ABSTRACT:
Felbamate is a PEGylated phenylcarbamate derivative that acts as an antagonist of NMDA receptors. It is used as an anticonvulsant, primarily for the treatment of seizures in severe refractory epilepsy. It is slightly soluble in water with t 1/2 of 4-6 hours. Felbamate loaded solid lipid nanoparticles (SLN) have been developed using placket and burman design of experiments. SLN’s were prepared by microemulsion technique. Based on preliminary experiments and on literature, the influence of independent variable parameters selected were lipid (X1), surfactant (X2), and co-surfactant concentration (X3), aqueous phase volume (X4),magnetic stirrer rate (X5), probe sonication duration (X6), volume of beaker used for sonication (X7), volume of cold aqueous phase (X8) on the dependent variable such as particle surface area (Y1) was studied. Other parameters, i.e., magnetic stirrer rate and probe sonication duration were not having a significant impact on particle size and their levels were kept constant for all the experiments. Magnetic stirrer rate has an impact on particle size and was included in the design. It was concluded from the study that the composition prepared with lipid concentration of 50mg, surfactant concentration of 75mg, Co-surfactant concentration of 0.75ml, aqueous phase volume of 5ml, magnetic stirring speed of 400rpm, probe sonication duration 30 minutes, volume of beaker used for sonication 500ml and volume of cold aqueous phase 30ml has shown the highest surface area of 51.9m2g-1.
Cite this article:
Ramanuj Prasad Samal, Pratap Kumar Sahu. Formulation Development and In vitro Characterization of solid lipid Nanoparticles of Felbamate. Research J. Pharm. and Tech 2020; 13(9):4185-4189. doi: 10.5958/0974-360X.2020.00739.8
Cite(Electronic):
Ramanuj Prasad Samal, Pratap Kumar Sahu. Formulation Development and In vitro Characterization of solid lipid Nanoparticles of Felbamate. Research J. Pharm. and Tech 2020; 13(9):4185-4189. doi: 10.5958/0974-360X.2020.00739.8 Available on: https://www.rjptonline.org/AbstractView.aspx?PID=2020-13-9-27
REFERENCES:
1. Ilangaratne, NB, Mannakkara NN, BellGS, Sander JW. Phenobarbital: missing in action. Bulletin on World Health Organization 2012; 90(12): 871-871a.
2. De RG, Salzano G, Caraglia M, Abbruzzese A. Nanotechnologies: A Strategy to Overcome Blood-Brain Barrier. Current Drug Metabolism 2012; 13(1): 61-69.
3. BauerB, Schlichtiger J, Pekcec A. In Clinical and Genetic Aspects of Epilepsy. Afawi, Z., Ed.; Intech, 2011.
4. LoscherW, Potschka H. Drug resistance in brain diseases and the role of drug efflux transporters. Natural review on Neuroscince 2005; 6(8):591-602.
5. Pati S, Alexopoulos AV. Pharmacoresistant epilepsy: From pathogenesis to current and emerging therapies. Cleveland Clinical Journal of Medicine 2010; 77(7):457-467.
6. Benbadis SR, Tatum WOT. Advances in the treatment of epilepsy. American family Physician 2001; 64(1): 91-98.
7. Rossi MA. Targeting anti-epileptic drug therapy without collateral damage: nanocarrier-based drug delivery. Epilepsy Currents 2012; 12(5):199-200.
8. Iqbal A, AhmadI, Khalid MH, Nawaz MS, Gan SH, Kamal MA. Nanoneurotoxicity to nanoneuroprotection using biological and computational approaches. Journal of Environmental Science and Health Part C Environmental Carcinogenesis 2013; 31(3): 256-284.
9. Alam Q, Haque A, Alam MZ, Karim S, Kamal MA, JimanFatani A, Damanhouri GA, Abuzenadah AM, Chaudhary AG. Nanotechnological Approach in Management of Alzheimer's Diseases and Type- 2 Diabetes. CNS and Neurological DisordersandDrug Targets 2013.
10. Wong HL, Wu XY, Bendayan R. Nanotechnological advances for the delivery of CNS therapeutics. Advances in Drug Delivery Review 2012; 64(7):686-700.
11. Modi G, PillayV, ChoonaraYE, Ndesendo VMK, du ToitLC, NaidooD. Nanotechnological applications for the treatment of neurodegenerative disorders. Progress in Neurobiology 2009; 88(4): 272-285.
12. Thorne RG, NicholsonC. In vivo diffusion analysis with quantum dots and dextrans predicts the width of brain extracellular space. PNAS 2006; 103(14): 5567-5572.
13. Lockman PR, Koziara JM, Mumper RJ, Allen DD. Nanoparticle surface charges alter blood-brain barrier integrity and permeability. Journal of Drug Targeting 2004; 12(9-10): 635-641.
14. Xiao K, Li Y, Luo J, Lee JS, Xiao W, Gonik AM, Agarwal RG, Lam KS. The effect of surface charge on in vivo biodistribution of PEG-oligocholic acid based micellar nanoparticles. Biomaterials2011; 32(13): 3435-3446.
15. Bhaskar S, Tian F, Stoeger T, Kreyling W, de la Fuente JM, Grazu V, Borm P, Estrada G, NtziachristosV, Razansky D. Multifunctional Nanocarriers for diagnostics, drug delivery and targeted treatment across blood-brain barrier: perspectives on tracking and neuroimaging. Particles and Fibre Toxicology 2010; 7.
16. Jabir NR, Tabrez S, Ashraf GM, Shakil S, Damanhouri GA, Kamal MA. Nanotechnology-based approaches in anticancer research. International Journal of Nanomedicine 2012; 7:4391-4408.
17. Uner M, YenerG. Importance of solid lipid nanoparticles (SLN) in various administration routes and future perspectives. International Journal of Nanomedicine 2007; 2(3):289-300.
18. WissingSA, KayserO, Muller RH. Solid lipid nanoparticles for parenteral drug delivery. Advances in drug delivery review 2004;56(9): 1257-1272.
19. Pandey R, KhullerGK. Solid lipid particle-based inhalable sustained drug delivery system against experimental tuberculosis. Tuberculosis (Edinb) 2005; 85(4): 227-234
20. Burdette David E, Sackellares J Chris. Felbamate Pharmacology and Use in Epilepsy, Clinical Neuropharmacology 1994; 17(5):389-402.
21. Vicki C, WilliamsA. Selective antagonism of the anticonvulsant effects of felbamate by glycine. European Journal of Pharmacology 1994; 256(2): R9-R10.
22. Giovambattista DS, Ennio O, Rosalia B, Umberto A, Angela DS. Excitatory amino acid neurotransmission through both NMDA and non-NMDA receptors is involved in the anticonvulsant activity of felbamate in DBA/2 mice. European Journal of Pharmacology 1994; 262(1-2): 11-19.
23. Nancy WK, Jill CG, Chi CC, Tammy DM. Subtype-Selective Antagonism of N-Methyl-D-Aspartate Receptors by Felbamate: Insights into the Mechanism of Action. Journal of Pharmacology and Experimental Therapeutics 1999; 289 (2): 886-894.
24. Ticku MK, Kamatchi GL, Sofia RD. Effect of Anticonvulsant Felbamate on GABAA Receptor System. Epilepsia1991; 32: 389–391.
25. Swinyard EA, Sofia RD, Kupferberg HJ. Comparative Anticonvulsant Activity and Neurotoxicity of Felbamate and Four Prototype Antiepileptic Drugs in Mice and Rats. Epilepsia 1986; 27: 27–34