Transcript Slide 1

Technology Licensing Opportunity
Gene Bound Cationic Polymer Assemblies Based on Fully
Degradable Carbonate Platform
Keywords:
(1) Self-assembled nanoparticles with potential for drug, protein and gene
delivery
(2) Biodegradable carbonate-based copolymers synthesized by organocatalytic
ring-opening polymerization method
Key Features
• Lower cytotoxicity
than many other
polymers reported
• Molecular weight
& functionalities of
the polymers can be
easily controlled
Background:
Although PEI (Polyethylene imines) is recognized as a good nonviral vector with
superior transfection efficiency due to high positive charge density to form
compacted polyplexes as well as high density of near-neutral pka group for
buffering, it is not biodegradable and considered highly cytotoxic. Hence, the major
challenge in the design of synthetic transfection vectors is cationic polymers
showing low cytotoxicity with spontaneously high transfection efficiency. The other
cationic polymers, such as modified PEIs, poly(amino acid)s, poly(betaaminosulfonamide)s (PBASs), dendrimers based on poly(L-lysine) (PLL) and
poly(amidoamine) (PAMAM) dendrimers have also been reported as efficient
nonviral vectors for safe gene delivery.
• Ease of scaling up
Patents
A patent application
have been filed for
this technology
Key issues with these polymers are:
(a)Broad distributed molecular weight
(b)Difficulty in controlling molecular structure
(c)High cost of production
Publications
Unpublished
Commercialisation
CF
Polymer-gene complexation via electrostatic interactions is an effective
trafficking
Opportunities
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R-(OH)
and
protection
strategy
for
genetic
materials,
however,
this
tight
packing
also
(i)
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Technology is
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OHpresents a problem in the unpacking of genes
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available for HO
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licensing from
The Invention:
OBn
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Exploit
The
formation
of
a
library
of
functional
cyclic carbonate monomers and used in (ii)
Technologies PteBnMPA
1
various
combinations
to
provide
polymers
with both quaternary amine for
Ltd.
1a; m = 3, X = Cl
gene-binding, tertiary amines
for
buffering
and
functionalities to facilitate cargo
1b; m = 3. X = Br
1c; m = 2, X = I
These polymers
by organocatalytic ring-opening
OHrelease.
1d; m =were
1, X =prepared
H
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polymerization
(ROP)
that
allows
exquisite
control
over the molecular
weight
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Exploit
R
O
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OHand narrow polydispersities, and is tolerant to a variety of functional groups.
Technologies
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Private Limited Bis-MPA
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These polycarbonates for gene
delivery
have the following generic chemical
(A member of
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structure:
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2a; m = 3, X = Cl, R
30 Biopolis Street,
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2b; m = 3. X = Br, R
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#09-02 Matrix
2c; m = 2, X = I, R =
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2d; m = 3, X = Br, R
Singapore 138671
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3a; m = 3, X = Cl, R
Email: bms_techX
3b-L; m = 3. X = Br,
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3b-D; m = 3, X = Br,
m~3
offer@exploitN
4,
5
tech.com
3
2
3
m~3
a
b
2
+
4a;
4b;
4c;
4d;
m
m
m
m
=
=
=
=
3,
3.
2,
3,
X
X
X
X
=
=
=
=
Cl, R = BnMPA, a : b = 0 : 1
Br, R = BnMPA, a : b = 0 : 1
I, R = BnMPA, a : b = 0 : 1
Br, R = BnMPA, a : b = 1 : 1
5a; m = 3, X = Cl, R = PTMC, a : b = 0 : 1
5b-L; m = 3. X = Br, R = PLLA, a : b = 0 : 1
5b-D; m = 3, X = Br, R = PDLA, a : b = 0 : 1
Disclaimer
Although due care and attention have been taken to ensure that the preparation of this material is as accurate as possible, the contents of this
brochure are provided for information purposes only. Neither the Agency for Science, Technology and Research, Exploit Technologies Pte Ltd nor
the inventors offer any warranty, written expressed or implied, as to the accuracy of the said contents. Applicants are advised to undertake
independent evaluation of the technology.
Technology Licensing Opportunity
Potential Applications:
(1) Drug, gene and protein delivery
The Advantages:
(1) These polymers have lower cyctotoxicity than many other polymers
reported in the literature
(2) The molecular weight and functionalities of the polymers can be easily
controlled, and the synthesis of these polymers can be readily scaled
up in large quantities for preclinical and clinical trials
Disclaimer
Although due care and attention have been taken to ensure that the preparation of this material is as accurate as possible, the contents of this
brochure are provided for information purposes only. Neither the Agency for Science, Technology and Research, Exploit Technologies Pte Ltd nor
the inventors offer any warranty, written expressed or implied, as to the accuracy of the said contents. Applicants are advised to undertake
independent evaluation of the technology.