title: Fabrication of dendrimer-releasing lipidic nanoassembly for cancer drug delivery.
abstract: An inherent dilemma in the use of nanomedicines for cancer drug delivery is their limited penetration into tumors due to their large size. We have demonstrated that dendrimer/lipid nanoassemblies can solve this problem by means of tumor-triggered disassembly and the release of small (several nanometers) dendrimers to facilitate tumor penetration. Herein, we report a general strategy for the fabrication of nanoassemblies from hydrophobic and hydrophilic dendrimers with phospholipids. Hydrophobic dendrimers could assemble with lipids via hydrophobic interactions, whereas hydrophilic dendrimers could only assemble with lipids in the presence of anionic surfactants via both electrostatic and hydrophobic interactions. The nanoassemblies of hydrophobic dendrimers/lipids were found to be capable of stripping off their lipid layers via fusion with the cell membrane and then intracellular or extracellular release of dendrimers, whereas the nanoassemblies of hydrophilic dendrimers/lipids were internalized via endocytosis and then released their dendrimers inside the cells. Therefore, these dendrimer/lipid nanoassemblies could be used for the delivery of different cancer drugs.
authors.affiliation: Center for Bionanoengineering and State Key Laboratory of Chemical Engineering, Department of Chemical and Biological Engineering, Zhejiang University, Hangzhou, 310027, China.
authors.forename: Qihang
authors.initials: Q
authors.lastname: Sun
authors.forename: Xinpeng
authors.initials: X
authors.lastname: Ma
authors.forename: Bo
authors.initials: B
authors.lastname: Zhang
authors.forename: Zhuxian
authors.initials: Z
authors.lastname: Zhou
authors.forename: Erlei
authors.initials: E
authors.lastname: Jin
authors.forename: Youqing
authors.initials: Y
authors.lastname: Shen
authors.forename: Edward A
authors.initials: EA
authors.lastname: Van Kirk
authors.forename: William J
authors.initials: WJ
authors.lastname: Murdoch
authors.forename: Maciej
authors.initials: M
authors.lastname: Radosz
authors.forename: Weilin
authors.initials: W
authors.lastname: Sun
mesh_terms: D000970:Antineoplastic Agents / Q000737:chemistry / Q000378:metabolism; D045744:Cell Line, Tumor / Q000166:cytology / Q000378:metabolism / Q000648:ultrastructure; D050091:Dendrimers / Q000737:chemistry* / Q000378:metabolism; D016503:Drug Delivery Systems; D005260:Female; D006801:Humans; D057927:Hydrophobic and Hydrophilic Interactions; D008051:Lipid Bilayers / Q000737:chemistry*; D050997:Nanomedicine; D010051:Ovarian Neoplasms; D011073:Polyamines / Q000737:chemistry; D055672:Static Electricity
chemical_list: D000970:Antineoplastic Agents; D050091:Dendrimers; D008051:Lipid Bilayers; C531249:Poly(amidoamine); D011073:Polyamines