An Intensified Vibratory Milling Process for Enhancing the Breakage Kinetics during the Preparation of Drug Nanosuspensions

AAPS PharmSciTech

Volumn 17, Issue 2, 2016, Pages 389-399

  Li, Meng ^a   Zhang, Lu ^a   Davé, Rajesh N ^a   Bilgili, Ecevit ^a  

^a NEW JERSEY INSTITUTE OF TECHNOLOGY   (United States)

Author keywords

bioavailability enhancement; drug nanoparticles; LabRAM; process intensification; vibratory milling

Indexed keywords

GRISEOFULVIN; NANOPARTICLE; SUSPENSION; WATER;

ARTICLE; COMPARATIVE STUDY; DENSITY; DIFFERENTIAL SCANNING CALORIMETRY; DRUG SOLUBILITY; DRUG SYNTHESIS; LASER DIFFRACTION; NANOSUSPENSION; PARTICLE SIZE; PRIORITY JOURNAL; PROCESS OPTIMIZATION; REPRODUCIBILITY; SCANNING ELECTRON MICROSCOPY; SUSPENSION; VIBRATORY MILLING PROCESS; X RAY DIFFRACTION; CHEMISTRY; DRUG FORMULATION; KINETICS; PROCEDURES; SOLUBILITY;

CALORIMETRY, DIFFERENTIAL SCANNING; DRUG COMPOUNDING; GRISEOFULVIN; KINETICS; MICROSCOPY, ELECTRON, SCANNING; NANOPARTICLES; PARTICLE SIZE; SOLUBILITY; SUSPENSIONS; WATER; X-RAY DIFFRACTION;

EID: 84937138820     PISSN: None     EISSN: 15309932     Source Type: Journal    
DOI: 10.1208/s12249-015-0364-3     Document Type: Article

References (52)

1. Kipp JE. The role of solid nanoparticle technology in the parenteral delivery of poorly water-soluble drugs. Int J Pharm. 2004;284:109–22.
2. Lipinski CA. Poor aqueous solubility: an industry wide problem in drug discovery. Am Pharm Rev. 2002;5:82–5.
3. Adamson A, Gast A. Physical chemical of surfaces. New York: Wiley; 1997.
4. Singh SK, Srinivasan K, Gowthamarajan K, Singare DS, Prakash D, Gaikwad NB. Investigation of preparation parameters of nanosuspension by top-down media milling to improve the dissolution of poorly water-soluble glyburide. Eur J Pharm Biopharm. 2011;78:441–6.
5. Tanaka Y, Inkyo M, Yumoto R, Nagai J, Takano M, Nagata S. Nanoparticulation of probucol, a poorly water-soluble drug, using a novel wet-milling process to improve in vitro dissolution and in vivo oral absorption. Drug Dev Ind Pharm. 2012;38:1015–23.
6. Noyes AA, Whitney WR. The rate of solution of solid substances in their own solutions. J Am Chem Soc. 1897;19:930–4.
7. Basa S, Muniyappan T, Karatgi P, Prabhu R, Pillai R. Production and in vitro characterization of solid dosage form incorporating drug nanoparticles. Drug Dev Ind Pharm. 2008;34:1209–18.
8. Bhakay A, Davé R, Bilgili E. Recovery of BCS class II drugs during aqueous redispersion of core–shell type nanocomposite particles produced via fluidized bed coating. Powder Technol. 2013;236:221–34.
9. Bhakay A, Azad M, Vizzotti E, Dave RN, Bilgili E. Enhanced recovery and dissolution of griseofulvin nanoparticles from surfactant-free nanocomposite microparticles incorporating wet-milled swellable dispersants. Drug Dev Ind Pharm. 2014;40:1509–22.
10. Van Eerdenbrugh B, Van den Mooter G, Augustijns P. Top-down production of drug nanocrystals: nanosuspension stabilization, miniaturization and transformation into solid products. Int J Pharm. 2008;364:64–75.
11. Sievens-Figueroa L, Bhakay A, Jerez-Rozo JI, Pandya N, Romañach RJ, Michniak-Kohn B, et al. Preparation and characterization of hydroxypropyl methyl cellulose films containing stable BCS class II drug nanoparticles for pharmaceutical applications. Int J Pharm. 2012;423:496–508.
12. Cooper ER. Nanoparticles: a personal experience for formulating poorly water soluble drugs. J Control Release. 2010;141:300–2.
13. Müller RH, Gohla S, Keck CM. State of the art of nanocrystals—special features, production, nanotoxicology aspects and intracellular delivery. Eur J Pharm Biopharm. 2011;78:1–9.
14. Leleux J, Williams RO. Recent advancements in mechanical reduction methods: particulate systems. Drug Dev Ind Pharm. 2013:1–12.
15. Sun B, Yeo Y. Nanocrystals for the parenteral delivery of poorly water-soluble drugs. Curr Opin Solid St M. 2012;16:295–301.
16. Azad MA, Knieke C, To D, Davé R. Preparation of concentrated stable fenofibrate suspensions via liquid antisolvent precipitation. Drug Dev Ind Pharm. 2014;40:1693–703.
17. Duarte ARC, Costa MS, Simplício AL, Cardoso MM, Duarte CMM. Preparation of controlled release microspheres using supercritical fluid technology for delivery of anti-inflammatory drugs. Int J Pharm. 2006;308:168–74.
18. Chen X, Young TJ, Sarkari M, Williams Iii RO, Johnston KP. Preparation of cyclosporine A nanoparticles by evaporative precipitation into aqueous solution. Int J Pharm. 2002;242:3–14.
19. Shegokar R, Müller RH. Nanocrystals: industrially feasible multifunctional formulation technology for poorly soluble actives. Int J Pharm. 2010;399:129–39.
20. Merisko-Liversidge E, Liversidge GG. Nanosizing for oral and parenteral drug delivery: a perspective on formulating poorly-water soluble compounds using wet media milling technology. Adv Drug Deliver Rev. 2011;63:427–40.
21. Keck CM, Müller RH. Drug nanocrystals of poorly soluble drugs produced by high pressure homogenisation. Eur J Pharm Biopharm. 2006;62:3–16.
22. Juhnke M, Märtin D, John E. Generation of wear during the production of drug nanosuspensions by wet media milling. Eur J Pharm Biopharm. 2012;81:214–22.
23. Kumar S, Burgess DJ. Wet milling induced physical and chemical instabilities of naproxen nano-crystalline suspensions. Int J Pharm. 2014;466:223–32.
24. Afolabi A, Akinlabi O, Bilgili E. Impact of process parameters on the breakage kinetics of poorly water-soluble drugs during wet stirred media milling: a microhydrodynamic view. Eur J Pharm Sci. 2014;51:75–86.
25. Kesisoglou F, Panmai S, Wu Y. Nanosizing—oral formulation development and biopharmaceutical evaluation. Adv Drug Deliver Rev. 2007;59:631–44.
26. Merisko-Liversidge EM, Liversidge GG. Drug nanoparticles: formulating poorly water-soluble compounds. Toxicol Pathol. 2008;36:43–8.
27. Monteiro A, Afolabi A, Bilgili E. Continuous production of drug nanoparticle suspensions via wet stirred media milling: a fresh look at the Rehbinder effect. Drug Dev Ind Pharm. 2013;39:266–83.
28. Müller RH, Jacobs C, Kayser O. Nanosuspensions as particulate drug formulations in therapy: rationale for development and what we can expect for the future. Adv Drug Deliver Rev. 2001;47:3–19.
29. Brough C, Williams III RO. Amorphous solid dispersions and nano-crystal technologies for poorly water-soluble drug delivery. Int J Pharm. 2013;453:157–66.
30. Leung DH, Lamberto DJ, Liu L, Kwong E, Nelson T, Rhodes T, et al. A new and improved method for the preparation of drug nanosuspension formulations using acoustic mixing technology. Int J Pharm. 2014;473:10–9.
31. Kardous F, Yahiaoui R, Aoubiza B, Manceau JF. Acoustic mixer using low frequency vibration for biological and chemical applications. Sensor Actuat A-Phys. 2014;211:19–26.
32. Shrivastava A, Sakthivel S, Pitchumani B, Rathore A. A statistical approach for estimation of significant variables in wet attrition milling. Powder Technol. 2011;211:46–53.
33. Connell Jr TL, Risha GA, Yetter RA, Young G, Sundaram DS, Yang V. Combustion of alane and aluminum with water for hydrogen and thermal energy generation. P Combust Inst. 2011;33:1957–65.
34. Sullivan KT, Kuntz JD, Gash AE. The role of fuel particle size on flame propagation velocity in thermites with a nanoscale oxidizer. Propell Explos Pyrot. 2014;39:407–15.
35. Capece M, Huang Z, To D, Aloia M, Muchira C, Davé RN, et al. Prediction of porosity from particle scale interactions: surface modification of fine cohesive powders. Powder Technol. 2014;254:103–13.
36. Huang Z, Scicolone JV, Han X, Davé RN. Improved blend and tablet properties of fine pharmaceutical powders via dry particle coating. Int J Pharm. 2015;478:447–55.
37. Knieke C, Azad MA, To D, Bilgili E, Davé RN. Sub-100 micron fast dissolving nanocomposite drug powders. Powder Technol. 2015;271:49–60.
38. Mullarney MP, Beach LE, Langdon BA, Polizzi MA. Applying dry powder coatings. Pharm Technol. 2011;35:94–102.
39. Howe HW, Warriner JJ, Cook AM, Coguill SL, Farrar LC. Apparatus and method for resonant-vibratory mixing. US Patent, 2007; US7188993 B1.
40. Howe HW, Warriner JJ, Cook AM, Coguill SL, Farrar LC. Method for resonant-vibratory mixing. US Patent, 2011; US7866878 B2.
41. Lim J-Y, Moon J-D. Multiphase mixing apparatus using acoustic resonance. US Patent, 2001; US6283626 B1.
42. Ghosh I, Schenck D, Bose S, Ruegger C. Optimization of formulation and process parameters for the production of nanosuspension by wet media milling technique: effect of vitamin E TPGS and nanocrystal particle size on oral absorption. Eur J Pharm Sci. 2012;47:718–28.
43. Peltonen L, Hirvonen J. Pharmaceutical nanocrystals by nanomilling: critical process parameters, particle fracturing and stabilization methods. J Pharm Pharmacol. 2010;62:1569–79.
44. Li M, Yaragudi N, Afolabi A, Dave R, Bilgili E. Sub-100 nm drug particle suspensions prepared via wet milling with low bead contamination through novel process intensification. Chem Eng Sci. 2015;130:207–20.
45. Bilgili E, Afolabi A. A combined microhydrodynamics–polymer adsorption analysis for elucidation of the roles of stabilizers in wet stirred media milling. Int J Pharm. 2012;439:193–206.
46. Bilgili E, Li M, Afolabi A. Is the combination of cellulosic polymers and anionic surfactants a good strategy for ensuring physical stability of BCS Class II drug nanosuspensions? Pharm Dev Technol. 2015. doi:10.3109/10837450.2015.1022788.
47. Bilgili E, Hamey R, Scarlett B. Production of pigment nanoparticles using a wet stirred mill with polymeric media. China Particuology. 2004;2:93–100.
48. Ghosh I, Bose S, Vippagunta R, Harmon F. Nanosuspension for improving the bioavailability of a poorly soluble drug and screening of stabilizing agents to inhibit crystal growth. Int J Pharm. 2011;409:260–8.
49. Azad M, Afolabi A, Bhakay A, Leonardi J, Davé R, Bilgili E. Enhanced physical stabilization of fenofibrate nanosuspensions via wet co-milling with a superdisintegrant and an adsorbing polymer. Eur J Pharm Biopharm. 2015;94:372–85.
50. Yang H, Teng F, Wang P, Tian B, Lin X, Hu X, et al. Investigation of a nanosuspension stabilized by Soluplus® to improve bioavailability. Int J Pharm. 2014;477:88–95.
51. Patel C, Chakraborty M, Murthy ZVP. Preparation of fenofibrate nanoparticles by combined stirred media milling and ultrasonication method. Ultrason Sonochem. 2014;21:1100–7.
52. Eskin D, Zhupanska O, Hamey R, Moudgil B, Scarlett B. Microhydrodynamic analysis of nanogrinding in stirred media mills. AlChE J. 2005;51:1346–58.