TY - JOUR
T1 - Molecular design of biodegradable polymeric micelles for temperature-responsive drug release
AU - Nakayama, Masamichi
AU - Okano, Teruo
AU - Miyazaki, Takanari
AU - Kohori, Fukashi
AU - Sakai, Kiyotaka
AU - Yokoyama, Masayuki
N1 - Funding Information:
This work was supported by the Ministry of Education, Culture, Sports, Science and Technology, Japan (a Millenium project No. 12415, Grant No. 10145104 on Priority areas, No. 296, Bio-molecular Design for Biotargeting, and the Program for Promoting the Establishment of Strategic Research Centers, Special Coordination Funds for Promoting Science and Technology), the Japan Society for the Promotion of Science (The Grant-in-Aid for Young Scientists (B) No. 16700368), and the Ministry of Health, Labour and Welfare of Japan.
PY - 2006/9/28
Y1 - 2006/9/28
N2 - We designed thermo-responsive and biodegradable polymeric micelles for an ideal drug delivery system whose target sites are where external stimuli selectively release drugs from the polymeric micelles. The thermo-responsive micelles formed from block copolymers that were composed both of a hydrophobic block and a thermo-responsive block. Poly(N-isopropylacrylamide-co-N,N-dimethylacrylamide) showing a lower critical solution temperature (LCST) around 40 °C was synthesized for the thermo-responsive block, while biodegradable poly(d,l-lactide), poly(ε-caprolactone), or poly(d,l-lactide-co-ε-caprolactone) was used for the hydrophobic block. By changing both the block lengths of the poly(d,l-lactide)-containing block copolymers, physical parameters such as micelle diameter and critical micelle concentration were varied. On the other hand, the choice of the hydrophobic block was revealed to be critical in relation to both on the thermo-responsive release of the incorporated anti-cancer drug, doxorubicin, and the temperature-dependent change of the hydrophobicity of the micelles' inner core. One polymeric micelle composition successfully exhibited rapid and thermo-responsive drug release while possessing a biodegradable character.
AB - We designed thermo-responsive and biodegradable polymeric micelles for an ideal drug delivery system whose target sites are where external stimuli selectively release drugs from the polymeric micelles. The thermo-responsive micelles formed from block copolymers that were composed both of a hydrophobic block and a thermo-responsive block. Poly(N-isopropylacrylamide-co-N,N-dimethylacrylamide) showing a lower critical solution temperature (LCST) around 40 °C was synthesized for the thermo-responsive block, while biodegradable poly(d,l-lactide), poly(ε-caprolactone), or poly(d,l-lactide-co-ε-caprolactone) was used for the hydrophobic block. By changing both the block lengths of the poly(d,l-lactide)-containing block copolymers, physical parameters such as micelle diameter and critical micelle concentration were varied. On the other hand, the choice of the hydrophobic block was revealed to be critical in relation to both on the thermo-responsive release of the incorporated anti-cancer drug, doxorubicin, and the temperature-dependent change of the hydrophobicity of the micelles' inner core. One polymeric micelle composition successfully exhibited rapid and thermo-responsive drug release while possessing a biodegradable character.
KW - Biodegradable polymer
KW - Polymeric micelle
KW - Targeting
KW - Temperature
KW - Thermo-response
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U2 - 10.1016/j.jconrel.2006.07.007
DO - 10.1016/j.jconrel.2006.07.007
M3 - Article
C2 - 16920217
AN - SCOPUS:33748870763
SN - 0168-3659
VL - 115
SP - 46
EP - 56
JO - Journal of Controlled Release
JF - Journal of Controlled Release
IS - 1
ER -
