FORMULATION AND CHARACTERIZATION OF ROPINIROLE HYDROCHLORIDE LOADED SOLID LIPID NANOPARTICLES
Keywords:Ropinirole hydrochloride, Solid lipid nanoparticles, Double emulsion method
Objective: The aim of the present study was to formulate and evaluate the Solid Lipid Nanoparticles (SLNs) of Ropinirole Hydrochloride (ROP).
Methods: ROP-loaded SLNs were prepared by a double emulsion method using glyceryl monostearate (GMS) as lipid and soya lecithin as a stabilizer. All formulated ROP-loaded SLNs were characterized for its particle size and size distribution, zeta potential, % Entrapment Efficiency (EE) and drug loading. The formulations were optimized in terms of GMS to soya lecithin ratio and sonication time of primary emulsion. Shape and surface morphology of the optimized formulation was studied using optical microscopy and scanning electron microscopy. In vitro and ex vivo Study of optimized formulation was also performed and compared with a pure drug solution.
Results: The particle size and polydispersity index (PDI), zeta potential and EE of optimized formulation were found to be 320Â±5.15 nm, 0.260Â±0.012,-37.9Â±1.43, 56.13Â±2.33% respectively. In vitro and ex vivo permeation study revealed that percentage cumulative drug release of optimized formulation was found to be 58.45Â±1.75% and 53.75Â±1.34 % respectively in 24 h and more than 90% drug release from pure drug solution was found to be within 6 h. Drug release from the formulation is sustained as compared to the plain drug solution which release 97.74 % (in vitro) and 88.15 % (ex vivo) of the drug within 6 h.
Conclusion: From the results, it concludes that drug released from SLNs follows sustained release pattern and it will enhance the overall activity of the drug.
Salawu F, Olokoba A, Danburam A. Current management of Parkinsonâ€™s disease. Ann Afr Med 2010;9:55â€“61.
Maffot AC, Osselton MD, Widdop B. Clarke's Analysis of Drugs and Poisons. 4th ed. London: Pharmaceutical Press; 2004.
Daily Med [Internet]. Bethesda MD) U. S. National Library of Medicine. Ropinirole Hydrochloride; September; 2009. Available from: URL: http://dailymed.nlm.nih.gov/ dailymed/lookup. cfm?setid=9a8eb66e-21fe-468d-aeec-44a8aa4c7869. [Last accessed on 30 Jul 2013].
Avachat AM, Bornare PN, Dash RR. Sustained release microspheres of ropinirole hydrochloride: Effect of process parameters. Acta Pharm 2011;61:363â€“76.
Spuch C, Navarro C. Liposomes for targeted delivery of active agents against neurodegenerative diseases (Alzheimerâ€™s disease and Parkinsonâ€™s disease). J Drug Delivery 2011. doi: 10.1155/2011/469679. [Article in Press]
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;7:4169â€“76.
Kumar M, Kakkar V, Mishra AK, Chuttani K, Kaur IP. Intranasal delivery of streptomycin sulfate (STRS) loaded solid lipid nanoparticles to brain and blood. Int J Pharm 2014;461:223â€“33.
Arumugam K, Subramanian GS, Mallayasamy SR, Averineni RK, Reddy MS, Udupa N. A study of rivastigmine liposomes for delivery into the brain through intranasal route. Acta Pharm 2008;58:287â€“97.
Roney C, Kulkarni P, Arora V, Antich P, Bonte F, Wu A, et al. Targeted nanoparticles for drug delivery through the bloodâ€“brain barrier for Alzheimerâ€™s disease. J Controlled Release 2005;108:193â€“214.
Mistry A, Stolnik S, Illum L. Nanoparticles for direct nose-to-brain delivery of drugs. Int J Pharm 2009;379:146â€“57.
Liu JXF, Fawcett R, Thorne RG, De For TA, Frey WH. Intranasal administration of insulin-like growth factor-I bypasses the blood-brain barrier and protects against focal cerebral ischemic damage. J Neurol Sci 20011;87:91â€“7.
MÃ¼ller RH, MÃ¤der K, Gohla S. Solid lipid nanoparticles (SLN) for controlled drug delivery-A review of the state of the art. Eur J Pharm Biopharm 2000;50:161-77.
Pardeshi CV, Rajput PV, Belgamwar VS, Tekade AR, Surana SJ. Novel surface modified solid lipid nanoparticles as intranasal carriers for ropinirole hydrochloride: application of factorial design approach. Drug Delivery 2013;20:47-56.
Jain S, Mistry MA, Swarnakar NK. Enhanced dermal delivery of acyclovir using solid lipid nanoparticles. Drug Delivery Transl Res 2011;1:395â€“406.
Kumar SP, Arivuchelvan A, Jagadeeswaran A, Subramanian N, Senthil Kumar SC, Mekala P. Formulation, Optimization and evaluation of enrofloxacin solid lipid nanoparticles for sustained oral delivery. Asian J Pharm Clin Res 2015;8:231-6.
Dash S, Murthy PN, Nath L, Chowdhury P. Kinetic modeling on drug release from controlled drug delivery systems. Acta Pol Pharm Drug Res 2010;67:217-23.
You J, Wan F, de Cui F, Sun Y, Du Y-Z, Hu Fq. Preparation and characteristic of vinorelbine bitartrate-loaded solid lipid nanoparticles. Int J Pharm 2007;343:270â€“6.
Westesen K, Siekmann B. Investigation of the gel formation of phospholipid-stabilized solid lipid nanoparticles. Int J Pharm 1997;151:35â€“45.
Viveksarathi K, Kannan K. Effect of the moist-heat sterilization on fabricated nanoscale solid lipid particles containing rasagiline mesylate. Int J Pharm Invest 2015;5:87-91.
Jain SA, Chauk DS, Mahajan HS. Formulation and evaluation of nasal mucoadhesive microspheres of Sumatriptan succinate. J Microencapsulation 2009;26:711â€“21.