1,721,006 research outputs found

    Poly(ε-caprolactone) Nanocapsules Carrying The Herbicide Atrazine: Effect Of Chitosan-coating Agent On Physico-chemical Stability And Herbicide Release Profile

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    Polymeric nanoparticles can be used as carrier systems for a variety of bioactive compounds, altering the physico-chemical properties of the substances that are incorporated in the particle matrix. Coating techniques are employed to modify the interactions of the particles with the target medium. The objective of this work was to prepare nanocapsules of poly(ε-caprolactone) containing the herbicide atrazine and study the effect of coating the nanocapsule surfaces using different concentrations of chitosan. The encapsulation efficiency, release kinetics profile, and physico-chemical stability of the formulations were evaluated. Encapsulation percentages of 64-84 % were achieved. The release kinetics profile of the herbicide was altered when the nanocapsules were coated, and the release mechanism could be described by a combination of diffusion and relaxation of the polymeric chains. The stability of the formulations was influenced by the concentration of chitosan used in the preparation procedure. Given the global application of herbicides in agriculture, the results indicate that their association with coated modified release carrier systems could be beneficial from both ecological and economic perspectives. These systems offer delivery that is more efficient, as well as improved adhesion of herbicides to the target plants. © 2013 Islamic Azad University (IAU).11616911700Baker, E.A., Chemistry and morphology of plant epicuticular waxes (1982) The Plant Cuticle, pp. 139-165. , D. J. Cutler, K. L. Alvin, and A. L. 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    Development And Characterization Of Poli (l-lactide) Nanocapsules Containing Benzocaine [desenvolvimento E Caracterização De Nanocápsulas De Poli (l-lactídeo) Contendo Benzocaína]

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    In this paper we describe the preparation poly (L-lactide) (PLA) nanocapsules as a drug delivery system for the local anesthetic benzocaine. The characterization and in vitro release properties of the system were investigated. The characterization results showed a polydispersity index of 0.14, an average diameter of 190.1± 3 nm, zeta potential of -38.5 mV and an entrapment efficiency of 73%. The release profile of Benzocaine loaded in PLA nanocapsules showed a significant different behavior than that of the pure anesthetic in solution. This study is important to characterize a drug release system using benzocaine for application in pain treatment.3316569Covino, B.G., Vassalo, H.G., (1985) Anestésicos Locais: Mecanismos de Ação e uso Clínico, , Colina: Rio de JaneiroFraceto, L.F., Oyama Jr., S., Nakaie, C.R., Spisni, A., De Paula, E., Pertinhez, T.A., (2006) Biophys. Chem., 20, p. 29Malheiros, S.V.P., Pinto, L.M.A., Gottardo, L., Yokaichiya, D.K., Fraceto, L.F., Meirelles, N.C., De Paula, E., (2004) Biophys. Chem., 110, p. 213De Paula, E., Schreier, S., Jarrel, H.C., Fraceto, L.F., (2008) Biophys. Chem., 132, p. 47De Araújo, D.R., De Paula, E., Fraceto, L.F., (2008) Quim. Nova, 31, p. 1775Yagiela, J.A., Neidle, E.A., Dowd, F.J., (1998) Farmacologia e Terapêutica Para Dentistas, , 4a ed. Guanabara Koogan: Rio de JaneiroBennett, R.C., (1989) Monheim: Anestesiologia Local e Controle da Dor Na Prática Dentária, , 7a ed. Guanabara Koogan: Rio de JaneiroEllis, B.F., Seiler, J.G., Palmore, M.M., (1995) J. Bone Joint Surg. Am., 77, p. 937Pinto, L.M.A., Yokaichiya, D.K., Fraceto, L.F., De Paula, E., (2000) Biophys. Chem., 87, p. 213Balicer, R.D., Kitai, E., (2004) The Scientific World Journal, 4, p. 517Gorner, T., Gref, R., Michenot, D., Sommer, F., Tran, M.N., Dellacherie, E., (1999) J. Control. Release, 57, p. 259Govender, T., Stolnik, S., Garnett, M.C., Illum, L., Davis, S.S., (1999) J. Control. Release, 57, p. 171Moraes, C.M., De Paula, E., Rosa, A.H., Fraceto, L.F., (2008) Quim. Nova, 31, p. 2152Moraes, C.M., Matos, A.P., Lima, R., Rosa, A.H., De Paula, E., Fraceto, L.F., (2007) J. Biol. Phys., 33, p. 455Polakovic, M., Gorner, T., Gref, R., Dellacherie, E., (1999) J. Control. Release, 60, p. 169Govender, T., Riley, T., Ehtezazi, T., Garnett, M.C., Stolnik, S., Illum, L., Davis, S.S., (2000) Int. J. Pharm., 199, p. 95Schaffazick, S.R., Guterres, S.S., Freitas, L.L., Pohlmann, A.R., (2003) Quim. Nova, 26, p. 726Durán, N., Mattoso, L.H.C., Morais, P.C., (2006) Nanotecnologia, Artliber, , São PauloMura, P., Maestrelli, F., González-Rodrýguez, M.L., Michelacci, I., Ghelardini, C., Rabasco, A.M., (2007) Eur. J. Pharm. Biopharm., 67, p. 86Pinto, L.M., Fraceto, L.F., Santana, M.H., Pertinhez, T.A., Junior, S.O., De Paula, E., (2005) J. Pharm. Biomed. Anal., 39, p. 956Blanco, M.D., Bernardo, M.V., Sastre, R.L., Olmo, R., Muniz, E., Teijón, J.M., (2003) Eur. J. Pharm. Biopharm., 55, p. 229Klose, D., Siepmann, F., Elkharraz, K., Krenzlin, S., Siepmann, J., (2006) Int. J. Pharm., 314, p. 198Fessi, H., Puiseiux, F., Devissaguet, J.-P., (1988), European Patent, 0274961 A1Venkatraman, S.S., Jie, P., Min, F., Freddy, B.Y.C., Leong-Huat, G., (2005) Int. J. Pharm., 298, p. 219Anal, A.K., Tobiassen, A., Flanagan, J., Singh, H., (2008) Colloids Surf., B, 64, p. 104Guarino, A.J., Lee, S.P., Tulenko, T.N., Wrenn, S.P., (2004) J. Colloid Interface Sci., 279, p. 109Gamisans, F., Lacoulonche, F., Chauvet, A., Espina, M., Garcia, M.L., Egea, M.A., (1999) Int. J. Pharm., 179, p. 37Paavola, A., Yliruusi, J., Kalso, E., Wahlström, T., Rosenberg, P., (1995) Pharm. Res., 12, p. 1997Korsmeyer, R.W., Gurny, R., Doelker, E.M., Buri, P., Peppas, N.A., (1983) Int. J. Pharm., 15, p. 25Peppas, N.A., (1985) Pharm. Acta Helv., 60, p. 110Mohanraj, V.J., Chen, Y., (2006) Trop. J. Pharm. Res., 5, p. 561Guterres, S.S., Fessi, H., Barrat, G., Devissaguet, J.P., Puisieux, F., (1995) Int. J. Pharm., 113, p. 57Pohlmann, A.R., Weiss, V., Mertins, O., Silveira, N.P., Guterres, S.S., (2002) Eur. J. Pharm. Sci., 16, p. 305Romero-Cano, M.S., Vicent, B., (2002) J. Control. Release, 82, p. 127Costa, P., Lobo, J.M.S., (2001) Eur. J. Pharm. Sci., 13, p. 12

    Ecotoxicological Evaluation Of Poly(ε-caprolactone) Nanocapsules Containing Triazine Herbicides

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    The triazine class of herbicides includes the compounds ametryn, atrazine, and simazine, which are used to control weeds in plantations of crops such as maize, sorghum, and sugar cane. Despite their acceptance in agriculture, these herbicides can be dangerous to the environment, depending on their toxicity, the degree of contamination, and the duration of exposure. Controlled release systems are increasingly used to mitigate problems of toxicity and minimize environmental impacts, and can also increase herbicide efficiency. The objective of this work was to prepare poly(ε-caprolactone) nanocapsules containing ametryn and atrazine, and evaluate their toxicity to aquatic organisms as well as in cytogenetic tests employing human lymphocyte cultures. The PCL nanocapsules were prepared according to the interfacial deposition of pre-formed polymer method. Ecotoxicological assays were performed with the alga Pseudokirchneriella subcapitata and the microcrustacean Daphnia similis. The cytogenetic tests consisted of observing mitotic index alterations after exposing lymphocyte cell cultures to different formulations. Encapsulation of the herbicides in the nanocapsules resulted in lower toxicity to the alga and higher toxicity to the microcrustacean, compared to the herbicides alone. The cytogenetic tests showed that formulations of nanocapsules containing the herbicides were less toxic than the herbicides alone. The findings indicate the potential of the nanocapsule formulations in agricultural applications, where they could help to reduce the quantities of herbicides used as well as impacts on the environment and human health. Copyright © 2014 American Scientific Publishers All rights reserved.14749114917Pacakova, V., Stulik, K., Jiskra, J., (1996) J. Chromatogr. 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    Validation Of Analytical Methodology By Hplc For Quantification Of Bupivacaine (s75-r25) In Poli-lactide-co-glicolide Nanospheres [validação De Metodologia Analítica Por Cromatografia Líquida De Alta Eficiência Para Quantificação De Bupivacaína (s75-r25) Em Nanoesferas De Poli(lactídeo- Coglicolídeo)]

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    Bupivacaine (S75-R25, NovaBupi®) is an amide type local anesthetic widely used. The present work consists of the development and validation of analytical methodology for evaluation of NovaBupi® content in the poly-lactide-co-glycolide nanospheres (PLGA-NS) by high performance liquid chromatography. The separation was made using the reversed-phase column LC-18, acetonitrile/phosphate buffer 85:15 v/v as mobile phase and detection at 220 nm. The results obtained show that the analytical methodology is accurate, reproducible, robust and linear over the concentration range 10-220.0 μg/mL of NovaBupi®. The method was applied to determine the encapsulation efficiency and evaluate the release profile of NovaBupi®, showing good results.31821522155Gupta, S.P., (1991) Chem. Rev, 91, p. 1109de Araújo, D.R., Fraceto, L.F., Braga, A.F.A., de Paula, E., (2005) Rev. Bras. Anestesiol, 55, p. 316Goodman, A.G., Gilman, A.G., (1996) As Bases Farmacológicas da Terapêutica, , McGraw-Hill: Rio de JaneiroMclure, H.A., Rubin, A.P., (2005) Minerva Anestesiol, 71, p. 59David, J.S., Ferreti, C., Amour, J., Vivien, B., Eve, O., Petit, P., Riou, B., Gueugniaud, P.Y., (2007) Can. J. Anesth, 54, p. 208Albright, G.A., (1979) Anesthesiology, 51, p. 285Malamed, S.F., (2001) Manual de anestesia local, , Guanabara Koogan: Rio de JaneiroUdelsmann, A., Lorena, S.E.R.S., Girioli, S.U., Silva, W.A., Moraes, A.C., (2007) Rev. Bras. Anestesiol, 57, p. 63Moraes, C.M., Abrami, P., de Paula, E., Andreo Filho, N., Fraceto, L.F., (2007) Quim. Nova, 30, p. 777Moraes, C.M., Abrami, P., de Araújo, D.R., Braga, A.F.A., Issa, M.G., Ferraz, H.G., de Paula, E., Fraceto, L.F., (2007) J. Incl. Phenom. Macrocycl. Chem, 57, p. 313Clarkson, C.W., Hondeghem, L.M., (1985) Anesthesiology, 62, p. 396Casati, A., Santorsola, R., Aldegheri, G., Ravasi, F., Fanelli, G., Berti, M., Franchini, G., Torri, G., (2003) J. Clin. Anesth, 15, p. 126Moraes, C.M., Abrami, P., de Paula, E., Braga, A.F., Fraceto, L.F., (2007) Int. J. Pharm, 331, p. 99Cangiani, L.H., CangianI, L.M., Pereira, A.M.S.A., (2007) Rev. Bras. Anestesiol, 57, p. 136de Araújo, D.R., Braga, A.F.A., Moraes, C.M., Fraceto, L.F., de Paula, E., (2006) Rev. Bras. Anestesiol, 56, p. 495Kuzma, P.J., Kline, M.D., Calkins, M.D., Staats, P.S., (1997) Reg. Anesth, 22, p. 543de Araújo, D.R., Pinto, L.M.A., Braga, A.F.A., de Paula, E., (2003) Rev. Bras. Anestesiol, 53, p. 663Pinto, L.M., Fraceto, L.F., Santana, M.H.A., Pertinhez, T.A., Junior, S.O., de Paula, E., (2005) J. Pharm. Biomed. Anal, 39, p. 956Grant, G.J., Bansinath, M., (2001) Reg. Anesth. Pain Med, 26, p. 61Grant, S.A., (2002) Best Pract. Res. Clin. Anaesth, 16, p. 345de Araújo, D.R., Cereda, C.M.S., Brunetto, G.B., Pinto, L.M.A., Santana, M.H.A., de Paula, E., (2004) Can. J. Anesth, 51, p. 566Cereda, C.M.S., de Araújo, D.R., Brunetto, G.B., de Paula, E., (2004) J. Pharm. Pharmacol. Sci, 7, p. 235Rose, J.S., Neal, J.M., Kopacz, D.J., (2005) Reg. Anesth. Pain Med, 30, p. 275Le Guévello, P., Le Corre, P., Chevanne, F., Le Verge, R., (1993) J. Chromatogr, 622, p. 284Gorner, T., Gref, R., Michenot, D., Sommer, F., Tran, M.N., Dellach- Dellacherie, E., (1999) J. Controlled Release, 57, p. 259Govender, T., Stolnik, S., Garnett, M.C., Illum, L., Davis, S.S., (1999) J. Controlled Release, 57, p. 171Polakovic, M., Gorner, T., Gref, R., Dellacherie, E., (1999) J. Controlled Release, 60, p. 169Govender, T., Riley, T., Ehtezazi, T., Garnett, M.C., Stolnik, S., Illum, L., Davis, S.S., (2000) Int. J. Pharm, 199, p. 95Agência Nacional de Vigilância Sanitária, resolução RE no 899, de 23 de maio de 2003, Brasil(1996) Guidance for Industry - Q2B Validation of Analytical Procedures: Methodology, , European Agency for the Evaluation of Medicinal Products ICH, LondresFessi, H., Puiseiux, F., Devissaguet, J.-P., (1988) Procèdé de preparation de systèmes colloidaux displesibles d'une substance sous forme de nanocapsules, Eur. Pat., 0274961 A1Gamisans, F., Lacoulonche, F., Chauvet, A., Espina, M., Garcia, M.L., Egea, M.A., (1999) Int. J. Pharm, 179, p. 37Schaffazick, S.R., Guterres, S.S., Freitas, L.L., Pohlmann, A.R., (2003) Quim. Nova, 26, p. 726Kilic, A.C., Capan, Y., Vural, I., Gursoy, R.N., Dalkara, T., Cuine, A., Hincal, A.A., (2005) J. Microencapsulation, 22, p. 633Ribani, M., Bottoli, C.B.G., Collins, H.C., Jardim, I.C.S.F., Melo, L.F.C., (2004) Quim. Nova, 27, p. 77

    Interaction Between Nitroheterocyclic Compounds With β-cyclodextrins: Phase Solubility And Hplc Studies

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    Chagas disease is a serious health problem for Latin America. Nitrofurazone (NF) and Hidroxymethylnitrofurazone (NFOH) are active against Trypanosoma cruzi. The effect of β-cyclodextrin (β-CD) and dimethyl-β-cyclodextrin (DM-β-CD) complexation on the UV absorption and retention time of nitrofurazone (NF) and its hydroxymethylated analog (NFOH) were studied in solution. The retention behavior was analyzed on a reversed phase C18 column and the mobile phase used was acetonitrile-water (20/80 v/v), in which cyclodextrins (β-CD or DM-β-CD) were incorporated as a mobile phase additive. The decrease in the retention times of NF (or NFOH) with increasing concentration of HP-β-CD enables the determination of the complex stability constants by HPLC. A phase-solubility study was performed, according to the method reported by Higuchi and Connors, to evaluate the changes of NF/NFOH in the complexation state, and the diagrams obtained suggested that it forms complexes with a stoichiometry of 1:1. This is an important study for the characterization of potential formulations to be used as therapeutic options for the treatment of Chagas disease. © 2008 Elsevier B.V. All rights reserved.474-5865869WHO, Chagas Disease: Strategic Direction for Research. Disease Burden and Epidemiological Trends, http://www.who.int/tdr/diseases/chagas/direction.htm, accessed in January 2007Coura, J.R., de Castro, S.L., (2002) Membr. Inst. Oswaldo Cruz, 97, pp. 3-24Dodd, M.C., Stillman, W.B., (1944) J. Pharmacol. Exp. Ther., 82, p. 11Henderson, G.B., Ulrich, P., Fairlamb, A.H., Rosenberg, I., Pereira, M., Sela, M., Cerami, A., (1998) Proc. Natl. Acad. Sci. U.S.A., 85, p. 5374A. Korolkovas, Dicionário Terapêutico Guanabara, Ed. (2000)/2001, Guanabara Koogan: Rio de Janeiro, 2002Chung, M.C., Guido, R.V.C., Martinelli, T.F., Gonçalves, M.F., Polli, M.C., Botelho, K.C.A., Varanda, E.A., Ferreira, E.I.F., (2003) Bioorg. Med. Chem., 11, pp. 4779-4783Szejtli, J., (1998) Cyclodextrin Technology, , Kluwer Academic Publishers, LondonDollo, G., Thompson, D.O., Le Corre, P., Chevanne, F., Le Verge, R., (1998) Int. J. Pharm., 164, pp. 11-19Szejtli, J., (1994) Med. Res. Rev., 14, pp. 353-386Shuang, S.M., Pan, J.H., Guo, S.Y., Cai, M.Y., Liu, C.S., (1998) Anal. Lett., 30, p. 2261Stella, V.J., Rajewski, R.A., (1997) Pharm. Res., 14, p. 556Melo, N.F., Grillo, R., Moraes, C.M., Brito, C.L., Trosssini, G.H.G., Menezes, C.M., Ferreira, E.I., Fraceto, L.F., (2007) Rev. Ciênc. Farm. Básica Apl., 28, p. 35Grillo, R., Melo, N.F., Brito, C.L., Trosssini, G.H.G., Menezes, C.M., Ferreira, E.I., Moraes, C.M., Fraceto, L.F., (2008) Quím. Nova, 31, pp. 290-295Atwood, J.L., Davies, J.E.D., Macnicol, D.D., Vögtle, F., (1996) Cyclodextrins, 3. , Szejtli J., and Osa T. (Eds), Elsevier Science Ltd., OxfordHiguchi, T., Connors, K.A., (1965) Adv. Anal. Chem. Inst., 4, pp. 117-212Loftsson, T., Hreinsdóttir, D., Másson, M., (2005) Int. J. Pharm., 302, pp. 18-28Loftsson, T., Vogensen, S.B., Brewster, M.E., Konrádsdóttir, F., (2007) J. Pharm. Sci., 10, pp. 2532-2546Uekama, K., Hirayama, F., Irie, T., (1978) Chem. Lett., p. 661Uekama, K., Hirayama, F., Nasu, S., Matsuo, N., Irie, T., (1978) Chem. Pharm. Bull., 26, pp. 3477-3484Ravelet, C., Geze, A., Villet, A., Grosset, C., Ravel, A., Wouessid-jewe, D., Peyrin, E., (2002) J. Pharm. Biomed. Anal., 29, pp. 425-430Moraes, C.M., Abrami, P., de Paula, E., Braga, A.F., Fraceto, L.F., (2007) Int. J. Pharm., 331, pp. 99-106Jullian, C., Moyano, L., Yañez, C., Olea-Azar, C., (2007) Spectrochim. Acta Part A, 67, pp. 230-234Chadha, R., Jain, D.V.S., Aggarwal, A., Singh, S., Thakur, D., (2007) Thermochim. Acta, 459, pp. 111-115Hamada, H., Ishihara, K., Masuoka, N., Mikuni, K., Nakajima, N., (2006) J. Biosci. Bioeng., 102, pp. 369-371Cabral Marques, H.M., Hadgraft, J., Kellaway, I.W., (1990) Int. J. Pharm., 63, pp. 259-266Gazpio, C., Sánchez, M., García-Zubiri, I.X., Vélaz, I., Martinez-Ohárriz, C., Martín, C., Zornoza, A., (2004) J. Pharm. Biomembr. Anal., 9, pp. 487-492Loftsson, T., Hreinsdóttir, D., Másson, M., (2007) J. Incl. Phenom. Macrocycl. Chem., 57, pp. 545-55

    Physico-chemical Characterization Of Inclusion Complex Between Hydroxymethylnitrofurazone And Hydroxypropyl-β-cyclodextrin [caracterização Físico-química De Complexo De Inclusão Entre Hidroximetilnitrofurazona E Hidroxipropil-β- Ciclodextrina]

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    Hydroxymethylnitrofurazone (NFOH) is a prodrug that is active against Trypanosoma cruzi. It however presents low solubility and high toxicity. Hydroxypropyl-β-cyclodextrin (HP-β-CD) can be used as a drug-delivery system for NFOH modifying its physico-chemical properties. The aim of this work is to characterize the inclusion complex between NFOH and HP-β-CD. The rate of NFOH release decreases after complexation and thermodynamic parameters from the solubility isotherm studies revealed that a stable complex is formed (ΔG° = - 1.7 kJ/mol). This study focuses on the physico-chemical characterization of a drug-delivery formulation that comes out as a potentially new therapeutic option for Chagas disease treatment.312290295Dias, J.C.P., (1999) Parasitologia humana e seus fundamentos gerais, , Atheneu Ed, São PauloAndrade, Z.A., (1999) Mem. Inst. Oswaldo Cruz, 94, p. 71Brener, Z., Andrade, Z., Barral-Netto, M.E., (2000) Trypanosoma cruzi e doença de Chagas, , Brener, Z, Zilton, A. A, Barral-Neto, M, eds, 2a ed, Guanabara Koogan: Rio de JaneiroSchmuñis, G., Em ref, A., , 3Urbina, J.A., Docampo, R., (2003) Trends Parasitol, 19, p. 495Coura, J.R., Castro, S.L.A., (2002) Mem. Inst. Oswaldo Cruz, 97, p. 3Gonçalves, M.F., Chung, M.C., Colli, W., Miranda, M.T.M., Ferreira, E.I., (1994) Rev. Soc. Bras. Med. Trop, 27, p. 164Chung, M.C., (1996) Tese de Doutorado, , Universidade de São Paulo, BrasilGuido, R.V.C., Ferreira, E.I., Nassute, J.C., Varanda, E.A., Chung, M.C., (2001) Rev. Bras. Cienc. Farm, 22, p. 319Chung, M.C., Guido, R.V.C., Martinelli, T.F., Gonçalves, M.F., Polli, M.C., Botelho, K.C.A., Varanda, E.A., Ferreira, E.I., (2003) Bioorg. Med. Chem, 11, p. 4779Amidon, G.L., Lennernäs, H., Shah, V.P., Crison, J.R., (1995) Pharm. Res, 12, p. 413Liu, R., (2000) Water Insoluble Drug Formulation, , Interpharm/CRC Press:New YorkDavis, M.E., Brewster, M.E., (2004) Nat. Rev. Drug Discovery, 3, p. 1023de Araújo, D.R., Pinto, L.M.A., Braga, A.F.A., de Paula, E., (2003) Rev. Bras. Anestesiol, 53, p. 663Frömming, K.H., Szejtli, J., (1994) Topics in Inclusion Science - Cyclodextrins in Pharmacy, Kluwer Academic Publishers: Hungriade Azevedo, M.B.M., Alderete, J.B., Rodriguez, J.A., Souza, A.O., Rettori, D., Torsoni, M.A., Faljoni-Alario, A., Duran, N., (2000) J. Inclusion Phenom. Macrocyclic Chem, 37, p. 93Connors, K.A., (1997) Chem. Rev, 97, p. 1325Ismaili, L., André, C., Nicod, L., Mozer, J.L., Millet, J., Refouvelet, B., Makki, S., Guillaume, Y.C., (2003) J. Liq. Chromatogr. Relat. Technol, 26, p. 871Ravelet, C., Ravel, A., Grosset, C., Villet, A., Geze, A., Wouessidjewe, D., Peyrin, E., (2002) J. Liq. Chromatogr. Relat. Technol, 25, p. 421Ravelet, C., Geze, A., Villet, A., Grosset, C., Ravel, A., Wouessidjewe, D., Peyrin, E., (2002) J. Pharm. Biomed. Anal, 29, p. 425Paavola, A., Yliruusi, J., Kajimoto, Y., Kalso, E., Wahlström, T., Rosenberg, P., (1997) Pharm. Res, 1995, p. 12de Araújo, D.R., Fraceto, L.F., Braga, A.F.A., de Paula, E., (2005) Rev. Bras. Anestesiol, 55, p. 316Pinto, L.M.A., Fraceto, L.F., Santana, M.H.A., Pertinhez, T.A., Oyama Junior, S., de Paula, E., (2005) J. Pharm. Biomed. Anal, 30, p. 956de Jesus, M.B., Pinto, L.M.A., Fraceto, L.F., Takahata, Y., Lino, A.C.S., Jaime, C., de Paula, E., (2006) J. Pharm. Biomed. Anal, 41, p. 1428Matioli, G., (2000) Ciclodextrinas e suas aplicações em: Alimentos, fármacos, cosméticos, agricultura, biotecnologia, química analítica e produtos gerais, EDUEM, , MaringáDodziuk, H., (2006) Cyclodextrins and their complexes, , Wiley-VCH: GermanySzejtli, J., (1996) Comprehensive Supramolecular Chemistry, , Pergamon: OxfordMásson, M., Loftsson, T., Másson, G., Stefánsson, E., (1999) J. Controlled Release, 59, p. 107Bekers, O., Uijtendaal, E.V., Beijnen, J.H., Bult, A., Underberg, W.J.M., (1991) Drug Dev. Ind. Pharm, 17, p. 1503Flood, K.G., Reynolds, E.R., Snow, N.H., (2000) J. Chromatogr., A, 903, p. 49Tong, W.Q., Lach, J.L., Chin, T.F., Guillory, J.K., (1991) J. Pharm. Biomed. Anal, 9, p. 1139Stalcup, A.M., Chang, S.S., Armstrong, D.W., Pitha, J.J., (1990) J. Chromatogr., A, 513, p. 181Morin, N., Guillaume, Y.C., Peyrin, E., Rouland, J.C., (1998) J. Chromatogr., A, 808, p. 51Del Valle, E.M.M., (2004) Process Biochem, 39, p. 1033Moraes, C.M., Abrami, P., de Paula, E., Braga, A.F.A., Fraceto, L.F., (2007) Int. J. Pharm, 331, p. 99Langerman, L., Grant, G.J., Zakowski, M., Golomb, E., Ramanathan, S., Turndorf, H., (1992) Anesth. Analg, 75, p. 900Mowat, J.J., Mok, M.J., MacLeod, B.A., Madden, T.D., (1996) Anesthesiology, 85, p. 635Moraes, C.M., Abrami, P., Gonçalves, M.M., Andreo-Filho, N., Fernandes, S.A., de Paula, E., Fraceto, L.F., (2007) Quim. Nova, 30, p. 777Moraes, C.M., Abrami, P., de Araújo, D.R., Braga, A.F.A., Issa, M.G., Ferraz, H.G., de Paula, E., Fraceto, L.F., (2007) J. Incl. Phenom. Macrocycl. Chem, 57, p. 313Moraes, C.M., Abrami, P., Braga, A.F.A., de Paula, E., Fraceto, L.F., (2007) Int. J. Pharm, 331, p. 9

    Poly(e{open}-caprolactone)nanocapsules As Carrier Systems For Herbicides: Physico-chemical Characterization And Genotoxicity Evaluation

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    The toxicity of herbicides used in agriculture is influenced by their chemical stability, solubility, bioavailability, photodecomposition, and soil sorption. Possible solutions designed to minimize toxicity include the development of carrier systems able to modify the properties of the compounds and allow their controlled release. Polymeric poly(e{open}-caprolactone) (PCL) nanocapsules containing three triazine herbicides (ametryn, atrazine, and simazine) were prepared and characterized in order to assess their suitability as controlled release systems that could reduce environmental impacts. The association efficiencies of the herbicides in the nanocapsules were better than 84%. Assessment of stability (considering particle diameter, zeta potential, polydispersity, and pH) was conducted over a period of 270 days, and the particles were found to be stable in solution. In vitro release kinetics experiments revealed controlled release of the herbicides from the nanocapsules, governed mainly by relaxation of the polymer chains. Microscopy analyses showed that the nanocapsules were spherical, dense, and without aggregates. In the infrared spectra of the PCL nanocapsules containing herbicides, there were no bands related to the herbicides, indicating that interactions between the compounds had occurred. Genotoxicity tests showed that formulations of nanocapsules containing the herbicides were less toxic than the free herbicides. The results indicate that the use of PCL nanocapsules is a promising technique that could improve the behavior of herbicides in environmental systems. © 2012 Elsevier B.V.231-23219Pelaez, V., Melo, M., Hofmann, R., Hamerschmidt, P., Medeiros, G., Matsushita, A., Teodorovicz, T., Hermida, C., (2010) Monitoramento do Mercado de Agrotóxicos, , Departamento de Economia, UFPRBreckenridge, C.B., Eldridge, J.C., Stevens, J.T., Simpkins, J.W., Symmetrical triazine herbicides: a review of regulatory toxicity endpoints (2010) Hayes' Handbook of Pesticide ToxicologyCastro, J.S.M., Confalonieri, U., Uso de agrotóxicos no Município de Cachoeiras de Macacu (RJ) (2005) Ciênc Saúde Coletiva, 10, pp. 473-482Sanchez-Verdejo, T., Undabeytia, T., Nir, S., Maqueda, C., Morillo, E., Environmentally friendly slow release formulations of alachlor based on clay-phosphatidylcholine (2008) Environ. Sci. Technol., 42, pp. 5779-5784Guo, H.Q., Zhang, J., Liu, Z.Y., Yang, S.G., Sun, C., Effect of Tween80 and beta-cyclodextrin on the distribution of herbicide mefenacet in soil-water system (2010) J. Hazard. Mater., 177, pp. 1039-1045Villaverde, J., Maqueda, C., Morillo, E., Effect of the simultaneous addition of beta-cyclodextrin and the herbicide norflurazon on its adsorption and movement in soils (2006) J. Agric. Food Chem., 54, pp. 4766-4772Zhou, S., Wang, L., Zhang, A., Lin, K., Liu, W., Preparation, stabilization, and bioefficacy of beta-cyclodextrin inclusion compounds of chloramidophos (2008) J. Agric. 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    Screening Of Formulation Variables For The Preparation Of Poly(ε-caprolactone) Nanocapsules Containing The Local Anesthetic Benzocaine

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    In this work we describe the screening of four parameters in the preparation, by nanoprecipitation, of poly(ε-caprolactone) nanocapsules, used as a drug carrier system for the local anesthetic, benzocaine. A 2 4-1 factorial experimental design was used to study the influence of four different independent variables (polymer, oily phase, Span 60 and Tween 80) on nanocapsule characteristics (size, polydispersion index, zeta potential) and drug loading capability. Best results were obtained using an aqueous formulation comprising 100 mg of polymer, 200 mg of oily phase, 40 mg of Span 60 and 60 mg of Tween 80 in a final volume of 10mL which produced a colloidal system with particle size of 188 nm, zeta potential -32 mV, polydispersion index 0.07, and benzocaine association efficiency >87%. These findings open the way for future clinical studies using such formulations. © 2011 American Scientific Publishers.11324502457Covino, B.G., Vassalo, H.G., (1985) Anestésicos Locais: Mecanismos de Ação e Uso Clínico, , Colina, Rio de JaneiroDe Jong, R.H., (1994) Local Anesthesics, , Springfield, C. C. Thomas, IllinoisSo, T., Farrington, E., (2008) J. Pediatric Health Care, 22, p. 335Malheiros, S.V.P., Pinto, L.M.A., Gottardo, L., Yokaichiya, D.K., Fraceto, L.F., Meirelles, N.C., De Paula, E., (2004) Biophys. Chem., 110, p. 213Fraceto, L.F., Oyama Junior, S., Nakaie, C.R., Spisni, A., De Paula, E., Pertinhez, T.A., (2006) Biophys. Chem., 1213, p. 29Moraes, C.M., Abrami, P., De Araújo, D.R., Braga, A.A., Issa, M.G., Ferraz, H.G., De Paula, E., Fraceto, L.F., (2007) J. Incl. Phenom. Macrocycl. Chem., 57, p. 313De Melo, N.F.S., Grillo, R., Rosa, A.H., Fraceto, L.F., (2008) J. Pharm. Biomed. Anal., 47, p. 865Grillo, R., De Melo, N.F.S., Moraes, C.M., De Lima, R., Menezes, C.M.S., Ferreira, E.I., Rosa, A.H., Fraceto, L.F., (2008) J. Pharm. Biomed. Anal., 47, p. 265Sinha, V.R., Bansal, K., Kaushik, R., Kumria, R., Trehan, A., (2008) Int. J. Pharm., 278, p. 1Fessi, H., Puisieux, F., Devissaguet, J.P., Ammoury, N., Benita, S., (1989) Int. J. Pharm., 55, pp. R1Fessi, H., Puisieux, F., Devissaguet, J.P., (1988), European Patent 0274961 A1Budhian, A., Siegel, S.J., Winey, K., (2007) Int. J. Pharm., 336, p. 367Murakami, H., Kobayashi, M., Takeuchi, H., Kawashima, Y., (1999) Int. J. Pharm., 187, p. 143Galindo-Rodriguez, S., Allémann, E., Fessi, H., Doelker, E., (2004) Pharm. Res., 21, p. 1428Derakhshandeh, K., Erfan, M., Dadashzadeh, S., (2007) Eur J. Pharm. Biopharm., 66, p. 34Quintanar-Guerrero, D., Fessi, H., Allémann, E., Doelker, E., (1996) Int. J. Pharm., 143, p. 133Barros Neto, B., Scarminio, I.S., Bruns, R.E., (2007) Como Fazer Experimentos, , Unicamp, CampinasPolletto, F.S., Silveira, R.S., Fiel, L.A., Donida, B., Rizzi, M., Guterres, S.S., Pohlmann, A.R., (2009) J. Nanosci. Nanotechnol., 9, p. 4933Moraes, C.M., Matos, A.P., De Paula, E., Rosa, A.H., Fraceto, L.F., (2009) Materials Science and Engineering B, Solid State Materials for Advanced Technology, 165, p. 243Woitiski, C.B., Veiga, F., Ribeiro, A., Neufeld, R., (2009) Eur. J. Pharm. Biopharm., 73, p. 25Namur, J.A.M., Cabral-Albuquerque, E.C.M., Quintilio, W., Santana, M.H.A., Politi, M.J., De Araújo, P.S., Lopes, A.C., Costa, M.H.B., (2006) J. Nanosci. Nanotechnol., 6, p. 2403Dillen, K., Vandervoort, J., Mooter, G.V., Verheyden, L., Ludwiga, A., (2007) Int. J. Pharm., 275, p. 171Chacon, M., Berges, L., Molpeceres, J., Aberturas, M.R., Guzman, M., (1996) Int. J. Pharm., 141, p. 81Riley, T., Govender, T., Stolnik, S., Xiong, C.D., Garnett, M.C., Illum, L., Davis, S.S., (1999) Colloids and Surfaces B: Biointerfaces, 16, p. 147Jie, P., Venkatraman, S.S., Min, F., Freddy, B.Y.C., Huat, G.L., (2005) J. Control. Release, 110, p. 20(2003) Brasil, ANVISA, Resolution RE no 899, , de 29 de Maio deDuan, Y., Sun, X., Gong, T., Wang, Q., Zhang, Z., (2006) J. Mater. Sci., 17, p. 509Vandervoort, J., Ludwig, A., (2002) Int. J. Pharm., 238, p. 77Bhavsar, D.M., Tiwari, S.B., Amiji, M.M., (2006) J. Control. Release, 110, p. 422Mondal, N., Samanta, A., Pal, T.K., Ghosal, S.K., (2008) Pharm. Soc. Japan, 128, p. 595Blanco, M.D., Alonso, M.J., (1997) Eur J. Pharm. Biopharm., 43, p. 287Bouchemal, K., Briançon, S., Perrier, E., Fessi, E., (2004) Int. J. Pharm., 280, p. 241Schaffazick, S.R., Guterres, S.S., Freitas, L.L., Pohlmann, A.R., (2003) Química Nova, 26, p. 726Görner, T., Gref, R., Michenot, D., Sommer, F., Tran, M.N., Dellacherie, E., (1999) J. Control. Release, 57, p. 259Mundargi, R.C., Babu, V.R., Rangaswamy, V., Patel, P., Aminabhavi, T.M., (2008) J. Control. Release, 125, p. 193Pense, A.M., Vauthier-Holtzscherer, C., Benoit, J.P., (1992) Microen-capsulation of Drugs, 1, p. 1. , edited by T. L. Whateley, Harwood Academic Publishers, Switzerlan

    Sufentanil-2-hydroxypropyl-β-cyclodextrin Inclusion Complex For Pain Treatment: Physicochemical, Cytotoxicity, And Pharmacological Evaluation

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    Sufentanil (SUF) is a synthetic analgesic opioid widely used for the management of acute and chronic pain. This drug was complexed with 2-hydroxypropyl-β-cyclodextrin (HP-β-CD) and the physicochemical characterization, in vitro/ex vivo toxicity assays, and pharmacological evaluation were performed. Differential scanning calorimetry, Fourier transform infrared spectroscopy (FTIR) analysis, and X-ray powder diffraction showed the formation and the morphology of the complex. Nuclear magnetic resonance afforded data regarding inclusion complex stoichiometry (1:1) with an association binding constant (Ka) value of 515.2 ± 1.2M-1 between SUF and HP-β-CD. Complexation with HP-β-CD protected SUF from light exposure and increased its photostability. Release kinetics revealed a decrease in SUF release rate (Krel = 7.05 ± 0.52 and 5.61 ± 0.39min-1/2 for SUF-HP-β-CD and SUF, respectively) and reduced hemolytic or myotoxic effects after complexation. Time course of tail-flick test showed that the duration of analgesia induced by SUF (150.0 ± 34.6min) was significantly increased (p < 0.001) after complexation with HP-β-CD (355.7 ± 47.2min) when injected at the same dose (1μg kg-1), prolonging the duration of analgesia after intramuscular administration and representing an alternative on the development of effective and safe drug-delivery system for opioid analgesics. © 2012 Wiley Periodicals, Inc.1011036983707Slingsby, L.S., Murison, P.J., Goossens, L., Engelen, M., Waterman-Pearson, A.E., A comparison between pre-operative carprofen and a long-acting sufentanil formulation for analgesia after ovariohysterectomy in dogs (2006) Vet Anaesth Analg, 33, pp. 313-327Meert, T.F., Pharmacotherapy of opioids: Present and future developments (1996) Pharm World Sci, 18, pp. 1-15Meert, T.F., Mesens, J., Verheyen, P., Noorduin, H., Hydroxypropyl-beta-cyclodextrin can modulate the activity of spinally administered sufentanil (1992) Eur J Anaesthesiol, 9, pp. 399-409Yaksh, T.L., Jang, J.D., Nishiuchi, Y., Braun, K.P., Goodman, M., The utility of 2-hydroxypropyl-beta-cyclodextrin as a vehicle for the intracerebral and intrathecal administration of drugs (1992) Life Sci, 48, pp. 623-633Jang, J., Yaksh, T.L., Hill, H.F., Use of 2-hydroxypropyl-β-cyclodextrin as an intrathecal drug vehicle with opioids (1992) J Pharm Exp Ther, 261, pp. 592-600Meert, T.F., Melis, W., Interactions between epiduraly and intrathecally administered sulfentanil and bupivacaine in hydroxypropyl-β-cyclodextrin in the rat (1992) Acta Anaesthesiol Scand, 43, pp. 79-89Holvoet, C., Plaizier-Vercammen, J., Vander Heyden, Y., Gabriels, M., Camu, F., Preparation and in vitro release rate of fentanyl-cyclodextrin complexes for prolonged action in epidural analgesia (2003) Int J Pharm, 265, pp. 13-26Ogawa, N.O., Higashi, K., Nagase, H., Endo, T., Moribe, K., Loftsson, T., Yamamoto, K., Ueda, H., Effects of cogrinding with β-cyclodextrin on the solid state fentanyl (2010) J Pharm Sci, 99, pp. 5019-5029Waldeck, A.R., Kuchel, P.W., Lennon, A.J., Chapman, B.E., NMR diffusion measurements to characterize membrane transport and solute binding (1997) Prog Nucl Magn Reson Spectrosc, 30, pp. 39-68Fraceto, L.F., Moraes, C.M., Abrami, P., Gonçalves, M.M., Andreo, F.N., Fernandes, S.A., de Paula, E., Preparação e caracterização Físico-química de complexos de inclusão entre anestésicos locais e hidroxipropilbeta-ciclodextrina (2007) Quim Nova, 30, pp. 777-784Wimmer, R., Aachamann, F.L., Larsen, K.L., Petersen, S.B., NMR diffusion as a novel tool for measuring the association constant between cyclodextrin and guest molecules (2002) Carbohydr Res, 337, pp. 841-849de Araujo, D.R., Tsuneda, S.S., Cereda, M.S., Carvallho, F.D.G.E., Preté, P.S.C., Fernandes, S.A., Yokaichiya, F., de Paula, E., Development and pharmacological evaluation of ropivacaine-2-hydroxypropyl-β-cyclodextrin inclusion complex (2008) Eur J Pharm Sci, 33, pp. 60-71Grillo, R., de Melo, N.F., Moraes, C.M., de Lima, R., Menezes, C.M., Ferreira, E.I., Rosa, A.H., Fraceto, L.F., Study of the interaction between hydroxymethylnitrofurazone and 2-hydroxypropyl-beta-cyclodextrin (2008) J Pharm Biomed Anal, 47, pp. 295-302Lambropoulos, J., Spanos, G.A., Lazaridis, N.V., Development and validation of an HPLC assay for fentanyl, alfentanil, and sufentanil in swab samples (2000) J Pharm Biomed Anal, 23, pp. 421-428Kranz, H., Brazeau, G.A., Napaporn, J., Martin, R.L., Millard, W., Bodmeier, R., (2001) Int J Pharm, 212, pp. 11-18. , Myotoxicity studies of injectable biodegradable in-situ forming drug delivery systemsMalheiros, S.V.P., Pinto, L.M.A., Gottardo, L., Yokaichiya, D.K., Fraceto, L.F., Meirelles, N.C., de Paula, E., A new look at the hemolytic effect of local anesthetics considering their real membrane/water partitioning at pH 7.4 (2004) Biophys Chem, 110, pp. 213-221Johnson Jr., C.S., Diffusion ordered nuclear magnetic resonance spectroscopy: Principles and applications progress in nuclear magnetic resonance (1999) Spectroscopy, 34, pp. 203-256Bakkour, Y., Vermeersch, G., Morcellet, M., Boschin, F., Martel, B., Azaroual, N., Formation of cyclodextrin inclusion complexes with doxycyclin-hyclate: NMR investigation of their characterization and stability (2006) J Incl Phenom Macrocycl Chem, 54, pp. 109-114Giordano, F., Novak, C., Moyano, J.R., Thermal analysis of cyclodextrins and their inclusion compounds (2001) Thermochim Acta, 380, pp. 123-151Yap, K.L., Liu, X., Thenmozhiyal, J.C., Ho, P.C., Characterization of the 13-cis-retinoic acid/cyclodextrin inclusion complexes by phase solubility, photostability, physicochemical and computational analysis (2005) Eur J Pharm Sci, 25, pp. 49-56Costa, P., Lobo, J.M.S., Modeling and comparison of dissolution profiles. (2001) Eur J Pharm Sci, 13, pp. 123-133Moraes, C.M., Abrami, P., de Paula, E., Braga, A.F., Fraceto, L.F., Study of the interaction between S(-) bupivacaine and 2-hydroxypropyl-beta-cyclodextrin (2007) Int J Pharm, 331, pp. 99-106Moraes, C.M., Abrami, P., de Araújo, D.R., Braga, A.F.A., Issa, M.G., Ferraz, H.G., de Paula, E., Fraceto, L.F., Characterization of lidocaine: Hydroxypropyl-β-cyclodextrin (2007) J Incl Phenom Macrocycl Chem, 57, pp. 313-316Bibby, D., Davies, N.M., Tueker, I.G., Mechanisms by which cyclodextrins modify drug release from polymeric drug delivery systems (2000) Int J Pharm, 197, pp. 1-11de Araújo, D.R., Fraceto, L.F., Braga, A.F.A., de Paula, E., Drug-delivery systems for racemic bupivacaine (S50-R50) and bupivacaine enantiomeric mixture (S75-R25): Cyclodextrins complexation effects on sciatic nerve blockade in mice (2005) Rev Bras Anestesiol, 55, pp. 316-328de Araújo, D.R., Moraes, C.M., Fraceto, L.F., Braga, A.F.A., de Paula, E., Cyclodextrin-bupivacaine enantiomeric mixture (S75-R25) inclusion complex and intrathecal anesthesia in rats (2006) Rev Bras Anestesiol, 56, pp. 495-506Irie, T., Uekama, K., Pharmaceutical applications of cyclodextrins. III. Toxicological issues and safety evaluation (1997) J Pharm Sci, 86, pp. 147-162Rajewski, R.A., Stella, V.J., Pharmaceutical applications of cyclodextrins. 2. In vivo drug delivery (1996) J Pharm Sci, 85, pp. 1142-1169Gordon, D.B., New opioid formulations and delivery systems (2007) Pain Manag Nurs, 8, pp. 6-1

    Preparation And Physico-chemical Characterization Of Inclusion Complexes Between Local Anesthetics And Hydroxypropyl-β-cyclodextrin [preparação E Caracterização Físico- Química De Complexos De Inclusão Entre Anestésicos Locais E Hidroxipropil-β-ciclodextrina]

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    S(-) Bupivacaine (S(-)BVC) and Lidocaine (LDC) are widely used local anesthetics (LA). Hydroxypropyl β-cyclodextrin (HP-β-CD) is used as a drug-carrier system. The aim of this work was to characterize inclusion complexes between LA and HP-β-CD. The affinity constants determined at different pHs show favourable complexation. The release kinetics experiments showed that S(-)BVC and LDC changed the released profiles in the presence of HP-β-CD. Nuclear magnetic resonance experiments gave information about the interaction between LA and the cyclodextrin cavity. This study focused on the physicochemical characterization of drug-delivery formulations that come out as potentially new therapeutic options for pain treatment.304777784Knudsen, K., Suurkula, M.B., Blomberg, S., Sjovall, J., Edvardsson, N., (1997) Br. J. Anesth, 78, p. 507Goodman, A.G., Gilman, A.G., (1996) As Bases Farmacológicas da Terapêutica, , 9a ed, McGraw-Hill: Rio de JaneiroButterword, J. F. 4thStrichartz, G. 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