Characterization Of The Inclusion Complex Ropivacaine: β-cyclodextrin [caracterização Do Complexo De Inclusão Ropivacaína: β-ciclodextrina]

Ropivacaine (RVC) is a widely used local anesthetic. The complexation of RVC with β-cyclodextrin (β-CD) is of great interest for the development of more efficient local anesthetic formulations. The present work focuses on the characterization of the RVC:β-CD complex by nuclear magnetic resonance (NMR). The stoichiometry of the complex is 1:2 RVC:β-CD. DOSY-NMR shows that the association constant is 55.5 M-1. Longitudinal relaxation time results show that RVC changes its mobility in the presence of β-CD. This study is focused on the physicochemical characterization of inclusion complexes that are potentials options for pain treatment.30512031207Covino, B.G., Vassalo, H.G., (1985) Anestésicos locais: Mecanismos de ação e uso clínico, , Colina: Rio de JaneiroCourtney, K.R., Strichartz, G.R., (1987) Local Anesthetics, Handbook of Experimental Pharmacology, , Springer-Verlag: BerlinGupta, S.P., (1991) Chem. Rev, 91, p. 1109Kuzma, P.J., Kline, M.D., Calkins, M.D., Staats, P.S., (1997) Reg. Anesth, 22, p. 543McClure, J.H., (1996) Brit. J. Anaesth, 76, p. 300Cederholm, I., (1997) Drug Saf, 16, p. 391Knudsen, K., Suurkula, M.B., Blomberg, S., Sjovall, J., Edvardsson, N., (1997) Br. J. Anesth, 78, p. 507Emanuelsson, B.M., Person, J., Sadin, S., Alm, C., Gustafsson, L.L., (1997) Ther. Drug Monit, 19, p. 126O'Keeffe, N.J., Healy, T.E.J., (1999) Pharmacol. Ther, 84, p. 233Bennett, G., Deer, T., Stuart, D.P., Rauck, R., Yaksh, T., Hassenbusch, S.J., (2000) J. Pain Symp. Manag, 20, p. 44Whiteside, J.B., Wildsmith, J.A.W., (2001) Br. J. Anesth, 87, p. 27de Araújo, D.R., Pinto, L.M.A., Braga, A.F.A., de Paula, E., (2003) Rev. Bras. Anestesiol, 53, p. 663de Araújo, D.R., Fraceto, L.F., Braga, A.F.A., de Paula, E., (2005) Rev. Bras. Anestesiol, 55, p. 316Loftsson, T., Masson, M., (2001) Int. J. Pharm, 225, p. 15McCormack, B., Gregoriadis, G., (1998) Int. J. Pharm, 162, p. 59Matioli, G.Ciclodextrinas e suas aplicações em: alimentos, fármacos, cosméticos, agricultura, biotecnologia, química analítica e produtos gerais, Ed. Eduem: Maringá, 2000Irie, T., Uekama, K., (1997) J. Pharm. Sci, 86, p. 147Pinto, L.M.A., de Jesus, M.B., de Paula, E., Lino, A.C.S., Alderetec, J.B., Duarte, H.A., Takahata, Y., (2004) J. Mol. Struct. (Theochem), 678, p. 63Pinto, L.M.A., Fraceto, L.F., Santana, M.H., Pertinhez, T.A., Oyama-Junior, S., de Paula, E., (2005) J. Pharm. Biomed. Anal, 39, p. 956Kopecký, F., Vojteková, M., Kaclik, P., Demko, M., Bieliková, Z., (2004) J. Pharm. Pharmacol, 56, p. 581Etos, S., Noda, H., Noda, A., (1994) J. Chromatogr., B: Anal. Technol. Biomed. Life Sci, 19, p. 385Loukas, Y.L., Vraka, V., Gregoriadis, G., (1998) Int. J. Pharm, 162, p. 137Ivanov, P.M., Salvatierra, D., Jaime, C., (1996) J. Org. Chem, 61, p. 7012Laverde Jr., A., da Conceição, G.J.A., Queiroz, S.C.N., Fujiwara, F.Y., Marsaioli, A.J., (2002) Magn. Reson. Chem, 40, p. 433Johnson Jr., C.S., (1999) Prog. Nucl. Magn. Reson. Spectrosc, 34, p. 203Xiliang, G., Yu, Y., Guoyan, Z., Guomei, Z., Jianbin, C., Shaomin, S., (2003) Spectrochim. Acta, Part A, 59, p. 3379Bratu, I., Gavira-Vallejo, J.M., Hernanz, A., (2005) Biopolymers, 77, p. 361Ikeda, Y., Hirayama, F., Arima, H., Uekama, K., Yoshitake, Y., Harano, K., (2004) J. Pharm. Sci, 93, p. 1659Zouvelekis, D., Yannakopoulou, K., Mavridis, I.M., Antoniadou-Vyza, A., (2002) Carbohydr. Res, 337, p. 1387Munoz-Botella, S., Martin, M.A., Del Castillo, B., Menendez, J.C., Vazquez, L., Lerner, D.A., (1996) J. Pharm. Biomed. Anal, 14, p. 909Garcia-Rio, L., Hervés, P., Leis, J.R., Mejuto, J.C., Pérez-Juste, J., Rodriguez-Dafonte, P., (2006) Org. Biomol. Chem, 4, p. 1038Abou-Zeid, O.K., (2005) Spectrochim. Acta, Part A, 62, p. 245Pascal, B., Maud, G., Georges, D., Adelin, A., Valery, B., Bruno, P., Didier, C., Brigitte, E., (2005) J. Pharm. Pharmaceut. Sci, 8, p. 164Morris, K.F., Johnson Jr., C.S., (1992) J. Am. Chem. Soc, 114, p. 3139Morris, K.F., Johnson Jr., C.S., (1993) J. Am. Chem. Soc, 115, p. 4291Dollo, G., Le Corre, P., Chevanne, F., Le Verge, R., (1996) Int. J. Pharm, 136, p. 165Fraceto, L.F., Spisni, A., Schreier, S., de Paula, E., (2005) Biophys. Chem, 115, p. 11Fraceto, L.F., Pinto, L.M.A., Franzoni, L., Braga, A.A.C., Spisni, A., Schreier, S., de Paula, E., (2002) Biophys. Chem, 99, p. 22