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http://dx.doi.org/10.4333/KPS.2010.40.S.083

Parenteral Formulations Based on Albumin Particulate Technology  

Lee, Hong-Hwa (College of Pharmacy, Ewha Womans University)
Lee, Min-Jung (College of Pharmacy, Ewha Womans University)
Heo, Sun-Ju (College of Pharmacy, Ewha Womans University)
Sah, Hong-Kee (College of Pharmacy, Ewha Womans University)
Publication Information
Journal of Pharmaceutical Investigation / v.40, no.spc, 2010 , pp. 83-95 More about this Journal
Abstract
Over the years, nanoparticle drug delivery systems have demonstrated versatile potentials in biological, medical and pharmaceutical applications. In the pharmaceutical industry nanotechnology research has mainly focused on providing controlled drug release, targeting their delivery to specific organs, and developing parenteral formulations for poorly water soluble drugs to improve their bioavailability. Achievement in polymer industry has generated numerous polymers applicable to designing nanoparticles. From viewpoints of product development, a nanocarrier material should meet requirements for biodegradability, biocompatibility, availability, and regulatory approval crieteria. Albumin is indeed a material that fulfills such requirements. Also, the commercialization of a first albumin-bound paclitaxel nanoparticle product (Abraxane$^{TM}$) has sparked renewed interests in the application of albumin in the development of nanoparticle formulations. This paper reviews the intrinsic properties of albumin, its suitability as a nanocarrier material, and albumin-based parenteral formulation approaches. Particularly discussed in detail are albumin-based particulate injectables such as Abraxane$^{TM}$. Information on key roles of albumin in the nab$^{TM}$ technology and representative manufacturing processes of albumin particulate products are provided. It is likely that albumin-based particulate technology would extend its applications in delivering drugs, polypeptides, proteins, vaccines, nucleic acids, and genes.
Keywords
albumin; nanoparticles; nanotechnology; injectables; parenteral formulation;
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1 Vauthier, C., Couvreur, P., 2000. Development of nanoparticles made of polysaccharides as novel drug carrier systems. In D.L. Wise (ed.), Handbook of Pharmaceutical Controlled Release Technology, Marcel Dekker, New York, 413-429.
2 Violanto, M.R., 1989. Method for making uniformly sized particles from water-insoluble organic compounds. US Patent 4,826,689.
3 Volcheck, G.W., Van Dellen, R.G., 1998. Anaphylaxis to intravenous cyclosporine and tolerance to oral cyclosporine: case report and review. Ann. Allergy, Asthma, & Immun. 80, 159-163.   DOI
4 Vorum, H., 1999. Reversible ligand binding to human serum albumin. Theoretical and clinical aspects. Dan Med Bull. 46, 379-399.
5 Weber, C., Kreuter, J., Langer, K., 2000. Desolvation process and surface characteristics of HSA-nanoparticles. Int. J. Pharm. 196, 197-200.   DOI
6 Weiss, R.B., Donehower, R.C., Wiernik, P.H., Ohnuma, T., Gralla, R.J., Trump, D.L., Baker Jr., J.R., Van Echo, D.A., Von Hoff, D.D., Leyland-Jones, B., 1990. Hypersensitivity reactions from Taxol. J. Clin. Oncol. 8, 1263-1268.   DOI
7 Yang, L., Cui, F., Cun, D., Tao, A., Shi, K., Lin, W., 2007. Preparation, characterization and biodistribution of the lactone form of 10-hydroxycamptothecin (HCPT)-loaded bovine serum albumin (BSA) nanoparticles. Int. J. Phram. 340, 163-172.   DOI
8 Toub, N., Malvy, C., Fattal, E., Couvreur, P., 2006. Innovative nanotechnologies for the delivery of oligonucleotides and siRNA. Biomed. Pharmacother. 60, 607-620.   DOI
9 Van Zuylen, L., Verweij, J., Sparreboom, A., 2001. Role of formulation vehicles in taxane pharmacology. Invest. New Drugs 19, 125-141.   DOI
10 Pavanetto, F., Genta, I., Giunchedi, P., Conti, B., Conte, U., 1994. Spray-dried albumin microspheres for the intra-articular delivery of dexamethasone. J. Microencapsulation 11, 445-454.   DOI
11 Peters, T., 1985. Serum albumin, Adv. Protein Chem. 37, 161-245.   DOI
12 Porter, P.L., Sage, E.H., Lane, T.F., Funk, S.E., Gown, A.M., 1995. Distribution of SPARC in normal and neoplastic human tissue. J. Histochem. Cytochem. 43, 791-800.   DOI   ScienceOn
13 Purcell, M., Neault, J.F., Tajmir-Riahi, H.A., 2000. Interaction of Taxol with human serum albumin. Biochim. Biophys. Acta. 1478, 61-68.   DOI
14 Reis, C.P., Neufeld, R.J., Ribeiro, A.J., Veiga, F., 2006. Nanoencapsulation I. Methods for preparation of drug-loaded polymeric nanoparticles. Nanomedicine 2, 8-21.   DOI   ScienceOn
15 Rustgi, V.K., 2009. Albinterferon alfa-2b, a novel fusion protein of human albumin and human interferon alfa-2b, for chronic hepatitis C. Curr. Med. Res. Opin. 25, 991-1002.   DOI
16 Sah, H., 1999. Stabilization of proteins against methylene chloride/water interface-induced denaturation and aggregation. J. Control. Release 58, 143-151.   DOI
17 Sheu, M.T., Moustafa, M.A., Sokoloski, T.D., 1986. Entrapment of bioactive compounds within native albumin beads: II. Effects of rate and extent of crosslinking on microbead properties. J. Parent. Sci. Technol. 40, 253-258.
18 Meeh, L., Cacheris, W.P., 1994. Microfluidization of calcium/oxyanion-containing particles. US Patent 5,342,609.
19 Sheu, M.T., Sokoloski, T.D., 1986. Entrapment of bioactive compounds within native albumin beads: III. Evaluation of parameters affecting drug release. J. Parent. Sci. Technol. 40, 259-265.
20 Sheu, M.T., Sokoloski, T.D., 1991. Entrapment of bioactive compounds within native albumin beads: IV. Characterization of drug release from polydisperse systems. Int. J. Pharm. 71, 7-18.   DOI
21 Merisko-Liversidge, E., Sarpotdar, P., Bruno, J., Hajj, S., Wei, L., Peltier, N., Rake, J., Shaw, J.M., Pugh, S., Polin, L., Jones, J., Corbett, T., Cooper, E., Liversidge, G.G., 1996. Formulation and antitumor activity evaluation of nanocrystalline suspensions of poorly soluble anticancer drugs. Pharm. Res. 13, 272-278.   DOI
22 Michaelis, K., Hoffmann, M.M., Dreis, S., Herbert, E., Alyautdin, R.N., Michaelis, M., Kreuter, J., Langer, K., 2006. Covalent linkage of apolipoprotein E to albumin nanoparticles strongly enhances drug transport into the brain. J. Pharm. Exp. Ther. 317, 1246-1253.   DOI
23 Minshall, R.D., Tiruppathi, C., Vogel, S.M., Malik, A.B., 2002. Vesicle formation and trafficking in endothelial cells and regulation of endothelial barrier function. Histochem. Cell Biol. 117, 105-112.   DOI
24 Morlock, M., Knoll, H., Winter, G., Kissel, T., 1997. Microencapsulation of rh-erythropoietin, using biodegradable poly (D,L-lactide-co-glycolide): protein stability and the effects of stabilizing excipients. Eur. J. Pharm. Biopharm. 43, 29-36.   DOI
25 Mosqueira, V.C., Legrand, P., Morgat, J.L., Vert, M., Mysiakine, E., Gref, R., Devissaguet, J.P., Barratt, G., 2001. Biodistribution of long-circulating PEG-grafted nanocapsules in mice: effects of PEG chain length and density. Pharm. Res. 18, 1411-1419.   DOI
26 Kreuter, J., 2004. Nanoparticles as drug delivery systems. In Nalwa, H.S. (Ed.), Encyclopedia of Nanoscience and Nanotechnology, vol. 7. American Scientific Publishers, Stevenson Ranch, USA, 161-180.
27 Muller, G.M., Leuenberger, H., Kissel, T., 1996. Albumin nanospheres as carriers for passive drug targeting: an optimized manufacturing technique. Pharm. Res. 13, 32-37.   DOI
28 Ohkawa, K., Hatano, T., Yamada, K., Joh, K., Takada, K., Tsukada, Y., Matsuda, M., 1993. Bovine serum albumin-doxorubicin conjugate overcomes multidrug resistance in a rat hepatoma. Cancer Res. 53, 4238-4242.
29 Paal, K., Muller, J., Hegedus, L., 2001. High affinity binding of paclitaxel to human serum albumin. Eur. J. Biochem. 268, 2187-2191.   DOI
30 Kumar, G.N., Walle, U.K., Bhalla, K.N., Walle, T., 1993. Binding of taxol to human plasma, albumin, and alpha1-acid glycoprotein. Research Communications in Chemical Pathology and Pharmacology 80, 337-344.
31 Lambert, G., Fattal, E., Pinto-Alphandary, H., Gulik, A., Couvreur, P., 2000. Polyisobutylcyanoacrylate nanocapsules containing an aqueous core as a novel colloidal carrier for the delivery of oligonucleotides. Pharm. Res. 17, 707-714.   DOI
32 Langer, K., Balthasar, S., Vogel, V., Dinauer, N., von Briesen, H., Schubert, D., 2003. Optimization of the preparation process for human serum albumin (HSA) nanoparticles. Int. J. Pharm. 257, 169-180.   DOI
33 Lee, T.K., Sokoloski, T.D., Royer, G.P., 1981. Serum albumin beads: an injectable, biodegradable system for the sustained release of drugs. Science 213, 233-235.   DOI
34 Lidgate, D.M., Tranner, T., Shultz, R.M., Maskiewicz, R., 1990. Sterile filtration of a parenteral emulsion. Pharm. Res. 9, 860-863.   DOI
35 Koosha, F., Muller, R.H., 1988. Nanoparticle production by microfluidization. Archiv Der Pharmazie 321, 680.
36 John, T.A., Vogel, S.M., Tiruppathi, C., Malik, A.B., Minshall, R.D., 2003. Quantitative analysis of albumin uptake and transport in the rat microvessel endothelialmonolayer. Am. J. Physiol., Lung Cell. Mol. Physiol. 284, 187-196.   DOI
37 Jung, T., Kamm, W., Breitenbach, A., Kaiserling, E., Xiao, J.X., Kissel, T., 2000. Biodegradable nanoparticles for oral delivery of peptides: is there a role for polymers to affect mucosal uptake? Eur. J. Pharm. Biopharm. 50, 147-160.   DOI
38 Kloover, J.S., den Bakker, M.A., Gelderblom, H., van Meerbeeck, J.P., 2004. Fatal outcome of a hypersensitivity reaction to paclitaxel: a critical review of premedication regimens. Br. J. Cancer 90, 304-305.   DOI
39 Kragh-Hansen, U., 1981. Molecular aspects of ligand binding to serum albumin. Pharmacological Reviews 33, 17-53.
40 Garrido, M.J., Jimenez, R.M., Rodriguez-Sasiain, J.M., Aguirre, C., Aguilera, L., Calvo, R., 1994. Caracterizacion de la fijacion de propofol a las proteinas plasmaticas y posibles interacciones. Rev. Esp. Anestestiol. Reanim. 41, 308-312.
41 Gelderblom, H., Verweij, J., Nooter, K., Sparreboom A., 2001. Cremophor EL: The drawbacks and advantages of vehicle selection for drug formulation. Eur. J. Cancer 37, 1590-1598.   DOI
42 Gianni, L., Kearns, C.M., Giani, A., Capri, G., Vigano, L., Lacatelli, A., Bonadonna, G., Egorin, M.J., 1995. Nonlinear pharmacokinetics and metabolism of paclitaxel and its pharmacokinetic/pharmacodynamic relationships in humans. J. Clin. Oncol. 13, 180-190.   DOI
43 Gligorov, J., Lotz, J.P., 2004. Preclinical pharmacology of the taxanes: implications of the differences. Oncologist 9, 3-8.
44 Dye, D., Watkins, J.,1980. Suspected anaphylactic reaction to Cremophor EL. Br. Med. J. 280, 1353.
45 Doegito, E., Fessi, H., Appel, M., Puisieux, F., Bolard, J., Devissaguet, J.P., 1994. New techniques for preparing submicronic emulsions-application to Amphotericine-B. STP Pharma Sciences 4, 155-162.
46 Dreis, S., Rothweiler, F., Michaelis, M., Cinatl Jr., J., Kreuter, J., Langer, K., 2007. Preparation, characterisation and maintenance of drug efficacy of doxorubicin-loaded human serum albumin (HSA) nanoparticles. Int. J. Pharm. 341, 207-214.   DOI
47 Duncan, R., 2003. The dawning era of polymer therapeutics. Nat. Rev. Drug Discov. 2, 347-360.   DOI
48 Eatock, M., Church, N., Harris, R., Angerson, W., McArdle, C., French, R., Twelves, C., 1999. Activity of doxorubicin covalently bound to a novel human serum albumin microcapsule. Invest. New Drugs 17, 111-120.   DOI
49 Faithfull, N.S., Cain, S.M., 1988. Cardiorespiratory consequences of flurocarbon reactions in dogs. Bio. Art. Organs 16, 463-472.
50 Fehske, K.J., Muller, W.E., Wollert, U., 1981. The location of drug binding sites in human serum albumin. Biochem Pharmacol. 30, 687-692.   DOI
51 Couvreur, P., Vauhtier, C., 2006. Nanotechnology: intelligent design to treat complex disease. Pharm. Res. 23, 1417-1450.   DOI
52 Curry, S., Mandelkow, H., Brick, P., Franks, N., 1998. Crystal structure of human serum albumin complexed with fatty acid reveals an asymmetric distribution of binding sites. Nat. Struct. Biol. 5, 827-835.   DOI
53 Carter, D.C., Ho, J.X., 1994. Structure of serum albumin. Adv. Protein Chem. 45, 153-203.   DOI
54 Barraud, L., Merle, P., Soma, E., Lefrancois, L., Guerret, S., Chevallier, M., Dubernet, C., Couvreur, P., Trepo, C.,Vitvitski, L., 2005. Increase of doxorubicin sensitivity by doxorubicin-loading into nanoparticles for hepatocellular carcinoma cells in vitro and in vivo. J. Hepatol. 42, 736-743.   DOI
55 Bodmeier, R., Chen, H., 1990. Indomethacin polymeric nanosuspensions prepared by microfluidization. J. Control. Release 12, 223-233.   DOI
56 Busch-vishniac, I., Buckman, A.B., Pavuluri, J.K., Wang, W., Qian, D., Mancevski, V., 1996. Noncontact position measurement system using optical sensors. US Patent 5,552,883.
57 Chanasattru, W., Jones, O.G., Decker, E.A., McClements, D.J., 2009. Impact of cosolvents on formation and properties of biopolymer nanoparticles formed by heat treatment of ${\beta}$ -lactoglobulin-pectin complexes. Food Hydrocolloids 23, 2450-2457   DOI
58 Chen, G.Q., Lin, W., Coombes, A.G.A., Davis, S.S., Illum, L., 1994. Preparation of human serum albumin microspheres by a novel acetone-heat denaturation method. J. Microencapsulation 11, 395-407.   DOI
59 Coombes, A.G.A., Breeze, V., Lin, W., Gray, T., Parker, K.G., Parker, T., 2001. Lactic acid-stabilized albumin for microsphere formation and biomedical coating. Biomaterials 22, 1-8.   DOI
60 Coombes, A.G.A., Lin, W., O'Hagen, D.T., Davis, S.S., 2003. Preparation of protein microspheres, films and coating. US Patent 6,592,844.
61 Ten Tije, A.J., Verweij, J., Loos, W.J., Sparreboom, A., 2003. Pharmacological effects of formulation vehicles: implications for cancer chemotherapy. Clin. Pharmacokinet. 42, 665-685.   DOI
62 Slack, J.D., Kanke, M., Simmons, G.H., DeLuca, P.P., 1981. Acute hemadynamic effects and blood pool kinetics of polystyrene microspheres following intravenous administration. J. Pharm. Sci. 70, 660-664.   DOI
63 Sugio, S., Kashima, A., Mochizuki, S., Noda, M., Kobayashi, K., 1999. Crystal structure of human serum albumin at 2.5 ${\AA}$ resolution. Protein Eng. 12, 439-446.
64 Talsma, H., Ozer, A.Y., VanBloois, L., Crommelin, D.J., 1989. The size reduction of liposomes with a high pressure homogenizer (microfluidizer): Characterization of prepared dispersions and comparison with conventional methods. Drug Dev. Ind. Pharm. 15, 197-207.   DOI
65 Thibaudeau, K., Léger, R., Huang, X., Robitaille, M., Quraishi, O., Soucy, C., Bousquet-Gagnon, N., van Wyk, P., Paradis, V., Castaigne, J.P., Bridon, D., 2005. Synthesis and evaluation of insulin-human serum albumin conjugates. Bioconjugate Chemistry 16, 1000-1008.   DOI
66 Tomkin, G.H., 2009. Albiglutide, an albumin-based fusion of glucagon-like peptide 1 for the potential treatment of type 2 diabetes. Curr. Opin. Mol. Ther. 11, 579-588.
67 Torchilin, V.P., Trubetskoy, V.S., 1995. Which polymers can make nanoparticulate drug carriers long-circulating? Adv. Drug Deliv. Rev. 16, 141-155.   DOI
68 Lorenz, W., Reimann, H.J., Schmal, A., Dormann, P., Schwarz, B., Neugebauer, E., Doenicke, A., 1977. Histamine release in dogs by Cremophore EL and its derivatives: Oxethylated oleic acid is the most effective constituent. Agents and Actions 7, 63-67.   DOI
69 Liversidge, G.G., Cundy, K.C., Bishop, J.F., Czekai, D.A., 1992. Surface modified drug nanoparticles. US Patent 5,145,684.
70 Liversidge, G.G., Liversidge, E., Sarpotdar, P.P., 1995. Surface modified anticancer nanoparticles. US Patent 5,399,363.
71 Maeda, H., Wu, J., Sawa, T., Matsumura, Y., Hori, K., 2000. Tumor vascular permeability and the EPR effect in macromolecular therapeutics: a review. J. Control. Release 65, 271-284.   DOI   ScienceOn
72 Howard, K.A., Kjems, J., 2007. Polycation-based nanoparticle delivery for improved RNA interference therapeutics. Expert. Opin. Biol. Ther. 7, 1811–1822.
73 Ibrahim, N.K., Desai, N., Legha, S., Soon-Shiong, P., Theriault, R.L., Rivera, E., Esmaeli, B., Ring, S.E., Bedikian, A., Hortobagyi, G.N., Ellerhorst, J.A., 2002. Phase I and pharmacokinetic study of ABI-007, a cremophor-free, proteinstabilized, nanoparticle formulation of paclitaxel. Clin. Cancer Res. 8, 1038-1044.
74 Ikuta, S., Chuang, V.T.G., Ishima, Y., Nakajou, K., Furukawa, M., Watanabe, H., Maruyama, T., Otagiri, M., 2010. Albumin fusion of thioredoxinæThe production and evaluation of its biological activity for potential therapeutic applications. J. Control. Release 147, 17-23.   DOI
75 Jette, L., Léger, R., Thibaudeau, K., Benquet, C., Robitaille, M., Pellerin, I., Paradis, V., van Wyk, P., Pham, K., Bridon D.P., 2005. Human growth hormone-release factor (hGRF)1-29-albumin bioconjugates activate the GRF receptor on the anterior pituitary in rats: Identification of CJC-1295 as a long-lasting GRF analog. Endocrinology 146, 3052-3058.   DOI
76 Hawkins, M.J., Soon-Shiong, P., Desai, N., 2008. Protein nanoparticles as drug carriers in clinical medicine. Advanced Drug Delivery Reviews 60, 876-885.   DOI
77 Gradishar, W.J., Tjulandin, S., Davidson, N., Shaw, H., Desai, N., Bhar, P., Hawkins, M., O’Shaughnessy, J., 2005. Phase III trial of nanoparticle albumin-bound paclitaxel compared with polyethylated castor oil-based paclitaxel in women with breast cancer. J. Clin. Oncol. 23, 7794-7803.   DOI
78 Gregoriadis, G., Da Silva, H., Florence, A.T., 1990. A procedure for the efficient entrapment of drugs in dehydration-rehydration liposomes (DRVs). Int. J. Pharm. 65, 235-242.   DOI
79 Grunewalder, J.F., Voelker, M.A., 1993. Water-borne treatment compositions for porous substrates. US Patent 5,228,905.
80 He, X.M., Carter, D.C., 1992. Atomic structure and chemistry of human serum albumin. Nature 358, 209-215.   DOI
81 Holmes, D.L., Thibaudeau, K., L'Archevêque, B., Milner, P.G., Ezrin, A.M., Bridon, D.P., 2000. Site specific 1:1 opoid:albumin conjugate with in vitro activity and long in vivo duration. Bioconjugate Chemistry 11, 439-444.   DOI
82 Desai, N.P., Soon-Shiong, P., Sandford, P.A., Grinstaff, M.W., Suslick, K.S., 1995. Methods for in vivo delivery of substantially water insoluble pharmacologically active agents and compositions useful therefor. US Patent 5,439,686.
83 Desai, N.P., Tao, C., Yang, A., Louie, L., Zheng, T., Yao, Z., Soon-Shiong, P., Magdassi, S., 1999. Protein stabilized pharmacologically active agents, methods for the preparation thereof and methods for the use thereof. US Patent 5,916,596.
84 Desai, N.P., Yang, A., De, T., Ci, S.X., Soon-shiong, P., Trieu, V., Yao, O., Grim, B.B., 2005. Compositions and methods of delivery of pharmacological agents. US Patent app. Pub. No. 2005/0004002A1.
85 Desai, N., Trieu, V., Yao, Z., Louie, L., Ci, S., Yang, A., Tao, C., De, T., Beals, B., Dykes, D., Noker, P., Yao, R., Labao, E., Hawkins, M., Soon-Shiong, P., 2006. Increased antitumor activity, intratumor paclitaxel concentrations, and endothelial cell transport of cremophor-free, albumin-bound paclitaxel, ABI-007, compared with cremophor-based paclitaxel. Clin. Cancer Res. 12, 1317-1324.   DOI   ScienceOn
86 Damascelli, B., Cantu, G., Mattavelli, F., Tamplenizza, P., Bidoli, P., Leo, E., Dosio, F., Cerrotta, A.M., Di Tolla, G., Frigerio, L.F., Garbagnati, F., Lanocita, R., Marchiano, A., Patelli, G., Spreafico, C., Ticha, V., Vespro, V., Zunino, F., 2001. Intraarterial chemotherapy with polyoxyethylated castor oil free paclitaxel, incorporated in albumin nanoparticles (ABI-007): phase II study of patients with squamous cell carcinoma of the head and neck and anal canal: preliminary evidence of clinical activity. Cancer 92, 2592-2602.   DOI
87 De Garavilla, L., Liversidge, E.M., Liversidge, G.G., 1998. Reduction of intravenously administered nanoparticulate-formulation-induced adverse physiological reactions. US Patent 5,834,025.
88 Desai, N., Trieu, V., Vao, R., Frankel, T., Soon-Shiong, P., 2004. SPARC expression in breast tumors may correlate to increased tumor distribution of nanoparticle albumin-bound paclitaxel (ABI-007) vs Taxol. Presented at the 27th Annual San Antonio Breast Cancer Symposium, San Antonio, Texas.
89 Desai, N.P., Soon-Shiong, P., De, T.K., 2010. Methods and compositions for treating proliferative diseases. US Patent 7,780,984.
90 Avgoustakis, K., 2004. Pegylated poly(lactide) and poly(lactidecoglycolide) nanoparticles: preparation, properties and possible applications in drug delivery. Curr. Drug Deliv. 1, 321-333.   DOI
91 Bagchi, P., Stewart, R.C., Mclntire, G.L., Minter, J.R., 1997. Microprecipitation of micro-nanoparticulate pharmaceutical agents. US Patent 5,662,883.
92 Altmayer, P., Büch, U., Büch, H.P., 1995. Arzneimittelforschung 45, 1053-1056.