Determination of relevant properties of eudragit e100-flurbiprofen complex. Implicances on its potential useful as pharmaceutical carrier

DANIELA QUINTEROS; BATTISTINI F; MANZO RUBEN; ALLEMANDI D A.

Rosario

Congreso; 2° Reunión Internacional de Ciencias Farmacéuticas. RICiFa 2012; 2012

DETERMINATION OF RELEVANT PROPERTIES OF EUDRAGIT E100-FLURBIPROFEN COMPLEX. IMPLICANCES ON ITS POTENTIAL USEFUL AS PHARMACEUTICAL CARRIER. Quinteros DA, Battistini FD, Manzo RH , Allemandi DA Departamento de Farmacia, Facultad de Ciencias Químicas, Universidad Nacional de Córdoba. UNITEFA-CONICET.Ciudad Universitaria, X5000HUA-Córdoba, Argentina Introduction Ionic interaction between Eudragit E100 (EU) and flurbiprofen (FBH) produced the formation of a complex able to improve aqueous compatibility of FB. This solid is readily dispersed in aqueous solution achieving high drug aqueous compatibility. The aim of this present work is to evaluate the influence of different concentrations of NaCl on FB release, compatibility and surface tension of EU-FB complex. Materials Eudragit® E100(Etilfarma, Buenos Aires), Flurbiprofen (Quimica Luar, Buenos Aires)Aqueous dispersions of EU-FB at 0.1-0.5% EU in saline solutions 0, 0.1 and 0.9% NaCl were assayed. Methods Properties such as partition coeficient, pH, electrokinetic potential (ζ), surface tension (γ), conductivity(µs/cm) of the complex dispersed in NaCl solution were determined. Besides, in vitro drug release using Franz cells with synthetic membranes was also assayed. Results In aqueous media the predominant specie (>99%) is the complex [EUH+FB- ] which was able to modulate the release of FBH towards the media through its acid-base equilibrium. This equilibrium was influenced by the presence of electrolytes such as NaCl. This means that the presence of the ionic species like Cl-would compete with FB- for the EUH+ producing the interchange with the consequent increment in drug release ratio. Aside from this, it must be taken into account that EU behaves as surfactant in aqueous media so that it is able to decrease surface tension in this environment. The critical aggregation concentration (CAC) of this complex was determined using different techniques. As expected, EU´s CAC was greatly affected by electrolyte (i.e. NaCl) concentration.Regarding this, it was observed that the assemblies such formed possesses positive electro kinetic potential which, as it is well known, may favour the interactions with membrane components. Conclusions The EU-FB50-Cl50 complex significantly increases the aqueous compatibility of the drug, it is able to modulate FBH release and posses high electrokinetic potential and positive. Also, it works as surfactant since produce a diminution of surface tension in aqueous media. This could be advantageous in the formulation of ophthalmic solutions containing anti-inflammatory drugs. Acknowledgements: UNITEFA, CONICET, FONCYT and Universidad Nacional de Córdoba, Etilfarma S.A.. References. (1) Alasino RV, Leonhard V, Bianco ID, Beltramo DM. Eudragit E100 surface activity and lipid interactions. Colloids and Surfaces B: Biointerfaces. 2012; 91:84– 89. (2)Quinteros DA, Ramirez Rigo V, Jimenez Kairuz AF, Olivera ME, Manzo RH, Allemandi DA. Interaction between a cationic polymethacrylates (Eudragit E100) and anionic drugs. Eur. J. Pharm. Sci., 2008, 3372–79. (3)Romero VL, Pons P, Bocco, J.L, Manzo, R. H., Alovero, F.,.Eudragit E100 potentiates the bactericidal action of ofloxacin against fluoroquinolone-resistant Pseudomonas aeruginosa. FEMS Microbiol Letters. 2012; 1–9. DOI: 10.1111/j.1574-6968.2012.02626.x