Design of Lipid Matrix Particles for Fenofibrate: Effect of Polymorphism of Glycerol Monostearate on Drug Incorporation and Release
文献类型：期刊论文
| 作者 | Xia, Dengning1,2; Cui, Fude2; Gan, Yong3 ; Mu, Huiling1; Yang, Mingshi1
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| 刊名 | JOURNAL OF PHARMACEUTICAL SCIENCES
 |
| 出版日期 | 2014-02 |
| 卷号 | 103期号:2页码:697-705 |
| 关键词 | polymorphism lipids drug-excipient interaction stability dissolution glycerol monostearate fenofibrate lipid matrix particles drug incorporation |
| ISSN号 | 0022-3549 |
| DOI | 10.1002/jps.23830 |
| 文献子类 | Article |
| 英文摘要 | The effect of polymorphism of glycerol monostearate (GMS) on drug incorporation and release from lipid matrix particles (LMPs) was investigated using fenofibrate as a model drug. X-ray powder diffraction and differential scanning calorimetry were used to study the polymorphism change of GMS and the drug incorporation in GMS matrix. When medium-chain triglycerides (MCT) was absent, melted GMS was frozen to alpha-form of GMS with drug molecularly dispersed, whereas beta-form of GMS was formed with part of drug crystallized out when the ratio of GMS/MCT in the lipid matrix was 2:1 (w/w). For LMP composed of GMS/MCT (2:1, w/w) prepared, GMS was in alpha-form when the particles were in nanometer range, whereas GMS was in beta-form when lipid particles were in micrometer range. The model drug was molecularly dispread in alpha-form lipid nanoparticles, whereas part of drug was expulsed out from microparticles because of the denser crystalline packing than alpha-form of GMS, and caused a faster drug release from lipid microparticles than that from nanoparticles. During the storage, the transformation of GMS from alpha-form into the more stable beta-form promoted drug expulsion and caused drug precipitation. In conclusion, the polymorphism of GMS is an important factor determining particle stability, drug incorporation, and the release of the drug from LMP. Critical attention should be paid on the investigation as well as control of the lipid polymorphism when formulating lipid-based matrix particles. (c) 2013 Wiley Periodicals, Inc. and the American Pharmacists Association |
| WOS关键词 | WATER-SOLUBLE DRUGS ; NANOPARTICLES SLN ; SOLID DISPERSIONS ; ORAL DELIVERY ; SOLUBILITY ; CRYSTALLIZATION ; FORMULATIONS ; MISCIBILITY ; PARAMETERS |
| 资助项目 | Lundbeckfonden (Copenhagen, Denmark)[479/06] |
| WOS研究方向 | Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000341311100039 |
| 出版者 | WILEY-BLACKWELL |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/277192]  |
| 专题 | 药物制剂研究中心 |
| 通讯作者 | Yang, Mingshi |
| 作者单位 | 1.Univ Copenhagen, Dept Pharm, Fac Hlth & Med Sci, DK-2100 Copenhagen, Denmark; 2.Shenyang Pharmaceut Univ, Sch Pharmaceut Sci, Dept Pharmaceut, Shenyang 110016, Peoples R China; 3.Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Xia, Dengning,Cui, Fude,Gan, Yong,et al. Design of Lipid Matrix Particles for Fenofibrate: Effect of Polymorphism of Glycerol Monostearate on Drug Incorporation and Release[J]. JOURNAL OF PHARMACEUTICAL SCIENCES,2014,103(2):697-705. |
| APA | Xia, Dengning,Cui, Fude,Gan, Yong,Mu, Huiling,&Yang, Mingshi.(2014).Design of Lipid Matrix Particles for Fenofibrate: Effect of Polymorphism of Glycerol Monostearate on Drug Incorporation and Release.JOURNAL OF PHARMACEUTICAL SCIENCES,103(2),697-705. |
| MLA | Xia, Dengning,et al."Design of Lipid Matrix Particles for Fenofibrate: Effect of Polymorphism of Glycerol Monostearate on Drug Incorporation and Release".JOURNAL OF PHARMACEUTICAL SCIENCES 103.2(2014):697-705. |
入库方式： OAI收割
来源：上海药物研究所
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