Thermosensitive and photocleavable polyaspartamide derivatives for drug delivery

The development of novel thermo- and photo-dual-responsive biodegradable polymeric micelles based on amphiphilic polyaspartamide derivatives (NB-g-PHPA-g-mPEG) for anticancer drug delivery is reported. The obtained polymers containing hydrophobic photocleavable o-nitrobenzyl groups exhibit thermo- and photosensitivity. The micelles and paclitaxel-loaded micelles based on the thermo- and photo-dual-sensitive polymers were prepared by a quick heating method without using toxic organic solvent. The paclitaxel release from the drug-loaded micelles can be triggered under photoirradiation. Enhancement of the anticancer activity against HeLa cells was observed for paclitaxel-loaded NB-g-PHPA-g-mPEG micelles after light irradiation, while the empty NB-g-PHPA-g-mPEG micelles with or without irradiation did not show any toxicity. Therefore, the thermo- and photo-dual-responsive NB-g-PHPA-g-mPEG micelles have a promising future applied as a light controlled drug delivery system for anticancer drugs.</p

A facile modular approach toward multifunctional supramolecular polyplexes for targeting gene delivery

Extensive efforts and numerous methodologies have been explored to develop safe and efficient gene carriers that are capable of overcoming multiple extra- and intracellular barriers during the transfection process. However, it is a great challenge to fabricate a gene carrier system containing multiple functional components. In this work, we propose a facile modular approach to design targeted multifunctional gene delivery systems, which are based on building blocks with pre-defined functions to tackle specific barriers. These building blocks can be rationally combined and self-assemble into an integrated gene delivery system via host-guest interactions. As a proof of concept, three adamantyl-terminated targeting guest modules, adamantyl terminated RGD peptide (Ad-RGD), folate and lactobionic acid terminated PEGs (FA-PEG-Ad and LA-PEG-Ad), were synthesized, characterized, and utilized for post-functionalizing of adamantyl decorated cationic PEI based supramolecular polyplexes (PEI-Ad4/PCD/DNA) through the free CD units of the poly(β-cyclodextran) (PCD) host module. These multifunctional targeting supramolecular polyplexes exhibited enhanced cellular uptake and excellent transfection activity in receptor-positive cells. By modulating the functional components of the supramolecular platform, we can customize the gene carriers for further research on different tissues or cells in vitro or in vivo

A facile modular approach toward multifunctional supramolecular polyplexes for targeting gene delivery

Extensive efforts and numerous methodologies have been explored to develop safe and efficient gene carriers that are capable of overcoming multiple extra- and intracellular barriers during the transfection process. However, it is a great challenge to fabricate a gene carrier system containing multiple functional components. In this work, we propose a facile modular approach to design targeted multifunctional gene delivery systems, which are based on building blocks with pre-defined functions to tackle specific barriers. These building blocks can be rationally combined and self-assemble into an integrated gene delivery system via host-guest interactions. As a proof of concept, three adamantyl-terminated targeting guest modules, adamantyl terminated RGD peptide (Ad-RGD), folate and lactobionic acid terminated PEGs (FA-PEG-Ad and LA-PEG-Ad), were synthesized, characterized, and utilized for post-functionalizing of adamantyl decorated cationic PEI based supramolecular polyplexes (PEI-Ad4/PCD/DNA) through the free CD units of the poly(β-cyclodextran) (PCD) host module. These multifunctional targeting supramolecular polyplexes exhibited enhanced cellular uptake and excellent transfection activity in receptor-positive cells. By modulating the functional components of the supramolecular platform, we can customize the gene carriers for further research on different tissues or cells in vitro or in vivo