Stealth and Cationic Nanoliposomes as Drug Delivery Systems to Increase Andrographolide BBB Permeability

隐形阳离子纳米脂质体作为药物输送系统可增加穿心莲内酯 BBB 通透性

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作者:Vieri Piazzini, Elisa Landucci, Giulia Graverini, Domenico E Pellegrini-Giampietro, Anna Rita Bilia, Maria Camilla Bergonzi

Background

Andrographolide (AG) is a natural compound effective for the treatment of inflammation-mediated neurodegenerative disorders. The

Conclusions

This study shows that developed liposomes might be ideal candidates for brain delivery of AG.

Methods

LPs-AG and CLPs-AG were physically and chemically characterized. The ability of liposomes to increase the permeability of AG was evaluated by artificial membranes (PAMPA) and hCMEC/D3 cells. (3)

Results

Based on obtained results in terms of size, homogeneity, ζ-potential and EE%. both liposomes are suitable for parenteral administration. The systems showed excellent stability during a month of storage as suspensions or freeze-dried products. Glucose resulted the best cryoprotectant agent. PAMPA and hCMEC/D3 transport studies revealed that LPs-AG and CLPs-AG increased the permeability of AG, about an order of magnitude, compared to free AG without alterations in cell viability. The caveolae-mediated endocytosis resulted the main mechanism of up-take for both formulations. The presence of positive charge increased the cellular internalization of nanoparticles. (4) Conclusions: This study shows that developed liposomes might be ideal candidates for brain delivery of AG.

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