FORMULATION AND EVALUATION OF IBRUTINIB NANOSPONGES INCOPORATED TABLET
Keywords:Ibrutinib, Nanosponges, Anti-cancer agents, Polaxamer 188, Eudragit RL 30 D
Objective: The present investigation was undertaken to prepare polymeric nanosponges of an anti-cancer drug ibrutinib to achieve controlled and improved drug release.
Methods: Nanosponges using a polymer (ethyl cellulose, poloxamer 188 and eudragit RL 30 D) and polyvinyl alcohol as a cross-linker were prepared successfully by the emulsion solvent evaporation method. Prepared nanosponges were evaluated for particle size, zetapotential, entrapment efficiency and in-vitro drug release. Nanosponges with good drug release were formulated into tablets and evaluated for miromeritic properties, post compression parametrs and in-vitro release and final optimised formulation was characterised for globule size, zetapotential, FTIR, SEM and stability studies.
Results: The nanosponges' particle sizes were discovered to range between 86.31 nm and 162.4 nm, the Zeta Potential ranges from -22.1 to -29. It was discovered that the drug entrapment efficiency ranged from 92.21 to 99.23% and Formulation F18 exhibited the highest drug release rate of 99.73% in 12h and was discovered to demonstrate good, satisfying results. The tablet formulation's micromeritic and post compression parameters were examined, and it was discovered that F18 had good flow qualities. F18 had a mean globule size of 133.6 nm, a zeta potential of -22.1 mV, and SEM images revealed a sphere-like structure. The complexation of ibrutinib and the amorphous condition of the medication and formulation were confirmed by the FT-IR, and stability investigations to be stable for three months.
Conclusion: Hence, Ibrutinib loading into nanosponges made using the emulsion solvent evaporation process thus successfully boosted and controlled the drug release.
Gedam SS and Basarkar GD: Nanosponges: An attractive strategy for enhanced therapeutic profile. J Pharm Sci & Res 2019; 11(6): 2479-87.
Kaur, Simranjot & Kumar, Sandeep. The Nanosponges: An Innovative Drug Delivery System. Asian Journal of Pharmaceutical and Clinical Research. 2019, 60-67.
S.C.B. Penjuri, N. Ravouru, S. Damineni, S. Bns, S.R. Poreddy, Formulation and evaluation of lansoprazole loaded nanosponges, Turk J Pharm Sci 2016, 13 (3) 304–310,
Bhowmik, Himangshu & Venkatesh, D. & Kuila, Anuttam & Kumar, Kammari. Nanosponges: A review. International Journal of Applied Pharmaceutics, 2018 10. 1. 10.
P. Jyoti, B. Tulsi, K. Popin, B. Chetna, An innovative advancement for targeted drug delivery: Nanosponges, Indo Global J. Pharmaceut. Sci. 2016, 6 (2) 59–64.
Amin A, Ranjana HA. Bruton’s tyrosine kinase inhibitors and their clinical potential in the treatment of B-cell malignancies: focus on ibrutinib. TherAdvHematol. August 2014; 5(4): 121–133.
El-Assal, Mona. Nano-Sponge Novel Drug Delivery System as Carrier of Anti-Hypertensive Drug. International Journal of Pharmacy and Pharmaceutical Sciences. 2019, 47-63.
David MS, Brown JR. Ibrutinib: a first in class covalent inhibitor of Bruton’s tyrosine kinase. Future Oncol. May 2014; 10(6): 957–967.
Honigberg LA, Smith AM, Sirisawad M, Verner E, Loury D, Chang B, et al. The Bruton tyrosine kinase inhibitor PCI-32765 blocks B-cell activation and is efficacious in models of autoimmune disease and B-cell malignancy. Proc Natl Acad Sci. 2010;107(29):13075–80.
Kassem, M. A., Abdallah, F. I., & Elsherif, Y. A. Design, Evaluation and bioavailability of oxybutynin chloride nanosponges on healthy human volunteers. Journal of Drug Delivery Science and Technology, 2020, 101943
Solunke, Rahul & Borge, Uday & Murthy, Krishna & Deshmukh, Madhuri & Shete, Rajkumar. Formulation and evaluation of gliclazide nanosponges. International Journal of Applied Pharmaceutics. 2019, 11. 181-189.
Swaminathan S, Vavia PR, Trotta F, Torne S. Formulation of Βcyclodextrin based nanosponges of itraconazole. J Incl Phenom Macrocycl Chem 2007; 57:89–94. 11.
Arvapally S, Harini M, Harshitha G, Arun Kumar A. Formulation and in vitro evaluation of glipizide nanosponges. Am J Pharmtech Res 2017;7:341-61.
Rangaraj, N., Pailla, S.R., Chowta, P. et al. Fabrication of Ibrutinib Nanosuspension by Quality by Design Approach: Intended for Enhanced Oral Bioavailability and Diminished Fast Fed Variability. AAPS PharmSciTech 2019 20, 326.
Remya PN, Saraswathi TS, Sangeetha S and Damodharan NK: Formulation and Evaluation of Immediate Release Tablets of Acyclovir. Journal of Pharmaceutical Sciences and Research 2016; 8(11): 1258-61.
Alburyhi M, Alwan M and Aboghanem A: Effect of different excipients on formulation of immediate-release Artemether/Lumefantrine tablets. Journal of Chem and Pharma Res 2013; 5(11): 617-25.
Chime SA, Brown S and Ugwu: Effect of binder type and concentrationon the in-vitro properties of Alstonia boonei Int J Pharm Sci Rev Res 2012; 2(2): 5-9.
Dubey P, Sharma HK, Shah S, Tyagi CK, Chandekar A. Jadon SR. Formulation and evaluation of cyclodextrin complexed ceadroxil loaded nanosponges. Int J Drug Delivery 2017; 9:84-100.
ICH, Q1A, (R2) Stability testing guidelines: stability of new drug substances and product: methodology in processing of ICH Geneva; 2003.
Chen Z, Zhai J, Liu X, Mao S, Zhang L, Rohani S, et al. Solubility measurement and correlation of the form an of ibrutinib in organic solvents from 278.15 to 323.15 K. J ChemThermodyn. 2016; 103:342–8.
Vamshi Priya V, Rao GC, Reddy DS and Reddy VP: The Effect of different superdisintegrants and their concentrations on the dissolution of topiramate. Immediate Release Tablets 2009; 2(2): 531-36.
Mamatha Palanati, Jarpula Arun Kumar1, D. V. R. N. Bhikshapathi, Design And Optimization Of Ibrutinib Solid Lipid Nanoparticles Using Design Of Experiment, IJBPAS, September, Special Issue, 2021, 10(9): 723-737
Atram SC: Formulation and evaluation of immediate release tablet using response surface methodology. Asian Journal of Pharmaceutics 2011; 46-51.
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