Liposomes modified with P-aminophenyl-α-d-mannopyranoside: A carrier for targeting cerebral functional regions in mice

Hao, Zhongfei; Cui, Yuxia; Li, Minghui; Du, Dan; Liu, Meifang; Tao, Haiquan; Li, Sen; Cao, Fangyuan; Chen, Yingli; Lei, Xuhui; Wang, Lin; Zhu, Da-ling; Peng, Haisheng; Jiang, Chuan-lu

doi:10.1016/j.ejpb.2012.12.020

Cited by 46 publications

(19 citation statements)

References 33 publications

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“…It is worth also noting that no significant reductions in TEER values were observed in any group during this study to indicate that the both the preincubation with the inhibitors and sertraline transport did not disrupt the BBB barrier properties. Similar observations were reported by other researchers that glycosylated liposomes not only could promote the transendothelial penetration but also could be accumulated in the brain with a distinct spatiotemporal pattern (44).…”

Section: In Vitro Bbb Transport Modelsupporting

confidence: 78%

“…b Uptake assay. c Fluorescence photographs of C6 glioma cells (blue, BisBenzimide H 33258 stained nucleus; green, DiO stained cell membrane; red, Rholabeled liposomes) from 0 s to 30 min of incubation with Rho-labeled optimized liposomal formulations phenobarbital can interact then inhibit the intrinsic activity of GLUT1 (43,44). Hence, in the current investigation, the synchronous transcytosis route mediated by glucose transporters was significantly inhibited by phenobarbital.…”

Section: C6 Glioma Cellular Uptakementioning

confidence: 93%

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Glycosylated Sertraline-Loaded Liposomes for Brain Targeting: QbD Study of Formulation Variabilities and Brain Transport

et al. 2016

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Abstract. Effectiveness of CNS-acting drugs depends on the localization, targeting, and capacity to be transported through the blood-brain barrier (BBB) which can be achieved by designing brain-targeting delivery vectors. Hence, the objective of this study was to screen the formulation and process variables affecting the performance of sertraline (Ser-HCl)-loaded pegylated and glycosylated liposomes. The prepared vectors were characterized for Ser-HCl entrapment, size, surface charge, release behavior, and in vitro transport through the BBB. Furthermore, the compatibility among liposomal components was assessed using SEM, FTIR, and DSC analysis. Through a thorough screening study, enhancement of SerHCl entrapment, nanosized liposomes with low skewness, maximized stability, and controlled drug leakage were attained. The solid-state characterization revealed remarkable interaction between SerHCl and the charging agent to determine drug entrapment and leakage. Moreover, results of liposomal transport through mouse brain endothelialpolyoma cells demonstrated greater capacity of the proposed glycosylated liposomes to target the cerebellar due to its higher density of GLUT1 and higher glucose utilization. This transport capacity was confirmed by the inhibiting action of both cytochalasin B and phenobarbital. Using C6 glioma cells model, flow cytometry, time-lapse live cell imaging, and in vivo NIR fluorescence imaging demonstrated that optimized glycosylated liposomes can be transported through the BBB by classical endocytosis, as well as by specific transcytosis. In conclusion, the current study proposed a thorough screening of important formulation and process variabilities affecting brain-targeting liposomes for further scale-up processes.

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Section: In Vitro Bbb Transport Modelsupporting

confidence: 78%

Section: C6 Glioma Cellular Uptakementioning

confidence: 93%

Glycosylated Sertraline-Loaded Liposomes for Brain Targeting: QbD Study of Formulation Variabilities and Brain Transport

et al. 2016

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“…17 It was demonstrated that liposomes modified with MAN not only promote the penetration through the BBB into the brain, but also target the selected intracerebral regions, including the cortex, cerebellum, brainstem, hippocampus, and pontine nuclei. 18 Curcumin is a kind of dietary polyphenol derived from the rhizomes of turmeric (Curcuma longa), which is usually used in the preparation of mustard and curry. 19 The anticancer effect of curcumin has been shown in many studies on cells and animals.…”

Section: Introductionmentioning

confidence: 99%

The functional curcumin liposomes induce apoptosis in C6 glioblastoma cells and C6 glioblastoma stem cells in vitro and in animals

Wang

Xue

et al. 2017

IJN

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Glioblastoma is a kind of malignant gliomas that is almost impossible to cure due to the poor drug transportation across the blood–brain barrier and the existence of glioma stem cells. We prepared a new kind of targeted liposomes in order to improve the drug delivery system onto the glioma cells and induce the apoptosis of glioma stem cells afterward. In this experiment, curcumin was chosen to kill gliomas, while quinacrine was used to induce apoptosis of the glioma stem cells. Also, p -aminophenyl-α-D-mannopyranoside could facilitate the transport of liposomes across the blood–brain barrier and finally target the brain glioma cells. The cell experiments in vitro indicated that the targeted liposomes could significantly improve the anti-tumor effects of the drugs, while enhancing the uptake effects, apoptosis effects, and endocytic effects of C6 glioma cells and C6 glioma stem cells. Given the animal experiments in vivo, we discovered that the targeted liposomes could obviously increase the survival period of brain glioma-bearing mice and inhibit the growth of gliomas. In summary, curcumin and quinacrine liposomes modified with p -aminophenyl-α-D-mannopyranoside is a potential preparation to treat brain glioma cells and brain glioma stem cells.

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“…Hao et al have confirmed that glucose transporters (GLUT) can facilitate MAN-LIP to cross the BBB. They also found that MAN-LIP can target the cortex, cerebellum, brainstem, brainstem, hippocampus and pontine nuclei [5]. The experimental data demonstrated that MAN-LIP not only improved the brain delivery, but targeted intracerebral regions, particularly, in the cerebellum and cerebral cortex.…”

mentioning

confidence: 74%

The Bright Future of Liposome Mediated Drug Delivery

Tang¹

2014

Biochem Physiol

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Liposomes modified with P-aminophenyl-α-d-mannopyranoside: A carrier for targeting cerebral functional regions in mice

Cited by 46 publications

References 33 publications

Glycosylated Sertraline-Loaded Liposomes for Brain Targeting: QbD Study of Formulation Variabilities and Brain Transport

Glycosylated Sertraline-Loaded Liposomes for Brain Targeting: QbD Study of Formulation Variabilities and Brain Transport

The functional curcumin liposomes induce apoptosis in C6 glioblastoma cells and C6 glioblastoma stem cells in vitro and in animals

The Bright Future of Liposome Mediated Drug Delivery

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