DESIGN AND OPTIMIZATION OF SOLID LIPID NANOPARTICLES (SLNs) OF ZOLMITRIPTAN FOR THE MANAGEMENT OF MIGRAINE

Akanksha Garud; Deepti Singh; Navneet Garud

doi:10.14499/indonesianjpharm0iss0pp245-252

DESIGN AND OPTIMIZATION OF SOLID LIPID NANOPARTICLES (SLNs) OF ZOLMITRIPTAN FOR THE MANAGEMENT OF MIGRAINE

Akanksha Garud, Deepti Singh, Navneet Garud

Abstract

Solid lipid nanoparticles (SLNs) of zolmitriptan were produced by solvent emulsification-diffusion technique. Soya lecithin and poloxamer 188 were used as surfactants and stabilizers of the particles. The formulations were optimized for independent variables (amount of stearic acid, amount of lecithin and homogenization time) in order to achieve desired particle size with maximum percent entrapment efficiency (% EE). Prepared SLNs were characterized by transmission electron microscopy (TEM), atomic force microscopy (AFM) and zeta potential measurements. To achieve our goal, eight formulations (F1–F8) of SLNs were prepared by solvent injection technique and optimized by 23 full-factorial design. The responses of the design were analyzed using Minitab 15. On the basis of software analysis, formulation F8 was selected as optimized formulation and was evaluated for the independent parameters. Optimized formulation showed particle size of 340nm, percent entrapment efficiency (EE) of 81.36 and 79.11% of in-vitro drug release after 24h. The release kinetics of the optimized formulation best fitted the Higuchi model.
Key words: solid lipid nanoparticles, zolmitriptan, solvent emulsificationdiffusion technique, in-vitro release.

Full Text:

Untitled

References

Belvís R., Pagonabarraga J., Kulisevsky J. 2009. Individual Triptan Selection in Migraine Attack Therapy. Recent Pat. CNS Drug Discov. 4: 70-81.

Bhaskar K., Anbu J., Ravichandiran V., Vankateswarlu V., Rao YM. 2009. Lipid nanoparticles for transdermal delivery of flurbiprofen: formulation, in vitro ex vivo and in vivo studies. Lipids Health Dis. 8: 1-15.

Bunjes H., Drechsler M., Koch MH., Westesen K. 2001. Incorporation of the model drug ubidecarenone into solid lipid nanoparticles. Pharm. Res. 18: 287-293.

Doijad RC., Manvi FV., Godhwani DM., Joseph R., Deshmukh NV. 2008. Formulation and targeting efficiency of cisplatin engineered solid lipid nanoparticles, Indian J. Pharm. Sci. 70: 203-207.

Dubes A., Parrot LH., Abdelwahed W., Degobert G., Fessi H., Shahgaldian P., Coleman AW. 2003. Scanning electron microscopy and atomic force microscopy imaging of solid lipid nanoparticles derived from amphiphilic cyclodextrins. Eur. J. Pharm. Biopharm. 55:279-282.

Garcia-FM., Torres D., Alonso MJ. 2003. Design of lipid nanoparticles for the oral delivery of hydrophilic macromolecules. Colloids and Surfaces B: Biointerfaces. 27:159-168.

Gayathri DS., Venkatesh P., Udupa, N. 2000. Niosomal sumatriptan succinate for nasal administration. Indian J. Pharm. Sci. 62: 479-481.

Goadsby PJ., Lipton RB., Ferrari MD. 2002. Migraine-current understanding and treatment. N. Engl. J. Med. 346: 257- 270.

Hu FQ., Yuan H., Zhang HH., Fang M. 2002. Preparation of solid lipid nanoparticles with clobetasol propionate by a novel solvent diffusion method in aqueous system and physicochemical characterization. Int. J. Pharm. 239: 121-128.

Kolsure PK., and Rajkapoor B. 2012. Development of zolmitriptan gel for nasal administration. .Asian J. Pharm. Clin. Res. 5: 88-94.

Lai J., Chen J., Lu Y., Sun J., Hu F., Yin Z., Wu W. 2009. Glyceryl monooleate/ poloxamer 407 cubic nanoparticles as vitro evaluation and enhanced oral bioavailability of the poorly watersoluble drug simvastatin. AAPS Pharm. Sci. Tech. 10: 960-966.

Lv Q., Yu A., Xi Y., Cui J., Cao F., Zhai G. 2009. Development and evaluation of penciclovir-loaded solid lipid nanoparticles for topical delivery. Int. J. Pharm. 372: 191-198.

Mehnert W., and Mader K. 2001. Solid lipid nanoparticles. Production, characterization and applications. Adv. Drug Del. Rev. 47: 165-196.

Mukherjee S., Ray S., Thakur RS. 2007. The current status of solid lipidnanoparticles.Pharmabit 1: 53-60.

Muller RH., Maaßen S., Weyhers H., Specht F., Lucks JS. 1996. Cytotoxicity of magnetite loaded polylactide, polylactide/glycolide particles and solid lipid nanoparticles. Int. J. Pharm. 138: 85-94.

Reddy LH., andMurthy RSR. 2005. Etoposideloaded nanoparticles made from glyceride lipids: formulation, characterization, in vitro drug release, and stability evaluation. AAPS Pharm. Sci.Tech. 6: 158-166.

Sarmento B., Martins S., Ferreira D., Souto EB. 2007. Oral insulin delivery by means of solid lipid nanoparticles. Int. J. Nanomedicine. 2: 743-749.

Schubert MA., Muller-Goymann CC. 2003. Solvent injection as a new approach for manufacturing lipid nanoparticlesevaluation of the method and process parameters. Eur. J. Pharm. Biopharm. 55: 125-131.

Shah M., Pathak K. 2010. Development and Statistical Optimization of Solid Lipid Nanoparticles of Simvastatin by Using 23 Full-Factorial Design. AAPS Pharm.Sci. Tech. 11: 489-496.

Souto EB. 2006. Application of lipid nanoparticles (SLN and NLC) in food industry. J Food Tech. 4: 90-95.

Yang S., Zhu J., Lu Y., Liang B., Yang C. 1999. Body distribution of camptothecin solid lipid nanoparticles after oral administration. Pharm. Res. 16: 751-757.

DOI: http://dx.doi.org/10.14499/indonesianjpharm0iss0pp245-252