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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)...

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Detalles Bibliográficos
Autores principales: Dong, Fuxia, Xie, Yunchang, Qi, Jianping, Hu, Fuqiang, Lu, Yi, Li, Sanming, Wu, Wei
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Dove Medical Press 2013
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.
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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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