Nanoformulation and Evaluation of Oral Berberine-Loaded Liposomes
Berberine (BBR) is a poorly water-soluble quaternary isoquinoline alkaloid of plant origin with potential uses in the drug therapy of hypercholesterolemia. To tackle the limitations associated with the oral therapeutic use of BBR (such as a first-pass metabolism and poor absorption), BBR-loaded lipo...
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| Format: | Article |
| Language: | English |
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MDPI AG
2021-04-01
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| Series: | Molecules |
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| Online Access: | https://www.mdpi.com/1420-3049/26/9/2591 |
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| author | Thuan Thi Duong Antti Isomäki Urve Paaver Ivo Laidmäe Arvo Tõnisoo Tran Thi Hai Yen Karin Kogermann Ain Raal Jyrki Heinämäki Thi-Minh-Hue Pham |
| author_facet | Thuan Thi Duong Antti Isomäki Urve Paaver Ivo Laidmäe Arvo Tõnisoo Tran Thi Hai Yen Karin Kogermann Ain Raal Jyrki Heinämäki Thi-Minh-Hue Pham |
| author_sort | Thuan Thi Duong |
| collection | DOAJ |
| description | Berberine (BBR) is a poorly water-soluble quaternary isoquinoline alkaloid of plant origin with potential uses in the drug therapy of hypercholesterolemia. To tackle the limitations associated with the oral therapeutic use of BBR (such as a first-pass metabolism and poor absorption), BBR-loaded liposomes were fabricated by ethanol-injection and thin-film hydration methods. The size and size distribution, polydispersity index (PDI), solid-state properties, entrapment efficiency (EE) and in vitro drug release of liposomes were investigated. The BBR-loaded liposomes prepared by ethanol-injection and thin-film hydration methods presented an average liposome size ranging from 50 nm to 244 nm and from 111 nm to 449 nm, respectively. The PDI values for the liposomes were less than 0.3, suggesting a narrow size distribution. The EE of liposomes ranged from 56% to 92%. Poorly water-soluble BBR was found to accumulate in the bi-layered phospholipid membrane of the liposomes prepared by the thin-film hydration method. The BBR-loaded liposomes generated by both nanofabrication methods presented extended drug release behavior in vitro. In conclusion, both ethanol-injection and thin-film hydration nanofabrication methods are feasible for generating BBR-loaded oral liposomes with a uniform size, high EE and modified drug release behavior in vitro. |
| first_indexed | 2024-03-10T11:50:12Z |
| format | Article |
| id | doaj.art-75e169ab8226437293291e6e38266c54 |
| institution | Directory Open Access Journal |
| issn | 1420-3049 |
| language | English |
| last_indexed | 2024-03-10T11:50:12Z |
| publishDate | 2021-04-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Molecules |
| spelling | doaj.art-75e169ab8226437293291e6e38266c542023-11-21T17:45:03ZengMDPI AGMolecules1420-30492021-04-01269259110.3390/molecules26092591Nanoformulation and Evaluation of Oral Berberine-Loaded LiposomesThuan Thi Duong0Antti Isomäki1Urve Paaver2Ivo Laidmäe3Arvo Tõnisoo4Tran Thi Hai Yen5Karin Kogermann6Ain Raal7Jyrki Heinämäki8Thi-Minh-Hue Pham9Faculty of Pharmacy, Duy Tan University, 03 Quang Trung Street, Da Nang 550000, VietnamBiomedicum Imaging Unit, University of Helsinki, 8 Haartmaninkatu, 00014 Helsinki, FinlandInstitute of Pharmacy, Faculty of Medicine, University of Tartu, 1 Nooruse Street, 50411 Tartu, EstoniaInstitute of Pharmacy, Faculty of Medicine, University of Tartu, 1 Nooruse Street, 50411 Tartu, EstoniaInstitute of Physics, University of Tartu, 1 W. Ostwaldi Street, 50411 Tartu, EstoniaDepartment of Pharmaceutics, Hanoi University of Pharmacy, 13-15 Le Thanh Tong Street, Hoan Kiem District, Hanoi 110403, VietnamInstitute of Pharmacy, Faculty of Medicine, University of Tartu, 1 Nooruse Street, 50411 Tartu, EstoniaInstitute of Pharmacy, Faculty of Medicine, University of Tartu, 1 Nooruse Street, 50411 Tartu, EstoniaInstitute of Pharmacy, Faculty of Medicine, University of Tartu, 1 Nooruse Street, 50411 Tartu, EstoniaDepartment of Pharmaceutics, Hanoi University of Pharmacy, 13-15 Le Thanh Tong Street, Hoan Kiem District, Hanoi 110403, VietnamBerberine (BBR) is a poorly water-soluble quaternary isoquinoline alkaloid of plant origin with potential uses in the drug therapy of hypercholesterolemia. To tackle the limitations associated with the oral therapeutic use of BBR (such as a first-pass metabolism and poor absorption), BBR-loaded liposomes were fabricated by ethanol-injection and thin-film hydration methods. The size and size distribution, polydispersity index (PDI), solid-state properties, entrapment efficiency (EE) and in vitro drug release of liposomes were investigated. The BBR-loaded liposomes prepared by ethanol-injection and thin-film hydration methods presented an average liposome size ranging from 50 nm to 244 nm and from 111 nm to 449 nm, respectively. The PDI values for the liposomes were less than 0.3, suggesting a narrow size distribution. The EE of liposomes ranged from 56% to 92%. Poorly water-soluble BBR was found to accumulate in the bi-layered phospholipid membrane of the liposomes prepared by the thin-film hydration method. The BBR-loaded liposomes generated by both nanofabrication methods presented extended drug release behavior in vitro. In conclusion, both ethanol-injection and thin-film hydration nanofabrication methods are feasible for generating BBR-loaded oral liposomes with a uniform size, high EE and modified drug release behavior in vitro.https://www.mdpi.com/1420-3049/26/9/2591berberinepoorly water-soluble alkaloidliposomesethanol-injectionthin-film hydration |
| spellingShingle | Thuan Thi Duong Antti Isomäki Urve Paaver Ivo Laidmäe Arvo Tõnisoo Tran Thi Hai Yen Karin Kogermann Ain Raal Jyrki Heinämäki Thi-Minh-Hue Pham Nanoformulation and Evaluation of Oral Berberine-Loaded Liposomes Molecules berberine poorly water-soluble alkaloid liposomes ethanol-injection thin-film hydration |
| title | Nanoformulation and Evaluation of Oral Berberine-Loaded Liposomes |
| title_full | Nanoformulation and Evaluation of Oral Berberine-Loaded Liposomes |
| title_fullStr | Nanoformulation and Evaluation of Oral Berberine-Loaded Liposomes |
| title_full_unstemmed | Nanoformulation and Evaluation of Oral Berberine-Loaded Liposomes |
| title_short | Nanoformulation and Evaluation of Oral Berberine-Loaded Liposomes |
| title_sort | nanoformulation and evaluation of oral berberine loaded liposomes |
| topic | berberine poorly water-soluble alkaloid liposomes ethanol-injection thin-film hydration |
| url | https://www.mdpi.com/1420-3049/26/9/2591 |
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