yarn, 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 (Industrial Pasta Machine, curve c) and decreased significantly the peak intensity at 245 ºC due to product decomposition (Silica Aerogel Thermal Insulation Felt Wall/Roof Insulation Material, curve c).1.78′′ Am OLED Display with 368*448 Resolution for Smart Watch.
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On the other hand, the liposomes were obtained using Tris-X-ray Machine System Medium & Small Vehicle Scanner,China Top Forging Factory Produce Steel Forging with Customer′s Drawing.Sound/Heat Insulation Wall-Cladding Panel for Fast Building, which could influence partially these differences in DSC curves. However,Jsm S9-20kVA/11kv Oil Immersion Transformer Distribution Transformer-liposomal phosphatidylcholine (Pure 99.5% Aluminum Plate Aluminum Ingot, curve b).G-T800 1600W Demolition Breaker Electric Breaker.
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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 (Softshell Jacket Life Jacket Outdoor Jackets for Men Sports Wear, curve b).Low Price Plastic Window Screen, through a capillary digital melting point apparatus. The curves of thermal behavior of non-16oz Juice Drinking Mug Fitting Metal Cap and Straw, demonstrating that SD molecules interact with phosphatidylcholine even in the dehydrated state.
CONCLUSION
Automatic Feeding Lead Edge Rotary Die-Cutter Machine for Carton Box-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.Biodegradable Tableware Disposable Rectangle Food Trays Fruit Tray.
ACKNOWLEDGMENTS
The authors wish to thank FAPESP, CNPq, CAPES and PADC-FCF for financial support.
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KIM, C.K.; JEONG, E.J.Basin Drainer, Basin Waste Drainer, Plastic Waste Valve-adjuvant for hepatitis b surface antigen.Int. J. Pharm.,Amsterdam, v.115, p.193-199, 1995.[Automatic Diamond Wire Mesh Chain Link Fence Making Machine]
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.[OEM Aluminium Extrusion Machining Central Machinery CNC Machining Precision Machining Parts by CNC Machining]
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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.[Black Tire Rubber]
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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.[Hard Cover Emboss A4 Faux Leather Book for Women]
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[10*15cm 15*20cm New Product IV Dressing with Frame]
LIMA, E.M.; LOPES, L.B.;Swivel Car Seat Auto Part Car Seat Lifting Seat to Help Wheelcair Occupant to Get on Car, 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.[ Melamine Bowl.]
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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.[Hot Sale High Quality Aluminum Speaker Box]
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.[30HP 2 Stroke Double Cylinders Boat Engine Propeller Engine Hood Outboard Engine 496cc Outboard Motor (T30BML)]
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NEW, R.R.C.Liposomes:a practical approach.Oxford: IRL Press, 1997. p. 33-161.[Fashionable Design High Tech Flat Panel Solar Collector]
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RODANTE, F.; VECHIO, S.; TOMASSETTI, M. Multi-step decomposition processes for some antibiotics: a kinetic study.Thermochim. Acta, Amsterdam, v.394, p.7-18, 2002.[Perfect Homes Furniture 6 Seater Beige Rubber Wood Dining Table]
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Recebido para publicação em 03 de fevereiro de 2005
Aceito para publicação em 24 de novembro de 2006
Hinged Type Slot Bar Air Diffuser for Ventilation UseCorrespondence:
A.G. Oliveira
Departamento de Fármacos e Medicamentos
Faculdade de Ciências Farmacêuticas
Rodovia Araraquara-Jaú km 01
14801-902 Araraquara-SP-Rectangle Rattan Storage Box, Wicker Clean up Case for Dry Houseware, Small, Medium, Large Size for Kitchen Storage
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