Investigating the correlation between in vivo absorption and in vitro release of fenofibrate from lipid matrix particles in biorelevant medium
文献类型：期刊论文
| 作者 | Borkar, Nrupa5; Xia, Dengning1,4,5; Holm, Rene3,5; Gan, Yong1 ; Muellertz, Anette2,5; Yang, Mingshi5; Mu, Huiling5
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| 刊名 | EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
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| 出版日期 | 2014-01-23 |
| 卷号 | 51页码:204-210 |
| 关键词 | Lipid matrix particle In vitro lipolysis Fenofibrate Absorption Particle size |
| ISSN号 | 0928-0987 |
| DOI | 10.1016/j.ejps.2013.09.022 |
| 文献子类 | Article |
| 英文摘要 | Lipid matrix particles (LMP) may be used as better carriers for poorly water-soluble drugs than liquid lipid carriers because of reduced drug mobilization in the formulations. However, the digestion process of solid lipid particles and their effect on the absorption of poorly water-soluble drugs are not fully understood. This study aimed at investigating the effect of particle size of LMP on drug release in vitro as well as absorption in vivo in order to get a better understanding on the effect of degradation of lipid particles on drug solubilisation and absorption. Fenofibrate, a model poorly water-soluble drug, was incorporated into LMP in this study using probe ultrasound sonication. The resultant LMP were characterised in terms of particle size, size distribution, zeta potential, entrapment efficiency, in vitro lipolysis and in vivo absorption in rat model. LMP of three different particle sizes i.e. approximately 100 nm, 400 nm, and 10 mu m (microparticles) were produced with high entrapment efficiencies. The in vitro lipolysis study showed that the recovery of fenofibrate in the aqueous phase for 100 nm and 400 nm LMP was significantly higher (p < 0.05) than that of microparticles after 30 min of lipolysis, suggesting that nano-sized LMP were digested to a larger extent due to greater specific surface area. The 100 nm LMP showed faster initial digestion followed by 400 nm LMP and microparticles. The area under the plasma concentration time curve (AUC) following oral administration of 100 nm LMP was significantly higher (p < 0.01) than that of microparticles and fenofibrate crystalline suspension (control). However, no significant difference was observed between the AUCs of 100 nm and 400 nm LMP. The same rank order on the in vivo absorption and the in vitro response was observed. The recovery (%) of fenofibrate partitioning into the aqueous phase during in vitro lipolysis and the AUC of plasma concentration time curve of fenofibric acid was in the order of 100 nm LMP > microparticles > control. In summary, the present study demonstrated the particle size dependence of bioavailability of fenofibrate loaded LMP in rat model which correlates well with the in vitro drug release performed in the biorelevant medium. (C) 2013 Elsevier B.V. All rights reserved. |
| WOS关键词 | WATER-SOLUBLE DRUGS ; NANOPARTICLES SLN ; LIPOLYSIS MODEL ; ORAL BIOAVAILABILITY ; FORMULATIONS ; DELIVERY ; SOLUBILITY ; DIGESTION ; DESIGN ; IMPACT |
| 资助项目 | School of Pharmaceutical Sciences, Faculty of Health and Medical Sciences, University of Copenhagen[00000000] |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000328872200024 |
| 出版者 | ELSEVIER SCIENCE BV |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/277224]  |
| 专题 | 药物制剂研究中心 |
| 通讯作者 | Mu, Huiling |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China; 2.Univ Copenhagen, Fac Hlth & Med Sci, FARMA, Dept Pharm, DK-2100 Copenhagen, Denmark 3.H Lundbeck & Co AS, Biol & Pharmaceut Sci, DK-2500 Valby, Denmark; 4.Shenyang Pharmaceut Univ, Sch Pharmaceut Sci, Dept Pharmaceut, Shenyang 110016, Peoples R China; 5.Univ Copenhagen, Fac Hlth & Med Sci, Dept Pharm, DK-2100 Copenhagen, Denmark; |
| 推荐引用方式 GB/T 7714 | Borkar, Nrupa,Xia, Dengning,Holm, Rene,et al. Investigating the correlation between in vivo absorption and in vitro release of fenofibrate from lipid matrix particles in biorelevant medium[J]. EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES,2014,51:204-210. |
| APA | Borkar, Nrupa.,Xia, Dengning.,Holm, Rene.,Gan, Yong.,Muellertz, Anette.,...&Mu, Huiling.(2014).Investigating the correlation between in vivo absorption and in vitro release of fenofibrate from lipid matrix particles in biorelevant medium.EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES,51,204-210. |
| MLA | Borkar, Nrupa,et al."Investigating the correlation between in vivo absorption and in vitro release of fenofibrate from lipid matrix particles in biorelevant medium".EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES 51(2014):204-210. |
入库方式： OAI收割
来源：上海药物研究所
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