Proliposomes of exemestane for improved oral delivery: Formulation and in vitro evaluation using PAMPA, Caco-2 and rat intestine

International Journal of Pharmaceutics

Volumn 380, Issue 1-2, 2009, Pages 96-104

  Hiremath, Praveen S ^a   Soppimath, Kumaresh S ^a   Betageri, Guru V ^a  

^a WESTERN UNIVERSITY OF HEALTH SCIENCES   (United States)

Author keywords

Calorimetry (DSC); Dissolution; Intestinal transport; Parallel artificial membrane permeability assay (PAMPA) and Caco 2 cells; Permeability; Proliposomes

Indexed keywords

CHOLESTEROL; DIMYRISTOYLPHOSPHATIDYLGLYCEROL; DISTEAROYLPHOSPHATIDYLCHOLINE; EXEMESTANE; LIPOSOME; PHOSPHOLIPID; SOLVENT;

ANIMAL TISSUE; ARTICLE; CELL STRAIN CACO 2; CONTROLLED STUDY; DIFFERENTIAL SCANNING CALORIMETRY; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG FORMULATION; DRUG PENETRATION; DRUG SOLUBILITY; EVAPORATION; HUMAN; HUMAN CELL; IN VITRO STUDY; INTESTINE MUCOSA PERMEABILITY; LIPID COMPOSITION; MEMBRANE PERMEABILITY; NONHUMAN; PARTICLE SIZE; PHOSPHOLIPID BILAYER; POWDER; PRIORITY JOURNAL; RAT;

ABSORPTION; ADMINISTRATION, ORAL; ANDROSTADIENES; ANIMALS; AROMATASE INHIBITORS; CACO-2 CELLS; CHOLESTEROL; DRUG CARRIERS; HUMANS; INTESTINES; LIPOSOMES; MEMBRANES, ARTIFICIAL; PARTICLE SIZE; PERMEABILITY; PHOSPHATIDYLCHOLINES; PHOSPHOLIPIDS; RATS; RATS, SPRAGUE-DAWLEY; SOLUBILITY;

EID: 69549112751     PISSN: 03785173     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.ijpharm.2009.07.008     Document Type: Article

References (35)

1. Arien A., Goigouux 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
2. Artursson P., and Karlsson J. Correlation between oral drug absorption in humans and apparent drug permeability coefficients in human intestinal epithelial (CACO-2) cells. Biochem. Biophys. Res. Commun. 175 (1991) 880-885
3. Balimane P.V., Han Y.H., and Chong S. Current industrial practices of assessing permeability and p-glycoprotein interaction. AAPS J. 8 (2006) E1-E13
4. Bermejo M., Avdeef A., Ruiz A., Nalda R., Ruell J.A., Tsinman O., Gonzalez I., Fernandez C., Sanchez G., Garrigues T.M., and Merino V. PAMPA-a drug absorption in vitro model 7. Comparing rat in situ, Caco-2, and PAMPA permeability of fluoroquinolones. Eur. J. Pharm. Sci. 21 (2004) 429-441
5. Bernsdorff C., Wolf A., Winter R., and Gratton E. Effect of hydrostatic pressure on water penetration and rotational dynamics in phospholipid-cholesterol bilayers. Biophys. J. 72 (1997) 1264-1277
6. Betageri G.V. Delivery of liposomal formulations by oral or transdermal route. In: Hirota S., Okada S., Kimura R., Nozawa Y., and Oku N. (Eds). Progress in Drug Delivery System. 11th ed. (2002), Biomedical Research Foundation Publishing 77-95
7. Betageri, G.V., 2004. Enteric-coated proliposomal formulations for poorly water soluble drugs. US Patent 6,759,058.
8. Betageri, G.V., 2005. Proliposomal drug delivery system. US Patent 6,849,269.
9. Betageri G.V., Jenkins S.A., and Ravis W.R. Drug delivery using antibody-liposome conjugates. Drug Dev. Ind. Pharm. 19 (1993) 2109-2116
10. Breda M., Pianezzola E., and Benedetti M.S. Determination of exemestane, a new aromatase inhibitor, in plasma by high-performance liquid chromatography with ultraviolet detection. J. Chromatogr. 620 (1993) 225-231
11. Brocks D.R., and Betageri G.V. Enhanced oral absorption of halofantrine enantiomers after liposomal encapsulation. J. Pharm. Pharmacol. 54 (2002) 1049-1053
12. Camenisch G., Folkers G., and Waterbeemd H. Comparison of passive drug transport through Caco-2 cells and artificial membranes. Int. J. Pharm. 147 (1997) 61-70
13. Chaudhari K.B., Labhasetwar V., and Dorle A.K. Liposomes as a carrier for oral administration of insulin: effect of formulation factors. J. Microencapsul. 11 (1994) 319-325
14. Chen X., Murawski A., Patel K., Crespi C.L., and Balimane P.V. A novel design of artificial membrane for improving the PAMPA model. Pharm. Res. 25 (2008) 1511-1520
15. Costa P., and Lobo J.M.S. Modeling and comparison of dissolution profiles. Eur. J. Pharm. Sci. 13 (2001) 123-133
16. 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
17. Fukunaga M., Miller M.M., and Deftos L.J. Liposome-entrapped calcitonin and parathyroid hormone are orally effective in rats. Horm. Metab. Res. 23 (1991) 166-167
18. Kansy M., Senner F., and Gubernator K. Physicochemical high throughput screening: parallel artificial membrane permeation assay in the description of passive absorption processes. J. Med. Chem. 41 (1998) 1007-1010
19. Karlsson J., and Artursson P. A method for the determination of cellular permeability coefficients and aqueous boundary layer thickness in monolayers of intestinal epithelial (Caco-2) cells grown in permeable filter chambers. Int. J. Pharm. 71 (1991) 55-64
20. Kerns E.H., Di L., Petusky S., Farris M., Ley R., and Jupp P. Combined application of parallel artificial membrane permeability assay and Caco-2 permeability assays in drug discovery. J. Pharm. Sci. 93 (2004) 1440-1453
21. Lakeram M., Lockley D., Pendlington R., and Forbes B. Optimization of the Caco-2 permeability assay using experimental design methodology. Pharm. Res. 25 (2008) 1544-1551
22. Lennernas H. Human intestinal permeability. J. Pharm. Sci. 87 (1998) 403-410
23. Payne N.I., Timmis P., Ambrose C.V., and Warel M.D. Proliposomes: a novel solution to an old problem. J. Pharm. Sci. 75 (1986) 325-329
24. Rajesh K., Gupta R.B., and Betageri G.V. Formulation, characterization, and in vitro release of glyburide from proliposomal beads. Drug Deliv. 8 (2001) 25-27
25. Sandhya K.V., Devi G.S., and Mathew S.M. Liposomal formulations of serratiopeptidase: in vitro studies using PAMPA and Caco-2 models. Mol. Pharm. 5 (2008) 92-97
26. Scott L.J., and Wiseman L.R. Exemestane. Drugs 58 (1999) 675-680
27. 2. Pharm. Res. 15 (1998) 889-896
28. Singh A.K., Chaurasiya A., Singh M., Upadhyay S.C., Mukherjee R., and Khar R.K. Exemestane loaded self-microemulsifying drug delivery system (SMEDDS): development and optimization. AAPS PharmSciTech. 9 (2008) 628-634
29. 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
30. 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
31. Valle M., Salle E.D., Jannuzzo M.G., Poggesi I., Rocchetti M., Spinelli R., and Verotta D. A predictive model for exemestane pharmacokinetics/pharmacodynamics incorporating the effect of food and formulation. Br. J. Clin. Pharmacol. 59 (2005) 355-364
32. Watanabe E., Takahashi M., and Hayashi M. A possibility to predict the absorbability of poorly water-soluble drugs in humans based on rat intestinal permeability assessed by an in vitro chamber method. Eur. J. Pharm. Biopharm. 58 (2004) 659-665
33. Wohnsland F., and Faller B. High-throughput permeability pH profile and high-throughput alkane/water log P with artificial membranes. J. Med. Chem. 44 (2001) 923-930
34. Yan-yu X., Yun-mei S., Zhi-peng C., and Qi-neng P. Preparation of silymarin proliposome: a new way to increase oral bioavailability of silymarin in beagle dogs. Int. J. Pharm. 319 (2006) 162-168
35. Yukihiko A., Hitoshi T., Toshifumi H., Kiyoto Y., Hiroshi K., and Seishi T. Stability of liposomes in vitro and their uptake by rat Peyer's patches following oral administration. Pharm. Res. 10 (1993) 1228-1231