Supramolecularly engineered phospholipids constructed by nucleobase molecular recognition: upgraded generation of phospholipids for drug delivery.
نویسندگان
چکیده
Despite of great advances of phospholipids and liposomes in clinical therapy, very limited success has been achieved in the preparation of smart phospholipids and controlled-release liposomes for in vivo drug delivery and clinical trials. Here we report a supramolecular approach to synthesize novel supramolecularly engineered phospholipids based on complementary hydrogen bonding of nucleosides, which greatly reduces the need of tedious chemical synthesis, including reducing the strict requirements for multistep chemical reactions, and the purification of the intermediates and the amount of waste generated relative more traditional approaches. These upgraded phospholipids self-assemble into liposome-like bilayer structures in aqueous solution, exhibiting fast stimuli-responsive ability due to the hydrogen bonding connection. In vitro and in vivo evaluations show the resulted supramolecular liposomes from nucleoside phospholipids could effectively transport drug into tumor tissue, rapidly enter tumor cells, and controllably release their payload in response to an intracellular acidic environment, thus resulting in a much higher antitumor activity than conventional liposomes. The present supramolecularly engineered phospholipids represent an important evolution in comparison to conventional covalent-bonded phospholipid systems.
منابع مشابه
Supramolecularly engineered phospholipids constructed by nucleobase molecular recognition: upgraded generation of phospholipids for drug delivery† †Electronic supplementary information (ESI) available: Synthesis detail and characterization of supramolecular nucleoside phospholipids; fabrication of supramolecular liposomes and conventional liposomes, including fabrication of DOX-loaded supramolecular liposomes and conventional liposomes; details of in vitro experiments, including in vitro cytotoxicity studies, intracellular drug release, examination of cell viability of MCF-7 cells, apoptosis analyses and western blotting analysis; details of in vivo experiments, including pharmacokinetic studies, in vivo biodistribution and tumor targeting capability in tumor-bearing mice and in vivo antitumor efficacy. See DOI: 10.1039/c5sc01188d
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ورودعنوان ژورنال:
- Chemical science
دوره 6 7 شماره
صفحات -
تاریخ انتشار 2015