overcoming physiological barriers, such as the blood–brain barrier [70], suggesting
the potential for reaching inaccessible tissues in the body after systemic injection of
these nanoassemblies.
Macromolecular nanoassemblies have the potential to control the intracellular
trafficking and subcellular delivery of their cargo, which can augment the activity
of the incorporated drugs [71]. For example, polymeric micelles incorporating
(1,2-diaminocyclohexane)platinum(II) selectively delivered the drug to its therapeutic target (i.e., nuclear DNA), which allowed the micelles to overcome cytoplasmic resistance mechanisms [72]. For delivering genes, nanoassemblies should
escape from endosomes into the cytoplasm or nucleus. Various mechanisms such as
pore formation in the lipid bilayer of endosomes, fusion with the endosomal
membrane, and the pH-buffering effect of protonable moieties have been proposed
for assisting in the endosomal escape of nanoassemblies [73]. Moreover, several
cell-penetrating peptides can be installed on the surface of nanoassemblies for
translocation across the plasma membrane into the cytosol of cells, which enhances
the delivery of their cargo [74]. In addition, installation of ligands on the surface of
nanoassemblies may also direct their subcellular localization after reaching the
cytosol [75].
Supramolecular structures allow the complexity and functions to be increased
for producing innovative nanodevices in which loaded materials and the carrier are
integrated both structurally and functionally for sensing, processing, reporting, and
operating inside the cells [76], undertaking precise roles at specific subcellullar
compartments. Staudinger’s dream of polymers and the biosciences is here and
now, and the continuous innovations in materials and polymer sciences, together
with life sciences, will keep promoting the development of novel synthetic biopolymers, with unparalleled control of supramolecular architectures and unprecedented biological activities. These new polymeric structures will eventually allow
controlled in situ interaction with specific biomolecules, modulating their expression and tailoring their function in molecular and physiological events.
References
1. Staudinger H (1920) U ¨ ber polymerisation. Ber Dtsch Chem Ges A/B 53:1073–1085
2. Nobelprize.org (1964) Hermann Staudinger – Nobel lecture, December 11, 1953: Macromolecular chemistry. In: Nobel lectures, chemistry 1942–1962. Elsevier, Amsterdam. http://
www.nobelprize.org/nobel_prizes/chemistry/laureates/1953/staudinger-lecture.pdf
3. Charnley J (1960) Anchorage of the femoral head prosthesis to the shaft of the femur. J Bone Jt
Surg 42-B:28–30
4. Harken DE, Taylor WJ, Lefemine AA, Lunzer S, Low HB, Cohen ML, Jacobey JA (1962)
Aortic valve replacement with a caged ball valve. Am J Cardiol 9:292–299
5. Eilert JB, Binder P, McKinney PW, Beal JM, Conn J Jr (1971) Polyglycolic acid synthetic
absorbable sutures. Am J Surg 121:561–565
6. Jatzkewitz H (1955) Peptamin (glycyl-L-leucyl-mescaline) bound to blood plasma expander
(polyvinylpyrrolidone) as a new depot form of a biologically active primary amine (mescaline). Z Naturforsch 10:27–31
258
H. Cabral and K. Kataoka
the potential for reaching inaccessible tissues in the body after systemic injection of
these nanoassemblies.
Macromolecular nanoassemblies have the potential to control the intracellular
trafficking and subcellular delivery of their cargo, which can augment the activity
of the incorporated drugs [71]. For example, polymeric micelles incorporating
(1,2-diaminocyclohexane)platinum(II) selectively delivered the drug to its therapeutic target (i.e., nuclear DNA), which allowed the micelles to overcome cytoplasmic resistance mechanisms [72]. For delivering genes, nanoassemblies should
escape from endosomes into the cytoplasm or nucleus. Various mechanisms such as
pore formation in the lipid bilayer of endosomes, fusion with the endosomal
membrane, and the pH-buffering effect of protonable moieties have been proposed
for assisting in the endosomal escape of nanoassemblies [73]. Moreover, several
cell-penetrating peptides can be installed on the surface of nanoassemblies for
translocation across the plasma membrane into the cytosol of cells, which enhances
the delivery of their cargo [74]. In addition, installation of ligands on the surface of
nanoassemblies may also direct their subcellular localization after reaching the
cytosol [75].
Supramolecular structures allow the complexity and functions to be increased
for producing innovative nanodevices in which loaded materials and the carrier are
integrated both structurally and functionally for sensing, processing, reporting, and
operating inside the cells [76], undertaking precise roles at specific subcellullar
compartments. Staudinger’s dream of polymers and the biosciences is here and
now, and the continuous innovations in materials and polymer sciences, together
with life sciences, will keep promoting the development of novel synthetic biopolymers, with unparalleled control of supramolecular architectures and unprecedented biological activities. These new polymeric structures will eventually allow
controlled in situ interaction with specific biomolecules, modulating their expression and tailoring their function in molecular and physiological events.
References
1. Staudinger H (1920) U ¨ ber polymerisation. Ber Dtsch Chem Ges A/B 53:1073–1085
2. Nobelprize.org (1964) Hermann Staudinger – Nobel lecture, December 11, 1953: Macromolecular chemistry. In: Nobel lectures, chemistry 1942–1962. Elsevier, Amsterdam. http://
www.nobelprize.org/nobel_prizes/chemistry/laureates/1953/staudinger-lecture.pdf
3. Charnley J (1960) Anchorage of the femoral head prosthesis to the shaft of the femur. J Bone Jt
Surg 42-B:28–30
4. Harken DE, Taylor WJ, Lefemine AA, Lunzer S, Low HB, Cohen ML, Jacobey JA (1962)
Aortic valve replacement with a caged ball valve. Am J Cardiol 9:292–299
5. Eilert JB, Binder P, McKinney PW, Beal JM, Conn J Jr (1971) Polyglycolic acid synthetic
absorbable sutures. Am J Surg 121:561–565
6. Jatzkewitz H (1955) Peptamin (glycyl-L-leucyl-mescaline) bound to blood plasma expander
(polyvinylpyrrolidone) as a new depot form of a biologically active primary amine (mescaline). Z Naturforsch 10:27–31
258
H. Cabral and K. Kataoka