Research PaperNo Access

Factorial Design-Based Nanocarrier Mediated Formulation of Efavirenz and Its Characterization

Department of Pharmaceutical Engineering and Technology, Indian Institute of Technology (Banaras Hindu University), Varanasi 221005, Uttar Pradesh, India

E-mail Address: rchawla.phe@iitbhu.ac.in

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Venkatanaidu Karri

Department of Pharmaceutical Engineering and Technology, Indian Institute of Technology (Banaras Hindu University), Varanasi 221005, Uttar Pradesh, India

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Varsha Rani

Department of Pharmaceutical Engineering and Technology, Indian Institute of Technology (Banaras Hindu University), Varanasi 221005, Uttar Pradesh, India

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Mohini Mishra

Department of Pharmaceutical Engineering and Technology, Indian Institute of Technology (Banaras Hindu University), Varanasi 221005, Uttar Pradesh, India

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, and

Krishan Kumar

Department of Pharmaceutical Engineering and Technology, Indian Institute of Technology (Banaras Hindu University), Varanasi 221005, Uttar Pradesh, India

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https://doi.org/10.1142/S1793984422500027Cited by:1 (Source: Crossref)

Abstract

Efavirenz (EFV) suffers from poor aqueous solubility which results in low bioavailability of the drug. Nanocarrier-based drug delivery systems offer a suitable alternative for improving the physico-chemical properties of the drug and hence its efficacy. Nanosuspension (NS) of EFV was formulated by solvent-anti solvent precipitation method using PVP K-30 as stabilizer and sodium lauryl sulphate (SLS) as the wetting agent. Multi-level factorial design was applied to select the optimal formulation which was further characterized. The optimal batch exhibited mean particle size of 305nm and polydispersity index (PDI) of 0.345. Solid-state characterization studies of the NS conducted using scanning electron microscopy, Fourier transform infrared spectroscopy (FTIR), X-ray powder diffraction, and differential scanning calorimetry (DSC) revealed compatibility between the drug and the excipients and modest alteration in the crystallinity of the drug. There was progressive increase in the solubility of the drug when incorporated in NS from 17.39 $μ$ g/ml to 256 $μ$ g/ml. Further, drug release studies showed significantly better and controlled drug release pattern in comparison to the free drug due to the presence of nanosized particles in the formulation.

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References

1. B. V. Hari, N. Narayanan, K. Dhevendaran and D. Ramyadevi, Mater. Sci. Eng. C 67, 522 (2016). Crossref, Google Scholar
2. C. R. Hoffmeister, C. Fandaruff, M. A. da Costa, L. M. Cabral, L. R. Pitta, S. E. Bilatto, L. D. Prado, D. S. Corrêa, L. Tasso, M. A. Silva and H. V. Rocha, Eur. J. Pharm. Sci. 99, 310 (2017). Crossref, Google Scholar
3. P. Sharma and S. Garg, Adv. Drug Deliv. Rev. 62, 491 (2010). Crossref, Google Scholar
4. U. Gupta and N. K. Jain, Adv. Drug Deliv. Rev. 62, 478 (2010). Crossref, Google Scholar
5. S. Taneja and K. Khatri, Pharm. Nanotechnol. 1, 259 (2013). Crossref, Google Scholar
6. K. P. Chowdary and G. S. Devi, Int. J. Res. Pharm. Chem. 2, 311 (2012). Google Scholar
7. T. Dutta, M. Garg and N. K. Jain, Eur. J. Pharm. Sci. 34, 181 (2008). Crossref, Google Scholar
8. C. J. Destache, T. Belgum, K. Christensen, A. Shibata, A. Sharma and, A. Dash, BMC Infect. Dis. 9, 198 (2009). Crossref, Google Scholar
9. V. R. Patel and Y. K. Agrawal, J. Adv. Pharm. Technol. Res. 2, 81 (2011). Crossref, Google Scholar
10. R. L. Carrier, L. A. Miller and I. Ahmed, J. Control Release 123, 78 (2007). Crossref, Google Scholar
11. C. M. Keck and R. H. Müller, Eur. J. Pharm. Biopharm. 62, 3 (2006). Crossref, Google Scholar
12. B. van Eerdenbrugh, G. van den Mooter and P. Augustijns, Int. J. Pharm. 364, 64 (2008). Crossref, Google Scholar
13. E. Reverchon, J. Supercrit. Fluids 15, 1 (1999). Crossref, Google Scholar
14. P. Pathak, M. J. Meziani, T. Desai and Y. P. Sun, J. Supercrit. Fluids 37, 279 (2006). Crossref, Google Scholar
15. B. van Eerdenbrugh, B. Stuyven, L. Froyen, J. van Humbeeck, J. A. Martens, P. Augustijns and G. van den Mooter, AAPSPharmSciTech. 10, 44 (2009). Google Scholar
16. H. Zhao, J. X. Wang, Q. A. Wang, J. F. Chen and J. Yun, Ind. Eng. Chem. Res. 46, 8229 (2007). Crossref, Google Scholar
17. L. Gao, D. Zhang and M. Chen, J. Nanopart. Res. 10, 845 (2008). Crossref, Google Scholar
18. Y. Zhang and J. Zhang, Artif. Cells Nanomed. Biotechnol. 44, 285 (2016). Crossref, Google Scholar
19. H. Kathpalia, S. Juvekar and S. Shidhaye, Colloids Interface Sci. Commun. 29, 26 (2019). Crossref, Google Scholar
20. L. H. Reddy and R. S. R. Murthy, AAPSPharmSciTech. 6, E158 (2005). Google Scholar
21. M. K. Rawat, A. Jain, A. Mishra, M. S. Muthu and S. Singh, Ther. Deliv. 1, 63 (2010). Crossref, Google Scholar
22. E. G. Mira, M. A. Egea, E. B. Souto and M. L. Garcia, Nanotechnology 22, 045101 (2011), Available at: https://pubmed.ncbi.nlm.nih.gov/21169662/. Crossref, Google Scholar
23. D. K. Koradai and H. R. Parikh, J. Pharm. Bioall. Sci. 4, 62 (2012), doi: 10.4103/0975-7406.94141. Crossref, Google Scholar
24. X. Teng and H. Yang, J. Mater. Chem. 14, 774 (2004). Crossref, Google Scholar
25. V. Kanchan and A. K. Panda, Biomaterials 28, 5344 (2007). Crossref, Google Scholar
26. M. Z. Uddin, J. A. Chowdhury, I. Hasan and M. S. Reza, Dhaka Univ. J. Pharm. Sci. 15, 195 (2016). Crossref, Google Scholar
27. M. W. Park and S. D. Yeo, Chem. Eng. Res. Des. 90, 2202 (2012). Crossref, Google Scholar
28. S. Ubgade, A. Bapat and V. Kilor, J. Appl. Pharm. Sci. 11, 85 (2021). Google Scholar
29. N. Soltani et al., Int. J. Mol. Sci. 13, 12412 (2012). Available at: /pmc/articles/PMC3497280/. Crossref, Google Scholar
30. C. Sharma, M. A. Desai and S. R. Patel, Chem. Pap. 73, 1685 (2019). Crossref, Google Scholar
31. R. Yadollahi, K. Vasilev, C. A. Prestidge and S. Simovic, J. Nanomater. 2013, 170201 (2013). Crossref, Google Scholar
32. M. A. Jordaan and M. Shapi, Antivir. Chem. Chemother. 25, 94 (2017). Available at: https://pubmed.ncbi.nlm.nih.gov/28893089/. Crossref, Google Scholar
33. A. D. Panikumar, R. Y. Venkat, G. Sunitha, B. P. Sathesh and C. V. S. Subrahmanyam, Asian J. Pharm. Clin. Res. 5, 220 (2012). Google Scholar