Incorporation of cyclosporin A in solid lipid nanoparticles (SLN)

被引:121
作者
Ugazio, E [1 ]
Cavalli, R [1 ]
Gasco, MR [1 ]
机构
[1] Univ Turin, Dipartimento Sci & Tecnol Farmaco, I-10125 Turin, Italy
关键词
cyclosporin A; solid lipid nanoparticles; colloidal carriers;
D O I
10.1016/S0378-5173(02)00268-5
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
The cyclic undecapeptide cyclosporin A (CyA) a potent immunosuppressive drug used in many therapies, is extremely hydrophobic. Commercial products employ solubilising agents to improve gastrointestinal absorption. In the present study CyA solid lipid nanoparticles (SLN) are prepared from warm o/w microemulsion. dispersed in cold water. The matrix chiefly consists of stearic acid. phospliatidylcholine and taurocholate LIP to 13% of CyA can be incorporated. The average diameter of CyA-loaded SLNs is below 300 rim and transmission electron microscopy (TEM) analysis shows them to be spherical. In vitro release of CyA from SLNs is low. CyA-loaded SLNs can be proposed for most administration routes. in particular for the duodenal route. (C) 2002 Elsevier Science B.V. All rights reserved.
引用
收藏
页码:341 / 344
页数:4
相关论文
共 14 条
[1]  
[Anonymous], 1981, J ETHNOBIOL
[2]   Solid lipid nanoparticles in lymph and plasma after duodenal administration to rats [J].
Bargoni, A ;
Cavalli, R ;
Caputo, O ;
Fundarò, A ;
Gasco, MR ;
Zara, GP .
PHARMACEUTICAL RESEARCH, 1998, 15 (05) :745-750
[3]   Transmucosal transport of tobramycin incorporated in SLN after duodenal administration to rats.: Part I -: A pharmacokinetic study [J].
Cavalli, R ;
Zara, GP ;
Caputo, O ;
Bargoni, A ;
Fundarò, A ;
Gasco, MR .
PHARMACOLOGICAL RESEARCH, 2000, 42 (06) :541-545
[4]   CYCLOSPORINE CLINICAL PHARMACOKINETICS [J].
FAHR, A .
CLINICAL PHARMACOKINETICS, 1993, 24 (06) :472-495
[5]  
Gasco M.R., 1997, PHARM TECHNOL EUR, V9, P52
[6]  
GASCO MR, 2001, PHARM TECHNOL EUR, V13, P32
[7]   Lecithin vesicular carriers for transdermal delivery of cyclosporin A [J].
Guo, JX ;
Ping, QN ;
Sun, GQ ;
Jiao, CH .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2000, 194 (02) :201-207
[8]  
Mueller R., 1998, Patent, Patent No. [19819273, DE19819273A1]
[9]   CYCLOSPORINE - A REVIEW OF THE PHARMACOKINETIC PROPERTIES, CLINICAL EFFICACY AND TOLERABILITY OF A MICROEMULSION-BASED FORMULATION (NEORAL) [J].
NOBLE, S ;
MARKHAM, A .
DRUGS, 1995, 50 (05) :924-941
[10]  
PENKLER L, 1999, PHARM CICLOSPORIN FO