ETORICOXIB-LOADED SOLID LIPID NANOPARTICLE DOSAGE FORM: FORMULATION, OPTIMIZATION, CHARACTERIZATION, STABILITY STUDYAND IN-VITRO IN-VIVO EVALUATION
Keywords:
Etoricoxib, Pluronic F-68, Solid lipid nanoparticles, Surface response methodologyAbstract
Objective: The aim of present research work is to increase the bioavailability of poorly water soluble drug etoricoxib by developing solid lipid nanoparticle (SLN). Due to their unique size dependent properties, lipid nanoparticles offer the possibility to develop new therapeutics and enhance the bioavailability.
Methods: An aqueous-based etoricoxib loaded solid lipid nanoparticles were prepared by hot and high speed homogenization technique, using different ratio of stearic acid and tripalmitin as lipid and different amount of pluronic F-68 as emulsifier. Optimization was done by surface response methodology (SRM) technique. The formulations are charecterised by drug content, drug entrapment efficiency, particle size and zea potential determination, SEM etc and evaluated by pharmacokinetic, pharmacodynamic and stability study.
Results: Particle size distribution, entrapment efficiency and drug release were found 499.20 nm, 72% and 98.36% simultaneously, for selected optimized formulations. Zeta potential and span of optimized formulation found to be within the range of+34.2±0.9 and 0.29. in-vivo studies shows that pain reaction time (PRT) has increased from 6.2±0.42 to 8.45±0.19 second. Pharmacokinetic study shows an increasing remarkable result for Cmax which one is increased from 6274.290 μg ml−1 h to 8558.134 μg ml−1 h when compared with the standard formulation and for AUC it has been observed from 94202.963 mg. h. l-1 to 124310.201 mg. h. l-1
Conclusion: Development of SLN formulations could be a better approach to increase the bioavailability of poorly water soluble drug like etoricoxib.
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Saeed Moharrer, Behroz Mohammadi, Reza Azizi Gharamohamaddi, Mehdi Yargoli. Biological synthesis of sliver nanoparticles by aspergillus flavus isolated from soil ahar copper mine. Indian J Sci Technol 2012;5(3):2443.
Deene Manikprabhu, K Lingappa. Microwave assisted rapid and green synthesis of silver nanoparticles using a pigment produced by Streptomyces coelicolor klmp33. Bioinorg Chem Appl 2013. Available from: URL http://dx.doi.org/10.1155/2013/341798. [Last accessed on 10 Oct 2014].
Ankit K, Kumar SP, Arunabha B. Microencapsulation as a novel drug delivery system. Int Pharm Sci 2011;1(1):1-7.
Velasco M, Ford JL, Rowe P, Rajabi-Siahboomi AR. Influence of drug: hydroxypropyl methylcellulose ratio, drug and polymer particle size and compression force on the release of diclofenac sodium from HPMC matrices. J Controlled Release 1999;57:75–85.
Higuchi T. Mechanism of sustained action medication, theoretical analysis of rate of release of solid drugs dispersed in solid matrices: J Pharm Sci 1963;52:1145-9.
Martins S, Tho I, Ferreira D, Souto E, Brandl M. Multivariance design for the evaluation of lipid and surfactant composition effect for optimization of lipid nanoparticles. Eur J Pharm Sci 20i2;45:613-23.
Das S, Kong W, Tan R. Are nanostructured lipid carriers (NLCs) better than solid lipid nanoparticles ((SLNs): development, characterization and comparative evaluations of clotramazole loaded SLNs and NLCs. Eur J Pharm Sci 2013;47:139-51.
Kheradmandinia S, Vasheg-Farahani E, Nostrati, MAtyabi F. Preparation and characterization of ketoprofen-loaded solid lipid nanoparticles made from beeswax and carnauba wax. J Nanomed 2010;6:753-9.
Zhang Q, Jiang X, Jiang W, Su L, Shi Z. Preparation of nimodipine loaded microemulsion for intestinal delivery and evaluation on the targeting efficiency to braim. Int J Pharm 2004;275:85-96.
Veerawat Teeranachaideekul, Rainer H Müller. Encapsulation of ascorbyl palmitate in nanostructured lipid carriers (NLC)-Effects of formulation parameters on physicochemical stability. Int J Pharm 2007;340:198–206.
Spiclin P, Gasperlin M, Kmetec V. Stability of ascorbyl palmitate in topical microemulsions. Int J Pharm 2001;222:271–9.
Rachmat Mauludin, Rainer H Müller. Physicochemical properties of hesperidin nanocrystal. Int J Pharm Pharm Sci 2013;5(Suppl 3):954-60.
Lewis GA, Mathieu D, Phan-Tan-Luu R. Pharmaceutical experimental design. New York, NY: Marcel Dekker; 1999.
Singh B, Ahuja N. Book review on pharmaceutical experimental design. Int J Pharm 2000;195:247-8.
Pan Y. Relationship between drug effects and particle size of insulin loaded bio adhesive microspheres. Acta Pharmacol Sin 2002;23(11):1051-6.
Rakesh P Patel, Grishma Patel, Ashok Baria. Formulation and evaluation of transdermal patch of aceclofenac. Int J Drug Delivery 2009;1:41-51.
Kunal N Patel, Hetal K Patel, Vishnu A Patel. Formulation and evaluation of drug in adhesive transdermal patches of Diclofenacacid. Int J Pharm Pharm Sci 2012;4(1):296-9.
Venter JP, Müller DG, du Plessis J, Goosen C. A comparative study of an in situ adapted diffusion cell and an in vitro Franz diffusion cell method for transdermal absorption of doxylamine. Eur J Pharm Sci 2001;13:169-77.