Preparation and evaluation of polyelectrolyte complexes for oral controlled drug delivery

L Srinivas, K V Ramana Murthy


The electrostatic interaction between oppositely charged polyelectrolytes leads to formation of insoluble polyelectrolyte complexes in aqueous medium. The polyelectrolyte complexes formed between a polyacid and a polybase are little
affected by the pH variation of the dissolution medium. In the present study attempts were made to prepare polyelectrolyte complexes of polyvinyl pyrrolidone (polybase) and carbopol (polyacid) into which diclofenac sodium is incorporated and studied for its controlled release.The polyelectrolyte complexation was evaluated by pH, conductivity, Fourier transformed infrared spectroscopy, and X-ray difractometry. The dried polyelectrolyte complexes were also evaluated for micromeritic properties and drug release kinetics. Selected PECs were compressed into tablets and compared with commercial SR product for drug release.The tablets showed comparable results with commercial SR product following zero-order release, and drug release is by erosion as well as the diffusion mechanism. Promising results were obtained suggesting the application of these
polyelectrolyte complexes in the design of controlled release systems.

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Krishnendu R, Hai QM, Shau-Ku H, Kam WL. Oral gene delivery with

chitosan–DNA nanoparticles generates immunologic protection in a

murine model of peanut allergy. Nat Med 1999;5:387-91.

Genta I, Perugini P, Modena T, Pavanetto F, Castelli F, Muzzarelli RA,

et al. Miconazole-loaded 6-oxychitin–chitosan microcapsules.

Carbohydr Polymers 2003;52:11-8.

Macleod GS, Collett JH, Fell JT. The potential use of mixed films of

pectin, chitosan and HPMC for bimodal drug release. J Control Release


Chang R, Arun Y. Brownian dynamics simulations of salt-free

polyelectrolyte solutions. J Chem Phys 2002;116:5284-98.

Petzold G, Nebel A, Buchhammer HM, Lunkwitz K. Preparation and

characterization of different polyelectrolyte complexes and their

application as flocculants. Colloid Polym Sci 1998;276:125-30.

Lee W, Malcolm BH. Observations on complex formation between

polyelectrolytes in dilute aqueous solution. Eur Polym J 1997;33:1173-7.

Burgess DJ. Practical analysis of complex coacervate systems. J Colloid

Interfac Sci 1990;140:227-38.

Tsuchida E. Formation of polyelectrolyte complexes and their

structures. J Macromol Sci Pure Appl Chem 1994;A31:1-15.

Senuma M, Kuwabara S, Kaeriyama K, Hase F, Shimura Y. Polymer

complex from copolymers of acrylonitrile and ionic vinyl benzyl

compounds. J Appl Polym Sci 1986;31:1687-97.

Sato H, Maeda M, Nakajima A. Mechanochemistry and permeability of

polyelectrolyte complex membranes composed of poly (vinyl alcohol)

derivatives. J Appl Polym Sci 1979;23:1759-67.

Harris EL, Angal S. Protein purification methods. New York: Oxford

University Press; 1993.

Janne L, Lindström T. Topo chemical modification of cellulosic fibers

with bipolar activators: An overview of some technical applications.

Sci Technol 2001;1:40-5.

Hirouki Y, Takeshi K. Adsorption of BSA on cross-linked chitosan: The

equilibrium isotherm. Chem Engg Jpn 1989;41:11-5.

Dubin PL, Gao J, Mattison K. Protein purification by selective phase

separation with polyelectrolytes. Sep Purif Met 1994;23:1-16.

Cordes RM, Sima WB, Glatz CE. Precipitation of nucleic acids with poly

(ethyleneimine). Biotechnol Prog 1990;6:283-5.

Atkinson, Jack GW. Precipitation of nucleic acids with polyethyleneimine

and the chromatography of nucleic acids on immobilized

polyethyleneimine. Biochem Biophys Acta 1973;308:41-52.

Jendrisak J. In: Burgerss R, editor. Protein Purification: Micro to Macro,

New York: Alan R Liss Inc; 1987. p. 75-97.

Chen J, Jo S, Park K. Polysaccharide hydrogels for protein drug delivery.

Carbohydr Polymer 1995;28:69-76.

Dautzenberg H, Kotz J, Linow KJ, Philipp B, Rother G. Static light

scattering of polyelectrolyte complex solutions. In: Dubin P, Bock J,

Davis R, Schulz DN, Thies C, editors. Macromolecular complexes in

chemistry and biology. Berlin: Springer–Verlag; 1994. p. 119-33.

Artur B, David H. Carrageenan–oligochitosan microcapsules:

optimization of the formation process. Colloids Surf B Biointerfaces


Murakami R, Takashima R. Mechanical properties of the capsules of

chitosan–soy globulin polyelectrolyte complex. Food Hydrocolloids


Krone V, Magerstadt M, Walch A, Groner A, Hoffmann D. Pharmacological

composition containing polyelectrolyte complexes in micro particulate

form and at least on active agent. United States Patent 5,700,459,

Dec 23, 1997.

Willis JV, Kendall MJ, Flinn RM, Thornhill DP, Welling PG. The

pharmacokinetics of diclofenac sodium following intravenous and oral

administration. Eur J Clin Pharmacol 1979;16:405-10.

Joel GH, Lee EL. Goodman and gilman’s the pharmacological basis

of therapeutics. 10th ed. New York: The McGraw-Hill Companies Inc;

p. 709-10.

Physicians’ Desk Reference. 54th ed. NJ: Medical Economics Co; 2000.

p. 2004-8.

Marshall K. In: Lachman L, Lieberman HA, Kanig JL, editors. The

theory and practice of industrial pharmacy. 3rd ed. Mumbai: Varghese

Publishing House; 1991. p. 66-99.

Indian Pharmacopoeia, Govt of India, Ministry of Health and Family

Welfare. Vol 2. Delhi: The Controller of Publications; 1996. p. 736.

Shivakumar HN, Desai BG, Deshmukh G. Design and optimization of

diclofenac sodium controlled release solid dispersions by response

surface methodology. Indian J Pharm Sci 2008;70:22-30.

Higuchi T. Mechanism of sustained release medication: Theoretical

analysis of rate of release of solid drugs dispersed in solid matrices. J

Pharm Sci 1961;52:1145-9.

Paulo C, Jose MS. Modeling and comparison of dissolution profiles. Eur

J Pharm Sci 2001;13:123-33.

Moore JW, Flanner HH. Mathematical comparison of dissolution profiles.

Pharm Tech 1996;20:64-74.



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