FORMULATION DESIGN AND CHARACTERIZATION OF ROPINIROLE HYDROCHORIDE MICROSPHERE FOR INTRANASAL DELIVERY

Shubhrajit Mantry; Anna Balaji

doi:10.22159/ajpcr.2017.v10i7.18475

Authors

Shubhrajit Mantry Department of Pharmaceutics, Research Scholar, Institute of Pharmaceutical Sciences and Research Center, Bhagwant University, Ajmer, Rajasthan, India.
Anna Balaji Department of Pharmaceutics, Pathfinder Institute of Pharmacy Education & Research. Beside Mamnoor Camp, Khammam Road, Warangal, Telangana, India.

DOI:

https://doi.org/10.22159/ajpcr.2017.v10i7.18475

Keywords:

Ropinirole hydrochloride, Nil, Microspheres

Abstract

Objective: The objective of this research work to design nasal microspheres of ropinirole hydrochloride (HCL) using different mucoadhesive polymers by adopting the suitable technique. To study the influence of formulation and process variables on microsphere formation and release characteristics. To perform the physicochemical characterization of the prepared microspheres. To carry out in vitro drug release studies and to explore the release behavior using various kinetic models.

Methods: Experiments were performed with ropinirole HCL as a drug, chitosan, guar gum, carbopol 974P as a polymer. Span 80 and Tween 80 used light liquid paraffin, concentrated hydrochloric acid as solvent.

Result: The in vitro drug release studies were conducted for all the formulations, that is, F1-F21 in 250 ml phosphate buffer pH 6.6 for 12 hrs. Among them, F15 showed 82.7Â±0.23% drug release and F21 showed 81.2% in 12 hrs in a sustained manner.

Conclusion: Microspheres were formulated by emulsion solvent evaporation technique using different polymers. Apart from preventing nasal irritation, the microsphere possesses two major advantages over plain solutions, one is a high solubilization capacity for ropinirole HCL that exceeds their aqueous solubility and thus allows a reduction in the application volume. The results of this work indicate that intranasal microsphere of ropinirole may be beneficial for the treatment of Parkinson's disease.

Downloads

Download data is not yet available.

References

Chaudhari A, Jadhav KR, Kadam VJ. An over view: Microspheres as a nasal drug delivery system. Int J Pharm Sci Rev Res 2010;5(1):8-17.

Koyani V, Dedakia A, Matholiya C, Patel P. Microspheres for intranasal delivery system: As review. Bio Inf Drug Targets 2014;2(1):14-9.

Sharma A, Khatri K, Patil UK. Nasal route: A potential alternative for antiparkinsonism drug delivery. Int J PharmTech Res 2008;2(4):2291-306.

Pardridge WM. The blood-brain barrier: Bottleneck in brain drug development. NeuroRx 2005;2:3-14.

Illum L, Watts P, Fisher AN, Hinchcliffe M, Norbury H, Jabbal-Gill I, et al. Intranasal delivery of morphine. J Pharmacol Exp Ther 2002;301:391-400.

Kisan RJ, Manoj NG, Ishaque MS, Vilarsrao JK, Sambjahi SP. Nasal drug delivery system-factors affecting and applications. Curr Drug Ther 2007;2:27-38.

Johnson NJ, Leah RH, William HF. Trigeminal pathways deliver a low molecular weight drug from the nose to the brain and orofacial structures. Mol Pharm 2010;7:884.

Talegaonkar S, Mishra PR. Intranasal delivery: An approach to bypass the blood brain barrier. Indian J Pharmacol 2004;36:140.

Illum L. Nasal drug delivery--possibilities, problems and solutions. J Control Release 2003;21:187.

Vyas TK, Babbar AK, Sharma RK, Singh S, Mishra A. Intranasal mucoadhesive microemulsions of clonazepam: Preliminary studies on brain targeting. J Pharm Sci 2006;54:570.

Vyas SP, Khar RK. Targeted and Controlled Drug Delivery Novel Carrier Systems. New Delhi: CBS Publishers and Distributers; 2002. p. 489-509.

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

Aspden TJ, Mason JD, Jones NS, Lowe J, Skaugrud O, Illum L. Chitosan as a nasal delivery system: The effect of chitosan solutions on in vitro and in vivo mucociliary transport rates in human turbinates and volunteers. J Pharm Sci 1997;86(4):509-13.

Bhosale NR, Hardikar SR, Ashok BV. Formulation and evaluation of transdermal patches of ropinirole HCl. Res J Pharm Bio Chem Sci 2011;2(1):138-48.

Adnan A, Talegaonkar S, Negi LM, Farhan JA, Khar RK, Zeenat I. Oil based nanocarrier system for transdermal delivery of ropinirole: A mechanistic, pharmacokinetic and biochemical investigation. Int J Pharm 2011. (Article under Press).

Priya S, Koland M, Kumari NS. Formulation and characterization of ropinirole hydrochloride loaded solid lipid nanoparticles. Int J Pharm Pharm Sci 2015;7(9):85-9.

Chandrakala V, Saral AM. Quality by design approach in formulation of bioadhesive levodopa microspheres. Int J Pharm Pharm Sci 2013;5 Suppl 4:172-8.