28. Yokoyama M, Inoue S, Kataoka K, Yui N, Okano T, Sakurai Y (1989) Molecular design for
missile drug: synthesis of adriamycin conjugated with immunoglobulin G using poly(ethylene
glycol)-block-poly(aspartic acid) as intermediate carrier. Makromol Chem 190:2041–2054
29. Yokoyama M, Miyauchi M, Yamada N, Okano T, Sakurai Y, Shohei I, Kataoka K (1990)
Polymeric micelles as novel drug carrier: adriamycin-conjugated poly(ethylene glycol)–poly
(aspartic acid) block copolymer. J Contr Release 11:269–278
30. Matsumura Y, Hamaguchi T, Ura T, Muro K, Yamada Y, Shimada Y, Shirao K, Okusaka T
(2004) Phase I clinical trial and pharmacokinetic evaluation of NK911, a micelle-encapsulated
doxorubicin. Br J Cancer 91:1775–1781
31. Matsumura Y, Kataoka K (2009) Preclinical and clinical studies of anticancer agentincorporating polymer micelles. Cancer Sci 100:572–579
32. Plummer R, Wilson RH, Calvert H, Boddy AV, Griffin M, Sludden J, Tilby MJ, Eatock M,
Pearson DG, Ottley CJ, Matsumura Y, Kataoka K, Nishiya T (2011) A phase I clinical study of
cisplatin-incorporated polymeric micelles (NC-6004) in patients with solid tumours. Br J
Cancer 104:593–598
33. Kato K, Chin K, Yoshikawa T, Yamaguchi K, Tsuji Y, Esaki T, Sakai K, Kimura M,
Hamaguchi T, Shimada Y, Matsumura Y, Ikeda R (2012) Phase II study of NK105, a
paclitaxel-incorporating micellar nanoparticle, for previously treated advanced or recurrent
gastric cancer. Invest New Drugs 30:1621–1627
34. Kataoka K, Harada A, Nagasaki Y (2001) Block copolymer micelles for drug delivery: design,
characterization and biological significance, characterization and biological significance.
Adv Drug Deliv Rev 47:113–131
35. Nishiyama N, Kataoka K (2006) Current state, achievements, and future prospects of polymeric micelles as nanocarriers for drug and gene delivery. Pharmacol Ther 112:630–648
36. Nance EA, Woodworth GF, Sailor KA, Shih T-Y, Xu Q, Swaminathan G, Xiang D,
Eberhart C, Hanes J (2012) A dense poly(ethylene glycol) coating improves penetration of
large polymeric nanoparticles within brain tissue. Sci Transl Med 4:149ra119
37. Reddy ST, van der Vlies AJ, Simeoni E, Angeli V, Randolph GJ, O’Neil CP, Lee LK, Swartz MA,
Hubbell JA (2007) Exploiting lymphatic transport and complement activation in nanoparticle
vaccines. Nat Biotechnol 25:1159–1164
38. Cabral H, Matsumoto Y, Mizuno K, Chen Q, Murakami M, Kimura M, Terada Y, Kano MR,
Miyazono K, Uesaka M, Nishiyama N, Kataoka K (2011) Accumulation of sub-100 nm
polymeric micelles in poorly permeable tumours depends on size. Nat Nanotechnol 6:815–822
39. Cabral H, Kataoka K (2010) Multifunctional nanoassemblies of block copolymers for future
cancer therapy. Sci Technol Adv Mater 11:014109
40. Bae Y, Kataoka K (2009) Intelligent polymeric micelles from functional poly(ethylene
glycol)-poly(amino acid) block copolymers. Adv Drug Deliv Rev 61:768–784
41. Discher DE, Eisenberg A (2002) Polymeric vesicles. Science 297:967–973
42. Park S, Lim J-H, Chung S-W, Mirkin CA (2004) Self-assembly of mesoscopic metal-polymer
amphiphiles. Science 303:348–351
43. Harada A, Kataoka K (1995) Formation of polyion complex micelles in an aqueous milieu
from a pair of oppositely-charged block-copolymers with poly(ethylene glycol) segments.
Macromolecules 28:5294–5299
44. Harada A, Kataoka K (1999) Chain length recognition: core-shell supramolecular assembly
from oppositely charged block copolymers. Science 283:65–67
45. Kataoka K, Togawa H, Harada A, Yasugi K, Matsumoto T, Katayose S (1996) Spontaneous
formation of polyion complex micelles with narrow distribution from antisense oligonucleotide and cationic block copolymer in physiological saline. Macromolecules 29:8556–8557
46. Katayose S, Kataoka K (1997) Water-soluble polyion complex associates of DNA and poly
(ethylene glycol)–poly(L-lysine) block copolymer. Bioconjug Chem 8:702–707
47. Lee Y, Ishii T, Cabral H, Kim HJ, Seo JH, Nishiyama N, Oshima H, Osada K, Kataoka K
(2009) Charge-conversional PIC micelles – an efficient protein delivery nanocarrier into
cytoplasm. Angew Chem Int Ed 48:5309–5312
260
H. Cabral and K. Kataoka
missile drug: synthesis of adriamycin conjugated with immunoglobulin G using poly(ethylene
glycol)-block-poly(aspartic acid) as intermediate carrier. Makromol Chem 190:2041–2054
29. Yokoyama M, Miyauchi M, Yamada N, Okano T, Sakurai Y, Shohei I, Kataoka K (1990)
Polymeric micelles as novel drug carrier: adriamycin-conjugated poly(ethylene glycol)–poly
(aspartic acid) block copolymer. J Contr Release 11:269–278
30. Matsumura Y, Hamaguchi T, Ura T, Muro K, Yamada Y, Shimada Y, Shirao K, Okusaka T
(2004) Phase I clinical trial and pharmacokinetic evaluation of NK911, a micelle-encapsulated
doxorubicin. Br J Cancer 91:1775–1781
31. Matsumura Y, Kataoka K (2009) Preclinical and clinical studies of anticancer agentincorporating polymer micelles. Cancer Sci 100:572–579
32. Plummer R, Wilson RH, Calvert H, Boddy AV, Griffin M, Sludden J, Tilby MJ, Eatock M,
Pearson DG, Ottley CJ, Matsumura Y, Kataoka K, Nishiya T (2011) A phase I clinical study of
cisplatin-incorporated polymeric micelles (NC-6004) in patients with solid tumours. Br J
Cancer 104:593–598
33. Kato K, Chin K, Yoshikawa T, Yamaguchi K, Tsuji Y, Esaki T, Sakai K, Kimura M,
Hamaguchi T, Shimada Y, Matsumura Y, Ikeda R (2012) Phase II study of NK105, a
paclitaxel-incorporating micellar nanoparticle, for previously treated advanced or recurrent
gastric cancer. Invest New Drugs 30:1621–1627
34. Kataoka K, Harada A, Nagasaki Y (2001) Block copolymer micelles for drug delivery: design,
characterization and biological significance, characterization and biological significance.
Adv Drug Deliv Rev 47:113–131
35. Nishiyama N, Kataoka K (2006) Current state, achievements, and future prospects of polymeric micelles as nanocarriers for drug and gene delivery. Pharmacol Ther 112:630–648
36. Nance EA, Woodworth GF, Sailor KA, Shih T-Y, Xu Q, Swaminathan G, Xiang D,
Eberhart C, Hanes J (2012) A dense poly(ethylene glycol) coating improves penetration of
large polymeric nanoparticles within brain tissue. Sci Transl Med 4:149ra119
37. Reddy ST, van der Vlies AJ, Simeoni E, Angeli V, Randolph GJ, O’Neil CP, Lee LK, Swartz MA,
Hubbell JA (2007) Exploiting lymphatic transport and complement activation in nanoparticle
vaccines. Nat Biotechnol 25:1159–1164
38. Cabral H, Matsumoto Y, Mizuno K, Chen Q, Murakami M, Kimura M, Terada Y, Kano MR,
Miyazono K, Uesaka M, Nishiyama N, Kataoka K (2011) Accumulation of sub-100 nm
polymeric micelles in poorly permeable tumours depends on size. Nat Nanotechnol 6:815–822
39. Cabral H, Kataoka K (2010) Multifunctional nanoassemblies of block copolymers for future
cancer therapy. Sci Technol Adv Mater 11:014109
40. Bae Y, Kataoka K (2009) Intelligent polymeric micelles from functional poly(ethylene
glycol)-poly(amino acid) block copolymers. Adv Drug Deliv Rev 61:768–784
41. Discher DE, Eisenberg A (2002) Polymeric vesicles. Science 297:967–973
42. Park S, Lim J-H, Chung S-W, Mirkin CA (2004) Self-assembly of mesoscopic metal-polymer
amphiphiles. Science 303:348–351
43. Harada A, Kataoka K (1995) Formation of polyion complex micelles in an aqueous milieu
from a pair of oppositely-charged block-copolymers with poly(ethylene glycol) segments.
Macromolecules 28:5294–5299
44. Harada A, Kataoka K (1999) Chain length recognition: core-shell supramolecular assembly
from oppositely charged block copolymers. Science 283:65–67
45. Kataoka K, Togawa H, Harada A, Yasugi K, Matsumoto T, Katayose S (1996) Spontaneous
formation of polyion complex micelles with narrow distribution from antisense oligonucleotide and cationic block copolymer in physiological saline. Macromolecules 29:8556–8557
46. Katayose S, Kataoka K (1997) Water-soluble polyion complex associates of DNA and poly
(ethylene glycol)–poly(L-lysine) block copolymer. Bioconjug Chem 8:702–707
47. Lee Y, Ishii T, Cabral H, Kim HJ, Seo JH, Nishiyama N, Oshima H, Osada K, Kataoka K
(2009) Charge-conversional PIC micelles – an efficient protein delivery nanocarrier into
cytoplasm. Angew Chem Int Ed 48:5309–5312
260
H. Cabral and K. Kataoka