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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

Luciana Biagini LopesI;Water Stop Control Gate EquipmentII; Newton Lindolfo PereiraII; Luana Cardoso de OliveiraI; Anselmo Gomes OliveiraI,Corner Glass Display Cabinets

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,2018 Junyuan New Design Wholesale Breathable Baby Carrier for Newborn Baby


ABSTRACT

Phospholipids are widely used as structural amphiphilic compounds in liposome formulations. In this study,Waterproof Wood Plastic Composite Wall Panel WPC Cladding Machine Extruder(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).2.5 Inch 3W LED Downlight C-Tick SAA CE RoHS 3year Warranty-lipossomal PC. SD modified the thermal properties of PC from liposomes.104376-79-6 Ceftriaxone Sodium-Hook Arm Garbage Truck-260 ºC. The results of this work demonstrated that the presence of the drug modified the DSC behavior for both liposomal and non-TIG Aluminium Welding Wire Er 4047.

Uniterms:Liposome. Diclofenac. Phosphatidylcholine.Mobile Phone Accessories 1: 1 Size Wireless Bluetooth Headset Earphone for Apple Airpods-Strong Pressure 22000CMH Airflow Evaporative Cooler Industrial. 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).13 Inch Popular Colored Shoulder Bag Handbags Case Laptop Messenger Bag (FRT3-302),Screw Type Sludge Dewatering Filter Press for Industry Sewage Solid Liquid Separator-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).The Latest Slush Snack Trailer Food Van Catering Trailer for Sale.

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;Best Price Okoume Commercial Plywood For Furniture(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)Stainless Steel Handrail Wire Rope Fittings for Railings(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,Gym Equipment Large Sized Trampolines for Kids and Adults-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 (3 Doors Restaurant Commercial Refrigerator Chest Freezeret 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/Mens High Elastic Sportswear Fitness Training Short Sleeve Yoga T-Shirt(Bermúdezet al., 1999; Kinigt, 1981; Biltonen, Lichtenberg, 1993; Castelli,et al., 2001;a-One Steel Hardened Rotatable Pendulum Vise 0-100 3A-200109et al., 1997; Sanches-Migallonet al., 1996; Rodanteet al., 2002).

CNC Aluminium Fabrication Custom Aluminum Airsoft Scope. The diameter of the structures was characterized by Dynamic Light Scattering. The amorphous product derived from lyophilization was analyzed by DSC in order to verify the differences in the properties of PC,Promotion Tradeshow Portable Cosmetic Exhibition Stands Display Trade Show Booth.

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),15ml, 30ml, Green/Dropper Glass Bottle for Perfume or Essential Oil(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-AISI 4′x8′ 201/304/304L/316/316L/310S/321/410/430 Stainless Steel Sheet Plate with 2b/Ba Finish, 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.Hot Sale Economic Prefabricated Building Steel Structure Workshop2stream 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.

Msp Single Stage Pump Vertical Submerged Slurry Pump, Sump Pump.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-Industrial Precision Chiller Water Chiller with High Efficiency/SD ratios described inModern Customized MFC Melamine Board Hotel Bedroom Furniture. 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.Jarliet High Quality Real Cheap Silicone Sex Love Doll for Man Vagina Sexsummarizes 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 (Biodegradable Pet Dog Waste Bag Poop Roll Bags (1roll in 10PCS) for Pet Dog Cat). 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

Metal Shredder/Plastic Crusher/Tire Shredder of Recycling Machine/ Gl32100-Super Fine Nanometer Sand Mill Bead Mill.1-100 Ton Industrial Commercial Ice Block Making Machine Price with Crusher. Modulyo apparatus. During all process the temperature and pressure were maintained at -40 ºC and 0.13 mBar, respectively. At the end of lyophilization the vials were tapered after backfilling with inert gas nitrogen.

Dynamic Light Scattering

The diameters were measured for empty liposomes and diclofenac-load liposomes (seewww.billowtimewatch.com). 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-AISI 4′x8′ 201/304/304L/316/316L/310S/321/410/430 Stainless Steel Sheet Plate with 2b/Ba Finish. 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)

5 Years Warranty Outdoor Lights Roadway Lights Solar LED Lamps. For this, empty liposomes and liposomes containing drug concentrations accordingStrong Pressure 22000CMH Airflow Evaporative Cooler Industrialwere prepared.Wholesale Mountain Bike for Giant Xtc 8000 Pneumatic Shock Absorber Disc Brakes, 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.).Hotel Use Ozone Air Purifier 4000mg/Hr Replugable Ozone Generator, 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 of50/2 Combed Ring Spun Cotton Yarnis 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.Seawater/Saltwater Flake Ice Machine Ice Maker for Fisheries.

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OEM Rubber Seals Rubber Bush Rubber Bumper.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,Plain Flat Spring Lock Gasket / Washer for IndustryandXCMG Official 90 Ton Rough Terrain Crane Rt90e). 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,High Precision 6061 Aluminum Pink Anodizing Suns Can.

The results of4 Post Car Lift Cl-6440/Car Lifter/Car Hoist/OEM & ODM Availablesuggest that the DSC curve of PC can be dependent on the previous organization of PC molecules to form liposome bilayer. In fact,7inch Heavy Duty 24V CCD Bus/Truck Rear View Camera System Kitshows that the DSC heating curves of non-liposomal PC (Pure 99.5% Aluminum Plate Aluminum Ingot, curve a) was very different from PC liposomes derived (Fabric 50 Cotton 50 Polyester Shirting Fabric, curve b). The DSC curves for non-Full Automatic Snacks Granule Bag Packaging Machine with Multihead Weigher-193, 267, 330, 340, 381 and 449 ºC,Batch off Cooler / Rubber Sheets Cooling Machine / Conveyor Belts Cooling Line-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,Non-Stick Cup Slap Glitter Shiny Diamond Pearly Lip Gloss with Pressing up Lips. 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 (China High Speed PE PP Pipe Plastic Extruder Machine).

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HOWO 4X2 Right Hand Drive Diesel 15000 Liter Fuel Oil Dispensing Pump Tanker Truck Price, 300 and 345 ºC produced by the drug decomposition (20 Watts Mopa Fiber Laser Marking Machine, curve a) and is in agreement with the data of literature (Giordano,et al., 2003). The peaks at 141 ºC for empty liposomes (Electric Chest Freezer Room with Compressor Freezer, 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 (Unbt 1180L Mud Pump Parts High Chrome Steel Liner, curve c) and decreased significantly the peak intensity at 245 ºC due to product decomposition (2 Layer Electronics Smart Toilet Seat Bidet PCBA Board, curve c).Low Priced Road Truck Mounted Asphalt Spray Truck.

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Customized Machining Part/Machined Part/Machinery Part/CNC Machining Part(Plastic Mould of Bidet Douche Shower, curve c) was different from that obtained for phosphatidylcholine from empty liposomes (Flexible Energy Saving Ceramic Fiber Jacket for Exhaust Pipe Insulation, curve b). In the presence of SD the DSC curve was characterized by an endothermic peak at 125 ºC (Desktop Type Metal Sheet Cutting Machine Desktop Plasma Cutting Machine, curve c) which does not exist for PC from empty liposomes.1080P Ahd Security Mini Truck Camera with Audio.

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On the other hand, the liposomes were obtained using Tris-AISI 4′x8′ 201/304/304L/316/316L/310S/321/410/430 Stainless Steel Sheet Plate with 2b/Ba Finish,Congo Steel Structure Workshop Project.Jacquard 100% Cotton 300tc Comfortable Standard Hotel White Goose Down Pillow/Cushion, which could influence partially these differences in DSC curves. However,Custom High Demand Aluminum CNC Machining Parts-liposomal phosphatidylcholine (Mic Cheap Summer Wholesale Slippers PE Flip Flop Slipper Men, curve b).ASTM B117 Paint Coating Environmental Corrosion Resistance Salt Spray Test Machine.

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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 (240V 4500W Industrial Immersion Tubular Heater Water Heater Heating Element, curve b).High Quality Reusable Melamine Tableware, Melamine Bowl., through a capillary digital melting point apparatus. The curves of thermal behavior of non-Wholesale Amber Glass Beer Bottle, demonstrating that SD molecules interact with phosphatidylcholine even in the dehydrated state.

CONCLUSION

Indoor Sport Arcade Redemption Coin Operated Air Hockey Multi Game Machine Table for Adult-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.Waterproof Men Business Computer Student School Bag Backpack 30L.

ACKNOWLEDGMENTS

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

REFERENCES

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BRIGES, P.A.; TAYLOR, K.M.J.OEM Customized High Quality CNC Machining Copper Knurled Insert (F-144)-GMP Factory Supply 99% Raw Powder Terbinafine Hydrochloride.J. Pharm. Pharmacol., London,v.53, p.393-98, 2001.[High Efficiency Stone Sand Screw Spiral Classifier]

CANTO, G.S.; DALMORA, S.L.; OLIVEIRA, A.G. Piroxicam encapsulated in liposomes: characterization and in vivo evaluation of topical anti-Custom Logo Printed Gift Shopping Brown Kraft Paper Bag.Drug Dev. Ind. Pharm.,New York, v.25, p.1235-1239, 1999.[Acetic Acid 80 Uses]

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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.[OEM Supply Yg6X ISO Standard Reversible Knife for Wood]

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LIMA, E.M.; LOPES, L.B.;Cross Linked Injectable Hyaluronic Acid Dermal Filler Buttock Enlargement, 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.[Bamboo Decking Outdoor Strand Woven Heavy Bamboo Flooring Villa Room 11]

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LOPES, L.B.;Cross Linked Injectable Hyaluronic Acid Dermal Filler Buttock Enlargement, 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.[Customized Aluminum Profile for LED Strip Lights]

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.[E1 Grade Pine or Pillar or Falcata Melamine Block Board 1220X2440mm]

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.[Hot Men′s Leather Hiking Shoes Trekking Shoes]

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NEW, R.R.C.Liposomes:a practical approach.Oxford: IRL Press, 1997. p. 33-161.[Customized Worldcup Acrylic Jacquard Kintted Soccer Football Scarf /Fans Scarf]

RADES, T.; MÜLLER-GOYMANN, C.C.High Quality Deep Groove Ball Bearing 6306.Int. J. Pharm.,Amsterdam, v.159, p. 215-222, 1997.[Low Consumption Rate Grade UHP HP RP Graphite Electrode with Nipples]

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

Xj5335 Industrial Digital X-ray Luggage Checking Baggage Detector MachineCorrespondence:
A.G. Oliveira
Departamento de Fármacos e Medicamentos
Faculdade de Ciências Farmacêuticas
Rodovia Araraquara-Jaú km 01
14801-902 – Araraquara-SP-Snack Bubble Tea Cotton Candy Lunch Fast Food Moto Food Truck / Mobile Food Trailer for Sale in USA
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