An Investigation of the Dimensional Changes of Polymer Mixture Tablets Containing a Soluble Drug, Using an Image Analysis Method. Influence of These Characteristics on Drug Release and Its Mechanism

DOI: 10.4236/jbnb.2012.32026   PDF   HTML   XML   6,310 Downloads   8,909 Views  


The properties and characteristics of the polymer used for the preparation of matrix drug delivery systems considerably influence their performance and the extent of drug release and its mechanism. The objective of this research was to examine the dimensional changes, and gel evolution of polymer matrices consisting of three different polymers Polyox, sodium alginate (hydrophilic) and Ethocel (hydrophobic), using an image analysis method. Furthermore to explore how these changes influence the release rate of a soluble drug namely, venlafaxine. All tablets displayed marked dimensional expansion and gel growth particularly those consisting of two hydrophilic polymers Polyox/sodium alginate (POL/SA/V) compared to those consisting of the hydrophilic/hydrophobic Polyox/Ethocel (POL/ET/V). Similarly the thickness of the gel layer in POL/SA/V matrices increased considerably with time up to 8 hours. In general our findings show that the POL/SA/V matrices, due to their thicker gel layer produced a more effective barrier which results in a more pronounced sustained release delivery. This accounts for the slower and smaller overall drug release observed with the POL/SA/V matrices compared to those containing POL/ET/V and indicates that the formation of a thick and durable gel barrier is a characteristic necessary for the preparation of sustained drug release systems. Moreover the solubility of venlafaxine in combination with the polymer’s properties appears to play an important role on the extent of drug release and the release mechanism. Overall the polymer mixtures examined comprise a useful and promising combination of materials for the development and manufacture of sustained release preparations based on these polymers.

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M. Efentakis and D. Tavoulari, "An Investigation of the Dimensional Changes of Polymer Mixture Tablets Containing a Soluble Drug, Using an Image Analysis Method. Influence of These Characteristics on Drug Release and Its Mechanism," Journal of Biomaterials and Nanobiotechnology, Vol. 3 No. 2, 2012, pp. 200-207. doi: 10.4236/jbnb.2012.32026.

Conflicts of Interest

The authors declare no conflicts of interest.


[1] S. Tomic, S. Dimitrijevic, A. Marinkovic, S. Najman and J. Filipovic, “Synthesis and Characterization of Poly(2-Hydroxyethyl Methacrylate/Itaconic Acid) Copolymeric Hydrogels,” Polymer Bulletin, Vol. 63, No. 6, 2009, pp. 837-851. doi:10.1007/s00289-009-0123-2
[2] R. Dey, G. Tiwary, T. Patnaik and U. Jha, “Controlled Release of 5-Aminosalisylic Acid from New pH Responsive Polymer Derived from Tamarind Seed Polysaccharide, Acrylic Acid and Polyamidoamine,” Polymer Bulletin, Vol. 66, No. 5, 2010, pp. 583-598.
[3] M. Vlachou, H. Naseef and Efentakis M, “Utilization of Hydrophilic Swellable Polymers as Carriers for Sustained Drug Delivery from Matrices and Three Layer Tablet Systems,” Current Drug Delivery, Vol. 7, No. 4, 2010, pp. 334-342. doi:10.2174/156720110793360568
[4] J. Escudero, C. Ferrero and M. Jiménez-Castellanos, “Compaction properties Drug Release Kinetics and Fronts Movement Studies from Matrices Combining Mixtures of Swellable and Inert Polymers II. Effect of HPMC with Different Degrees of Methoxyhydroxypropyl Substitution,” International Journal of Pharmaceutics, Vol. 387, No. 1-2, 2010, pp. 56-64. doi:10.1016/j.ijpharm.2009.12.001
[5] M. Efentakis and Vlachou M, “Evaluation of High Molecular Weight Poly(Oxyethylene) (POLYOX) Polymer: Studies of Flow Properties Release Rate of Furosemide and Captopril from Controlled Release Hard Gelatin Capsules,” Pharmaceutical Development Technnology, Vol. 5, No. 3, 2000, pp. 339-346.
[6] A. Domb, J. Kost and D. Wiseman, “Handbook of Biodegradable Polymers” Harwood Academic Publishers, Newark, 1997.
[7] M. Efentakis and G. Buckton, “The Effect of Erosion and Swelling on the Dissolution of Theophylline from Low and High Molecular Weight Sodium Alginate Matrices,” Pharmaceutical Development Technnology, Vol. 7, 2002, pp. 69-77.
[8] S. Riyajan and J. Sakdapipanich, “Development of a Controlled Release Capsule with a Sodium Alginate Matrix, Crosslinked by Glutaraldehyde and Coated with Natural Rubber,” Polymer Bulletin, Vol. 63, No. 4, 2009, pp. 609- 622. doi:10.1007/s00289-009-0126-z
[9] S. Indiran Pather, I. Russel, J. Syce and S. Neau, “Sustained Release Theophylline Tablets by Direct Compression Part 1: Formulation and in Vitro Testing,” International Journal Pharmaceutics, Vol. 164, No. 1-2, 1998, pp. 1-10. doi:10.1016/S0378-5173(97)00348-7
[10] R. Bettini, P. Catellani, P. Santi, G. Massimo, N. Peppas and P. Colombo, “Translocation of Drug Particles in HPMC Matrix Gel Layer: Effect of Drug Solubility and Influence on Release Rate,” Journal Controlled Release Vol. 70, No. 3, 2001, pp. 383-39. doi:10.1016/S0168-3659(00)00366-7
[11] P. Colombo, R. Bettini, P. Santi, A. De Asentiis and N. Peppas, “Analysis of the Swelling and Release Mechanisms from Drug Delivery Systems with Emphasis on Drug Solubility and Water Transport,” Journal Controlled Release, Vol. 39, No. 2-3, 1996, pp. 231-242. doi:10.1016/0168-3659(95)00158-1
[12] M. Εfentakis, I. Pagoni, M. Vlachou and K. Avgoustakis, “Dimensional Changes, Gel Layer Evolution and Drug Release Studies in Hydrophilic Matrices Loaded with Drugs of Different Solubility,” International Journal Pharmaceutics, Vol. 339, No. 1-2, 2007, pp. 66-75. doi:10.1016/j.ijpharm.2007.02.023
[13] E. Papadimitriou, G. Buckton and M. Efentakis, ” Probing the Mechanism of Swelling of Hydropropylmethyl-cellulose Matrices,” International Journal Pharmaceutics, Vol. 98, No. 1-3, 1993, pp. 57-62. doi:10.1016/0378-5173(93)90041-D
[14] M. Vlachou, H. Naseef and M. Efentakis, “Image Analysis Studies of Dimensional Changes in Swellable Hydrophilic Polymer Matrices,” Polymers Advanced Technologies, Vol. 15, No. 11, 2004, pp. 683-689. doi:10.1002/pat.531
[15] M. Efentakis and K. Stamoulis, “An Investigation into the Swelling Properties, Dimensional Changes and Gel Layer Evolution in Chitosan Tablets Undergoing Hydration,” Advances Polymer Technology, Vol. 28, No. 1, 2009, pp. 32-39. doi:10.1002/adv.20147
[16] R. Korsmeyer, R. Gurny, E. Doelker, P. Buri and N. Peppas, “Mechanisms of Solute Release from Porous Hydrophilic Polymers,” International Journal Pharmaceutics, Vol. 15, No. 1, 1983, pp. 25-35. doi:10.1016/0378-5173(83)90064-9

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