Drug nanocrystals: A novel formulation approach for poorly soluble drugs

International Journal of PharmTech Research

Volumn 1, Issue 3, 2009, Pages 682-694

  Katteboinaa, Suman ^a   Chandrasekhar P, V S R ^b   Balaji, S ^c  

^a BAPATLA COLLEGE OF PHARMACY   (India)

^b HINDU COLLEGE OF PHARMACY   (India)

^c ANDHRA UNIVERSITY   (India)

Author keywords

Bioavailability enhancement; Nanocrystals; Nanosuspensions; Stabilizers; Surfactants

Indexed keywords

ANTIINFECTIVE AGENT; APHIDICOLIN; APREPITANT; BECLOMETASONE DIPROPIONATE; BUDESONIDE; BUPARVAQUONE; BUSULFAN; CARBAMAZEPINE; CLOFAZIMINE; CYCLOSPORIN; DANAZOL; DICHLOROMETHANE; DODECYL SULFATE SODIUM; FENOFIBRATE; GRISEOFULVIN; HYDROXYPROPYLCELLULOSE; LEUCINE ENKEPHALIN[2 DEXTRO ALANINE 6 ARGININE]; MEGAACE ES; MEGESTROL ACETATE; MICROCRYSTALLINE CELLULOSE; NANOCRYSTAL; NAPROXEN; OMEPRAZOLE; PACLITAXEL; POLOXAMER; POLYSORBATE 80; POVIDONE; PREDNISOLONE; RAPAMYCIN; SUCROSE; UNCLASSIFIED DRUG; UNINDEXED DRUG;

ATYPICAL MYCOBACTERIOSIS; CRYPTOSPORIDIOSIS; DISPERSION; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG DOSAGE FORM COMPARISON; DRUG EFFICACY; DRUG ELIMINATION; DRUG FORMULATION; DRUG RETENTION; DRUG SOLUBILITY; FREEZE DRYING; HUMAN; MICROFLUIDICS; NONHUMAN; PARTICLE SIZE; PHYSICAL CHEMISTRY; PRECIPITATION; REVIEW; SUSPENSION; TABLET;

EID: 77953408726     PISSN: None     EISSN: 09744304     Source Type: Journal    
DOI: None     Document Type: Review

References (76)

1. C. Lipinski, Poor aqueous solubility- an industry wide problem in drug discovery, Am.Pharm. Rev. 5 (2002) 82-85.
2. Troester F. Cremophor-free aqueous paclitaxel nanosuspension-production andchemical stability. Controlled Release Society 31st annual meeting, Honolulu, HI, 2004.
3. Liversidge E, Wei L. Stabilization of chemical compounds using nanoparticulateformulations. US 2001;952032 20010914. CAN 138:243327, US 2003054042 A1, 2003.
4. Möschwitzer J, Achleitner G, Pomper H, Muller RH. Development of an intravenously injectable chemically stable aqueous omeprazole formulation using nanosuspension technology. Eur J Pharm Biopharm 2004; 58(3):615-619.
5. Müller RH, Keck CM. Challenges and solutions for the delivery of biotech drugs-a review of drug nanocrystal technology and lipid nanoparticles. J Biotechnol 2004; 113(1 3):151-170.
6. A. Noyes,W. Whitney, The rate of solution of solid substances in their own solutions, J. Am. Chem. Soc. 19 (1897) 930-934.
7. W. Nernst, Theorie der Reaktionsgeschwindigkeit in heterogenen Systemen, Z. Phys.Chem. 47 (1) (1904) 52-55.
8. E. Brunner, Reaktionsgeschwindigkeit in heterogenen Systemen, Z. Phys. Chem. 47 (1) (1904) 56-102.
9. V.B. Patravale, A.A. Date, R.M. Kulkarni, Nanosuspensions: a promising drug delivery strategy, J. Pharm. Pharmacol. 56 (7) (2004) 827-840.
10. Y. Wu, A. Loper, E. Landis, L. Hettrick, L. Novak, K. Lynn, C. Chen, K. Thompson, R. Higgins, U. Batra, S. Shelukar, G. Kwei, D. Storey, The role of biopharmaceutics in thedevelopment of a clinical nanoparticle formulation of MK-0869: a beagle dog model predicts.improved bioavailability and diminished food effect on absorption in human, Int. J. Pharm.285 (1-2) (2004) 135-146.
11. M. Mosharraf, C. Nystrom, The effect of particle size and shape on the surface specific dissolution rate of micronized practically insoluble drugs, Int. J. Pharm. 122 (1995) 35-47.
12. R.H. Muller, K. Peters, Nanosuspensions for the formulation of poorly soluble drugs I. Preparation by a size-reduction technique, Int. J. Pharm. 160 (1998) 229-237.
13. Buchmann S, Fischli W, Thiel FP, Alex R. Aqueous microsuspension, an alternative intravenous formulation for animal studies. In: 42nd annual congress of the International Association for Pharmaceutical Technology (APV), Mainz, 1996.
14. Bruno JAD, Brian D. Gustow Evan, Illig, Kathleen J, Rajagopalan, Nats, Sarpotdar. Method of grinding pharmaceutical substances. US 5,518,187, 1992.
15. Wyeth Research Drug Information, Rapamune (Sirolumus) Oral Solutions and Tablets. Company Communications, 2004.
16. Merck, Drug Information Emend. 2004.
17. Speiser PP (1998) Poorly soluble drugs, a challenge in drug delivery, in Muller RH, Benita S and Bohm B (eds.), Emulsions and Nanosuspensions for the Formulation of Poorly Soluble Drugs, Medpharm Scientific Publishers: Stuttgart.
18. Bruno RPM (1999) Microfluidizer Processor Technology for High Performance Particle Size Reduction, Mixing and Dispersion. Microfluidizer Processor Technology.
19. Sunstrom JEM and Marshik-Guerts B (1996) General Route to Nanocrystalline Oxids by Hydrodynamic Cavitation. Chem. Mater.
20. Gruverman IJ and Thum JR, Production of Nanostructures Under Turbulent Collision Reaction Conditions - Application to Catalysts, Superconductors, CMP Abrasives, Ceramics and other Nanoparticles. Microfluidics Research.
21. Parikh IS, Ulagaraj. Composition and method of preparing microparticles of waterinsoluble substances. 93969997, 1997.
22. Dearn AR. Atovaquone pharmaceutical compositions. US, 974248, 6,018,080, 2000.
23. Haynes DH. Phospholipid-coated microcrystals: injectable formulations of waterinsoluble drugs. US 5,091,187, 1992.
24. Miiller RH, Jacobs C and Kayser O (2000) Nanosuspensions for the formulation of poorly soluble drugs, in Nielloud F and Marti-Mestres G (eds.) Pharmaceutical Emulsions and Suspensions, Marcel Dekker.
25. Miiller RH, Becker R, Kruss B and Peters K (1994) Pharmazeutische Nanosuspensionen zur Arzneistoffapplikation als Systeme mit erhohter Sattigungsloslichkeit und Losungsgeschwindigkeit. German patent 4440337.2, US Patent 5.858.410 (1999).
26. Miiller RH, Peters K, Becker R and Kruss B (1995) Nanosuspensions - A Novel Formulation for the i.v. Administration of Poorly Soluble Drugs, in 1st World Meeting of the International Meeting on Pharmaceutics, Biopharmaceutics and Pharmaceutical Technology
27. Muller RH, Dingier A, Schneppe T and Gohla S (2000) Large scale production of solid lipid nanoparticles (SLNTM) and nanosuspensions (DissoCubes™). in Wise D (ed.), Handbook of Pharmaceutical Controlled Release Technology.
28. Muller RH, Jacobs C and Kayser O (2003) DissoCubes - A novel formulation for poorly soluble and poorly bioavailable drugs, in Rathbone MJ, Hadgraft}, Roberts MS (eds.), Modified- Release Drug Delivery Systems, Marcel Dekker.
29. Rabinow BE (2004) Nanosuspensions in Drug Delivery. Nat Rev 3:785-796.
30. Müller RH, Krause K, Mader K. Method for controlled production of ultrafine microparticles and nanoparticles, Application. WO 2000-EP6535, 2001003670, 2001.
31. Muller RH (2002) Nanopure Technology for the Production of Drug Nanocrystals and Polymeric Particles, in 4th World Meeting ADRITELF/APV/APGI. Florence.
32. Bushrab NF and Muller RH (2003) Nanocrystals of Poorly Soluble Drags for Oral Administration. New Drugs 5: 20-22.
33. Radtke M (2001) Nanopure™ pure drug nanoparticles for the formulation of poorly soluble Drugs. New Drugs 3: 62-68.
34. Fichera MA, Keck CM and Muller RH (2004) Nanopure Technology - Drug Nanocrystals for the Delivery of Poorly Soluble Drugs, in Particles. Orlando.
35. Fichera MA, Wissing SA and Muller RH (2004) Effect of 4000 Bar Homogenisation Pressure on Particle Diminution in Drug Suspensions, in APV. Niirnberg.
36. Keck CM, Bushrab NF and Muller RH (2004) Nanopure® Nanocrystals for Oral Delivery of Poorly Soluble Drugs, in Particles. Orlando.
37. Muller RH, Mader K and Krause K (2000) Verfahren zur schonenden Herstellung von hochfeinen Micro-/Nanopartikeln, in PCT Application PCT/EP00/06535: Germany.
38. Li Zhiyi, Preparation of griseofulvin microparticles by supercritical fluid expansion depressurization processPowderTechnology Volume 182, Issue 3, 10 March 2008, Pages 459-465.
39. Andrian Tandya, Micronization of cyclosporine using dense gas techniques, The Journal of SupercriticalFluids, Volume 37, Issue 3, May 2006, Pages 272-278.
40. Young, Phospholipid-Stabilized Nanoparticles of Cyclosporine A by Rapid Expansion from Supercritical to Aqueous Solution AAPS PharmSciTech 2003; 5 (1) Article 11.
41. Physical stability of micronized powders produced by spray-freezing into liquid (SFL) to enhance the dissolution of an insoluble drug. Rogers TL, Johnston KP, Williams RO 3rd. Pharm Dev Technol. 2003;8(2):187-97.
42. Vaughn, Evaporative Precipitation into Aqueous Solution Process: Investigation of Processing Parameters to Enhance Dissolution of Danazol http://www.aapsj.org/abstracts/Am-2003/AAPS2003-02263.PDF \
43. Böhm B. Production and characterisation of nanosuspensions as novel delivery system for drugs with low bioavailability. In: Pharmaceutical Technology. Berlin: Free University of Berlin, 1999.
44. Grau M. Investigation of dissolution velocity, saturation solubility and stability of ultrafine drug suspensions. Dissertation. Pharmazeutische Technologie. Berlin: Free University of Berlin, 2000.
45. Stewart PJ, Zhao FY. Understanding agglomeration of indomethacin during the dissolution of micronised indomethacin mixtures through dissolution and deagglomeration modeling approaches. Eur J Pharm Biopharm 2005; 59(2):315-323.
46. Kirkof N. Creation and characterization of Nanoparticles. In: 32nd annual meeting and exposition of the Controlled Release Society, Miami, 2005.
47. Möschwitzer J, Müller RH. From the drug nanocrystal to the final mucoadhesive oral dosage form, 2004.
48. Möschwitzer J, Müller RH. Spray coated pellets as carrier system for mucoadhesive drug nanocrystals. Eur J Pharm Biopharm. Submitted.
49. Möschwitzer J, Müller RH. Controlled drug delivery system for oral application of drug nanocrystals. In: 2004 AAPS annual meeting and exposition, Baltimore, MD, 2004.
50. Bushrab NF, Müller RH. Nanocrystals of poorly soluble drugs for oral administration. NewDrugs 2003; 5:20-22.
51. Bushrab FN, Müller RH. Drug nanocrystals for oral delivery-compounds by spray drying. Philadelphia: AAPS, 2004.
52. Müller RH. Preparation of a matrix material-excipient compound containing a drug. WO 1997-EP6893, WO 9825590, 1998.
53. Liversidge GG, Cundy KC. Particle size reduction for improvement of oral bioavailability of hydrophobic drugs. I Absolute oral bioavailability of nanocrystalline danazol in beagle dogs. Int J Pharm 1995; 125:91-97.
54. Merisko-Liversidge E, Liversidge GG, Cooper ER. Nanosizing: a formulation approach for poorly watersoluble compounds. Eur J Pharm Sci 2003; 18(2):113-120.
55. Liversidge GG, Conzentino, Phil. Drug particle size reduction for decreasing gastric irritancy and enhancing absorption of naproxen in rats. Int J Pharm 1995; 125:309-313.
56. Eickhoff WM, Engers DA, Mueller KR. Nanoparticulate NSAID compositions, Application. US 95-385614, 5518738, 1996.
57. Jacobs C, Kayser O, Müller RH. Production and characterisation of mucoadhesive nanosuspensions for the formulation of bupravaquone. Int J Pharm 2001; 214(1-2):3-7.
58. Müller RH, Jacobs C. Buparvaquone mucoadhesive nanosuspension: preparation, optimisation and long-term stability. Int J Pharm 2002; 237(1-2):151-161.
59. Lamprecht A, Ubrich N, Yamamoto H, et al. Biodegradable nanoparticles for targeted drug delivery in treatment of inflammatory bowel disease. J Pharmacol Exp Ther 2001; 299(2):775-781.
60. Hussain N, Jaitley V, Florence AT. Recent advances in the understanding of uptake of microparticulates across the gastrointestinal lymphatics. Adv Drug Deliv Rev 2001; 50(1 2):107-142.
61. Vergote GJ, An oral controlled release matrix pellet formulation containing nanocrystalline ketoprofen. Int J Pharm. 2001 May 21;219(1-2):81-7.
62. C. Jacobs, Production and characterisation of mucoadhesive nanosuspensions for the formulation of bupravaquone International Journal of Pharmaceutics Volume 214, Issues 1-2, 19 February 2001, Pages 3-7.
63. Möschwitzer J, Achleitner G, Pomper H, Muller RH. Development of an intravenously injectable chemically stable aqueous omeprazole formulation using nanosuspension technology. Eur J Pharm Biopharm 2004; 58(3):615-619.
64. Na GC, Stevens Jr J, Yuan BO, Rajagopalan N. Physical stability of ethyl diatrizoate nanocrystalline suspension in steam sterilization. Pharm Res 1999; 16(4):569-574.
65. Müller RH, Jacobs C, Kayser O. Nanosuspensions for the formulation of poorly soluble drugs. In: Nielloud F, Marti-Mestres G, eds. Pharmaceutical Emulsions and Suspensions. New York: Marcel Dekker, 2000:383-407.
66. Singla AK, Garg A, Aggarwal D. Paclitaxel and its formulations. Int J Pharm 2002; 235(1-2):179-192.
67. Peters K et al. Preparation of a clofazimine nanosuspension for intravenous use and evaluation of its therapeutic efficacy in murine Mycobacterium avium infection. J Antimicrob Chemother 2000; 45(1):77-83.
68. Scholer N et al. Atovaquone nanosuspensions show excellent therapeutic effect in a new murine model of reactivated toxoplasmosis. Antimicrob Agents Chemother 2001; 45(6):1771-1779.
69. Smith A and Hunneyball LM (1986) Evaluation of poly(lactic acid) as a biodegradable drug delivery system for parenteral administration. Int} Pharm 30(2-3):215-220.
70. MÖSCHWITZER Jan, Development of an intravenously injectable chemically stable aqueous omeprazole formulation using nanosuspension technology, Eur J Pharm Sci. 2004, vol. 58,615-619.
71. Hernandez-Trejo N, Kayser O, Miiller RH and Steckel H (2004) Physical Stability ofBuparvaquone Nanosuspensions Following Nebulization with Jet and Ultrasonic Nebulizers. Proceedings of the International Meeting on Pharmaceutics, Biopharmaceutics and Pharmaceutical Technology, Nuremberg Germany.
72. Jacobs Claudia, Production and characterization of a budesonide nanosuspension for pulmonary administration Pharmaceutical research, 2002, vol. 19, pp. 189-194
73. Hernandzo http://cat.inist.fr/.aModele=afficheN&cpsidt=17345613
74. Pignatello R, Eudragit RS100 nanosuspensions for the ophthalmic controlled delivery of ibuprofen. Eur J Pharm Sci. 2002 Jul;16(1-2):53-61.
75. O. Kayser, Nanosuspensions for the formulation of aphidicolin to improve drug targeting effects against Leishmania infected macrophages International Journal of Pharmaceutics Volume 196, Issue 2, 10 March 2000, Pages 253-256
76. http://www.pharmainfo.net/reviews/nanosuspensionsparticulate-drug- delivery-systems