Human serum albumin-based nanoparticles alter raloxifene administration and improve bioavailability
Osteoporosis is a disease that reduces bone mass and microarchitecture, which makes bones fragile. Postmenopausal osteoporosis occurs due to estrogen deficiency. Raloxifene is a selective estrogen receptor modulator used to treat postmenopausal osteoporosis. However, it has a low bioavailability, wh...
| Main Authors: | , , , , , |
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| Format: | Article |
| Language: | English |
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Taylor & Francis Group
2022-12-01
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| Series: | Drug Delivery |
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| Online Access: | https://www.tandfonline.com/doi/10.1080/10717544.2022.2111479 |
| _version_ | 1811321232601120768 |
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| author | Shu-Jyuan Yang Chih-Hao Chang Tai-Horng Young Chung-Hao Wang Tzu-Hao Tseng Man-Ling Wang |
| author_facet | Shu-Jyuan Yang Chih-Hao Chang Tai-Horng Young Chung-Hao Wang Tzu-Hao Tseng Man-Ling Wang |
| author_sort | Shu-Jyuan Yang |
| collection | DOAJ |
| description | Osteoporosis is a disease that reduces bone mass and microarchitecture, which makes bones fragile. Postmenopausal osteoporosis occurs due to estrogen deficiency. Raloxifene is a selective estrogen receptor modulator used to treat postmenopausal osteoporosis. However, it has a low bioavailability, which requires long-term, high-dose raloxifene administration to be effective and causes several side effects. Herein, raloxifene was encapsulated in human serum albumin (HSA)-based nanoparticles (Ral/HSA/PSS NPs) as an intravenous-injection pharmaceutical formulation to increase its bioavailability and reduce the treatment dosage and time. In vitro results indicated that raloxifene molecules were well distributed in HSA-based nanoparticles as an amorphous state, and the resulting raloxifene formulation was stabile during long-term storage duration. The Ral/HSA/PSS NPs were both biocompatible and hemocompatible with a decreased cytotoxicity of high-dose raloxifene. Moreover, the intravenous administration of the prepared Ral/HSA/PSS NPs to rats improved raloxifene bioavailability and improved its half-life in plasma. These raloxifene-loaded nanoparticles may be a potential nanomedicine candidate for treating postmenopausal osteoporosis with lower raloxifene dosages. |
| first_indexed | 2024-04-13T13:13:14Z |
| format | Article |
| id | doaj.art-b4ffab9569a34758b8d0ee1aed41c352 |
| institution | Directory Open Access Journal |
| issn | 1071-7544 1521-0464 |
| language | English |
| last_indexed | 2024-04-13T13:13:14Z |
| publishDate | 2022-12-01 |
| publisher | Taylor & Francis Group |
| record_format | Article |
| series | Drug Delivery |
| spelling | doaj.art-b4ffab9569a34758b8d0ee1aed41c3522022-12-22T02:45:33ZengTaylor & Francis GroupDrug Delivery1071-75441521-04642022-12-012912685269310.1080/10717544.2022.2111479Human serum albumin-based nanoparticles alter raloxifene administration and improve bioavailabilityShu-Jyuan Yang0Chih-Hao Chang1Tai-Horng Young2Chung-Hao Wang3Tzu-Hao Tseng4Man-Ling Wang5Institute of Biomedical Engineering, College of Medicine and College of Engineering, National Taiwan University, Taipei, TaiwanDepartment of Orthopedics, National Taiwan University Hospital Jin-Shan Branch, New Taipei City, TaiwanInstitute of Biomedical Engineering, College of Medicine and College of Engineering, National Taiwan University, Taipei, TaiwanCYBER ELITE LIMITED, Vistra Corporate Services Centre, Apia, SamoaInstitute of Biomedical Engineering, College of Medicine and College of Engineering, National Taiwan University, Taipei, TaiwanGraduate Institute of Clinical Medicine, National Taiwan University College of Medicine, Taipei, TaiwanOsteoporosis is a disease that reduces bone mass and microarchitecture, which makes bones fragile. Postmenopausal osteoporosis occurs due to estrogen deficiency. Raloxifene is a selective estrogen receptor modulator used to treat postmenopausal osteoporosis. However, it has a low bioavailability, which requires long-term, high-dose raloxifene administration to be effective and causes several side effects. Herein, raloxifene was encapsulated in human serum albumin (HSA)-based nanoparticles (Ral/HSA/PSS NPs) as an intravenous-injection pharmaceutical formulation to increase its bioavailability and reduce the treatment dosage and time. In vitro results indicated that raloxifene molecules were well distributed in HSA-based nanoparticles as an amorphous state, and the resulting raloxifene formulation was stabile during long-term storage duration. The Ral/HSA/PSS NPs were both biocompatible and hemocompatible with a decreased cytotoxicity of high-dose raloxifene. Moreover, the intravenous administration of the prepared Ral/HSA/PSS NPs to rats improved raloxifene bioavailability and improved its half-life in plasma. These raloxifene-loaded nanoparticles may be a potential nanomedicine candidate for treating postmenopausal osteoporosis with lower raloxifene dosages.https://www.tandfonline.com/doi/10.1080/10717544.2022.2111479Osteoporosisraloxifenehuman serum albuminpoly(sodium styrene sulfonate)nanoparticle |
| spellingShingle | Shu-Jyuan Yang Chih-Hao Chang Tai-Horng Young Chung-Hao Wang Tzu-Hao Tseng Man-Ling Wang Human serum albumin-based nanoparticles alter raloxifene administration and improve bioavailability Drug Delivery Osteoporosis raloxifene human serum albumin poly(sodium styrene sulfonate) nanoparticle |
| title | Human serum albumin-based nanoparticles alter raloxifene administration and improve bioavailability |
| title_full | Human serum albumin-based nanoparticles alter raloxifene administration and improve bioavailability |
| title_fullStr | Human serum albumin-based nanoparticles alter raloxifene administration and improve bioavailability |
| title_full_unstemmed | Human serum albumin-based nanoparticles alter raloxifene administration and improve bioavailability |
| title_short | Human serum albumin-based nanoparticles alter raloxifene administration and improve bioavailability |
| title_sort | human serum albumin based nanoparticles alter raloxifene administration and improve bioavailability |
| topic | Osteoporosis raloxifene human serum albumin poly(sodium styrene sulfonate) nanoparticle |
| url | https://www.tandfonline.com/doi/10.1080/10717544.2022.2111479 |
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