Rapid releasing naproxen Liqui-Pellet using effervescent agent and neusilin US2

Document Type : Original Article

Authors

1 Pharmaceutics Research Laboratory, Arundel Building, School of Life Sciences, University of Sussex, Brighton, UK

2 Department of Pharmacy, University of Huddersfield, Huddersfield, HD1 3DH, UK

Abstract

Objective(s): Liqui-Mass technology has shown promising advantages in terms of commercial production and formulation manipulation. This study attempts to further explore the potential of enhanced drug release of effervescent Liqui-Pellet by optimizing certain parameters.
Materials and Methods: In the current study, pellets containing co-solvent, naproxen, coating and carrier materials were prepared via extrusion and spheronisation (Liqui-Pellet). Parameters investigated included polysorbate 80 concentration (as a co-solvent), water content and the presence or absence of neusilin US2 as part of the new binary carrier mixture approach.
Results: It was found that the success of the Liqui-Pellet production was determined by the amount of polysorbate 80 and water used, where above a certain limit, agglomeration occurred, and the formulation failed. Liqui-Pellet formulation showed an excellent flow, narrow size distribution and was robust to pass friability testing. The key findings in the investigation were that the Liqui-Pellet was capable of a remarkably fast drug release, and 100% drug release achieved within 20 min at pH 1.2, wherein naproxen has been known to be practically insoluble in such pH.
Conclusion: Liqui-Pellets display the potential to enhance explosive dissolution where a combination of effervescent powders and binary carriers with the high surface area were used. Furthermore, X-ray microtomography revealed that the pellets were very uniform and homogenous.

Keywords

References

1. Lam M, Ghafourian T, Nokhodchi A. Liqui-pellet: the emerging next-generation oral dosage form which stems from liquisolid concept in combination with pelletization technology. AAPS Pharmscitech 2019; 20:231-246.
2. Lam M, Ghafourian T, Nokhodchi A. Optimising the release rate of naproxen liqui-pellet: a new technology for emerging novel oral dosage form. Drug Del Trans Res 2020;10:43-58.
3. Lam M. The making of liqui-pellet and liqui-tablet, the next generation oral dosage form, Unpublished PhD thesis, University of Sussex, Brighton, UK 2018.
4. Lam M, Nokhodchi A. International PCT patent GB2019/052065 2019.
5. Lam M, Ghafourian T, Nokhodchi A. Liquisolid system and liqui-mass system are not the same. AAPS PharmSciTech. 2020; 21:1-3.
6. Pezzini BR, Beringhs AO, Ferraz HG, Silva MA, Stulzer HK, Sonaglio D. Liquisolid technology applied to pellets: evaluation of the feasibility and dissolution performance using felodipine as a model drug. Chem Engin Res Design 2016; 110:62-69.  
7. Lam M, Commandeur D, Maniruzzaman M, Tan DK, Nokhodchi A. The crucial effect of water and co-solvent on Liqui-Pellet pharmaceutical performance. Adv Pow Technol. 2020; 31:1903-1924.
8. Spireas S, Bolton SM. Liquisolid systems and methods of preparing same. United States patent US 5,800,834. 1998
9. De Espíndola B,  Beringhs AO,  Sonaglio D,  Stulzer HK,  Segatto  MA, Silva MAS,  Ferraz HG, et al. Liquisolid pellets: A pharmaceutical technology strategy to improve the dissolution rate of ritonavir. Saudi Pharm J 2019; 27:702-712.
10. Pezzini BR, Beringhs AO, Ferraz HG, Silva MA, Stulzer HK, Sonaglio D. Liquisolid pellets and liqui-pellets are not different. AAPS Pharmscitech 2020; 21:72-75.
11. Rowe RC, Sheskey PJ, Quinn ME. Association, A. P. & Press, P. Handbook of Pharmaceutical Excipients, 6 (Pharmaceutical Press London, 2009).
12. Burra S, Yamsani M, Vobalaboina V. The Liquisolid technique: an overview. Brazilian J Pharm Sci 2011; 47:475-482.
13. Spireas S, Sadu S. Enhancement of prednisolone dissolution properties using liquisolid compacts. Int J Pharm 1998; 166:177-188.
14. Nokhodchi A, Hentzschel CM, Leopold CS. Drug release from liquisolid systems: speed it up, slow it down. Expert Opinion on Drug Del 2011; 8:191-205.
15. Spireas S, Sadu S, Grover R. In Vitro Release Evaluation of Hydrocortisone Liquisolid Tablets. J Pharm Sci 1998; 87:867-872.
16. Muley S, Nandgude T, Poddar S. Extrusion–spheronization a promising pelletization technique: In-depth review. Asian J Pharm Sci 2016; 11:684-99.
17. Sellassie IG. Pharmaceutical pelletization technology. Marcel Dekker Inc., New York. 1989; 37:1-2.
18. Dhandapani NV. Pelletization by Extrusion-Spheronization-A detailed review. The All Results Journals: Biol 2012; 3:10-23.
19. Vervaet C, Baert L, Remon JP. Extrusion-spheronisation A literature review. Int J Pharm 1995; 116:131-146.
20. Nakahara N. Method and Apparatus for Making Spherical Granules, Patent number US3277520A, 5–10. 1966.
21. Harrison PJ, Newton JM, Rowe RC. The characterization of wet powder masses suitable for extrusion/spheronization. J Pharm Pharmacol 1985; 37:686-691.
22. Rowe RC. Spheronization-a novel pill-making process. Pharm Int 1985; 6:119-123.
23. Bataille B, Ligarski K, Jacob N, Thohas C, Duru C. Study of the influence of spheronization and drying conditions on the physico-mechanical properties of neutral spheroids containing Avicel PH 101 and lactose. Drug Dev Ind Pharm 1993; 19:653-671.
24. Bianchini R, Vecchio C. Oral controlled release optimization of pellets prepared by extrusion-spheronization processing. Farmaco (Societa Chimica Italiana: 1989) 1989; 44:645-654.
25. Yuen KH, Deshmukh AA, Newton JM. Development and in vitro evaluation of a multiparticulate sustained release theophylline formulation. Drug Dev Ind Pharm 1993; 19:855-874.
26. Huyghebaert N, Snoeck V, Vermeire A, Cox E, Goddeeris BM, Remon JP. Development of an enteric-coated pellet formulation of F4 fimbriae for oral vaccination of suckling piglets against enterotoxigenic Escherichia coli infections. Eur J Pharm Biopharm 2005; 59:273-281.
27. Bashaiwoldu AB, Podczeck F, Newton JM. The application of non-contact laser profilometry to the determination of permanent structural change induced by compaction of pellets: II. Pellets dried by different techniques. Eur J Pharm Sci 2004; 22:55-61
28. Dyer AM, Khan KA, Aulton ME. Effect of the drying method on the mechanical and drug release properties of pellets prepared by extrusion-spheronization. Drug Dev Ind Pharm 1994; 20:3045-3068.
29. Dukić-Ott A, Remon JP, Foreman P, Vervaet C. Immediate release of poorly soluble drugs from starch-based pellets prepared via extrusion/spheronisation. Eur J Pharm Biopharm 2007; 67:715-724.
30. Chamsai B, Sriamornsak P. Novel disintegrating microcrystalline cellulose pellets with improved drug dissolution performance. Pow Technol 2013; 233:278-285.
31. Moore JW, Flanner HH. Mathematical comparison of dissolution profiles. Pharm Technol 1996; 20:64-74.
32. O’hara T, Dunne A, Butler J, Devane J, IVIVR Cooperative Working Group. A review of methods used to compare dissolution profile data. Pharm Sci Technol Today 1998; 1:214-223.
33. Costa P. An alternative method to the evaluation of similarity factor in dissolution testing. Int J Pharm 2001; 220:77-83.
34. Yuksel N, Kanık AE, Baykara T. Comparison of in vitro dissolution profiles by ANOVA-based, model-dependent and-independent methods. Int J Pharm 2000; 209:57-67.
35. Costa P, Lobo JM. Modeling and comparison of dissolution profiles. Eur J Pharm Sci 2001; 13:123-33.
36. Laity PR, Asare-Addo K, Sweeney F, Šupuk E, Conway BR. Using small-angle X-ray scattering to investigate the compaction behaviour of a granulated clay. Applied Clay Sci 2015; 108:149-164.
37. Nep EI, et al. The influence of hydroalcoholic media on the performance of Grewia polysaccharide in sustained release tablets. Int J Pharm 2017; 532:352-364.
38. Mora CP, Martínez F. Thermodynamic quantities relative to solution processes of naproxen in aqueous media at pH 1.2 and 7.4. Phys Chem Liq 2006; 44:585-596.
39. Otsuka M, Gao J, Matsuda Y. Effect of amount of added water during extrusion-spheronization process on pharmaceutical properties of granules. Drug Dev Ind Pharm 1994; 20:2977-2992.
40. Gandhi R, Kaul CL, Panchagnula R. Extrusion and spheronization in the development of oral controlled-release dosage forms. Pharm Sci Tech Today. 1999; 2:160-170.
41. Fielden KE, Newton JM, Rowe RC. The influence of moisture content on spheronization of extrudate processed by a ram extruder. Int J Pharm 1993; 97:79-92.
42. Sruti J, Patra CHN,  Swain SK,  Beg S,  Palatasingh HR,  Dinda SC, et al. Improvement in dissolution rate of cefuroxime axetil by using poloxamer 188 and Neusilin US2. Indian J Pharm Sci 2013; 75:67.
43. Tiong N, Elkordy AA. Effects of liquisolid formulations on dissolution of naproxen. Eur J Pharm Biopharm 2009; 73:373-384.
44. Adibkia K, Barzegar-Jalali M, Maheri-Esfanjani H, Ghanbarzadeh S, Shokri J, Sabzevari A, et al. Physicochemical characterization of naproxen solid dispersions prepared via spray drying technology. Pow Technol 2013; 246:448-455.
45. Baruchel J, Buffiere JY, Maire E. X-ray Tomography in Material Science. France: Hermes Science Publications 2000.
46. Stock SR. X-ray microtomography of materials. Int Mat Rev 1999; 44:141-164.
Iranian Journal of Basic Medical Sciences
Volume 24, Issue 1
January 2021
Pages 108-115

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