Nanoparticle formation and growth during in vitro dissolution of ketoconazole solid dispersion

Journal of Pharmaceutical Sciences

Volumn 100, Issue 7, 2011, Pages 2876-2885

  Kanaujia, Parijat ^a   Lau, Grace ^a   Ng, Wai Kiong ^a   Widjaja, Effendi ^a   Hanefeld, Andrea ^b   Fischbach, Matthias ^b   Maio, Mario ^b   Tan, Reginald B H ^a,c  

^a INSTITUTE OF CHEMICAL AND ENGINEERING SCIENCES   (Singapore)

^b MERCK KGAA   (Germany)

^c NATIONAL UNIVERSITY OF SINGAPORE   (Singapore)

Author keywords

Amorphous formulation; Dissolution rate; Melt extrusion; Nanoparticles; Solid dispersion; Solid solution

Indexed keywords

KETOCONAZOLE; NANOPARTICLE; POLYMER; VINYL ACETATE;

ARTICLE; CHEMICAL INTERACTION; DISPERSION; DRUG DISTRIBUTION; DRUG RELEASE; DRUG SOLUBILITY; IN VITRO STUDY; INFRARED SPECTROSCOPY; PARTICLE SIZE; RAMAN SPECTROMETRY; SCANNING ELECTRON MICROSCOPY; TRANSMISSION ELECTRON MICROSCOPY;

EID: 79955592721     PISSN: 00223549     EISSN: 15206017     Source Type: Journal    
DOI: 10.1002/jps.22491     Document Type: Article

References (36)

1. Lipinski C. 2002. Poor aqueous solubility-An industry wide problem in drug discovery. Am Pharm Rev 5:82-85.
2. Serajuddin ATM. 1999. Solid dispersion of poorly water-soluble drugs: Early promises, subsequent problems and recent breakthroughs. J Pharm Sci 88:1058-1066.
3. Karanth H, Shenoy VS, Murthy RR. 2006. Industrially feasible alternative approaches in the manufacturing of solid dispersions: A technical report. AAPS PharmSciTech 7:E1-E8.
4. Chiou WL, Rielman S. 1972. Pharmaceutical application of solid dispersion systems. J Pharm Sci 60:1281-1302.
5. Kawakami K. 2009. Current status of amorphous formulation and other special dosage forms as formulations for early clinical phases. J Pharm Sci 98:2875-2885.
6. Li L, AbuBaker O, Shao ZJ. 2006. Characterization of poly(ethylene oxide) as a drug carrier in hot-melt extrusion. Drug Dev Ind Pharm 32:991-1002.
7. Verreck G, Six K, Van den Mooter G, Baert L, Peeters J, Brewster ME. 2003. Characterization of solid dispersions of itraconazole and hydroxypropylmethylcellulose prepared by melt extrusion-Part I. Int J Pharm 251:165-174.
8. Nakamichi K, Yasuura H, Fukui H, Oka M, Izumi S. 2001. Evaluation of a floating dosage form of nicardipine hydrochloride and hydroxypropylmethylcellulose acetate succinate prepared using a twin-screw extruder. Int J Pharm 218:103-112.
9. Mididoddi PK, Repka MA. 2007. Characterization of hot-melt extruded drug delivery systems for onychomycosis. Eur J Pharm Biopharm 66:95-105.
10. Forster A, Hempenstall J, Rades T. 2001. Characterization of glass solutions of poorly water-soluble drugs produced by melt extrusion with hydrophilic amorphous polymers. J Pharm Pharmacol 53:303-315.
11. Ozgüney I, Shuwisitkul D, Bodmeier R. 2009. Development and characterization of extended release Kollidon® SR mini-matrices prepared by hot-melt extrusion. Eur J Pharm Biopharm 73:140-145.
12. Sun Y, Rui Y, Zhou W, Tang X. 2008. Nimodipine semi-solid capsules containing solid dispersion for improving dissolution. Int J Pharm 359:144-149.
13. Campbell K, Qi S, Craig DQM, McNally T. 2009. Paracetamol-loaded poly(epsilon-caprolactone) layered silicate nanocomposites prepared using hot-melt extrusion. J Pharm Sci 95:4831-4843.
14. Albers J, Alles R, Matthée K, Knop K, Nahrup JS, Kleinebudde P. 2009. Mechanism of drug release from polymethacrylate-based extrudates and milled strands prepared by hot-melt extrusion. Eur J Pharm Biopharm 71:387-394.
15. Lakshman JP, Cao Y, Kowalski J, Serajuddin ATM. 2008. Application of melt extrusion in the development of a physically and chemically stable high energy amorphous solid dispersion of a poorly water soluble drug. Mol Pharm 5:994-1002.
16. Breitenbach J. 2002. Melt extrusion: From process to drug delivery technology. Eur J Pharm Biopharm 54:107-117.
17. Breitenbach J. 2006. Melt extrusion can bring new benefits to HIV therapy: The example of Kaletra® tablets. Am J Drug Deliv 4:61-64.
18. Roth W, Setnik B, Zietsch M, Burst A, Breitenbach J, Sellers E, Brennan D. 2009. Ethanol effects on drug release from Verapamil Meltrex®, an innovative melt extruded formulation. Int J Pharm 368:72-75.
19. Hancock BC, Parks M. 2000. What is the true solubility advantage for amorphous pharmaceuticals? Pharm Res 17:397-404.
20. Bruce C, Fegely KA, Rajabi-Siahboomi AR, McGinity JW. 2007. Crystal growth formation in melt extrudates. Int J Pharm 341:162-172.
21. Bley H, Fussnegger B, Bodmeier R. 2010. Characterization and stability of solid dispersions based on PEG/polymer blends. Int J Pharm 390:165-173.
22. Shen SC, Ng WK, Chia L, Dong YC, Tan RB. 2010. Stabilized amorphous state of ibuprofen by co-spray drying with mesoporous SBA-15 to enhance dissolution properties. J Pharm Sci 99:1997-2007.
23. Karavas E, Ktistis G, Xenakis A, Georgarakis E. 2006. Effect of hydrogen bonding interactions on the release mechanism of felodipine from nanodispersions with polyvinylpyrrolidone. Eur J Pharm Biopharm 63:103-114.
24. Kanzer J, Hupfeld S, Vasskog T, Tho I, Hölig P, Mägerlein M, Fricker G, Brandl M. 2010. In situ formation of nanoparticles upon dispersion of melt extrudate formulations in aqueous medium assessed by asymmetrical flow field-flow fractionation. J Pharm Biomed Anal 53:359-365.
25. Hancock BC, York P, Rowe RC. 1997. The use of solubility parameters in pharmaceutical dosage form design. Int J Pharm 148:1-21.
26. Hansen CM. 2007. Hansen solubility parameters: A user's handbook. 2nd ed. Boca Raton: Taylor and Francis, pp 1-21.
27. Greenhalgh DJ, Williams AC, Timmins P, York P. 1999. Solubility parameters as predictors of miscibility in solid dispersions. J Pharm Sci 88:1182-1190.
28. Widjaja E, Li CZ, Chew W, Garland M. 2003. Band-target entropy minimization: A general and robust algorithm for pure component spectral recovery. Application to complex randomized mixtures of six components. Anal Chem 75:4499-4507.
29. Widjaja E, Seah RKH. 2008. Application of Raman microscopy and band-target entropy minimization to identify minor components in model pharmaceutical tablets. J Pharm Biomed Anal 46:274-281.
30. Breitenbach J, Schrof W, Neumann J. 1999. Confocal Raman spectroscopy: Analytical approach to solid dispersions and mapping of drugs. Pharm Res 16:1109-1113.
31. Jantratid E, Janssen N, Reppas C, Dressman JB. 2008. Dissolution media simulating conditions in the proximal human gastrointestinal tract: An update. Pharm Res 25:1663-1676.
32. Repka MA, Mididoddi PK, Stodghill SP. 2004. Influence of human nail etching for the assessment of topical onychomycosis therapies. Int J Pharm 282:95-106.
33. Van den Mooter G, Wuyts M, Blaton N, Busson R, Grobet P, Augustijns P, Kinget R. 2001. Physical stabilization of amorphous ketoconazole in solid dispersions with polyvinylpyrrolidone K25. Eur J Pharm Sci 12:262-269.
34. Tho I, Liepold B, Rosenberg J, Maegerlein M, Brandl M, Fricker G. 2010. Formation of nano/micro-dispersions with improved dissolution properties upon dispersion of ritonavir melt extrudate in aqueous media. Eur J Pharm Sci 40:25-32.
35. Sjökvist E, Nyström C. 1988. Physicochemical aspects of drug release VI. Drug dissolution from solid particulate dispersions and the importance of carrier and drug particle properties. Int J Pharm 47:51-66.
36. Craig DQM. 2002. The mechanisms of drug release from solid dispersions in water soluble polymers. Int J Pharm 231:131-144.