Poly(Beta-Amino Ester)s With Additives for Drug Delivery
AssigneeSagetis Biotech, Sl
InventorsSejin OH, Salvador BORROS GOMEZ
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Abstract
Disclosed are nanoparticles comprising an end-modified poly(β-amino ester) and an additive that is a sugar or sugar derivative, such as a sugar, a sugar alcohol or chitosan. The nanoparticles may be used in any field where polymers have been found useful, including in medical fields, particularly in drug delivery. The polymers are useful in delivering a polynucleotide such as DNA, RNA or siRNA, a small molecule or a protein. Also disclosed are compositions comprising said nanoparticles and an active agent, methods for preparing said nanoparticles, said nanoparticles and compositions for use in medicine, and in vitro methods using said nanoparticles and compositions.
Claims26
A nanoparticle comprising an end-modified poly(β-amino ester) and 1 to 35 weight percent, relative to the end-modified poly(β-amino ester), of a sugar or sugar alcohol.
A nanoparticle comprising an end-modified poly(β-amino ester) and chitosan, or a pharmaceutically acceptable salt thereof, at 0.15 to 3.0 weight percent relative to the end-modified poly(β-amino ester).
A nanoparticle according to any preceding claim, wherein each end modification of the end-modified poly(β-amino ester) is independently selected from an oligopeptide and Ry;
- wherein Ry is selected from the group consisting of hydrogen, halogen, alkyl, cycloalkyl, alkenyl, cycloalkenyl, heteroalkyl, heterocycloalkyl, acyl, aryl or heteroaryl.
A nanoparticle according to any preceding claim, wherein the end-modified poly(β-amino ester) is a polymer of formula I:
- wherein
- each L1 and L2 is independently selected from the group consisting of
- O, S, NRx and a bond;
- wherein Rx is independently selected from the group consisting of hydrogen, halogen, alkyl, cycloalkyl, alkenyl, cycloalkenyl, heteroalkyl, heterocycloalkyl, acyl, aryl or heteroaryl;
- L3 is independently selected from the group consisting of alkylene, alkenylene, heteroalkylene, heteroalkenylene, arylene, heteroarylene and
- wherein T1 is
- and
- T2 is selected from H, alkyl or
- wherein LT is independently selected from the group consisting of:
- O, S, NRx and a bond;
- wherein Rx is independently selected from the group consisting of hydrogen, halogen, alkyl, cycloalkyl, alkenyl, cycloalkenyl, heteroalkyl, heterocycloalkyl, acyl, aryl or heteroaryl;
- L4 is selected from the group consisting of
- L5 is independently selected from the group consisting of alkylene, alkenylene, heteroalkylene, heteroalkenylene, arylene or heteroarylene;
- R1, R2 and RT, where present, are independently selected from an oligopeptide and Ry;
- wherein Ry is selected from the group consisting of hydrogen, halogen, alkyl, cycloalkyl, alkenyl, cycloalkenyl, heteroalkyl, heterocycloalkyl, acyl, aryl or heteroaryl
- each R3 is independently selected from the group consisting of hydrogen, halogen, alkyl, cycloalkyl, alkenyl, cycloalkenyl, heteroalkyl, heterocycloalkyl, acyl, aryl or heteroaryl;
- and
- n is an integer from 5 to 10,000;
- or a pharmaceutically acceptable salt thereof.
The nanoparticle according to any preceding claim, further comprising an active agent.
A composition comprising at least one nanoparticle of any preceding claim.
A method for preparing nanoparticles comprising the steps of (i) preparing an end-modified poly(β-amino ester) in the presence of a sugar or sugar alcohol and (ii) preparing nanoparticles from the product of step (i).
A method for preparing nanoparticles comprising the steps of (i) preparing nanoparticles from an end-modified poly(β-amino ester) and (ii) contacting the nanoparticles with a sugar or sugar alcohol.
A method for preparing nanoparticles comprising the steps of (i) mixing an end-modified poly(β-amino ester) with chitosan and (ii) preparing nanoparticles from the product of step (i).
Dependencies are inferred from the claim text.