Evaluation of loading efficiency of azelaic acid-chitosan particles using artificial neural networks

Document Type: Research Paper

Authors

1 Nanobiotechology Research Center, Baqiyatallah University of Medical Sciences, Tehran, Iran

2 Department of Medical Nanotechnology, School of Advanced Technologies in Medicine, Tehran University of Medical Sciences, Tehran, Iran

3 Medical Biomaterials Research Center, Tehran University of Medical Sciences, Tehran, Iran

10.7508/nmj.2016.03.004

Abstract

Objective(s): Chitosan, a biodegradable and cationic polysaccharide with increasing applications in biomedicine, possesses many advantages including mucoadhesivity, biocompatibility, and low-immunogenicity. The aim of this study, was investigating the influence of pH, ratio of azelaic acid/chitosan and molecular weight of chitosan on loading efficiency of azelaic acid in chitosan particles.
Materials and Methods:  A model was generated using artificial neural networks (ANNs) to study interactions between the inputs and their effects on loading of azelaic acid.
Results: From the details of the model, pH showed a reverse effect on the loading efficiency. Also, a certain ratio of drug/chitosan (~ 0.7) provided minimum loading efficiency, while molecular weight of chitosan showed no important effect on loading efficiency.
Conclusion: In general, pH and drug/chitosan ratio indicated an effect on loading of the drug. pH was the major factor affecting in determining loading efficiency.

Keywords


[1] Mourya VK, Inamdar NN. Chitosan-modifications and applications: Opportunities galore. React Funct Polym. 2008; 68(6): 1013-1051.

[2] Jayakumar R, Prabaharan M, Reis RL, Mano JF. Graft copolymerized chitosan—present status and applications. Carbohydr Polym. 2005; 62(2): 142-158.

[3] Jayakumar R, Nwe N, Tokura S, Tamura H. Sulfated chitin and chitosan as novel biomaterials. Int J Biol Macromol. 2007; 40(3): 175-181.

[4] Jayakumar R, Prabaharan M, Nair SV, Tokura S, Tamura H, Selvamurugan N. Novel carboxymethyl derivatives of chitin and chitosan materials and their biomedical applications. Prog Mater Sci. 2010; 55(7): 675-709.

[5] Kumar MN, Muzzarelli RA, Muzzarelli C, Sashiwa H, Domb AJ. Chitosan chemistry and pharmaceutical perspectives. Chemical Reviews. 2004; 104(12): 6017-6084.

[6] Jayakumar R, Prabaharan M, Sudheesh Kumar PT, Nair SV, Tamura H. Biomaterials based on chitin and chitosan in wound dressing applications. Biotechnology Advances. 2011; 29(3): 322-337.

[7] Rinaudo M. Chitin and chitosan: Properties and applications. Prog Polym Sci. 2006; 31(7): 603-632.

[8] Suh JK, Matthew HW. Application of chitosan-based polysaccharide biomaterials in cartilage tissue engineering: a review. Biomaterials. 2000; 21(24): 2589-2598.

[9] Fu H, Kobayashi T. Self-assembly functionalized membranes with chitosan microsphere/polyacrylic acid layers and its application for metal ion removal. J Mater Sci. 2010; 45(24): 6694-6700.

[10] Breathnach A, Levi-Montalcini R. The story of azelaic acid. A tribute to Marcella Nazzaro-Porro. Rend Lincei. 1995; 6(4): 313-320.

[11] Passi S, Picardo M, Nazzaro-Porro M, Breathnach A, Confaloni AM, Serlupi-Crescenzi G. Antimitochondrial effect of saturated medium chain length (C8-C13) dicarboxylic acids. Biochemical Pharmacology. 1984; 33(1): 103-108.

[12] Nazzaro-Porro M, Passi S. Identification of tyrosinase inhibitors in cultures of Pityrosporum.  J Invest Dermatol.

[13] 1978; 71(3): 205-208.

[14] Schallreuter KU, Wood JM. Azelaic acid as a competitive inhibitor of thioredoxin reductase in human melanoma cells. Cancer Letters. 1987; 36(3): 297-305.

[15] Galhaup I. Azelaic acid: mode of action at cellular and subcellular levels. Acta Derm Venereol Suppl. 1989; 143: 75-82.

[16] Passi S, Picardo M, De Luca C, Breathnach AS, Nazzaro-Porro M. Scavenging activity of azelaic acid on hydroxyl radicals “in vitro”. Free Radic Res Commun. 1991; 11(6): 329-338.

[17] Passi S, Picardo M, Zompetta C, De Luca C, Breathnach AS, Nazzaro-Porro M. The oxyradical-scavenging activity of azelaic acid in biological systems. Free radical research communications. 1991; 15(1): 17-28.

[18] Fitton A, Goa KL. Azelaic acid. A review of its pharmacological properties and therapeutic efficacy in acne and hyperpigmentary skin disorders. Drugs. 1991; 41(5): 780-798.

[19] Vyas SP, Gupta S. Optimizing efficacy of amphotericin B through nanomodification. Int J Nanomedicine. 2006; 1(4): 417-432.

[20] Meier W. Polymer nanocapsules. Chem Soc Rev. 2000;29(5):295-303.

[21] Pathak Y, Thassu D. Drug Delivery Nanoparticles Formulation and Characterization: CRC Press; 2009.

[22] Gad SC. Pharmaceutical Manufacturing Handbook: Production and Processes: Wiley; 2008.

[23] Xu Y, Du Y. Effect of molecular structure of chitosan on protein delivery properties of chitosan nanoparticles. Int J Pharm. 2003; 250(1): 215-226.

[24] Genta I, Perugini P, Pavanetto F. Different molecular weight chitosan microspheres: influence on drug loading and drug release. Drug Dev Ind Pharm. 1998; 24(8): 779-784.

[25] Wang SB, Chen AZ, Weng LJ, Chen MY, Xie XL. Effect of drug-loading methods on drug load, encapsulation efficiency and release properties of alginate/poly-L-arginine/chitosan ternary complex microcapsules. Macromolecular Bioscience. 2004; 4(1): 27-30.

[26] Modaresi SMS, Faramarzi MA, Soltani A, Baharifar H, Amani A. Use of Artificial Neural Networks to Examine Parameters Affecting the Immobilization of Streptokinase in Chitosan. Iran J Pharm Res. 2014; 13(4): 1379-1386.

[27] Alsarra IA, Betigeri SS, Zhang H, Evans BA, Neau SH. Molecular weight and degree of deacetylation effects on lipase-loaded chitosan bead characteristics. Biomaterials. 2002; 23(17): 3637-3644.

[28] Zhang H, Oh M, Allen C, Kumacheva E. Monodisperse Chitosan Nanoparticles for Mucosal Drug Delivery. Biomacromolecules. 2004; 5(6): 2461-2468.

[29] Gan Q, Wang T. Chitosan nanoparticle as protein delivery carrier—Systematic examination of fabrication conditions for efficient loading and release. Colloids Surf B Biointerfaces. 2007; 59(1): 24-34.

[30] Patel JL, Goyal RK. Applications of artificial neural networks in medical science. Curr Clin Pharmacol. 2007; 2(3): 217-226.

[31] Behzadi SS, Prakasvudhisarn C, Klocker J, Wolschann P, Viernstein H. Comparison between two types of Artificial Neural Networks used for validation of pharmaceutical processes. Powder Tech. 2009; 195(2): 150-157.

[32] Amani A, York P, Chrystyn H, Clark BJ. Factors affecting the stability of nanoemulsions—use of artificial neural networks. Pharm Res. 2010; 27(1): 37-45.

[33] Khayet M, Cojocaru C, Essalhi M. Artificial neural network modeling and response surface methodology of desalination by reverse osmosis. J Memb Sci. 2011; 368(1): 202-214.

[34] Mansour AM, Ibrahiem MM. Simultaneous determination of azelaic and benzoic acids in topical preparations by liquid chromatography. Chromatographia. 2002; 55(7-8): 435-437.

[35] Amani A, York P, Chrystyn H, Clark BJ, Do DQ. Determination of factors controlling the particle size in nanoemulsions using artificial neural networks. Eur J Pharm Sci. 2008; 35(1-2): 42-51.

[36] Aghajani M, Shahverdi AR, Rezayat SM, Amini MA, Amani A. Preparation and optimization of acetaminophen nanosuspension through nanoprecipitation using microfluidic devices: an artificial neural networks study. Pharm Dev Technol. 2013; 18(3): 609-618.

[37] Sailakshmi G, Mitra T, Chatterjee S, Gnanamani A. Engineering Chitosan Using ل, ù-Dicarboxylic Acids—An Approach to Improve the Mechanical Strength and Thermal Stability. J Biomater Nanobiotechnol. 2013;Vol.04 No.02:14.

[38] Alsarra IA, Neau SH, Howard MA. Effects of preparative parameters on the properties of chitosan hydrogel beads containing Candida rugosa lipase. Biomaterials. 2004; 25(13): 2645-2655.

[39] Gazori T, Khoshayand MR, Azizi E, Yazdizade P, Nomani A, Haririan I. Evaluation of Alginate/Chitosan nanoparticles as antisense delivery vector: Formulation, optimization and in vitro characterization. Carbohydr Polym. 2009; 77(3): 599-606.

[40] Motwani SK, Chopra S, Talegaonkar S, Kohli K, Ahmad FJ, Khar RK. Chitosan-sodium alginate nanoparticles as submicroscopic reservoirs for ocular delivery: formulation, optimisation and in vitro characterisation. Eur J Pharm Biopharm. 2008; 68(3): 513-525.

[41] Vandenberg GW, Drolet C, Scott SL, de la Noue J. Factors affecting protein release from alginate-chitosan coacervate microcapsules during production and gastric/intestinal simulation. Journal of controlled release : official J Control Release. 2001; 77(3): 297-307.

[42] Wu Y, Yang W, Wang C, Hu J, Fu S. Chitosan nanoparticles as a novel delivery system for ammonium glycyrrhizinate. Int J Pharm. 2005; 295(1): 235-45.

[43] Kouchak M, Avadi M, Abbaspour M, Jahangiri A, Boldaji SK. Effect of different molecular weights of chitosan on preparation and characterization of insulin loaded nanoparticles by ion gelation method. Int J Drug Dev Res. 2012; 4: 271-277.