Eudragit ® FS 30 D polymeric films containing chondroitin sulfate as candidates for use in coating seeking modified delivery of drugs

ABSTRACT Polymeric films associating different concentrations of Eudragit(r) FS 30 D (EFS) and chondroitin sulfate (CS) were produced by casting for the development of a new target-specific site material. Formed films kept a final polymer mass of 4% (w/v) in the following proportions: EFS 100:00 CS (control), EFS 95:05 CS, EFS 90:10 CS and EFS 80:20 CS. They were analyzed for physical and chemical characteristics using Fourier transform infrared spectroscopy (FTIR), scanning electron microscopy (SEM) and Raman spectroscopy. Furthermore, they were characterized by their water vapor permeability and degree of hydration at different conditions simulating the gastrointestinal tract. No chemical interactions were observed between CS and EFS, suggesting only a physical interaction between them in the different combinations tested. The results suggest that EFS and CS, when combined, may form films that are candidates for coating processes seeking a modified drug delivery, especially due to the synergism between pH dependency and specific biodegradability properties by the colonic microbiota. EFS 90:10 CS proved to be the most suitable for this purpose considering hydration and permeability characteristics of different associations analyzed

A Ph/enzyme-responsive Polymer Film Consisting Of Eudragit® Fs 30 D And Arabinoxylane As A Potential Material Formulation For Colon-specific Drug Delivery System

Polymer film based on pH-dependent Eudragit® FS 30 D acrylic polymer in association with arabinoxylane, a polysaccharide issued from gum psyllium, was produced by way of solvent casting. Physical-chemical characterization of the polymer film samples was performed by means of thermogravimetry (TGA), differential scanning calorimetry (DSC), and scanning electron microscopy (SEM). Furthermore, water-equilibrium swelling index (Is) and weight loss of the films in KCl buffer solution of pH 1.2, in KH 2PO 4 buffer solution of pH 5.0, or in KH 2PO 4 buffer solution of pH 5.0 consisting of 4% enzyme Pectinex® 3X-L (w/v) were also carried out for the film characterization. No chemical interactions between the Eudragit® FS 30 D and the arabinoxylane polymer chains were evidenced, thus suggesting that the film-forming polymer structure was obtained from a physical mixture of both polymers. The arabinoxylane-loader films showed a more pronounced weight loss after their immersion in buffer solution containing enzyme Pectinex® 3X-L. The introduction of the arabinoxylane makes the film more susceptible to undergo an enzymatic degradation. This meant that the enzyme-dependent propriety issued from the arabinoxylane has been imprinted into the film formulation. This type of polymer film is an interesting system for applications in colon-specific drug delivery system. © 2012 Informa Healthcare USA, Inc.174429436Souto-Maior, J.F.A., Reis, A.V., Pedreiro, L.M., Cavalcanti, O.A., Phosphated crosslinked pectin as a potential excipient for specific drug delivery: Preparation and physicochemical characterization (2010) Polym. Int., 59, pp. 127-135Reddy, S.M., Sinha, V.R., Reddy, D.S., Novel oral colon-Specific drug delivery systems for pharmacotherapy of peptide and nonpeptide drugs (1999) Drugs Today, 35, pp. 537-580Sinha, V.R., Kumria, R., Microbially triggered drug delivery to the colon (2008) Eur. J. Pharm. Sci., 18, pp. 3-18Friend, D.R., New Oral delivery systems for treatment of inflammatory bowel disease (2005) Adv. Drug Deliv. Rev., 57, pp. 247-265Rubistein, A., Colonic drug delivery (2005) Drug Discov. Today, 2, pp. 33-37Freire, A.C., Podczeck, F., Sousa, J., Veiga, F., Liberação específica de fármacos no cólon por via oral- O cólon como local de liberação de fármacos (2006) Rev. Bras. Cienc. Farm., 42, pp. 319-335Freire, A.C., Podczeck, F., Sousa, J., Veiga, F., Liberação específica de fármacos no cólon por via oral II - Tipos de sistemas utilizados (2006) Rev. Bras. Cienc. Farm., 42, pp. 337-355Sinha, V.R., Mittal, B.R., Bhutani, K.K., Kumria, R., Colonic drug delivery of 5-Fluorouracil: An in vitro evaluation (2004) Int. J. Pharm., 269, pp. 101-108Jain, A., Gupta, Y., Jain, S.K., Perspectives of biodegradable natural polysaccharides for site-specific drug delivery to the colon (2008) J. Pharm. Pharm. Sci., 10, pp. 86-128Pinto, J.F., Site-specific drug delivery systems within the gastrointestinal tract: From the mouth to the colon (2010) Int. J. Pharm., 395, pp. 44-52Chourasia, M.K., Jain, S.K., Pharmaceutical aproaches to colon targeted drug delivery systems (2003) J. Pharm. Pharm. Sci., 6, pp. 33-66McConnell, E.L., Short, M.D., Basi, A.W., An in vivo comparison of intestinal pH and bacteria as physiological trigger mechanisms for colonic targeting in man (2008) J. Control. Release, 130, pp. 154-160Sinha, V.R., Kumria, R., Polysaccharides in colon-Specific drug delivery (2001) Int. J. Pharm., 224, pp. 19-38Yang, L., Chu, J.S., Fix, J.A., Colon-Specific drug delivery: New approaches and in vitro/in vivo evaluation (2002) Int. J. Pharm., 235, pp. 1-15Akhgari, A., Farahmand, F., Garekania, H.A., Sadeghia, F., Vandamme, T.F., Permeability and swelling studies on free films containing inulin in combination with different polymethacrylates aimed for colonic drug delivery (2006) Eur. J. Pharm. Sci., 28, pp. 307-314Wei, H., Li-Fang, F., Bai, X., Chun-Lei, L., Qing D.Yong-Zhen, C., De-Ying, C., An investigation into the characteristics of chitosan/Kollicoat SR30D free films for colonic drug delivery (2009) Eur. J. Pharm. Sci., 72, pp. 266-274Grootaert, C., Delcour, J.A., Courtinb, C.M., Broekaertb, W.F., Verstraetea, W., Wiele, T.V., Microbial metabolism and prebiotic potency of arabinoxylan oligosaccharides in the human intestine (2007) Trends food sci. technol., 18, pp. 64-71Vandamme, T.F., Lenourry, A., Charrueau, C., Chaumeil, J.C., The use of polysaccharides to target drugs to the colon (2002) Carbohyd. Polym., 48, pp. 219-231Van Craeyveld, V., Delcour, J.A., Courtin, C.M., Extractability and chemical and enzymic degradation of psyllium (Plantago ovata Forsk) seed husk arabinoxylans (2009) Food Chem., 111, pp. 812-819Saghir, S., Iqbal, M.S., Hussain, M.A., Koschella, A., Heinze, T., Structure characterization and carboxymethylation of arabinoxylan isolated from Ispaghula (Plantago ovata) seed husk (2008) Carbohyd.Polym., 74, pp. 309-317Singh, B., Psyllium as therapeutic and drug delivery agent (2007) Int. J. Pharm., 334, pp. 1-14Kaith, B.S., Kumar, K., In vacuum synthesis of psyllium and acrylic acid based hydrogels for selective water absorption from different oil-water emulsions (2008) Desalination, 229, pp. 331-341(2009) Eudragit® FS 30 D A Versatile Polymer for Controlled Release Aplications, , http://www.pharmapolymere.de/pharmapolymers/en/eudragitfs30d, Evonik Industries Available at Access: 3 Marc