title: Design and synthesis of lipidic organoalkoxysilanes for the self-assembly of liposomal nanohybrid cerasomes with controlled drug release properties.
abstract: This paper reports the facile design and synthesis of a series of lipidic organoalkoxysilanes with different numbers of triethoxysilane headgroups and hydrophobic alkyl chains linked by glycerol and pentaerythritol for the construction of cerasomes with regulated surface siloxane density and controlled release behavior. It was found that the number of triethoxysilane headgroups affected the properties of the cerasomes for encapsulation efficiency, drug loading capacity, and release behavior. For both water-soluble doxorubicin (DOX) and water-insoluble paclitaxel (PTX), the release rate from the cerasomes decreased as the number of triethoxysilane headgroups increased. The slower release rate from the cerasomes was attributed to the higher density of the siloxane network on the surface of the cerasomes, which blocks the drug release channels. In contrast to the release results with DOX, the introduction of one more hydrophobic alkyl chain into the cerasome-forming lipid resulted in a slower release rate of PTX from the cerasomes due to the formation of a more compact cerasome bilayer. An MTT viability assay showed that all of these drug-loaded cerasomes inhibited proliferation of the HepG2 cancer cell line. The fine tuning of the chemical structure of the cerasome-forming lipids would foster a new strategy to precisely regulate the release rate of drugs from cerasomes.
authors.affiliation: Department of Biomedical Engineering, College of Engineering, Peking University, Beijing 100871 (P. R. China) http://bme.pku.edu.cn/∼daizhifei/
authors.forename: Xiaolong
authors.initials: X
authors.lastname: Liang
authors.forename: Xiaoda
authors.initials: X
authors.lastname: Li
authors.forename: Lijia
authors.initials: L
authors.lastname: Jing
authors.forename: Peng
authors.initials: P
authors.lastname: Xue
authors.forename: Lingdong
authors.initials: L
authors.lastname: Jiang
authors.forename: Qiushi
authors.initials: Q
authors.lastname: Ren
authors.forename: Zhifei
authors.initials: Z
authors.lastname: Dai
mesh_terms: D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology; D049109:Cell Proliferation / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D003692:Delayed-Action Preparations; D004317:Doxorubicin / Q000737:chemistry / Q000494:pharmacology; D005990:Glycerol / Q000737:chemistry; D056945:Hep G2 Cells; D061307:Human Umbilical Vein Endothelial Cells; D006801:Humans; D057927:Hydrophobic and Hydrophilic Interactions; D008081:Liposomes / Q000737:chemistry*; D049329:Nanostructures / Q000737:chemistry*; D017239:Paclitaxel / Q000737:chemistry / Q000494:pharmacology; D011409:Propylene Glycols / Q000737:chemistry; D012821:Silanes / Q000138:chemical synthesis / Q000737:chemistry*
chemical_list: D000970:Antineoplastic Agents; D003692:Delayed-Action Preparations; D008081:Liposomes; D011409:Propylene Glycols; D012821:Silanes; D004317:Doxorubicin; C522569:triethoxysilane; D017239:Paclitaxel; D005990:Glycerol; C008783:pentaerythritol
keywords: cerasomes; drug delivery; lipids; liposomes; nanoparticles