Bile salts enhance the intestinal absorption of lipophilic drug loaded lipid nanocarriers: Mechanism and effect in rats

International Journal of Pharmaceutics

Volumn 452, Issue 1-2, 2013, Pages 374-381

  Zhang, Zhiwen ^a   Gao, Fang ^a   Jiang, Shijun ^b   Chen, Lingli ^a   Liu, Zeying ^b   Yu, Haijun ^a   Li, Yaping ^a  

^a SHANGHAI INSTITUTE OF MATERIA MEDICA   (China)

^b EAST CHINA UNIVERSITY OF SCIENCE AND TECHNOLOGY   (China)

Author keywords

Bile salts; Caco 2 cells; Intestinal absorption; Lipid nanocarriers; Lipophilic drugs; Lymphatic transport

Indexed keywords

CANDESARTAN HEXETIL; CHOLIC ACID; NANOCARRIER;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; AREA UNDER THE CURVE; ARTICLE; CELL STRAIN CACO 2; CELL TRANSPORT; COMPARATIVE STUDY; CONTROLLED STUDY; DRUG ABSORPTION; DRUG BLOOD LEVEL; DRUG EFFECT; DRUG UPTAKE; ENDOPLASMIC RETICULUM; INTESTINE ABSORPTION; LIPOPHILICITY; MALE; NONHUMAN; PLASMA CONCENTRATION-TIME CURVE; PRIORITY JOURNAL; RAT; SIGNAL TRANSDUCTION; SUSPENSION;

EID: 84884202738     PISSN: 03785173     EISSN: 18733476     Source Type: Journal    
DOI: 10.1016/j.ijpharm.2013.05.021     Document Type: Article

References (31)

1. Bargoni, A., Cavalli, R., Caputo, O., Fundarò, A., Gasco, M.R., Zara, G.P., 1998. Solid lipid nanoparticles in lymph and plasma after duodenal administration to rats. Pharm. Res. 15, 745-750. (Pubitemid 28275652)
2. Benny, O., Fainaru, O., Adini, A., Cassiola, F., Bazinet, L., Adini, I., Pravda, E., Nahmias, Y., Koirala, S., Corfas, G., D'Amato, R.J., Folkman, J., 2008. An orally delivered small-molecule formulation with antiangiogenic and anticancer activity. Nat. Biotechnol. 26, 799-807. (Pubitemid 351961454)
3. Cai, S., Yang, Q., Bagby, T.R., Forrest, M.L., 2011. Lymphatic drug delivery using engineered liposomes and solid lipid nanoparticles. Adv. Drug Deliv. Rev. 63, 901-908.
4. Chakraborty, S., Shukla, D., Mishra, B., Singh, S., 2009. Lipid - an emerging platform for oral delivery of drugs with poor bioavailability. Eur. J. Pharm. Biopharm. 73, 1-15.
5. Chen, Y., Lu, Y., Chen, J., Lai, J., Sun, J., Hu, F., Wu, W., 2009. Enhanced bioavailability of the poorly water-soluble drug fenofibrate by using liposomes containing a bile salt. Int. J. Pharm. 376, 153-160.
6. Dahan, A., Hoffman, A., 2005. Evaluation of a chylomicron flow blocking approach to investigate the intestinal lymphatic transport of lipophilic drugs. Eur. J. Pharm. Sci. 24, 381-388. (Pubitemid 40283521)
7. Date, A.A., Desai, N., Dixit, R., Nagarsenker, M., 2010. Self-nanoemulsifying drug delivery system: formulation insights, applications and advances. Nanomedicine (London) 5, 1595-1616.
8. Ensign, L.M., Cone, R., Hanes, J., 2012. Oral drug delivery with polymeric nanoparticles: the gastrointestinal mucus barriers. Adv. Drug Deliv. Rev. 64, 557-570.
9. Gao, F., Zhang, Z., Bu, H., Huang, Y., Gao, Z., Shen, J., Zhao, C., Li, Y., 2011. Nanoemulsion improves the oral absorption of candesartan cilexetil in rats: performance and mechanism. J. Control. Release 149, 168-174.
10. Gaucher, G., Satturwar, P., Jones, M.C., Furtos, A., Leroux, J.C., 2010. Polymeric micelles for oral drug delivery. Eur. J. Pharm. Biopharm. 76, 147-158.
11. Hearnden, V., Sankar, V., Hull, K., Juras, D.V., Greenberg, M.A., Kerr, R., Lockhart, P.B., Patton, L.L., Porter, S., Thornhill, M.H., 2012. New developments and opportunities in oral mucosal drug delivery for local and systemic disease. Adv. Drug Deliv. Rev. 64, 16-28.
12. Lind, M.L., Jacobsen, J., Holm, R., Mullertz, A., 2008. Intestinal lymphatic transport of halofantrine in rats assessed using a chylomicron flow blocking approach: the influence of polysorbate 60 and 80. Eur. J. Pharm. Sci. 35, 211-218.
13. Mudie, D.M., Amidon, G.L., Amidon, G.E., 2010. Physiological parameters for oral delivery and in vitro testing. Mol. Pharm. 7, 1388-1405.
14. Nassar, T., Attili-Qadri, S., Harush-Frenkel, O., Farber, S., Lecht, S., Lazarovici, P., Benita, S., 2011. High plasma level and effective lymphatic uptake of docetaxel in an orally available nanotransporter formulation. Cancer Res. 71, 3018-3028.
15. Paliwal, R., Rai, S., Vaidya, B., Khatri, K., Goyal, A.K., Mishra, N., Mehta, A., Vyas, S.P., 2009. Effect of lipid core material on characteristics of solid lipid nanoparticles designed for oral lymphatic delivery. Nanomedicine NBM 5, 184-191.
16. Porter, C.J.H., Trevaskis, N.L., Charman, W.N., 2007. Lipids and lipid-based formulations: optimizing the oral delivery of lipophilic drugs. Nat. Rev. Drug Discov. 6, 231-248. (Pubitemid 46344627)
17. Rais, R., Acharya, C., Mackerell, A.D., Polli, J.E., 2010. Structural determinants for transport across the intestinal bile acid transporter using C-24 bile acid conjugates. Mol. Pharm. 7, 2240-2254.
18. Roger, E., Lagarce, F., Garcion, E., Benoit, J.P., 2009. Lipid nanocarriers improve paclitaxel transport through human intestinal epithelial cells by using vesiclemediated transcytosis. J. Control. Release 140, 174-181.
19. Roger, E., Lagarce, F., Garcion, E., Benoit, J.P., 2010. Biopharmaceutical parameters to consider in order to alter the fate of nanocarriers after oral delivery. Nanomedicine (London) 5, 287-306.
20. Rupp, C., Steckel, H., Muller, B.W., 2010. Solubilization of poorly water-soluble drugs by mixed micelles based on hydrogenated phosphatidylcholine. Int. J. Pharm. 395, 272-280.
21. Samstein, R.M., Perica, K., Balderrama, F., Look, M., Fahmy, T.M., 2008. The use of deoxycholic acid to enhance the oral bioavailability of biodegradable nanoparticles. Biomaterials 29, 703-708. (Pubitemid 350181045)
22. Sha, X., Yan, G., Wu, Y., Li, J., Fang, X., 2005. Effect of self-microemulsifying drug delivery systems containing labrasol on tight junctions in Caco-2 cells. Eur. J. Pharm. Sci. 24, 477-486. (Pubitemid 40387261)
23. Söderlind, E., Karlsson, E., Carlsson, A., Kong, R., Lenz, A., Lindborg, S., Sheng, J.J., 2010. Simulating fasted human intestinal fluids: understanding the roles of lecithin and bile acids. Mol. Pharm. 7, 1498-1507.
24. Talavéra, S., Felgines, C., Texier, O., Besson, C., Lamaison, J.L., Rémésy, C., 2003. Anthocyanins are efficiently absorbed from the stomach in anesthetized rats. J. Nutr. 133, 4178-4182. (Pubitemid 37505495)
25. Trevaskis, N.L., Charman, W.N., Porter, C.J.H., 2008. Lipid-based delivery systems and intestinal lymphatic drug transport: a mechanistic update. Adv. Drug Deliv. Rev. 60, 702-716.
26. Trevaskis, N.L., Porter, C.J.H., Charman, W.N., 2005. Bile increases intestinal lymphatic drug transport in the fasted rat. Pharm. Res. 22, 1863-1870. (Pubitemid 41504339)
27. Trevaskis, N.L., Porter, C.J.H., Charman, W.N., 2006. The lymph lipid precursor pool is a key determinant of intestinal lymphatic drug transport. J. Pharmacol. Exp. Ther. 316, 881-891. (Pubitemid 43131018)
28. Wiedmann, T.S., Kamel, L., 2002. Examination of the solubilization of drugs by bile salt micelles. J. Pharm. Sci. 91, 1743-1764. (Pubitemid 34810521)
29. Wiedmann, T.S., Herrington, H., Deye, C., Kalllick, D., 2001. Distribution and diffusion of sodium taurocholate and egg phosphatidylcholine aggregates in rat intestinal mucin. Pharm. Res. 18, 1489-1496. (Pubitemid 33022402)
30. Zhang, Z., Gao, F., Bu, H., Xiao, J., Li, Y., 2012. Solid lipid nanoparticles loading candesartan cilexetil enhance oral bioavailability: in vitro characteristics and absorption mechanism in rats. Nanomedicine NBM 8, 740-747.
31. Zhang, Z., Huang, Y., Gao, F., Gao, Z., Bu, H., Gu, W., Li, Y., 2011. A self-assembled nano-delivery system enhancing the oral bioavailability of daidzein: in vitro characteristics and in vivo performance. Nanomedicine (London) 6, 1365-1379.