Open Access Open Access  Restricted Access Subscription Access
Open Access Open Access Open Access  Restricted Access Restricted Access Subscription Access

Formulation and Evaluation of Interpenetrating Polymer Network Microparticles of Diclofenac Sodium


Affiliations
1 Professor (Pharmaceutics), Arihant School of Pharmacy and Bio Research Institute, Adalaj, Gandhinagar,, India
2 Assistant Professor, Dayanand Sagar University, Bangalore,, India
     

   Subscribe/Renew Journal


Diclofenac sodium, a model anti-inflammatory drug, has adverse effects like gastric irritation and hepatic toxicity. To overcome these problems Interpenetrating Polymer Network microparticles can be used as a controlled drug delivery system. Preparation of Interpenetrating Polymer Network microparticles using two or more polymer is a novel approach as the polymers produce synergistic effect which could increase the mechanical strength and resilience of the microparticles. The aim of the study was to prepare Interpenetrating Polymer Network microparticles of Diclofenac Sodium using chitosan and Ghatti gum which were used to deliver Diclofenac Sodium to the intestine. Microparticles prepared by emulsion-cross-linking method using gluteraldehyde as a cross-linker were characterized by Fourier Transform Infrared Spectroscopy, Differential scanning calorimetry, Scanning electron microscopy and evaluated for in vitro dissolution rate. Fourier Transform Infrared Spectroscopy studies confirmed the absence of chemical interactions between drug, polymers and cross-linking agent. Differential scanning calorimetric results indicated amorphous dispersion of Diclofenac Sodium into Interpenetrating Polymer Network matrix. Scanning electron microscopy pictures showed that microparticles did not agglomerate and had a rough surface. Hydrated surface after swelling showed spongy porous surface which indicated the mechanism of drug release as diffusion. Particle size ranged between 294 to 366 μm. DS percentage encapsulation efficiency ranged from 84.09 to 96.81%. In vitro release studies indicated a dependence of drug release rates on both the amount of CS and GG used in preparation of microparticles. The release was extended up to 12 h and release rates indicated a non-Fickian and super case II mechanism.

Keywords

Chitosan, Ghatti gum, Interpenetrating polymer networks, Microparticles, Hydrophillic polymers.
Subscription Login to verify subscription
User
Notifications
Font Size


  • Bin W et al, Preparation, characterization and controlled release investigation of interpenetrating polymer networks of poly(acrylic acid)/triazole modified poly (vinyl alcohol), International Journal of Pharmaceutics, 2007; 331(1): 19–26.
  • Kallappa M Hosamani, Ramesh Babu V, Malladi Sairam, Tejraj M Aminabhavi, Preparation of sodium alginate-methylcellulose blend microspheres for controlled release of Nifedipine, Carbohydrate polymers, 2007; 69(2): 241-50.
  • Tejraj M. Aminabhavi, Mahaveer D Kurkuri, Poly(vinyl alcohol) and poly(acrylic acid) sequential interpenetrating network pHsensitive microspheres for the delivery of Diclofenac sodium to the intestine, Journal of Controlled Release, 2004; 96(1):9–20.
  • Sperling, L. H, Interpenetrating Polymer Networks and Related Materials, Plenum Press, 1981, Chpt. 1.
  • Chunhua Yin, Lichen Yin, Likun Fei, Fuying Cui, Cui Tang, Superporous hydrogels containing poly (acrylic acid-coacrylamide)/ O-carboxymethyl chitosan interpenetrating polymer networks, Biomaterials, 2007; 28(6): 1258–66.
  • Ajit P Rokhade, Sunil A Agnihotri, Sangamesh A Patil, Nadagouda N Mallikarjuna, Padmakar V Kulkarni, Tejraj M Aminabhavi, Semi-interpenetrating polymer network microspheres of gelatin and sodium carboxymethyl cellulose for controlled release of Ketorolac tromethamine, Carbohydrate Polymers, 2006; 65(3): 243–2.
  • Tejraj M Aminabhavi, Sangamesh A Patil, Ajit P Rokhade, Namdev B Shelke, Novel interpenetrating polymer network microspheres of chitosan and methylcellulose for controlled release of Theophylline, Carbohydrate polymers, 2007; 113(4): 678-687.
  • Elworthy PH, George TM, The Molecular properties of Ghatti gum: A naturally occurring Polyelectrolyte, J Pharm Pharmcol, 1963; 15(1): 781-93.
  • Tischer CA, Iacomini M, Wagner R, Gorin PA, New structural features of the polysaccharide from gum ghatti. Carbohydrate Res, 2002; 337(21-23): 2205-10.
  • P A Todd E, M Sorkin, Diclofenac sodium: A reappraisal of its pharmacodynamic and pharmacokinetic properties and therapeutic efficacy, Drugs, 1988; 35(3): 244-85.
  • Tejraj A, Sunil A, Novel interpenetrating network chitosanpoly( ethylene oxide-g-acrylamide) hydrogel microspheres for the controlled release of capecitabine, International Journal of Pharmaceutics, 2006; 324(2): 103–115.
  • Rapolu B, Vedavathi T, Formulation and Evaluation of Sumatriptan Succinate Oral Disintegrating Tablets and Comparision of disintegrating property between superdisintegrants and simple disintegrants, TPI Journal, 2012; 1(9): 73-92.
  • Keyur Patel, Mandev B Patel, Preparation and evaluation of chitosan microspheres containing Nicorandil, International Journal of Pharmaceutical Investigation, 2014; 4(1): 32-7
  • Priya P, Mane D Formulation and Evaluation of Microspheres of Glibenclamide by Ionotropic Gelation Method, Indo American Journal of Pharmaceutical Research, 2017; 7(09): 471-79.
  • Gohel M and Amin A, Formulation design and optimization of modified-release microspheres of Diclofenac sodium, Drug Development and Industrial Pharmacy, 1999, 25(2): 247–51.
  • Reddy J, Gnanaprakash K, Badrinath A, Chetty C, Formulation and Evaluation of Microparticles of Metronidazole, J. Pharm. Sci. & Res, 2009; 1(10): 131-36
  • Khonsari F, Milani P, Jelvehgarid M, Formulation and Evaluation of In-vitro Characterization of Gastic-Mucoadhesive Microparticles/Discs Containing Metformin Hydrochloride, Iran J Pharm Res, 2014; 13(1): 67–80.
  • Balwierz R, Jankowski A, Jasinska A, Marciniak D, Pluta J, Formulation and evaluation of microspheres containing Losartan potassium by spray-drying technique, Acta Pol Pharm, 2016; 73(5): 1275-86.
  • Madan R, Kadam V, Bandavane S, Dua K, Formulation and evaluation of microspheres containing Ropinirole hydrochloride using biodegradable polymers, Asian J Pharm, 2013; 7(4): 184-8.
  • Misirli Y, Oeztuerk E, Kursakligolu H, Denkbas E, Preparation and characterization of Mitomycin-C loaded chitosan-coated alginate microspheres for chemoembolization, J.Microencapsule, 2005; 22(2): 167-78.
  • Sriamornsak P, Nunthanid J, Calcium pectinate gel beads for controlled release drug delivery: I. Preparation and in vitro release studies, International Journal of Pharmaceutics, 1998; 160(2): 207-12.
  • Peppas A, Analysis of fickian and non-fickian drug release from polymers, Pharm Acta Helv, 1985; 60(4): 110-1.
  • Korsmeyer R, Gurny R, Doelker E, Buri P, Peppas N, Mechanisms of potassium chloride release from compressed hydrophilic polymeric matrices: effect of entrapped air, J Pharm Sci, 1983; 72(10): 1189-91.
  • Paulo C, Jose S, Modeling and comparison of dissolution profiles, Eur J Pharm Sci, 2001; 13(2): 123-33. 25. ICH Harmonized Tripartite Guidelines, 2003. Stability testing of New Drug Substances and Products. Q1A (R2).

Abstract Views: 117

PDF Views: 0




  • Formulation and Evaluation of Interpenetrating Polymer Network Microparticles of Diclofenac Sodium

Abstract Views: 117  |  PDF Views: 0

Authors

Arti Mohan
Professor (Pharmaceutics), Arihant School of Pharmacy and Bio Research Institute, Adalaj, Gandhinagar,, India
Gnana Ruba Priya
Assistant Professor, Dayanand Sagar University, Bangalore,, India

Abstract


Diclofenac sodium, a model anti-inflammatory drug, has adverse effects like gastric irritation and hepatic toxicity. To overcome these problems Interpenetrating Polymer Network microparticles can be used as a controlled drug delivery system. Preparation of Interpenetrating Polymer Network microparticles using two or more polymer is a novel approach as the polymers produce synergistic effect which could increase the mechanical strength and resilience of the microparticles. The aim of the study was to prepare Interpenetrating Polymer Network microparticles of Diclofenac Sodium using chitosan and Ghatti gum which were used to deliver Diclofenac Sodium to the intestine. Microparticles prepared by emulsion-cross-linking method using gluteraldehyde as a cross-linker were characterized by Fourier Transform Infrared Spectroscopy, Differential scanning calorimetry, Scanning electron microscopy and evaluated for in vitro dissolution rate. Fourier Transform Infrared Spectroscopy studies confirmed the absence of chemical interactions between drug, polymers and cross-linking agent. Differential scanning calorimetric results indicated amorphous dispersion of Diclofenac Sodium into Interpenetrating Polymer Network matrix. Scanning electron microscopy pictures showed that microparticles did not agglomerate and had a rough surface. Hydrated surface after swelling showed spongy porous surface which indicated the mechanism of drug release as diffusion. Particle size ranged between 294 to 366 μm. DS percentage encapsulation efficiency ranged from 84.09 to 96.81%. In vitro release studies indicated a dependence of drug release rates on both the amount of CS and GG used in preparation of microparticles. The release was extended up to 12 h and release rates indicated a non-Fickian and super case II mechanism.

Keywords


Chitosan, Ghatti gum, Interpenetrating polymer networks, Microparticles, Hydrophillic polymers.

References