Stable drug encapsulation in micelles and microemulsions

被引:320
作者
Narang, Ajit S. [2 ]
Delmarre, David [3 ]
Gao, Danchen [1 ]
机构
[1] Anchen Pharmaceut Inc, Irvine, CA 92618 USA
[2] Bristol Myers Squibb Co, Biopharmaceut R&D, New Brunswick, NJ 08903 USA
[3] Capsugel Pharmaceut R&D Ctr, F-67412 Illkirch Graffenstaden, France
关键词
bioavailability; hydrophobic drugs; micelles; microemulsions; precipitation; SEDDS; SMEDDS; self-emulsifying; solubilization; self-microemulsifying;
D O I
10.1016/j.ijpharm.2007.08.057
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Oral absorption of hydrophobic drugs can be significantly improved using lipid-based non-particulate drug delivery systems, which avoid the dissolution step. Micellar and microemulsion systems, being the most dispersed of all, appear the most promising. While these systems show high drug, entrapment and release under sink conditions, the improvement in oral drug bioavailability is often unpredictable. The formulation and drug-related biopharmaceutical aspects of these systems that govern oral absorption have been widely studied. Among these, preventing drug precipitation upon aqueous dilution could play a predominant role in many cases. Predictive ability and quick methods for assessment of such problems could be very useful to the formulators in selecting lead formulations. This review will attempt to summarize the research work that could be useful in developing these tools. (c) 2007 Elsevier B.V. All rights reserved.
引用
收藏
页码:9 / 25
页数:17
相关论文
共 79 条
[1]   Effect of adding an amphiphilic solubilization improver, sucrose distearate, on the solubilization capacity of nonionic microemulsions [J].
Aramaki, K ;
Hayashi, T ;
Katsuragi, T ;
Ishitobi, M ;
Kunieda, H .
JOURNAL OF COLLOID AND INTERFACE SCIENCE, 2001, 236 (01) :14-19
[2]   MONODISPERSE COLLOIDS OF TRANSITION-METAL AND LANTHANIDE COMPOUNDS [J].
BEATTIE, JK .
PURE AND APPLIED CHEMISTRY, 1989, 61 (05) :937-941
[3]   Amphotericin B in oil-water lecithin-based microemulsions: Formulation and toxicity evaluation [J].
Brime, B ;
Moreno, MA ;
Frutos, G ;
Ballesteros, MP ;
Frutos, P .
JOURNAL OF PHARMACEUTICAL SCIENCES, 2002, 91 (04) :1178-1185
[4]   Effects of epidermal growth factor microemulsion formulation on the healing of stress-induced gastric ulcers in rats [J].
Çelebi, N ;
Türkyilmaz, A ;
Gönül, B ;
Özogul, C .
JOURNAL OF CONTROLLED RELEASE, 2002, 83 (02) :197-210
[5]  
CHO YW, 1989, LANCET, V2, P1518
[6]   A lecithin-based microemulsion of rh-insulin with aprotinin for oral administration:: Investigation of hypoglycemic effects in non-diabetic and STZ-induced diabetic rats [J].
Çilek, A ;
Çelebi, N ;
Tirnaksiz, F ;
Tay, A .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2005, 298 (01) :176-185
[7]   LIPID MICROEMULSIONS FOR IMPROVING DRUG DISSOLUTION AND ORAL ABSORPTION - PHYSICAL AND BIOPHARMACEUTICAL ASPECTS [J].
CONSTANTINIDES, PP .
PHARMACEUTICAL RESEARCH, 1995, 12 (11) :1561-1572
[8]   Comparative bioavailability of neoral and sandimmune in cardiac transplant recipients over 1 year [J].
Cooney, GF ;
Jeevanandam, V ;
Choudhury, S ;
Feutren, G ;
Mueller, EA ;
Eisen, HJ .
TRANSPLANTATION PROCEEDINGS, 1998, 30 (05) :1892-1894
[9]   Use of a dynamic in vitro lipolysis model to rationalize oral formulation development for poor water soluble drugs:: Correlation with in vivo data and the relationship to intra-enterocyte processes in rats [J].
Dahan, Arik ;
Hoffman, Amnon .
PHARMACEUTICAL RESEARCH, 2006, 23 (09) :2165-2174
[10]   Crystallisation of oil-in-water emulsions - Amphiphile directed nucleation in aqueous emulsions of m-chloronitrobenzene [J].
Davey, RJ ;
Hilton, AM ;
Garside, J ;
delaFuente, M ;
Edmondson, M ;
Rainsford, P .
JOURNAL OF THE CHEMICAL SOCIETY-FARADAY TRANSACTIONS, 1996, 92 (11) :1927-1933