DEVELOPMENT OFRIZATRIPTAN BENZOATE MICROSPHERES FOR NOSE TO BRAIN TARGETING


Shital Butani, Tora Shah, Kunal Parmar, Amarjitsing Rajput

Abstract


Objective: Oral administration of rizatriptan benzoate shows poor bioavailability due to first pass metabolism, which can be avoided by nasal administration of drugs. Additionally, the nasal administration provides faster onset of action, which is desired to get relief from the intense pain of a migraine. The present research work was emphasised on design, development and evaluation of mucoadhesive microspheres for nasal delivery of rizatriptan benzoate through a systematic approach.

Methods: The microspheres of rizatriptan benzoate were prepared by the w/o/w double emulsion solvent diffusion method using the non-aqueous medium. Critical formulation and process parameters were identified through preliminary trial batches and 2[4-1] fractional factorial design was employed using polymer concentration (X1:2-5%), drug to polymer ratio (X2:1:2-1:6), amount of liquid paraffin (X3:100-200 ml) and the amount of magnesium stearate (X4:100-150 mg) as independent variables.

Results: Design batches were evaluated for percent yield (50-78%), percent entrapment efficiency (62-85%), drug loading (7.5-30%), % mucoadhesion (47-75%) and drug release at 6 h (44-78%). Scanning electron microscopic (SEM) study showed that microspheres were of 50 µm in size and spherical in shape with a smooth surface. The optimised batch (D10) showed 85% entrapment efficiency and 66.6% drug release within 6 h. The developed microspheres could be used to deliver rizatriptan benzoate through nasal administration for treatment of a migraine.

Conclusion: The developed microspheres can be considered as a promising system for nasal delivery system of rizatriptan benzoate


Keywords


Rizatriptan benzoate, Ethylcellulose, Mucoadhesive microspheres, Nasal route

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References


Adelman JU, Adelman RA. Current options for the prevention and treatment of a migraine. Clin Ther 2011;23:772–88.

Talegaonkar DA. Mishra PR. Intranasal delivery: an approach to bypass the blood brain barrier. Indian J Pharmacol 2004;36:140-7.

Illum L. Nasal drug delivery--possibilities, problems and solutions. J Controlled Release 2003;87:187-98.

Tushar TG, Vyas AK, Babbar RK. Intranasal mucoadhesive microemulsions of clonazepam: preliminary studies on brain targeting. J Pharm Sci 2006;95:570-80.

Vyas SP, Khar RK. 1st ed. New Delhi: CBS Publishers and Distributers. Targeted and Controlled drug delivery novel carrier Systems. 2006.

Chang SF, Chein YW. Intranasal drug administration for systemic medication. Pharm Int 1984;5:287.

Sakhare SS, Yadav AV, Jadhav PD. Design, development and characterization of mucoadhesive gastro spheres of carvedilol. Int J Appl Pharm 2016;8:37-42.

Gohel M, Bariya S. Advanced formulation design of venlafaxine hydrochloride coated and triple-layer tablets are containing hypromellose. Pharm Dev Technol 2009;14:1–10.

Koradia H, Butani S, Gohel M. Studies in oxcarbazepine microspheres employing Plackett and burman design. Int J Pharm Pharm Sci 2014;6:305-10.

Desai S, Vidyasagar G, Shah V. Preparation and in vitro characterization of mucoadhesive microspheres of midazolam: nose to brain administration. Asian J Pharm Clin Res 2011;1:100-2.

Partridge WM. The blood-brain barrier: a bottleneck in the brain. Drug Dev 2005;2:3-14.

Hasçiçek C, Gönül N, Erk N. Mucoadhesive microspheres containing gentamicin sulfate for nasal administration: preparation and in vitro characterization. Farmaco 2003;58:11-6.

Ganesan P, Soundararajan R, Shanmugam U. Development, characterization and solubility enhancement of comparative dissolution study of the second generation of solid dispersions and microspheres for poorly water soluble drug. Asian J Pharm Sci 2015;10:433-41.

Wenjia G, Peng Q, Lian F. Sustained release donepezil loaded PLGA microspheres for injection: preparation, in vitro and in vivo study. Asian J Pharm Sci 2015;10:405-14.

Giri TK, Choudhary C, Alexander A. Prospects of pharmaceuticals and biopharmaceuticals loaded microparticles prepared by double emulsion technique for controlled delivery. Saudi Pharm J 2011;21:125–41.

Suthar V, Gohel M, Butani S. Self-emulsifying drug delivery system containing aceclofenac: design and development using quality by design (QbD) concept. Indian Drugs 2014:51:15-26.

Kulkarni AD, Bari DB, Surana SJ, Pardeshi CV. In vitro, ex vivo and in vivo performance of chitosan-based spray-dried nasal mucoadhesive microspheres of diltiazem hydrochloride. J Drug Delivery Sci Technol 2016;31:108-17.

Kellaway W, Haeed MD. Preparation and in vitro characterization of mucoadhesive polymeric microspheres as intra-nasal delivery systems. Eur J Pharm Biopharm 1997:44:53–60.

Edmundson IC, Carless JE, Beckett AH. Advances in pharmaceutical sciences. London: Academic Press; 1967. p. 950.

Parmar KV, Gohel MC, Bariya S. Sustained release floating microspheres of acyclovir: formulation, optimisation, characterization and in vitro evaluation. Int J Drug Dev Res 2011;3:242-51.

Seju U, Kumar A, Sawant KK. Development and evaluation of olanzapine-loaded PLGA nanoparticles for nose-to-brain delivery: in vitro and in vivo studies. Acta Biomater 2011;7:4169-76.

Saraparn H, Vimolmas L, Narueporn S. Spray dried mucoadhesive microspheres: preparation and transport through nasal cell monolayer. AAPS Pharm Sci Technol 2006;7:E1–E10.

Pathak R, Dash RP, Misra M. Role of mucoadhesive polymers in enhancing delivery of nimodipine microemulsion to the brain via the intranasal route. Acta Pharm Sin B 2014;4:151–60.

Mahajan HS. Tatiya BV. Nerkar PP. Ondansetron loaded pectin based microspheres for nasal administration: in vitro and in vivo studies. Powder Technol 2012;221:168–76.

Yasir M, Sara UVS. Solid lipid nanoparticles for the nose to brain delivery of haloperidol: in vitro drug release and pharmacokinetics evaluation. Acta Pharm Sin B 2014;4:454–63.

Sood S, Jain K, Gowthamarajan K. Optimization of curcumin nanoemulsion for intranasal delivery using the design of the experiment and its toxicity assessment. Colloids Surf B 2014;113:330–7.

Gavini E, Hegge HB, Rassu G. Nasal administration of carbamazepine using chitosan microspheres: in vitro/in vivo studies. Int J Pharm 2006;307:9–15.

Jain SK, Jain NK, Gupta Y. Mucoadhesive chitosan microspheres for non-invasive and improved nasal delivery of insulin. Indian J Pharm Sci 2007;69;498-504.

Patil SB, Sawant KK. Chitosan microspheres as a delivery system for nasal insufflations. Colloids Surf B 2011;84:384–9.




About this article

Title

DEVELOPMENT OFRIZATRIPTAN BENZOATE MICROSPHERES FOR NOSE TO BRAIN TARGETING

Keywords

Rizatriptan benzoate, Ethylcellulose, Mucoadhesive microspheres, Nasal route

Date

01-10-2016

Additional Links

Manuscript Submission

Journal

International Journal of Applied Pharmaceutics
Vol 8, Issue 4, 2016 Page: 69-74

Online ISSN

0975-7058

Statistics

92 Views | 127 Downloads

Authors & Affiliations

Shital Butani
Department of Pharmaceutics, Institute of Pharmacy, Nirma University, S. G. Highway, Ahmedabad, Gujarat, India
India

Tora Shah
Department of Pharmaceutics, Institute of Pharmacy, Nirma University, S. G. Highway, Ahmedabad, Gujarat, India
India

Kunal Parmar
Drug Inspector, Food and Drug Control Administration, Himatnagar circle, Gujarat, India
India

Amarjitsing Rajput
Department of Pharmaceutics, Institute of Pharmacy, Nirma University, S. G. Highway, Ahmedabad, Gujarat, India
India


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