Enhanced bioavailability of the poorly water-soluble drug fenofibrate by using liposomes containing a bile salt

International Journal of Pharmaceutics

Volumn 376, Issue 1-2, 2009, Pages 153-160

  Chen, Yaping ^a   Lu, Yi ^a   Chen, Jianming ^b   Lai, Jie ^a   Sun, Jing ^b   Hu, Fuqiang ^c   Wu, Wei ^a  

^a FUDAN UNIVERSITY   (China)

^b SECOND MILITARY MEDICAL UNIVERSITY   (China)

^c ZHEJIANG UNIVERSITY   (China)

Author keywords

Bile salt; Bioavailability; Fenofibrate; Liposome; Oral; Sodium deoxycholate

Indexed keywords

BILE SALT; CHOLESTEROL; DEOXYCHOLATE SODIUM; FENOFIBRATE; LIPOSOME; PHOSPHATIDYLCHOLINE;

ANIMAL EXPERIMENT; AREA UNDER THE CURVE; ARTICLE; CONTROLLED STUDY; DISPERSION; DOG; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG DOSAGE FORM COMPARISON; DRUG FORMULATION; DRUG RELEASE; DRUG SOLUBILITY; IN VITRO STUDY; IN VIVO STUDY; LIPOSOMAL DELIVERY; MAXIMUM PLASMA CONCENTRATION; MEMBRANE FLUIDITY; NONHUMAN; PARTICLE SIZE; PRIORITY JOURNAL; TIME TO MAXIMUM PLASMA CONCENTRATION; ULTRASOUND;

ADMINISTRATION, ORAL; ANIMALS; BILE ACIDS AND SALTS; BIOLOGICAL AVAILABILITY; DOGS; DRUG CARRIERS; DRUG DELIVERY SYSTEMS; LIPOSOMES; MEMBRANE FLUIDITY; PARTICLE SIZE; PROCETOFEN; RANDOM ALLOCATION; SOLUBILITY;

EID: 67349097388     PISSN: 03785173     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.ijpharm.2009.04.022     Document Type: Article

References (39)

1. Amselem S., Gabizon A., and Barenholz Y. Optimization and upscaling of doxorubicin-containing liposomes for clinical use. J. Pharm. Sci. 79 (1990) 1045-1052
2. Andrieux K., Forte L., Lesieur S., Paternostre M., Ollivon M., and Grabielle-Madelmont C. Solubilisation of dipalmitoylphosphatidylcholine bilayers by sodium taurocholate: a model to study the stability of liposomes in the gastrointestinal tract and their mechanism of interaction with a model bile salt. Eur. J. Pharm. Biopharm. 71 (2009) 346-355
3. Aramaki Y., Tomizawa H., Hara T., Yachi K., Kikuchi H., and Tsuchiya S. Stability of liposomes in vitro and their uptake by rat Peyer's patches following oral administration. Pharm. Res. 10 (1993) 1228-1231
4. Ariën A., Goigoux C., Baquey C., and Dupuy B. Study of in vitro and in vivo stability of liposomes loaded with calcitonin or indium in the gastrointestinal tract. Life Sci. 53 (1993) 1279-1290
5. Ariën A., Henry-Toulmé N., and Dupuy B. Calcitonin-loaded liposomes: stability under acidic conditions and bile salts-induced disruption resulting in calcitonin-phospholipid complex formation. Biochim. Biophys. Acta 1193 (1994) 93-100
6. Aungust B.J. Novel formulation strategies for improving oral bioavailability of drugs with poor membrane permeation or presystemic metabolism. J. Pharm. Sci. 82 (1993) 979-987
7. Balfour J.A., McTavish D., and Heel R.C. Fenofibrate. A review of its pharmacodynamic and pharmacokinetic properties and therapeutic use in dyslipidaemia. Drugs 40 (1990) 260-290
8. Buch P., Langguth P., Kataoka M., and Yamashita S. IVIVC in oral absorption for fenofibrate immediate release tablets using a dissolution/permeation system. J. Pharm. Sci. (2008) 10.1002/jps.21576
9. Cevc G., Gebauer D., Stieber J., Schätzlein A., and Blume G. Ultraflexible vesicles, transfersomes, have an extremely low pore penetration resistance and transport therapeutic amounts of insulin across the intact mammalian skin. Biochim. Biophys. Acta 1368 (1998) 201-215
10. Cevc G. Lipid vesicles and other colloids as drug carriers on the skin. Adv. Drug Deliv. Rev. 56 (2004) 675-711
11. Cevc G., Vierl U., and Mazgareanu S. Functional characterisation of novel analgesic product based on self-regulating drug carriers. Int. J. Pharm. 360 (2008) 18-28
12. Dapergolas G., and Gregoriadis G. Hypoglycaemic effect of liposome entrapped insulin administered intragastrically into rats. Lancet 2 (1976) 824-827
13. Degim Z., Unal N., Eşsiz D., and Abbasoglu U. The effect of various liposome formulations on insulin penetration across Caco-2 cell monolayer. Life Sci. 75 (2004) 2819-2827
14. Deshmukh D.D., Ravis W.R., and Betageri G.V. Improved delivery of cromolyn from oral proliposomal beads. Int. J. Pharm. 358 (2008) 128-136
15. Dial E.J., Rooijakkers S.H., Darling R.L., Romero J.J., and Lichtenberger L.M. Role of phosphatidylcholine saturation in preventing bile salt toxicity to gastrointestinal epithelia and membranes. J. Gastroenterol. Hepatol. 23 (2008) 430-436
16. Guay D.R. Update on fenofibrate. Cardiovasc. Drug Rev. 20 (2002) 281-302
17. Guivarc'h P.H., Vachon M.G., and Fordyce D. A new fenofibrate formulation: results of six single-dose, clinical studies of bioavailability under fed and fasting conditions. Clin. Ther. 26 (2004) 1456-1469
18. Guo J., Ping Q., and Chen Y. Pharmacokinetic behavior of cyclosporine A in rabbits by oral administration of lecithin vesicle and sandimmun neoral. Int. J. Pharm. 216 (2001) 17-21
19. Hildebrand A., Beyer K., Neubert R., Garidel P., and Blume A. Temperature dependence of the interaction of cholate and deoxycholate with fluid model membranes and their solubilization into mixed micelles. Colloids Surf. B: Biointerfaces 32 (2003) 335-351
20. Ilardia-Arana D., Kristensen H.G., and Müllertz A. Biorelevant dissolution media: aggregation of amphiphiles and solubility of estradiol. J. Pharm. Sci. 95 (2006) 248-255
21. Kawano K., Onose E., Hattori Y., and Maitani Y. Higher liposomal membrane fluidity enhances the in vitro antitumor activity of folate-targeted liposomal mitoxantrone. Mol. Pharm. 6 (2009) 98-104
22. Keating G.M., and Ormrod D. Micronised fenofibrate: an updated review of its clinical efficacy in the management of dyslipidaemia. Drugs 62 (2002) 1909-1944
23. Lee H.J., Balasubramanian S.V., Murer H., Biber J., and Morris M.E. Modulation of sulfate renal transport by alterations in cell membrane fluidity. J. Pharm. Sci. 88 (1999) 976-980
24. Li C.Y., Zimmerman C.L., and Wiedmann T.S. Solubilization of retinoids by bile salt/phospholipid aggregates. Pharm. Res. 13 (1996) 907-913
25. Lim H.J., Masin D., McIntosh N.L., Madden T.D., and Bally M.B. Role of drug release and liposome-mediated drug delivery in governing the therapeutic activity of liposomal mitoxantrone used to treat human A431 and LS180 solid tumors. J. Pharmacol. Exp. Ther. 292 (2000) 337-345
26. Lu Y., Hou S.X., Zhang L.K., Li Y., He J.Y., and Guo D.D. Transdermal and lymph targeting transfersomes of vincristine. Acta Pharm. Sin. 42 (2007) 1097-1101
27. Martin G.P., and Marriott C. Membrane damage by bile salts: the protective function of phospholipids. J. Pharm. Pharmacol. 33 (1981) 754-759
28. Mourão S.C., Costa P.I., Salgado H.R., and Gremião M.P. Improvement of antischistosomal activity of praziquantel by incorporation into phosphatidylcholine-containing liposomes. Int. J. Pharm. 295 (2005) 157-162
29. Moutardier V., Tosini F., Vlieghe P., Cara L., Delpero J.R., and Clerc T. Colloidal anticancer drugs bioavailabilities in oral administration models. Int. J. Pharm. 260 (2003) 23-38
30. Park S.H., Oh S.G., Mun J.Y., and Han S.S. Loading of gold nanoparticles inside the DPPC bilayers of liposome and their effects on membrane fluidities. Colloids Surf. B: Biointerfaces 48 (2006) 112-118
31. Porter C.J., Trevaskis N.L., and Charman W.N. Lipids and lipid-based formulations: optimizing the oral delivery of lipophilic drugs. Nat. Rev. Drug Discov. 6 (2007) 231-248
32. Rogers J.A., and Anderson K.E. The potential of liposomes in oral drug delivery. Crit. Rev. Ther. Drug Carrier Syst. 15 (1998) 421-480
33. Song K.H., Chung S.J., and Shim C.K. Preparation and evaluation of proliposomes containing salmon calcitonin. J. Control. Rel. 84 (2002) 27-37
34. Song K.H., Chung S.J., and Shim C.K. Enhanced intestinal absorption of salmon calcitonin (sCT) from proliposomes containing bile salts. J. Control. Rel. 106 (2005) 298-308
35. Straka R.J., Burkhardt R.T., and Fisher J.E. Determination of fenofibric acid concentrations by HPLC after anion exchange solid-phase extraction from human serum. Ther. Drug Monit. 29 (2007) 197-202
36. Streel B., Hubert P., and Ceccato A. Determination of fenofibric acid in human plasma using automated solid-phase extraction coupled to liquid chromatography. J. Chromatogr. B: Biomed. Sci. Appl. 742 (2000) 391-400
37. Sun W., Zou W., Huang G., Li A., and Zhang N. Pharmacokinetics and targeting property of TFu-loaded liposomes with different sizes after intravenous and oral administration. J. Drug Target. 16 (2008) 357-365
38. Xiao Y.Y., Song Y.M., Chen Z.P., and Ping Q.N. Preparation of silymarin proliposome: a new way to increase oral bioavailability of silymarin in beagle dogs. Int. J. Pharm. 319 (2006) 162-168
39. Yang L., Yang W., Bi D., and Zeng Q. A novel method to prepare highly encapsulated interferon-alpha-2b containing liposomes for intramuscular sustained release. Eur. J. Pharm. Biopharm. 64 (2006) 9-15