Nanosizing: A formulation approach for poorly-water-soluble compounds

European Journal of Pharmaceutical Sciences

Volumn 18, Issue 2, 2003, Pages 113-120

  Merisko Liversidge, Elaine ^a   Liversidge, Gary G ^a   Cooper, Eugene R ^a  

^a King of Prussia PA 19406 USA   (United States)

Author keywords

Nanoparticles and drug delivery; Poorly water soluble compounds

Indexed keywords

CRYSTALLINE MATERIALS; DRUG DOSAGE; MARKETING; SOLUBILITY; SOLUTIONS;

MEDIA MILLING;

NANOSTRUCTURED MATERIALS;

CAMPTOTHECIN; DANAZOL; ETOPOSIDE; NANOPARTICLE; NAPROXEN; PACLITAXEL;

AREA UNDER THE CURVE; BIOAVAILABILITY; DELAYED DRUG RELEASE; DISPERSION; DRUG CAPSULE; DRUG DELIVERY SYSTEM; DRUG DOSAGE FORM; DRUG EFFICACY; DRUG FORMULATION; DRUG IDENTIFICATION; DRUG SOLUBILITY; DRUG STABILITY; MAXIMUM TOLERATED DOSE; NANOTECHNOLOGY; PRIORITY JOURNAL; PULSATILE DRUG RELEASE; REVIEW; SLOW DRUG RELEASE; TABLET; TABLET FORMULATION;

ANIMALS; HUMANS; NANOTECHNOLOGY; PHARMACEUTICAL PREPARATIONS; SOLUBILITY; WATER;

EID: 0037312695     PISSN: 09280987     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0928-0987(02)00251-8     Document Type: Review

References (58)

1. Adachi Y., Arii S., Funaki N., Higashitsuji H., Fijita S., Furutani M., Mise M., Zhang W., Tobe T. Tumoricidal activity of Kupffer cells augmented by anticancer drugs. Life Sci. 51:1992;177-183.
2. Akers M.J. Excipient-drug interactions in parenteral formulations. J. Pharm. Sci. 91:2002;2283-2300.
3. Allen T.M. Liposomes: opportunities in drug delivery. Drugs. 54:1997;8-14.
4. Aungst B. Intestinal permeation enhancers. J. Pharm. Sci. 89:2000;429-442.
5. Benet L.Z., Izumi T., Zhang Y., Silverman J.A., Wacher V.J. Intestinal MDR transport proteins and P-450 enzymes as barriers to oral drug delivery. J. Control. Release. 62:1999;25-31.
6. Bittner, B., Mountfield, R.J., 2002. Intravenous administration of poorly soluble new drug entities in early drug discovery: The potential impact of formulation on pharmacokinetic parameters. Cur. Opin. Drug Discovery and Dev., 59-71.
7. Breitenbach J. Melt extrusion: from process to drug delivery technology. EJPB. 54:2002;107-117.
8. Byrn S., Pfeiffer R., Ganey M., Hoiberg C., Poochikian G. Pharmaceutical solids: a strategic approach to regulatory considerations. Pharm. Res. 12:1995;945-954.
9. Cooper E. Nanoparticles in drug delivery. NanoTechnology Symposium, NIH, September:2000.
10. Couvreur P., Roblot-Treuple L., Poupon M.F., Brasseur F., Puisieux F. Nanoparticles as microcarriers for anticancer drugs. Adv. Drug Deliv. Rev. 5:1990;209-230.
11. Dressman J.B., Amidon G.L., Reppas C., Shah V.P. Dissolution testing as a prognostic tool for oral drug adsorption: immediate release dosage forms. Pharm. Res. 15:1998;11-22.
12. Floyd A.G. Top ten considerations in the development of parenteral emulsions. Pharm. Sci. Tech. 4:1999;134-143.
13. Gref R., Minamitake Y., Peracchia M.T., Trubetskoy V., Torchilin V., Langer R. Biodegradable long-circulating polymeric nanospheres. Science. 263:1994;1600-1603.
14. Gregoriades G. Engineering liposomes for drug delivery: progress and problems. TIBTECH. 13:1995;527-537.
15. Hobbs S.K., Monsdky W.L., Yuan F., Roberts G.W., Griffith L., Torchilin V., Jain R.K. Regulation of transport pathways in tumor vessels: role of tumor type and microenvironment. Proc. Natl. Acad. Sci. 95:1998;4607-4612.
16. Horter D., Dressman J.B. Influence of physicochemical properties on dissolution of drugs in the gastrointestinal tract. Adv. Drug Deliv. Rev. 46:2001;75-87.
17. Illum L., Davis S.S., Wilson C.G., Thomas N.W., Frier M., Hardy J.G. Blood clearance and organ disposition of intravenously administered colloidal particles. Effect of particle size, nature, and shape. Int. J. Pharm. 2:1982;135-136.
18. Jain R.K. Delivery of molecular medicine to solid tumors. Science. 271:1996;1079-1080.
19. Juliano R.L. Factors affecting the clearance kinetics and tissue distribution of liposomes, microspheres and emulsions. Adv. Drug Deliv. Rev. 2:1988;31-54.
20. Kibbe A.H. Handbook of Pharmaceutical Excipients. 3rd Edition:2000;AphA and PhP, Washington, DC.
21. Kong G., Braun R.D., Dewhirst M.W. Hypothermia enables tumor-specific nanoparticle delivery: effect of particle size. Cancer Res. 60:2000;4440-4445.
22. Kusuhara H., Suzuki H., Sugiyama Y. The role of p-glycoprotein and canalicular multispecific organic anion transporter in the hepatobiliary excretion of drugs. J. Pharm. Sci. 87:1998;1025-1040.
23. Lawrence M.J., Rees G.D. Microemulsion-based media as novel drug delivery systems. Adv. Drug Deliv. Rev. 45:2000;89-121.
24. Lee J.W., Park J.H., Robinson J.R. Bioadhesive-based dosage forms: the next generation. J. Pharm. Sci. 89:2000;850-866.
25. Leuner C., Dressman J. Improving drug solubility for oral delivery using solid dispersions. Eur. J. Pharm. Biopharm. 50:2000;47-60.
26. Lipinski C.A., Lombardo F., Dominy B.W., Feeney P.J. Experimental and computational approaches to estimate solubility and permeability in drug discovery and development setting. Adv. Drug Deliv. Rev. 23:1997;3-25.
27. Lipinski C.A. Avoiding investment in doomed drugs, is poor solubility an industry wide problem? Curr. Drug Dis. 2001;17-19.
28. Lipinski C. Poor aqueous solubility - an industry wide problem in drug discovery. Am. Pharm. Rev. 5:2002;82-85.
29. Lipper R.A. E pluribus product. Mod. Drug Dis. 2:1999;55-60.
30. Liversidge, G.G., Cundy, K.C., Bishop, J.F., Czekai, D.A., 1992. Surface modified drug nanoparticles. U.S. Patent 5,145,684.
31. Liversidge G.G., Cundy K.C. Particle size reduction for improvement of oral bioavailability of hydrophobic drugs: I. Absolute oral bioavailability of nanocrystalline danazol in beagle dogs. Int. J. Pharm. 125:1995;91-97.
32. Liversidge G.G., Conzentino P. Drug particle size reduction for decreasing gastric irritancy and enhancing absorption of naproxen in rats. Int. J. Pharm. 125:1995;309-313.
33. Liu Y., Bacon E.R., Ballinger K., Black C.D.V., Illig K., McIntire G.L., Wang P.P., O'Neil N., Kinter L., Desai V.C. Pharmacokinetic and hepatic disposition of Bis[1-ethoxycarbonyl)propyl]5-acetylamino-2,3,6-triiodoisophthalate in rats and isolated perfused rat livers. Drug Metab. Dispos. 28:2000;731-736.
34. Loftsson T., Brewster M.E. Pharmaceutical applications of cyclodextrins. J. Pharm. Sci. 85:1996;1017-1025.
35. Loper A. Poorly soluble compounds: vehicle selection and solubilization. Land O'Lakes Conference: Drug Metabolism and Pharmacokinetics:1999.
36. Martin F., Caignard A., Olsson O., Jeannin J.F., Leclerc A. Tumoricidal effect of macrophages exposed to adriamycin in vivo or in vitro. Cancer Res. 42:1982;3851-3857.
37. Merisko-Liversidge E., Sarpotdar P., Bruno J., Hajj S., Wei L., Peltier N., Rake J., Shaw J.M., Pugh L., Polin L., Jones J., Corbett T., Cooper E., Liversidge G.G. Formulation and antitumor activity evaluation of nanocrystalline suspensions of poorly soluble anticancer drugs. Pharm. Res. 13:1996;272-278.
38. Moghimi S.M., Hunter A.C., Murray J.C. Long-circulating and target-specific nanoparticles: theory to practice. Pharmacol. Rev. 53:2001;283-318.
39. Muller R.H., Jacobs C., Kayser O. Nanosuspensions as particulate drug formulations in therapy: rationale for development and what we can expect for the future. Adv. Drug Deliv. Rev. 47:2001;3-19.
40. Na G.C., Stevens H.J., Yuan B.O., Rajagopalan N. Physical stability of ethyl diazoate nanocrystalline suspension in steam sterilization. Pharm. Res. 16:1999;569-574.
41. Nakano M. Places of emulsions in drug delivery. Adv. Drug Deliv. Rev. 45:2000;1-4.
42. Neal J.C., Stolnik S., Garnett M.C., Davis S.S., Illum L. Modification of copolymers poloxamer 407 and poloxamine 908 can affect the physical and biological properties of surface modified nanospheres. Pharm. Res. 15:1998;318-324.
43. Nouchi Y., Wu J., Duncan R., Strohalm J., Ulbrich T., Akaike T., Maeda H. Early phase tumor accumulation of macromolecules: a great difference in clearance rate between tumor and normal tissue. Jpn. J. Cancer Res. 89:1998;307-314.
44. Pace S., Pace G.W., Parikh I., Mishra A. Novel injectable formulations of insoluble drugs. Pharm. Tech. 23:1999;116-134.
45. Papisov M. Theoretical considerations of RES-avoiding liposomes: molecular mechanics and chemistry of liposome interactions. Adv. Drug Deliv. Rev. 32:1998;119-138.
46. 2 and cryogenic spray-freezing technologies. Drug Dev. Ind. Pharm. 27:2001;1003-1015.
47. Schott H. Colloidal dispersions. Gennaro A.R. Remington's Pharmaceutical Sciences. 1955;252-277.
48. Serajuddin A.T.M. Solid dispersion of poorly water-soluble drugs: early promises, subsequent problems, and recent breakthroughs. J. Pharm. Sci. 88:1999;1058-1066.
49. Soma C.E., Dubernet C., Barratt G., Benita S., Couvreur P. Investigation of the role of macrophages on the cytotoxicity of doxorubicin and doxorubicin-loaded nanoparticles on M5076 cells in vitro. J. Control. Release. 68:2000;283-289.
50. Stella V.J., Rajewski R.A. Cyclodextrins: their future in drug formulation and delivery. Pharm. Res. 14:1997;556-567.
51. Stolnik S., Illum L., Davis S.S. Long circulating microparticulate drug carriers. Adv. Drug Deliv. Rev. 16:1995;195-214.
52. Tom J.W., Debenedetti P.G. Particle formation with supercritical fluids - a review. J. Aersol Sci. 22:1991;555-584.
53. Toster S.D., Muller R., Kreuter J. Modification of the body distribution of poly(methylmethacrylate) nanoparticles in rats by coating with surfactants. Int. J. Pharm. 61:1990;85-100.
54. Veber D.F., Johnson S.R., Cheng H.-Y., Smith B.R., Ward K.W., Kopple K.D. Molecular properties that influence oral bioavailability of drug candidates. J. Med. Chem. 45:2002;2615-2623.
55. Venkatesh S., Lipper R. Role of the development scientist in compound lead selection and optimization. J. Pharm. Sci. 89:2000;145-154.
56. Wiedmann T.S., DeCastro L., Woods R.W. Nebulization of nanocrystals: production of a respirable solid-in-liquid-in-air colloidal dispersion. Pharm. Res. 14:1997;112-116.
57. Woodle M.C. Controlling liposome blood clearance by surface-grafted polymers. Adv. Drug Deliv. Rev. 32:1998;139-152.
58. Zheng J.Y., Bosch H.W. Sterile filtration of nanocrystal drug formulations. Drug Dev. Ind. Pharm. 23:1997;1087-1093.