RIZATRIPTAN BENZOATE LOADED NATURAL POLYSACCHARIDE BASED MICROSPHERES FOR NASAL DRUG DELIVERY SYSTEM
Keywords:Rizatriptan benzoate, Polysaccharide, Microspheres, Nasal drug delivery
Objective: The objective of this research was to formulate and evaluate the different grades of rizatriptan benzoate loaded polysaccharide based microspheres for the nasal drug delivery system.
Methods: The polysaccharide was extracted from the seed of Trigonella foenum-graecum and microspheres were prepared by emulsification, followed by crosslinking using epichlorohydrin. A 32 full factorial design was employed in formulating the microspheres with polymer concentration (X1), and stirring rate (X2) as independent variables and particle size (Y1) and entrapment efficiency (Y2) were dependent variables.
Results: The microspheres were discrete and free-flowing. The mean particle size (Y1) of microspheres ranged from 40.82+12 Âµm to 62.48+0.41 Âµm and the encapsulation efficiency (Y2) was found to be increased from 60.7+0.2% to 79.22+0.2% as the drug polysaccharide ratio increased. A 32 full factorial design confirmed that the X1 and X2 both effect on particle size whereas X1 alone effect on entrapment efficiency. SEM revealed the smooth spherical surface of microspheres whereas kinetic model revealed that drug release followed the case II transport. FTIR indicated good compatibility of the excipients with rizatriptan benzoate. Stability studies were carried out for formulation F7 at 4Â°C ambient, 25+2Â°C/60+5%, 40+2Â°C/75+5% relative humidity revealed that the physical drug appearance, entrapment efficiency were within the permissible limits.
Conclusion: The result obtained in this research work indicate a promising potential of control release rizatriptan benzoate loaded microspheres whereas the Trigonella foenum-graecum polysaccharide used as rate controlling polymer for the effective treatment of migraine patients.
Chandna A, Batra D, Kakar S, Singh R. A review on target drug delivery: magnetic microspheres. Journal of Acute Disease 2013;2:189-95.
Pathaka R, Dashab RP, Misraa M, Nivs, Arkarb M. Role of mucoadhesive polysaccharides in enhancing delivery of nimodipine microemulsion to brain via intranasal route. Acta Pharm Sin B 2014;4:151â€“60.
Dhakar RC, Maurya SD, Tilak VK, Gupta AK. A review on factors affecting the design of nasal drug delivery system. Int J Drug Delivery 2011;3:194-208.
Kadam NR, Suvarna V. Microspheres: a brief review. Asian J Biomed Pharma Sci 2015;5:13-9.
Khedkar A, Rajendra V, Kulkarni A, Dehghan MH, Saifee M, Lahoti S. Spectrophotometric method for analysis of rizatriptan benzoate. Int J Pharm Sci 2009;1:307-13.
Prasanta S, Padma MS. Estimation of rizatriptan benzoate tablet by using uv spectrophotometric methods. Int J Pharm Sci Res 2013;19:97-100.
Basch E, Ulbricht C, Grace K, Pharm D, Philippe S, Smith M. Therapeutic applications of fenugreek. Altern Med Rev 2003;8:20-7.
Indian Herbal Pharmacopoeia. Indian drugs manufacturing association Mumbai. Regional Research Laboratory Jammu Tavi 1999;1:33.
Suruse PB, Shivhare UD, Mathur VB, Meshram KL, Pathak AD. Development of microcapsules of glimepiride using fenugreek seed extract. Int J Pharm Phytopharmacol Res 2013;3:212-5.
Jani GK, Prajapati VD. Gums and mucilage: versatile excipients for pharmaceutical formulations. Asian J Pharm Sci 2009;4:309-23.
Sharma N, Kulkarni GT, Sharma A, Bhatnagar A, Kumar N. Natural mucoadhesive microspheres of abelmoschus esculentus polysaccharide as a new carrier for nasal drug delivery. J Microencapsul 2013;30:589â€“98.
Mahajan HS, Tatiya BV, Nerkar PP. Ondansetron loaded pectin based microspheres for nasal administration: in vitro and in vivo studies. Pharm Dev Technol 2012;221:1-9.
Kellaway W, Hameed MD. Preparation and in vitro characterization of mucoadhesive polymeric microspheres as intra-nasal delivery systems. Eur J Pharm Biopharm 1997; 44:53â€“60.
Gavini E, Rassu G, Ciarnelli V, Spada G, Cossu M, Giunchedi P. Mucoadhesive drug delivery systems for nose-to-brain targeting of dopamine J. Nanoneurosci 2012;2:47â€“55.
Rawat A, Majumder QH, Ahsan F. Inhalable large porous microspheres of low molecular weight heparin: in vitro and in vivo evaluation. J Controlled Release 2008;128:224â€“32.
Gavini E, Hegge AB, Rassu G, Sanna V, Testa C, Pirisino G, et al. Nasal administration of carbamazepine using chitosan microspheres: in vitro/in vivo studies. Int J Pharm 2006; 307:9â€“15.
Kar K, Pal RN, Bala NN. Preparation, characterisation, and evaluation of ropinirole hydrochloride loaded controlled release microspheres using solvent evaporation technique. Int J Pharm Pharm Sci 2018;10:57-67.
Kumar R, Patil S, Patil MB, Patil SR, Paschapur MS. Isolation and evaluation of disintegrant properties of fenugreek seed mucilage. Int J Pharm Tech Res 2009;1:982-96.
Sunder Raj TJ, Bharathi CH, Kumar MS, Prabahar J, Kumar PN, Sharma HK, et al. Identification, isolation, and characterization of process-related impurities in rizatriptan benzoate. J Pharm Biomed Anal 2009;49:156â€“62.
Patil SB, Sawant K. Mucoadhesive chitosan microspheres as a delivery system for nasal insufflation. Colloids Surf B 2011;84:384-9.
Yang YY, Chung TS, Ng NP. Morphology, drug distribution, and in vitro release profiles of biodegradable polysaccharides microspheres containing protein fabricated by double-emulsion solvent extraction/evaporation method. Biomaterials 2001;22: 231â€“41.
Deshmukh M, Mohite S. Formulation and characterization of olanzapine-loaded mucoadhesive microspheres. Asian J Pharm Clin Res 2017;10:249-55.