DEVELOPMENT AND EVALUATION OF TIZANIDINE HYDROCHLORIDE LOADED SOLID LIPID NANOPARTICLES
Objectives: The primary objective of the present study is to develop and evaluate tizanidine hydrochloride (TZ) solid lipid nanoparticles (SLNs) using solid lipids/triglycerides.
Methods: TZ SLNs were prepared by hot homogenization followed by ultrasonication technique. The prepared SLNs were characterized for drug content, entrapment and loading efficiency, particle size, zeta potential, polydispersity index (PDI), and in intro release kinetics.
Results: TZ SLNs were prepared. The particle size ranged from 49.7 to 523.7 nm. PDI of all formulations was good within the range of 0.189–0.487. The zeta potential of blank SLNs was −15.2 mV whereas drug-loaded SLNs showed zeta potential from −8.85 mV to −42.0 mV. Entrapment efficiency observed was in the range of 34.5–75.0%. The cumulative percentage release of TZ from different TZ nanoparticles varied from 35.28% to 83.98% depending on the drug-lipid ratio and the type of lipid and surfactant used. The release kinetic studies of optimized formulation showed that the release was first order and the release mechanism was non-Fickian type.
Conclusion: The prepared SLNs were able to sustain the drug release for 24 h, thus reducing dosing frequency and occurrence of side effects, thereby increasing the effectiveness of the drug.
2. Kushwaha AK, Vuddanda PR, Karunanidhi P, Singh SK, Singh S. Development and evaluation of solid lipid nanoparticles of raloxifene hydrochloride for enhanced bioavailability. Biomed Res Int 2013;2013:584549.
3. Madan JR, Khude PA, Dua K. Development and evaluation of solid lipid nanoparticles of mometasone furoate for topical delivery. Int J Pharm Investig 2014;4:60-4.
4. Goldspink G, Williams PE. Muscle fiber and connective tissue changes associated with use and disuse. In: Ada A, Canning C, editors. Foundations for Practice. Topics in Neurological Physiotherapy. London: Heinemann; 1992. p. 197-218.
5. Available from: https://www.drugbank.ca/salts/DBSALT000550. [Last accessed on 2019 Apr 12].
6. Gupta R, Bajpai M. Preparation and physicochemical characterization of tizanidine hydrochloride nanoparticles. J Pharm Res 2013;12:15-22.
7. Shakir BS, Manikanta S, Jahnavi T. UV Spectrophotometric determination of rupatadine fumarate in bulk and tablet dosage form by using single-point standardization method. Int J Pharm Pharm Sci 2019;11:120-4.
8. Priyanka S, Shailendra KL. Modified kondagogu gum as matrix-forming material for sustained-release. Int J Curr Pharm Res 2016;8:82-7.
9. Wissing SA, Kayser O, Müller RH. Solid lipid nanoparticles for parenteral drug delivery. Adv Drug Deliv Rev 2004;56:1257-72.
10. Nair R, Kumar AC, Priya VK, Yadav CM, Raju PY. Formulation and evaluation of chitosan solid lipid nanoparticles of carbamazepine. Lipids Health Dis 2012;11:72.
11. Gouda R, Baishya H, Qing Z. Application of mathematical models in drug release kinetics of carbidopa and levodopa ER tablets. J Dev Drugs 2017;6:1-8.
12. Cirri M, Maestrini L, Maestrelli F, Mennini N, Mura P, Ghelardini C, et al. Design, characterization and in vivo evaluation of nanostructured lipid carriers (NLC) as a new drug delivery system for hydrochlorothiazide oral administration in pediatric therapy. Drug Deliv 2018;25:1910-21.
13. Rakesh KS, Navneet S, Sudha R, Hosakote GS. Solid lipid nanoparticles as a carrier of metformin for transdermal delivery. Int J Drug Del 2013;5:137-45.
14. Ahmed G, Samar F, Samar S. Design optimization and in vitro evaluation of antifungal activity of nanostructured lipid carriers of tolnaftate. Int J Pharm Pharm Sci 2019;11:109-15.
15. Moawad FA, Ali AA, Salem HF. Nanotransfersomes-loaded thermosensitive in situ gel as a rectal delivery system of tizanidine HCl: Preparation, in vitro and in vivo performance. Drug Deliv 2017;24:252-60.
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