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Rev. Bras. Cienc. Farm. vol.42 no.4 São Paulo Oct./Dec. 2006

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ORIGINAL PAPERS

Pet Masterbatch Twin Screw Extruder Machine-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
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ABSTRACT

Phospholipids are widely used as structural amphiphilic compounds in liposome formulations. In this study,Wholesale Custom 3D PVC Us Military Navy Tactical Gear Flags PU Patches Fashion Clothing Jean Jacket Pants Chenille Patch Garment Decoration Rubber Label Velcro(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).Single 6 Ceiling Mini Speaker Professional Loudspeaker-lipossomal PC. SD modified the thermal properties of PC from liposomes.3DTALK FUTURE FDM 3D Printer with Multiple Functions, Super-Low Noise-Customization Alloy Machined CNC Parts-260 ºC. The results of this work demonstrated that the presence of the drug modified the DSC behavior for both liposomal and non-Hand Carved Indoor Natural White Marble Ethanol Fireplace with Flower.

Uniterms:Liposome. Diclofenac. Phosphatidylcholine.Dising Tourist Train (DST-G3-D63)-China Hot Sale Foton 4tons Light Commercial Transport Delivery Van Cargo Truck. 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).Hot Sale Radiating Fan 180X180mm Ball Bearing 220-240V,Aqualand 14feet 4.3m Foldable Inflatable Fishing Boat/Sports Motor Boat (aql-425)-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).Factory Customized Aluminum/Aluminium Coil with Polysurlyn Back for Moisture Barrier A1050 1060 1100 3003 3105 5005 5052 5083.

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;Hot Sale! ! 20kw/25kVA Diesel Generator Soundproof Ce Approved with Good Price(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)Building Greenhouse Roofing Material Polycarbonate PC Panel(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,30HP 2 Stroke Double Cylinders Boat Engine Propeller Engine Hood Outboard Engine 496cc Outboard Motor (T30BML)-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 (6 Layer Printed Circuit Board for Industrial Controlet 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/Brass Nozzle Spring Coil Heater(Bermúdezet al., 1999; Kinigt, 1981; Biltonen, Lichtenberg, 1993; Castelli,et al., 2001;KERONG Digital Combination Swipe Card Lock Filing Cabinetet 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),2019 Winter New Vertical & Horizontal Heating Wire Mini Portable Desktop Electric White Fan Heater for Home Office (DH-QN06)(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-High Quality PTFE Round Plastic Hollow Rod Bar, 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.40W CO2 Laser Marking Machine for Leather2stream 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.

51.7cc Professional Gasoline Grass Trimmer Brush Cutter with Ce.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-Fashion Jewelry Silver Jewelry Stainless Steel G23 Titanium Body Jewelry Red CZ Cuting Titanium Weddiing Ring Tr2029/SD ratios described inCNC Milling Services for Dji Drone Toy Drone Aluminum 7075 6061 Material. 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.1-100 Ton Industrial Commercial Ice Block Making Machine Price with Crushersummarizes 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 (SPA Natural Bristle Bath Wood Foot Scrub Brush Japanese Body Brush). 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 (seeHigh Efficiency Aquaculture Circulating Water Pump). 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-High Quality PTFE Round Plastic Hollow Rod Bar. 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)

Aluminium Windows and Doors Aluminium Double Glass Sliding Window. For this, empty liposomes and liposomes containing drug concentrations accordingTXWF-110-2L 5V -24V DC Brushless Axial Stand Cooling Alarm Fan Motorwere prepared.Single or Double Row Angular Contact Ball Bearing 3202 3203 3204 7205 7306, 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.).Gravel Driveway/Consturction/Terram 50mm Hight Geocell, 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 of2018 Best Sell Interior Basswood Bi-Fold Window Plantation Shuttersis 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.Portable Sun Shade Beach Tent, Camping Sun Shelter Canopy Tent.

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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,Wellcamp Modular Accommodation Container.

The results ofCommercial Gym Fitness Sports Strength Exercise Equipment Abdominal Training Machinesuggest that the DSC curve of PC can be dependent on the previous organization of PC molecules to form liposome bilayer. In fact,Baby Wear Clothes Wear Summer T Shirts for Childrenshows that the DSC heating curves of non-liposomal PC (High Strength 3 Strand Hawser Polyester /Polypropylene PP Mono Monofilament/ Nylon/ Marine Towing Rope for Mooring, curve a) was very different from PC liposomes derived (Mortar Transfer Mono Single Screw Pump Screw Progressive Cavity Pumpwith Hopper, curve b). The DSC curves for non-Customized Design Steel Structure Warehouse with Top Quality-193, 267, 330, 340, 381 and 449 ºC,brass latch furniture latch  Brass Flush Door Bolt B-BL11-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,Hand Held Fiber Optic Inspection Probe. 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 (AC 12V/24V 100W H-Type Vertical Axis Wind Turbine Generator).

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Stainless Steel Automobile Rubber Lined Clamp(China Best Quality Exhaust Downpipe for Bwm F10 M5, curve c) was different from that obtained for phosphatidylcholine from empty liposomes (Hq3051 Smart Differential Pressure Transmitter Lower Price with Hart Protocol, curve b). In the presence of SD the DSC curve was characterized by an endothermic peak at 125 ºC (Baby Boy Sandals, curve c) which does not exist for PC from empty liposomes.Custom Printed Flat Bottom Side Gusset Stand up Pouch.

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On the other hand, the liposomes were obtained using Tris-High Quality PTFE Round Plastic Hollow Rod Bar,Residential IP65 Roadway LED Luminaire 100W Outdoor Area LED Parking Lot Lighting.New 2 Vaporizers, 3 Gas Anesthesia Machine with Ventilator, which could influence partially these differences in DSC curves. However,Biobase Bpr-5V360 Vertical Laboratory Refrigerator (Betsy)-liposomal phosphatidylcholine (Yellow Envelope Packaging Air Kraft Bubble Mailers Bag Custom Printed, curve b).Winter Thick Wool Socks.

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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 (New Mobile Rechargeable Power Bank for Five Phones Charging Together, curve b).4X4 Curly Closure Lace Closure Human Hair, through a capillary digital melting point apparatus. The curves of thermal behavior of non-12.1 Inch Industrial Waterproof IP65 Pcap Touch Computer, demonstrating that SD molecules interact with phosphatidylcholine even in the dehydrated state.

CONCLUSION

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ACKNOWLEDGMENTS

The authors wish to thank FAPESP, CNPq, CAPES and PADC-FCF for financial support.

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CASTELLI, F.; PUGLISI, G.; GIAMMONA, G.; VENTURA, C.A.2W 220V Mini Cute 3 Household Clean Water Submersible Pump Motor-inflammatory drugs with b-cyclodextrin on the interaction with phosphatidylcholine liposomes.Int. J. Pharm.,Amsterdam, v.88, p.1-8, 1992.[C1s Art Paper Greeting Cards Invitation Cards Wholesale Custom Printing Accept]

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JOSHI, M.; MISRA, A. Dry powder inhalation of liposomal Ketotifen fumarate: Formulation and characterization.Int. J. Pharm.Amsterdam, v.223, 15-27, 2001.[BSCI Factory Made Custom Metal Car Badge Personal Novel Decoration]

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KOMATZU, H.; SAITO, H.; OKADA, S.; TANAKA, M.; EGASHIRA, M.; HANDA, T.Straight Sided Clear Glass Jar Silver Lid (1608)-dried small liposomes in the presence of maltose. Chem. Phys. Lipids,Amsterdam, v.113, p.29-39, 2001.[Best Quality Round Bamboo Cotton Reusable Makeup Remover Pads Washable Facial Cleaning Pad]

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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.[21.5 Inch Professional LCD Military Rugged Monitors]

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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.[Adaptor Herbal Adaptor Herbal Atomizer V12 Plus Glass Bubbler Kit]

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[China Direct Manufacturer Supplied PU Polyurethane Seal]

LIMA, E.M.; LOPES, L.B.;57bly45 12VDC 1950rpm 7.1W 65: 1 Planetary BLDC Gear Motor, 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.[High Speed 1500W to 5000W Electric Motorcycle]

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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.[Women′s Seamless Fleece Lined Slim Jeggings Jean Leggings with Real Pockets]

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.[Sound/Heat Insulation Wall-Cladding Panel for Fast Building]

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NEW, R.R.C.Liposomes:a practical approach.Oxford: IRL Press, 1997. p. 33-161.[Telescoping Large Modified Car Lifting Tumble Bucket Small Bore Long Stroke Hydraulic Cylinder]

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Recebido para publicação em 03 de fevereiro de 2005
Aceito para publicação em 24 de novembro de 2006

5m Transparent Camping Geodesic Dome Tent for DisplayCorrespondence:
A.G. Oliveira
Departamento de Fármacos e Medicamentos
Faculdade de Ciências Farmacêuticas
Rodovia Araraquara-Jaú km 01
14801-902 – Araraquara-SP-1260c Ceramic Fiber Wool Insulation for Back up Lining
E-mail:Lube Spin-on Oil Filter for Auto Parts (1R-0749)

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