1. Bagwe RP, Kanicky JR, Palla BJ, Patanjali PK, Shah DO. Improved drug delivery using microemulsions: rationale, recent progress, and new horizons. Critical Rev in Therap Drug Carrier Syst 2001; 18(1):77-140.
2. Charman CH. Lipids, lipophilic drugs and oral drug delivery—some emerging concepts. J Pharm Sci 2000; 89:967-978.
3. Humberstone AJ, Charman WN. Lipid-based vehicles for oral delivery of poorly soluble drugs. Adv Drug Deliv Rev 1997; 25:103-128.
4. Pouton CW. Lipid formulations for oral administration of drugs: non-emulsifying, self-emulsifying and 'self-microemulsifying' drug delivery systems. Eur J Pharm Sci. 2000; 11(suppl 2)S93-S98.
5. Pouton CW. Formulations of self-emulsifying drug delivery systems. Adv Drug Dele Rev 1997; 25:47-48.
6. Hause D. Lipid based systems for oral drug delivery: enhancing the bioavailability of poorly soluble drugs. Am Pharm Rev 2002; Nov/Dec:22-26.
7. Vonderscher J, Meinzer A. Rationale for the development of sandimmune neoral. Transplant Proc 1994; 26(5):2925-2927.
8. Meinzer A, Mueller E, Vonderscher J. Microemulsion—a suitable galenical approach for the absorption enhancement of low soluble compounds? B T Gattefosse 1995; N88:21-27.
9. Pouton CW. Self-emulsifying drug delivery systems: assessment of the efficiency of emulsification. Int J Pharm 1996; 27:335-348.
10. Gao ZG, Choi HG, Shin HJ. Physicochemical characterization and evaluation of a microemulsion system for oral delivery of cyclosporin A. Int J Pharm 1998; 161: 75-86.
11. Devani M, Ashford M, Craig DQM. The emulsification and solubilization properties of polyglycolyzed oils in self-emulsifying formulations. J Pharm Pharmacol 2004; 56(3):307-316.
12. Nazzal S, Smalyukh II, Lavrentovich DO, Khan MA. Preparation and in vitro characterization of an eutectic based semisolid self-nanoemulsified drug delivery system (SNEDDS) of ubiquinone: mechanism and progress of emulsion formation. Int J Pharm 2002; 235:247-265.
13. Shah NH, Carvajal MT, Patel CI, Infeld MH, Malick AW. Self-emulsifying drug delivery systems (SEDDS) with polyglycolyzed glycerides for improving in vitro dissolution and oral absorption of lipophilic drugs. I J Pharm 1994; 106:15-23.
14. Porter CJH, Charman WN. In vitro assessment of oral lipid based formulations. Adv Drug Del Rev 2001; 50:S127-S147.
15. Wasan KM. Formulations and physiological and biopharmaceutical issues in the development of oral lipid-based drug delivery systems. Drug Devel Ind Pharm 2001; 27(4):267-276.
16. MacGregor KJ, Embleton JK, Lacy JE, Perry EA, Solomon LJ, Seager H, Pouton CW. Influence of lipolysis on drug absorption from the gastro-intestinal tract. Adv Drug Deliv Rev 1997; 25:33-46.
17. Odeberg JM, Kaufmann P, Kroon KG, Hoglund P. Lipid drug delivery and rational formulation design for liphilic drugs with low oral bioavailability, applied to cyclosporine. Europ J Pharm Sci 2003; 20:375-382.
18. UK Patent GB 2257359 B Cyclosporin compositions for oral administration.
19. Armand M, Borel P, Ythier P, et al. Effects of droplet size, triacylglycerol composition, and calcium on the hydrolysis of complex emulsions by pancreatic lipase: an in vitro study. J Nutri Biochem 1992; 3(7):333-341.
20. Pouton CW, Charman WN. The potential of oily formulations for drug delivery to the gastro-intestinal tract. Adv Drug Deliv Rev 1997; 25:1-2.
21. O'Driscoll CM. Lipid-based formulations for intestinal lymphatic delivery. Europ J Pharm Sci 2002; 15:405-415.
22. Bach A, Babayan VM. Medium chain triglycerides: an update. Am J Clin Nutr 1982; 36:950-962.
23. Bachynsky MO, Shah NH, Patel CI, Malick AW. Factors affecting the efficiency of a self-emulsifying oral delivery system. Drug Dev Ind Pharm 1997; 23(8): 809-816.
24. Corsico B, Cistola DP, Frieden C, Storch J. The helical domain of intestinal fatty acid binding protein is critical for collisional transfer of fatty acids to phospholipid membranes. Proc Natl Acad Sci USA 1998; 95:12174-12178.
25. Borgstrom B, Dahlquist A, Lundh G, Sjovall J. Studies of intestinal digestion and absorption in the human. J Clin Invest 1957; 36:1521-1529.
26. Borgstrom B, Patton JS. Luminal events in gastrointestinal lipid digestion. In: Schultz SG, ed. Handbook of Physiology Section 6. The Gastrointestinal System IV, Bethesda: American Physiological Society, 1991:475-504.
27. Staggers JE, Hernell O, Stafford RJ, Carey MC. Physical-chemical behavior of dietary and biliary lipids during intestinal digestion and absorption. 1. Phase behavior and aggregation states of model lipid systems patterned after aqueous duodenal contents of healthy adult human beings. Biochemistry 1990; 29: 2028-2040.
28. Hernell O, Staggers JE, Carey MC. Physical-chemical behavior of dietary and biliary lipids during intestinal digestion and absorption. 2. Phase analysis and aggregation states of luminal lipids during duodenal fat digestion in healthy adult human beings. Biochemistry 1990; 29:2041-2056.
29. Carey MC, Small DM. The characteristics of mixed micellar solutions with particular reference to bile. Am J Med 1970; 49:590-598.
30. Hofmann AF, Borgstrom B. The intraluminal phase of fat digestion in man: the lipid content of the micellar and oil phases of intestinal content obtained during fat digestion and absorption. J Clin Invest 1964; 43:247-257.
31. Mattson FH, Volpenhein RA. The digestion and absorption of triglycerides. J Biol Chem 1964; 239:2772-2777.
32. Simmonds WJ, Hofmann AF, Theodor E. Absorption of cholesterol from a micellar solution: intestinal perfusion studies in man. J Clin Invest 1967; 874-890.
33. Wilson FA, Dietschy JM. Characterization of bile acid absorption across the unstirred water layer and brush border of the rat jejunum. J Clin Invest 1972; 51(12):3015-3025.
34. Mattson FH, Nolen GA. Absorbability by rats of compounds containing one to eight ester groups. J Nutr 1972; 102:1171-1176.
35. Groves MJ, Mustafa RMA. Measurement of the "spontaneity" of self-emulsifiable oils. J Phar Pharmacol 1974; 26:671-681.
36. Mansbach CM, Cohen RS, Leff PB. Isolation and properties of the mixed lipid micelles present in intestinal content during fat digestion in man. J Clin Invest 1975; 56:781-791.
37. Westergaard H, Dietschy JM. The mechanism whereby bile acid micelles increase the rate of fatty acid and cholesterol uptake into the intestinal mucosal cell. J Clin Invest 1976; 58:97-108.
38. Ho NFH, Park JY, Morozowich W, Higuchi WI. In: Roche EB ed. Design of Biopharmaceutical Properties Through Prodrugs and Analogs. Washington: APHA, 1977:35-75
39. Montet C, Reynier MO, Montet AM, Gerolami A. Distinct effects of three bile salts on cholesterol solubilization by oleate-monoolein-bile salt micelles. Biochim Biophys Acta 1979; 575(2):289-294.
40. Shiau YF, Levine GM. pH dependence of micellar diffusion and dissociation. Am J Physiol 1980; 239:G177-G182.
41. Higuchi WI, Ho NFH, Park JY, Komiya I. Rate-limiting steps and factors in drug absorption. In: Prescott LF, Nimmo WS, eds. Drug Absorption. Edinburgh: MTP Press, 1981:35-90.
42. Thomson ABR, O'Brien BD. Uptake of cholesterol into rabbit jejunum using three in vitro techniques: importance of bile acid micelles and unstirred layer resistance. Am J Physiol 1981; 241:G270-G274.
43. Iranloye TA, Pilpel N, Groves MJ. Some factors affecting the droplet size and charge of dilute oil-in-water emulsions prepared by self-emulsification. J Disp Sci Tech 1983; 4(2):109-121.
44. Shiau YF. Lipid digestion and absorption. In: Johnson LR, ed. Physiology of the Gastrointestinal Tract. 2nd ed. New York: Raven Press, 1987:1527-1556.
45. Reynier MO, Crotte C, Montet JC, Sauve P, Gerolami A. Intestinal cholesterol and oleic acid uptake from solutions supersaturated with lipids. Lipids 1987; 22(1), 28-32.
46. Poelma FGJ, Tukker JJ, Crommelin DJA. Intestinal absorption of drugs. I. The influence of taurocholate on the absorption of dantrolene in the small intestine of the rat. J Pharm Sci 1989; 78:285-289.
47. Thurnhofer H, Hauser H. Uptake of cholesterol by small intestinal brush border membrane is protein-mediated. Biochemistry 1990; 29:2142-2148.
48. Poelma FG, Breas R, Tukker JJ, Crommelin DJ. Intestinal absorption of drugs. The influence of mixed micelles on the disappearance kinetics of drugs from the small intestine of the rat. J Pharm Pharmacol 1991; 43(5):317-24.
49. Small DM. The effects of glyceride structure on absorption and metabolism. Annu Rev Nutr 1991; 11:413-434.
50. Thurnhofer H, Schnabel J, Betz M, Lipka G, Pidgeon C, Hauser H. Cholesterol-transfer protein located in the intestinal brush border membrane. Partial purification and characterization. Biochim Biophys Acta 1991; 1064:275-286.
51. Lipka G, Imfeld D, Schulthess G, Thurnhofer H, Hauser H. Protein mediated cholesterol absorption by small intestinal brush border membranes. In: Structural and Dynamic Properties of Lipids and Membranes. London, UK: Portland Press, 1992:7-18.
52. Thomson ABR, Schoeller C, Keelan M, Smith L, Clandinin MT. Lipid absorption: passing through the unstirred layers, brush-border membrane, and beyond. Can J Physiol Parmacol 1993; 71:531-555.
53. Tso P. Intestinal lipid absorption. In: Johnson LR, ed. Physiology of the Gastrointestinal Tract. 3rd ed. New York: Raven Press, 1994:1867-1907.
54. Schoeller SC, Keelan M, Mulvey G, Stremmel W, Thomson ABR. Oleic acid uptake into rat and rabbit jejunal brush border membranes. Biochim Biophys Acta 1995; 1236:51-64.
55. Narayanan VS, Storch J. Fatty acid transfer in taurodeoxycholate mixed micelles. Biochemistry 1996; 35:7466-7473.
56. Dawson A, Rudel LL. Intestinal cholesterol absorption. Curr Opin Lipidol 1999; 10:315-320.
57. Bosner SM, Lange LG, Stenson WF, Ostlund RE. Percent cholesterol absorption in normal women and men quantified with dual stable isotopic tracers and negative ion mass spectrometry. J Lipid Res 1999; 40:302-308.
58. Wang DQH. New concepts of mechanism of intestinal cholesterol absorption. Ann Hepatol 2003; 2(3):113-121.
59. Kramer W, Girbig F, Corsiero D, et al. Intestinal cholesterol absorption: identification of different binding proteins for cholesterol and cholesterol absorption inhibitors in the enterocyte brush border membrane. Biochim Biophys Acta 2003; 1633(1):13-26.
60. Mel'nikov SM, Seijen T, Hoorn JW, Eijkelenboom AP. Effect of phytosterols and phytostanols on the solubilization of cholesterol by dietary mixed micelles: an in vitro study. Chem Phys Lipids 2004; 127(2):121-141.
61. Wiedmann TS, Liang W, Kamel L. Solubilization of drugs by physiological mixtures of bile salts. Pharm Res 2002; 19(8):1203-1208.
62. Bakatselou V, Oppenheim RC, Dressman JB. Solubilization and wetting effects of bile salts on the dissolution of steroids. Pharm Res 1991; 8(12):1461-1469.
63. TenHoor CN, Bakatselou V, Dressman JB. Solubility of mefenamic acid under simulated fed- and fasted-state conditions. Pharm Res 1991; 8(9):1203-1205.
64. Mithani SD, Bakatselou V, TenHoor CN, Dressman JB. Estimation of the increase in solubility of drugs as a function of bile salt concentration. Pharm Res 1996; 13(1):163-167.
65. Constantinides PP, Scalart JP. Formulation and physical characterization of water-in-oil microemulsions containing long- versus medium-chain glycerides. Int J Pharm 1997; 158:57-68.
66. Hauss DJ, Fogal SE, Ficorilli JV, et al. Lipid-based delivery systems for improving the bioavailability and lymphatic transport of a poorly water-soluble LTB4 inhibitor. J Pharm Sci 1998; 87:164-169.
67. Cho MJ, Chen FJ, Huczek DL. Effects of inclusion complexation on the transepithelial transport of a lipophilic substance in vitro. Pharm Res 1995; 12(4):560-564.
68. Ho SY, Storch J. Common mechanisms of monoacylglycerol and fatty acid uptake by human intestinal Caco-2 cells. Amer J Physio 2001; 281(4 Pt 1): C1106-C1117.
69. Schulthess G, Lipka G, Compassi S, et al. Absorption of monoacylglycerols by small intestinal brush border membrane. Biochemistry 1994; 33(15):4500-4508.
70. Hsu KT, Storch J. Fatty acid transfer from liver and intestinal fatty acid-binding proteins to membranes occurs by different mechanisms. J Biol Chem 1996; 271(23):13317-13323.
71. Trotter PJ, Ho SY, Storch J. Fatty acid uptake by Caco-2 human intestinal cells. J Lipid Res 1996; 37(2):336-46.
72. Ho SY, Delgado L, Storch J. Monoacylglycerol metabolism in human intestinal Caco-2 cells: evidence for metabolic compartmentation and hydrolysis. J Biol Chem 2002; 277(3):1816-1823.
73. Storch J, Kleinfeld AM. Transfer of long chain fluorescent free fatty acids between unilamellar vesicles. Biochemistry 1986; 25(7):1717-1726.
74. Dressman JB, Reppas C. In vitro-in vivo correlations for lipophilic poorly water soluble drugs. Europ J Pharm Sci 1986; 11(suppl 2):S73-S80.
75. Austgen L, Bowen RA, Rouge M. Pathophysiology of the Digestive System. Colorado State University, http://arbl.cvmbs.colostate.edu/hbooks/contrib.html (2004). See statement: "As the ingesta is mixed, the bile salt mixed micelles bump into the brush border and the lipids, including monoglyceride and fatty acids, are absorbed."
Was this article helpful?