127
Thomas Mavromoustakos et al. (eds.), Supramolecules in Drug Discovery and Drug Delivery: Methods and Protocols,
Methods in Molecular Biology, vol. 2207, https://doi.org/10.1007/978-1-0716-0920-0_10,
© Springer Science+Business Media, LLC, part of Springer Nature 2021
Chapter 10
Drug Delivery Through Multifunctional Polypeptidic
Hydrogels
Hermis Iatrou, Panagiota G. Fragouli, Dimitra Stavroulaki,
and Barbara Athanasiou
Abstract
Over the last two decades, remarkable progress has been made to the discovery of novel drugs as well as
their delivery systems for the treatment of cancer, the major challenge in medicine. Pharmaceutical scientists are trying to shift from traditional to novel drug delivery systems by applying nanotechnology and, in
particular, polymeric carriers to medicine. In complex diseases, very sophisticated nanocarriers should be
designed to encapsulate a significant quantity of drugs and bypass biological barriers with minimum cargo
loss to effectively and directly deliver the encapsulated drug to the desired pathological site. One of the
most promising classes of polymeric materials for drug delivery applications is polypeptides, combining the
properties of the traditional polymers with the 3D structure of natural proteins, i.e., a-helices and β-sheets.
In this chapter, we present the recent progress in the synthesis of polymers that form hydrogels in aqueous
solutions, based on polypeptides prepared through ring-opening polymerization of N-carboxy anhydrides
and which have been loaded with anticancer drugs and studied for their functionality. Advancements in
drug design and improvement of multifunctional nanocarriers from the combination of well-defined macromolecular architectures and smart materials are the future for the successful treatment of numerous
lethal diseases.
Key words Polypeptides, Ring-opening polymerization, Hydrogels, pH- and enzyme stimuliresponsive, Pancreatic cancer, Gemcitabine
1 Introduction
A novel, multifunctional hydrogel that exhibits a unique set of
properties for the effective treatment of pancreatic cancer (PC) is
presented. The material is comprised of a pentablock terpolypeptide of the type PLys-b-(PHIS-co-PBLG)-PLys-b-(PHIS-coPBLG)-b-PLys which is a noncytotoxic polymer [1]. It can be
implanted via the least invasive route and selectively delivers gemcitabine to efficiently treat PC. Mixing the novel terpolypeptide
with an aqueous solution of gemcitabine within a syringe results in
the facile formation of a hydrogel that has the ability to become
Thomas Mavromoustakos et al. (eds.), Supramolecules in Drug Discovery and Drug Delivery: Methods and Protocols,
Methods in Molecular Biology, vol. 2207, https://doi.org/10.1007/978-1-0716-0920-0_10,
© Springer Science+Business Media, LLC, part of Springer Nature 2021
Chapter 10
Drug Delivery Through Multifunctional Polypeptidic
Hydrogels
Hermis Iatrou, Panagiota G. Fragouli, Dimitra Stavroulaki,
and Barbara Athanasiou
Abstract
Over the last two decades, remarkable progress has been made to the discovery of novel drugs as well as
their delivery systems for the treatment of cancer, the major challenge in medicine. Pharmaceutical scientists are trying to shift from traditional to novel drug delivery systems by applying nanotechnology and, in
particular, polymeric carriers to medicine. In complex diseases, very sophisticated nanocarriers should be
designed to encapsulate a significant quantity of drugs and bypass biological barriers with minimum cargo
loss to effectively and directly deliver the encapsulated drug to the desired pathological site. One of the
most promising classes of polymeric materials for drug delivery applications is polypeptides, combining the
properties of the traditional polymers with the 3D structure of natural proteins, i.e., a-helices and β-sheets.
In this chapter, we present the recent progress in the synthesis of polymers that form hydrogels in aqueous
solutions, based on polypeptides prepared through ring-opening polymerization of N-carboxy anhydrides
and which have been loaded with anticancer drugs and studied for their functionality. Advancements in
drug design and improvement of multifunctional nanocarriers from the combination of well-defined macromolecular architectures and smart materials are the future for the successful treatment of numerous
lethal diseases.
Key words Polypeptides, Ring-opening polymerization, Hydrogels, pH- and enzyme stimuliresponsive, Pancreatic cancer, Gemcitabine
1 Introduction
A novel, multifunctional hydrogel that exhibits a unique set of
properties for the effective treatment of pancreatic cancer (PC) is
presented. The material is comprised of a pentablock terpolypeptide of the type PLys-b-(PHIS-co-PBLG)-PLys-b-(PHIS-coPBLG)-b-PLys which is a noncytotoxic polymer [1]. It can be
implanted via the least invasive route and selectively delivers gemcitabine to efficiently treat PC. Mixing the novel terpolypeptide
with an aqueous solution of gemcitabine within a syringe results in
the facile formation of a hydrogel that has the ability to become