“…the particle sizes of liposomes increased from 73.39 to 117.30 nm on DLS as increase the ratio of phospholipids, the polydispersity index (PDI) of DLS was keep blow 0.3, which meant that the liposomes show homogeneity morphology.To investigate the entrapment efficiency and drug loading capacity in Lipo-CJM-Pt, liposomes were prepared as reported previously[65][66][67][68] . Then the entrapment efficiency and drug loading capacity in Lipo-CJM-Pt were calculated by detected the CJM-Pt mass in liposomes with a High Performance Liquid Chromatograph at 293 nm (comparing with CJM-Pt calibration curve) after extracting CJM-Pt from the dried drug-loaded liposomes with methanol as well.…”
A synergic acting cisplatin derivative, made via conjugating CJM126 with cisplatin, was synthesized and delivered using liposomes to inhibit tumor cells.
“…the particle sizes of liposomes increased from 73.39 to 117.30 nm on DLS as increase the ratio of phospholipids, the polydispersity index (PDI) of DLS was keep blow 0.3, which meant that the liposomes show homogeneity morphology.To investigate the entrapment efficiency and drug loading capacity in Lipo-CJM-Pt, liposomes were prepared as reported previously[65][66][67][68] . Then the entrapment efficiency and drug loading capacity in Lipo-CJM-Pt were calculated by detected the CJM-Pt mass in liposomes with a High Performance Liquid Chromatograph at 293 nm (comparing with CJM-Pt calibration curve) after extracting CJM-Pt from the dried drug-loaded liposomes with methanol as well.…”
A synergic acting cisplatin derivative, made via conjugating CJM126 with cisplatin, was synthesized and delivered using liposomes to inhibit tumor cells.
Ibuprofen is one of the most potent non-steroid anti-inflammatory drugs (NSAIDs) and plays an important role in the treatment of neurodegenerative diseases. However, its poor brain penetration and serious side effects at therapeutic doses, has hindered its further application. Thus, it is of great interest to develop a carrier-mediated transporter (CMT) system that is capable of more efficiently delivering ibuprofen into the brain at smaller doses to treat neurodegenerative diseases. In this study, a dual-mediated ibuprofen prodrug modified by glucose (Glu) and vitamin C (Vc) for central nervous system (CNS) drug delivery was designed and synthesized in order to effectively deliver ibuprofen to brain. Ibuprofen could be released from the prepared prodrugs when incubated with various buffers, mice plasma and brain homogenate. Also, the prodrug showed superior neuroprotective effect in vitro and in vivo than ibuprofen. Our results suggest that chemical modification of therapeutics with warheads of glucose and Vc represents a promising and efficient strategy for the development of brain-targeting prodrugs by utilizing the endogenous transportation mechanism of the warheads.
“…A standard way of increasing BBB crossing by NPs is to use the mechanisms of transcytosis through the endothelial cells either through the adsorptive pathway used mainly by positively charged NPs or the, more specific, a receptor-mediated pathway that relies on the decoration of the NPs with ligands for receptors and transporters located on the luminal plasma membrane of the BBB’s endothelial cells. Several receptors and transporters have been used as targets for those ligands, such as the glucose transporter-1 (GLUT1) [28,29] or the transferrin receptor [30,31]. Another way to facilitate BBB crossing is to increase the NP circulation time since the longer the NP is in the bloodstream the more chances for the ligand coupled to the NP to interact with its target and to be internalized.…”
Section: The Delivery Challenge Into the Cnsmentioning
Alzheimer’s disease (AD) is one of the main causes of disability and dependency among elderly people. AD is a neurodegenerative disorder characterized by a progressive and irreversible cognitive impairment, whose etiology is unclear because of the complex molecular mechanisms involved in its pathophysiology. A global view of the AD pathophysiology is described in order to understand the need for an effective treatment and why nanoparticles (NPs) could be an important weapon against neurodegenerative diseases by solving the general problem of poor delivery into the central nervous system (CNS) for many drugs. Drug delivery into the CNS is one of the most challenging objectives in pharmaceutical design, due to the limited access to the CNS imposed by the blood-brain barrier (BBB). The purpose of this review is to present a comprehensive overview of the use of NPs as delivery systems for therapeutic and diagnostic purposes in models of AD.
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