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Bile salt/phospholipid mixed micelle precursor pellets prepared by fluid-bed coating
Bile salt/phospholipid mixed micelles (MMs) are potent carriers used for oral absorption of drugs that are poorly soluble in water; however, there are many limitations associated with liquid formulations. In the current study, the feasibility of preparing bile salt/phospholipid MM precursor (preMM)...
Autores principales: | , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Dove Medical Press
2013
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3639718/ https://www.ncbi.nlm.nih.gov/pubmed/23641154 http://dx.doi.org/10.2147/IJN.S42349 |
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author | Dong, Fuxia Xie, Yunchang Qi, Jianping Hu, Fuqiang Lu, Yi Li, Sanming Wu, Wei |
author_facet | Dong, Fuxia Xie, Yunchang Qi, Jianping Hu, Fuqiang Lu, Yi Li, Sanming Wu, Wei |
author_sort | Dong, Fuxia |
collection | PubMed |
description | Bile salt/phospholipid mixed micelles (MMs) are potent carriers used for oral absorption of drugs that are poorly soluble in water; however, there are many limitations associated with liquid formulations. In the current study, the feasibility of preparing bile salt/phospholipid MM precursor (preMM) pellets with high oral bioavailability, using fluid-bed coating technology, was examined. In this study, fenofibrate (FB) and sodium deoxycholate (SDC) were used as the model drug and the bile salt, respectively. To prepare the MMs and to serve as the micellular carrier, a weight ratio of 4:6 was selected for the sodium deoxycholate/phospholipids based on the ternary phase diagram. Polyethylene glycol (PEG) 6000 was selected as the dispersion matrix for precipitation of the MMs onto pellets, since it can enhance the solubilizing ability of the MMs. Coating of the MMs onto the pellets using the fluid-bed coating technology was efficient and the pellets were spherical and intact. MMs could be easily reconstituted from preMM pellets in water. Although they existed in a crystalline state in the preMM pellets, FB could be encapsulated into the reconstituted MMs, and the MMs were redispersed better than solid dispersion pellets (FB:PEG = 1:3) and Lipanthyl®. The redispersibility of the preMM pellets increased with the increase of the FB/PEG/micellar carrier. PreMM pellets with a FB:PEG:micellar carrier ratio of 1:1.5:1.5 showed 284% and 145% bioavailability relative to Lipanthyl® and solid dispersion pellets (FB:PEG = 1:3), respectively. Fluid-bed coating technology has considerable potential for use in preparing sodium deoxycholate/phospholipid preMM pellets, with enhanced oral bioavailability for poorly water-soluble drugs. |
format | Online Article Text |
id | pubmed-3639718 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2013 |
publisher | Dove Medical Press |
record_format | MEDLINE/PubMed |
spelling | pubmed-36397182013-05-02 Bile salt/phospholipid mixed micelle precursor pellets prepared by fluid-bed coating Dong, Fuxia Xie, Yunchang Qi, Jianping Hu, Fuqiang Lu, Yi Li, Sanming Wu, Wei Int J Nanomedicine Original Research Bile salt/phospholipid mixed micelles (MMs) are potent carriers used for oral absorption of drugs that are poorly soluble in water; however, there are many limitations associated with liquid formulations. In the current study, the feasibility of preparing bile salt/phospholipid MM precursor (preMM) pellets with high oral bioavailability, using fluid-bed coating technology, was examined. In this study, fenofibrate (FB) and sodium deoxycholate (SDC) were used as the model drug and the bile salt, respectively. To prepare the MMs and to serve as the micellular carrier, a weight ratio of 4:6 was selected for the sodium deoxycholate/phospholipids based on the ternary phase diagram. Polyethylene glycol (PEG) 6000 was selected as the dispersion matrix for precipitation of the MMs onto pellets, since it can enhance the solubilizing ability of the MMs. Coating of the MMs onto the pellets using the fluid-bed coating technology was efficient and the pellets were spherical and intact. MMs could be easily reconstituted from preMM pellets in water. Although they existed in a crystalline state in the preMM pellets, FB could be encapsulated into the reconstituted MMs, and the MMs were redispersed better than solid dispersion pellets (FB:PEG = 1:3) and Lipanthyl®. The redispersibility of the preMM pellets increased with the increase of the FB/PEG/micellar carrier. PreMM pellets with a FB:PEG:micellar carrier ratio of 1:1.5:1.5 showed 284% and 145% bioavailability relative to Lipanthyl® and solid dispersion pellets (FB:PEG = 1:3), respectively. Fluid-bed coating technology has considerable potential for use in preparing sodium deoxycholate/phospholipid preMM pellets, with enhanced oral bioavailability for poorly water-soluble drugs. Dove Medical Press 2013 2013-04-26 /pmc/articles/PMC3639718/ /pubmed/23641154 http://dx.doi.org/10.2147/IJN.S42349 Text en © 2013 Dong et al, publisher and licensee Dove Medical Press Ltd This is an Open Access article which permits unrestricted noncommercial use, provided the original work is properly cited. |
spellingShingle | Original Research Dong, Fuxia Xie, Yunchang Qi, Jianping Hu, Fuqiang Lu, Yi Li, Sanming Wu, Wei Bile salt/phospholipid mixed micelle precursor pellets prepared by fluid-bed coating |
title | Bile salt/phospholipid mixed micelle precursor pellets prepared by fluid-bed coating |
title_full | Bile salt/phospholipid mixed micelle precursor pellets prepared by fluid-bed coating |
title_fullStr | Bile salt/phospholipid mixed micelle precursor pellets prepared by fluid-bed coating |
title_full_unstemmed | Bile salt/phospholipid mixed micelle precursor pellets prepared by fluid-bed coating |
title_short | Bile salt/phospholipid mixed micelle precursor pellets prepared by fluid-bed coating |
title_sort | bile salt/phospholipid mixed micelle precursor pellets prepared by fluid-bed coating |
topic | Original Research |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3639718/ https://www.ncbi.nlm.nih.gov/pubmed/23641154 http://dx.doi.org/10.2147/IJN.S42349 |
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