Send to

Choose Destination
Curr Gene Ther. 2019 Aug 7. doi: 10.2174/1566523219666190808094225. [Epub ahead of print]

Biodegradable Polyester of Poly (Ethylene glycol)-sebacic Acid as a Backbone for β-Cyclodextrin-polyrotaxane: A Promising Gene Silencing Vector.

Author information

Department of Chemical Engineering, Institute of Chemical Technology, Matunga, Mumbai-400 019. India.
Department of Pharmaceutical Sciences and Technology, Institute of Chemical Technology, Matunga, Mumbai-400 019. India.
Polymer Science and Engineering Division, CSIR-National Chemical Laboratory, Pune 411008. India.



Polyrotaxane, a macromolecular interlocked assembly, consisting of cyclodextrin has excellent inclusion capabilities and functionalization capacity that makes it versatile material as a vector for gene delivery applications.


A biodegradable linear aliphatic polyester axle composed of polyethylene glycol (PEG) and sebacic acid (SA) was used to fabricate the β-Cyclodextrin (β-CD) based polyrotaxane as a cationic polymeric vector and evaluated for its potential gene silencing efficiency.


The water soluble aliphatic polyester was synthesized by solvent esterification process and characterized by viscometer, GPC, FT-IR and 1H NMR spectroscopy. The synthesized polyester was further evaluated for its biodegradability and cellular cytotoxicity. Hence, this water-soluble polyester was used for step-wise synthesis of polyrotaxane, via threading and blocking reactions. Threading of β-CD over PEG-SA polyester axle was conducted in water, followed by end-capping of polypseudorotaxane using 2,4,6-trinitrobenzenesulfonic acid to yield polyester-based polyrotaxane. For gene delivery application cationic polyrotaxane (PRTx+) was synthesized and evaluated for its gene loading and gene silencing efficiency.


The resulting novel macromolecular assembly was found to be safe for use in biomedical applications. Further, characterization by GPC and 1H NMR techniques revealed successful formation of PE-β-CD-PRTx with a threading efficiency of 16%. Additionally, the cellular cytotoxicity assay indicated biosafety of the synthesized polyrotaxane, suggesting its potential for gene delivery and other biomedical applications. Further, the biological profile of PRTx+:siRNA complexes was evaluated by measuring their zeta potential and gene silencing efficiency, which were found to be comparable to Lipofectamine 3000, the commercial transfecting agent.


The combinatory effect of various factors such as biodegradability, favourable complexation ability, near zero zeta potentials, good cytotoxicity properties of poly (ethylene glycol)-sebacic acid based β-Cyclodextrin-polyrotaxane makes it a potential gene delivery vector for therapeutic applications.


Biodegradation; Cyclodextrin; GFP; Gene Silencing; Polyester; Polyrotaxane; siRNA

Supplemental Content

Full text links

Icon for Bentham Science Publishers Ltd.
Loading ...
Support Center