FORMULATION, OPTIMIZATION AND EVALUATION OF ENROFLOXACIN SOLID LIPID NANOPARTICLES FOR SUSTAINED ORAL DELIVERY
The objective of the present study was to formulate and evaluate enrofloxacin SLNs using a hot homogenization coupled with ultrasonication method. The SLNs were prepared using tripalmitin as lipid carrier, tween 80 and span 80 as surfactants and poly vinyl alcohol (PVA) as a stabilizer. The influence of factors such as concentration of lipid carrier, composition and concentration of surfactant on the particle size were investigated to optimize the formulations. The optimized SLNs formulations were utilized to entrap 0.1% enrofloxacin and characterized for particle size, polydispersity index, zeta potential (using dynamic light scattering), shape (using atomic force microscopy and transmission electron microscopy), drug encapsulation efficiency (using by dialysis and ultracentrifugation methods), and in vitro drug release (using by dialysis). The prepared SLNs were analyzed by FT-IR spectroscopy to confirm the cross-linking reaction between drug, lipid and surfactants. The results demonstrated that the particle size, polydispersivity index, zeta potential, encapsulation efficiency and loading capacity of the SLNs were 154.72Â± 6.11nm, 0.42Â±0.11, -28.83Â±0.60mV, 59.66Â±3.22% and 6.13Â±0.32%, respectively. TEM and AFM images showed spherical to circular particles with well defined periphery. In vitro drug release exhibited biphasic pattern with an initial burst release of 18% within 2h followed by sustained release over 96h. FT-IR study suggested that during the process of formulations, lipid and surfactants have not reacted with the drug to give rise to reactant products and it was only physical mixture.
2. Martinez M, McDermott P, Walker R. Pharmacology of the fluoroquinolones: A perspective for the use in domestic animals. Vet J 2006;172(1):10-28.
3. Mitchell MA. Enrofloxacin. J Exotic Pet Med 2006;15:66-72.
4. 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(1):161-77.
5. MÃ¼ller RH, Runge S, Ravelli V, Mehnert W, ThÃ¼nemann AF, Souto EB. Oral bioavailability of cyclosporine: Solid lipid nanoparticles (SLN) versus drug nanocrystals. Int J Pharm 2006;317(1):82-9.
6. Mehnert W, MÃ¤der K. Solid lipid nanoparticles: Production, characterization and applications. Adv Drug Deliv Rev 2001;47(2â€‘3):165-96.
7. Statistical Package for the Social Sciences. Computer Software 11.00 SPSS Inc., Chicago, Ilinois-60606, USA; 1999.
8. Zhang L, Pornpattananangkul D, Hu CM, Huang CM. Development of nanoparticles for antimicrobial drug delivery. Curr Med Chem 2010;17:585-90.
9. Westesen K, Bunjes H, Koch MH. Physicochemical characterization of lipid nanoparticles and evaluation of their drug loading capacity and sustained release potential. J Control Rel 1997;48:223-31.
10. Souto EB, MÃ¼ller RH. Lipid nanoparticles: Effect on bioavailability and pharmacokinetic changes. Handb Exp Pharmacol 2010;115-41.
11. Bunjes H, Westesen K, Koch MH. Crystallization tendency and polymorphic transitions in triglyceride nanoparticles. Int J Pharm 1996;129:159-65.12. Lippacher A, MÃ¼ller RH, MÃ¤der K. Semisolid SLN dispersions for topical application: Influence of formulation and production parameters on viscoelastic properties. Eur J Pharm Biopharm 2002;53(2):155-60.
13. DeMerlis CC, Schoneker DR. Review of the oral toxicity of polyvinyl alcohol (PVA). Food Chem Toxicol 2003;41:319-24.
14. Schwarz C, Mehnert W, Muller R. Influence of production parameters of solid lipid nanoparticles (SLN) on the suitability for intravenous injection. Eur J Pharm Biopharm 1994;40:24-31.
15. Jensen LB, Magnussson E, Gunnarsson L, Vermehren C, Nielsen HM, Petersson K. Corticosteroid solubility and lipid polarity control release from solid lipid nanoparticles. Int J Pharm 2010;390(1):53-60.
16. Olbrich C, Kayser O, MÃ¼ller RH. Lipase degradation of Dynasan 114 and 116 solid lipid nanoparticles (SLN) â€“ Effect of surfactants, storage time and crystallinity. Int J Pharm 2002;237(1-2):119-28.
17. Anton N, Benoit JP, Saulnier P. Design and production of nanoparticles formulated from nano-emulsion templates-a review. J Control Release 2008;128(3):185-99.
18. Schwarz C, Mehnert W. Solid lipid nanoparticles (SLN) for controlled drug delivery. II. Drug incorporation and physicochemical characterization. J Microencapsul 1999;16(2):205-13.
19. Zimmermann E, MÃ¼ller RH, MÃ¤der K. Influence of different parameters on reconstitution of lyophilized SLN. Int J Pharm 2000;196(2):211-3.
20. Srinivas C, Sagar SV. Eenhancing the bioavailability of simvastatin using microemulsion drug delivery system. Asian J Pharm Clin Res 2012;5:132-9.
21. SchÃ¤fer-Korting M, Mehnert W, Korting HC. Lipid nanoparticles for improved topical application of drugs for skin diseases. Adv Drug Deliv Rev 2007;59(6):427-43.
22. Bunjes H, Koch MH, Westesen K. Effect of surfactants on the crystallization and polymorphism of lipid nanoparticles. Prog Colloid Polym Sci 2002;121:7-12.
23. Xie S, Zhu L, Dong Z, Wang X, Wang Y, Li X, et al. Preparation, characterization and pharmacokinetics of enrofloxacin-loaded solid lipid nanoparticles: Influences of fatty acids. Colloids Surf B Biointerfaces 2011;83(2):382-7.
24. Jenning V, Gysler A, SchÃ¤fer-Korting M, Gohla SH. Vitamin A loaded solid lipid nanoparticles for topical use: Occlusive properties and drug targeting to the upper skin. Eur J Pharm Biopharm 2000;49:211-21.
25. Sadiq AA, Rassol AA. A formulation and evaluation of silibininloaded solid lipid nanoparticles for peroral use targeting lower part of gastrointestinal tract. Int J Pharm Pharm Sci 2014;1:55-67.
26. Ji J, Hao S, Wu D, Huang R, Xu Y. Preparation, characterization and in vitro release of chitosan nanoparticles loaded with gentamicin and salicylic acid. Carbohydr Polym 2011;85:803-8.
27. Xie S, Zhu L, Dong Z, Wang Y, Wang X, Zhou W. Preparation and evaluation of ofloxacin-loaded palmitic acid solid lipid nanoparticles. Int J Nanomedicine 2011;6:547-55.
28. Pavia D, Lampman G, Kriz G. Introduction to Spectyroscopy. 6th ed. Belmont, California, USA: Brooks/Cole Pub Co.; 2000. p. 172.
The publication is licensed under CC By and is open access. Copyright is with author and allowed to retain publishing rights without restrictions.