Stealth and Cationic Nanoliposomes as Drug Delivery Systems to Increase Andrographolide BBB Permeability
(1) Background: Andrographolide (AG) is a natural compound effective for the treatment of inflammation-mediated neurodegenerative disorders. The aim of this investigation was the preparation of liposomes to enhance the penetration into the brain of AG, by modifying the surface of the liposomes by ad...
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MDPI AG
2018-08-01
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| Series: | Pharmaceutics |
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| Online Access: | http://www.mdpi.com/1999-4923/10/3/128 |
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| author | Vieri Piazzini Elisa Landucci Giulia Graverini Domenico E. Pellegrini-Giampietro Anna Rita Bilia Maria Camilla Bergonzi |
| author_facet | Vieri Piazzini Elisa Landucci Giulia Graverini Domenico E. Pellegrini-Giampietro Anna Rita Bilia Maria Camilla Bergonzi |
| author_sort | Vieri Piazzini |
| collection | DOAJ |
| description | (1) Background: Andrographolide (AG) is a natural compound effective for the treatment of inflammation-mediated neurodegenerative disorders. The aim of this investigation was the preparation of liposomes to enhance the penetration into the brain of AG, by modifying the surface of the liposomes by adding Tween 80 (LPs-AG) alone or in combination with Didecyldimethylammonium bromide (DDAB) (CLPs-AG). (2) 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. |
| first_indexed | 2024-04-11T13:22:52Z |
| format | Article |
| id | doaj.art-e341fead9e9a429a98a3ef1b80721298 |
| institution | Directory Open Access Journal |
| issn | 1999-4923 |
| language | English |
| last_indexed | 2024-04-11T13:22:52Z |
| publishDate | 2018-08-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceutics |
| spelling | doaj.art-e341fead9e9a429a98a3ef1b807212982022-12-22T04:22:09ZengMDPI AGPharmaceutics1999-49232018-08-0110312810.3390/pharmaceutics10030128pharmaceutics10030128Stealth and Cationic Nanoliposomes as Drug Delivery Systems to Increase Andrographolide BBB PermeabilityVieri Piazzini0Elisa Landucci1Giulia Graverini2Domenico E. Pellegrini-Giampietro3Anna Rita Bilia4Maria Camilla Bergonzi5Department of Chemistry, University of Florence, Via Ugo Schiff 6, Sesto Fiorentino, 50019 Florence, ItalyDepartment of Health Sciences, Section of Clinical Pharmacology and Oncology, University of Florence, Viale Pieraccini 6, 50139 Florence, ItalyDepartment of Chemistry, University of Florence, Via Ugo Schiff 6, Sesto Fiorentino, 50019 Florence, ItalyDepartment of Health Sciences, Section of Clinical Pharmacology and Oncology, University of Florence, Viale Pieraccini 6, 50139 Florence, ItalyDepartment of Chemistry, University of Florence, Via Ugo Schiff 6, Sesto Fiorentino, 50019 Florence, ItalyDepartment of Chemistry, University of Florence, Via Ugo Schiff 6, Sesto Fiorentino, 50019 Florence, Italy(1) Background: Andrographolide (AG) is a natural compound effective for the treatment of inflammation-mediated neurodegenerative disorders. The aim of this investigation was the preparation of liposomes to enhance the penetration into the brain of AG, by modifying the surface of the liposomes by adding Tween 80 (LPs-AG) alone or in combination with Didecyldimethylammonium bromide (DDAB) (CLPs-AG). (2) 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.http://www.mdpi.com/1999-4923/10/3/128liposomesbrain deliverysurfactantcationic liposomesandrographolidePAMPAhCMEC/D3 cells |
| spellingShingle | Vieri Piazzini Elisa Landucci Giulia Graverini Domenico E. Pellegrini-Giampietro Anna Rita Bilia Maria Camilla Bergonzi Stealth and Cationic Nanoliposomes as Drug Delivery Systems to Increase Andrographolide BBB Permeability Pharmaceutics liposomes brain delivery surfactant cationic liposomes andrographolide PAMPA hCMEC/D3 cells |
| title | Stealth and Cationic Nanoliposomes as Drug Delivery Systems to Increase Andrographolide BBB Permeability |
| title_full | Stealth and Cationic Nanoliposomes as Drug Delivery Systems to Increase Andrographolide BBB Permeability |
| title_fullStr | Stealth and Cationic Nanoliposomes as Drug Delivery Systems to Increase Andrographolide BBB Permeability |
| title_full_unstemmed | Stealth and Cationic Nanoliposomes as Drug Delivery Systems to Increase Andrographolide BBB Permeability |
| title_short | Stealth and Cationic Nanoliposomes as Drug Delivery Systems to Increase Andrographolide BBB Permeability |
| title_sort | stealth and cationic nanoliposomes as drug delivery systems to increase andrographolide bbb permeability |
| topic | liposomes brain delivery surfactant cationic liposomes andrographolide PAMPA hCMEC/D3 cells |
| url | http://www.mdpi.com/1999-4923/10/3/128 |
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