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Research Article

LIPID-BASED FORMULATIONS FOR ORAL ADMINISTRATION: OPPORTUNITIES FOR BIOAVAILABILITY ENHANCEMENT AND LIPOPROTEIN TARGETING OF LIPOPHILIC DRUGS

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Pages 215-257 | Published online: 31 Aug 2001

REFERENCES

  • Shiau Y.-F. Mechanism of intestinal fat absorption. Am. J. Physiol. 1981; 240: G1–G9
  • Bisgaier C. L., Glickman R. M. Intestinal synthesis, secretion and transport of lipoproteins. Annu. Rev. Physiol. 1983; 45: 625–636
  • Thomson A. B.R., Keelan M., Garg M. L., Clandinin M. T. Intestinal aspects of lipid absorption: in review. Can. J. Physiol. Pharmacol. 1989; 67: 179–191
  • Tso P. Intestinal lipid absorption. Physiology of the Gastrointestinal Tract, L. R. Johnson, Chief. Raven Press, New York 1994; 1867–1908
  • Carey M. C., Small D. M., Bliss C. M. Lipid digestion and absorption. Annu. Rev. Physiol. 1983; 45: 651–677
  • Staggers J. E., Hernell O., Stafford R. J., Carey M. C. Physical-chemical behaviour of dietary and biliary lipids during intestinal digestion and absorption. 1. Phase behaviour and aggregation states of model lipid systems patterned after aqueous duodenal contents of healthy adult human beings. Biochemistry 1990; 29: 2028–2040
  • Hernell O., Staggers J. E., Carey M. C. Physical-chemical behaviour 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
  • Hoffman N. E. The relationship between uptake in vitro of oleic acid and micellar solubilization. Biochim. Biophys. Acta 1970; 196: 193–203
  • Simmonds W. J. The role of micellar solubilisation in lipid absorption. Aust. J. Exp. Biol. Med. Sci. 1972; 50: 403–421
  • Westergaard H., Dietschy J. M. The mechanism whereby bile acid micelles increase the rate of fatty acid and cholesterol uptake into the mucosal cell. J. Clin. Invest. 1976; 58: 97–108
  • Shiau Y.-F., Fernandez P., Jackson M. J., McMonagle S. Mechanisms maintaining alow pH microclimate in the intestine. Am. J. Physiol. 1985; 248: G608–619
  • Shiau Y.-F. Mechanism of intestinal fatty acid uptake in the rat: the role of an acidic microclimate. J. Physiol. 1990; 421: 463–474
  • Kiyasu J. Y., Bloom B., Chaikoff I. L. The portal transport of absorbed fatty acids. J. Biol. Chem. 1952; 199: 415–419
  • Spady D. K. Lipoproteins in biological fluids and compartments: synthesis interconversions and catabolism. Lipoproteins as Carriers of Pharmacological Agents, J. M. Shaw. Marcel Dekker, New York 1991; 1–44
  • Fielding P. E., Fielding C. J. Dynamics of lipoprotein transport in the circulatory system. Biochemistry of Lipids Lipoproteins and Membranes, D. E. Vance, J. Vance. Elsevier, New York 1991; 427–459
  • Hunt J. N., Knox M. T. A relation between the chain length of fatty acids and the slowing of gastric emptying. J. Physiol. 1968; 194: 327–336
  • Anderberg E. K., Lindmark T., Artursson P. Sodium caprate elicits dilatations in human intestinal tight junctions and enhances drug absorption by the paracellular route. Pharm. Res. 1993; 10: 857–864
  • Aungst B. J. Novel formulation strategies for improving oral bioavailability of drugs with poor membrane permeation or presystemic metabolism. J. Pharm. Sci. 1993; 82: 979–987
  • Swenson E. S., Milisen W. B., Curatolo W. Intestinal permeability enhancement: efficacy, acute local toxicity, and reversibility. Pharm. Res. 1994; 11: 1132–1142
  • Armstrong N. A., James K. C. Drug release from lipid based dosage forms. Part 2. Int. J. Pharmaceut. 1980; 6: 195–204
  • Humberstone A. J., Charman W. N. Lipid-based vehicles for the oral delivery of poorly water soluble drugs. Adv. Drug Deliv. Rev. 1997; 25: 103–128
  • Charman W. N., Porter C. J.H., Mithani S., Dressman J. B. Physicochemical and physiological mechanisms for the effects of food on drug absorption: the role of lipids and pH. J. Pharm. Sci. 1997; 86: 269–282
  • Chakrabarti S., Belpaire F. M. Bioavailability of phenytoin in lipid containing dosage forms in rats. J. Pharm. Pharmac. 1978; 30: 330–331
  • Hargrove J. T., Maxson W. S., Wentz A. C. Absorption of oral progesterone is influenced by vehicle and particle size. Am. J. Obstet. Gynecol. 1989; 161: 948–951
  • Abrams L. S., Weintraub H. S., Patrick J. E., McGuire J. L. Comparative bioavailability of a lipophilic steroid. J. Pharm. Sci. 1978; 67: 1287–1290
  • Yamaoka Y., Roberts R. D., Stella V. J. Low-melting phenytoin prodrugs as alternative oral delivery modes for phenytoin: a model for other high-melting sparingly water-soluble drugs. J. Pharm. Sci. 1983; 72: 400–405
  • Stella V., Haslam J., Yata N., Okada H., Lindenbaum S., Higuchi T. Enhancement of bioavailability of a hydrophobic amine antimalarial by formulation with oleic acid in a soft gelatin capsule. J. Pharm. Sci. 1978; 67: 1375–1377
  • Tokumura T., Tsushima Y., Tatsuishi K., Kayano M., Machida Y., Nagai T. Enhancement of the oral bioavailability of cinnarizine in oleic acid in beagle dogs. J. Pharm. Sci. 1987; 76: 286–288
  • Yamahira Y., Noguchi T., Takenaka H., Maeda T. Biopharmaceutical studies of lipid containing oral dosage forms: relationship between drug absorption rate and digestibility of vehicles. Int. J. Pharmaceut. 1979; 3: 23–31
  • Myers R. A., Stella V. J. Systemic bioavailability of penclomedine (NSC338720) from oil-in-water emulsions administered intraduodenally to rats. Int. J. Pharmaceut. 1992; 78: 217–226
  • Palin K. J., Wilson C. M. The effect of different oils on the absorption of probucol in the rat. J. Pharm. Pharmac. 1984; 36: 641–643
  • Carrigan P. J., Bates T. R. Biopharmaceutics of drugs administered in lipid-containing dosage forms I: GI absorption of griseofulvin from an oil-in-water emulsion in the rat. J. Pharm. Sci. 1973; 62: 1476–1479
  • Bates T. R., Carrigan P. J. Apparent absorption kinetics of micronized griseofulvin after its oral administration on single- and multiple-dose regimens to rats as a corn oil-in-water emulsion and aqueous suspension. J. Pharm. Sci. 1975; 64: 1475–1481
  • Charman W. N., Rogge M. C., Boddy A. W., Berger B. M. Effect of food and a monoglyceride emulsion formulation on danazol bioavailability. J. Clin. Pharmacol. 1993; 33: 381–386
  • Serajuddin A. T., Sheen P., Mufson D., Bernstein D. F., Augustine M. A. Physicochemical basis of increased bioavailability of a poorly water-soluble drug following oral administration as organic solutions. J. Pharm. Sci. 1988; 77: 325–329
  • Hauss D. J., Fogal S. E., Ficorilli J. V., Price C. A., Roy T., Jayaraj A. A., Keirns J. J. Lipid-based delivery systems for improving the bioavailability and lymphatic transport of a poorly water soluble LTB4 inhibitor. J. Pharm. Sci. 1988; 87: 164–169
  • Kimura T., Fukui E., Kageyu A., Kurohara Y., Nakayama T., Morita Y., Shibusawa K., Ohsawa S., Takeda Y. Enhancement of oral bioavailability of d-a-tocopherol acetate by lecithin-dispersed aqueous preparations containing medium-chain triglyceridies in rats. Chem. Pharm. Bull. 1989; 37: 439–441
  • Groves M. J., de Galindez D. A. The self-emulsifying action of mixed surfactants in oil. Acta. Pharm. Suec. 1976; 13: 361–372
  • Groves M. J., Mustafa R. M.A., Carless J. E. Phase studies of mixed phosphated surfactants n-hexane and water. J. Pharm. Pharmac. 1974; 26: 616–623
  • Groves M. J., Mustafa R. M.A. Measurement of the ‘spontaneity’ of self-emulsifiable oils. J. Pharm. Pharmac. 1974; 26: 671–681
  • Pouton C. W. Self-emulsifying drug delivery systems: assessment of their efficiency of emulsification. Int. J. Pharmaceut. 1985; 27: 335–348
  • Wakerly M. G., Pouton C. W., Meakin B. J., Morton F. S. Self-emulsification of vegetable oil-nonsurfactant mixtures: a proposed mechanism of action. Am. Chem. Soc. Symp. Ser. 1986; 311: 242–255
  • Craig D. Q.M., Lievens H. S.R., Pitt K. G., Storey D. E. An investigation into the physico-chemical properties of self-emulsifying systems using low frequency dielectric spectroscopy, surface tension measurements and particle size analysis. Int. J. Pharmaceut. 1993; 96: 147–155
  • Craig D. Q., Barker S. A., Banning D., Booth S. W. Investigation into the mechanisms of self-emulsification using particle size analysis and low frequency dielectric spectroscopy. Int. J. Pharmaceut. 1995; 114: 103–110
  • Pouton C. W. Formulation of self-emulsifying drug delivery systems. Adv. Drug. Deliv. Rev. 1997; 25: 47–58
  • Gershanik T., Benita S. Positively charged self-emulsifying oil formulation for improving oral bioavailability of progersterone. Pharm. Dev. Technol. 1996; 1: 147–157
  • Charman S. A., Charman W. N., Rogge M. C., Wilson T. D., Dutko F. J., Pouton C. W. Self-emulsifying drug delivery systems: formulation and biopharmaceutical evaluation of an investigational lipophilic compound. Pharm. Res. 1992; 9: 87–93
  • Lin J. H., Chen I., Lievens H. The effect of dosage forms on the oral absorption of L-365,260, a potent CCKB receptor antagonist in dogs. Pharm. Res. 1991; 8: S-272
  • Shah N. H., Carvajal M. T., Patel C. I., Infeld M. H., Malick A. W. Self-emulsifying drug delivery systems (SEDDS) with polyglycolyzed glycerides for improving in vitro dissolution and oral absorption of lipophilic drugs. Int. J. Pharmaceut. 1994; 106: 15–23
  • Kinget R., De Greef H. Absorption characteristics of novel 8-MOP semi-solid-lipid-matrix formulations: in vitro–in vivo correlation. Int. J. Pharmaceut. 1994; 110: 65–73
  • Kelm G. R., Penafiel J. V., Deibel R. M., Kinnett G. O., Meredith M. P. The relative absorption of tebufalone from self-emulsifying solutions in the beagle dog. Pharm. Res. 1993; 10: S211
  • Matuszewska B., Hettrick L., Bondi J. V., Storey D. E. Comparative bioavailability of L-683,453, a 5α-reductase inhibitor, from a self emulsifying drug delivery system in beagle dogs. Int. J. Pharm. 1996; 136: 147–154
  • Gumkowski M. J., Fournier L. A., Tierney N. K., Curatolo W. J. Improved bioavailability through use of soft gelatin formulations of terlakiren, a tripeptide renin inhibitor. Pharm. Res. 1994; 11: S286
  • Malcolmson C., Satra C., Kantaria S., Sidhu A., Lawrence M. J. Effect of oil on the level of solubilisation of testosterone propionate into non-ionic oil-in-water microemulsions. J. Pharm. Sci. 1988; 87: 109–116
  • Malcolmson C., Lawrence M. J. Comparison of the incorporation of model steroids into non-ionic micellar and microemulsion systems. J. Pharm. Pharmacol. 1993; 45: 141–143
  • Sarciaux J. M., Acar L., Sado P. A. Using microemulsion formulations for oral drug delivery of therapeutic peptides. Int. J. Pharm. 1995; 120: 127–136
  • Constantinides P. P. Lipid microemulsions for improving drug dissolution and oral absorption: physical and biopharmaceutical aspects. Pharm. Res. 1995; 12: 1561–1572
  • New R. R.C., Kirby C. J. Solubilisation of hydrophilic drugs in oily formulations. Adv. Drug Deliv. Rev. 1997; 25: 59–69
  • Constantinides P. P., Scalart J. P. Formulation and physical characterisation of water-in-oil microemulsions containing long- versus medium chain glycerides. Int. J. Pharm. 1997; 158: 57–68
  • Reymond J., Sucker H. in vitro model for ciclosporin intestinal absorption in lipid vehicles. Pharm. Res. 1988; 5: 673–676
  • Reymond J., Sucker H., Vonderscher J. In vivo model for ciclosporin intestinal absorption in lipid vehicles. Pharm. Res. 1988; 5: 677–679
  • Behrens D., Fricker R., Bodoky A., Drewe J., Harder F., Heberer M. Comparison of cyclosporin A absorption from LCT and MCT solutions following intrajejunal administration in conscious dogs. J. Pharm. Sci. 1996; 85: 666–668
  • Beveridge T., Gratwohl A., Michot F., Niederberger W., Nuesch E., Nussbaumer K., Schaub P., Speck B. Cyclosporin A: pharmacokinetics after a single dose in man and serum levels after multiple dosing in recipients of allogenic bone marrow grafts. Curr. Ther. Res. 1981; 30: 5–18
  • Frey F. J., Horber F. F., Frey B. M. Trough levels and concentration time curves of cyclosporin in patients undergoing renal transplantation. Clin. Pharmac. Ther. 1988; 43: 55–62
  • Ptachcinski R., Venkataramanan R., Burckart G. J. Clinical pharmacokinetics of cyclosporin. Clinical Pharmacokin. 1986; 11: 107–132
  • Ptachcinski R. J., Venkataramanan R., Rosenthal J. T., Burckart G. J., Taylor R. J., Hakala T. R. The effect of food on cyclospocrin absorption. Transplantation 1985; 40: 174–176
  • Gupta S. K., Benet L. Z. High fat meals increase the clearance of cyclosporine. Pharm. Res. 1990; 7: 46–48
  • Tarr B. D., Yalkowsky S. H. Enhanced intestinal absorption of cyclosporine in rats through the reduction of emulsion droplet size. Pharm. Res. 1989; 6: 40–43
  • Ritschel W. A. Microemulsions for improved peptide absorption from the gastrointestinal tract. Meth. Find. Exp. Clin. Pharmacol. 1991; 13: 205–220
  • Ritschel W. A., Adolf S., Ritschel G. B., Schroeder T. Improvement of peroral absorption of cyclosporine A by microemulsions. Meth. Find. Exp. Clin. Pharmacol. 1990; 12: 127–134
  • Gao Z. G., Choi H. G., Shin H. J., Park K. M., Lim S. J., Hwang K. J., Kim C. K. Physicochemical characterisation and evaluation of a microemulsion system for oral delivery of cyclosporin A. Int. J. Pharmaceut. 1998; 161: 75–86
  • Drewe J., Meier R., Vonderscher J., Kiss D., Posanski U., Kissel T., Gyr K. Enhancement of the oral absorption of cyclosporin in man. Br. J. Clin. Pharmacol. 1992; 34: 60–64
  • Bojrup M., Qi Z., Bjorkman S., Ostraat O., Landin B., Ljusberg-Wahren H., Ekberg H. Bioavailability of cyclosporine in rats after intragastric administration: a comparitive study of the L2 phase and two other lipid-based vehicles. Transplant. Immunol. 1996; 4: 313–317
  • Mueller E. A., Kovarik J. M., van Bree J. B., Tetzloff W., Grevel J., Kutz K. Improved dose linearity of cyclosporine pharmacokinetics from a microemulsion formulation. Pharm. Res. 1994; 11: 301–304
  • Kovarik J. M., Mueller E. A., van Bree J. B., Tetzloff W., Kutz K. Reduced inter and intraindividual variability in cyclosporine pharmacokinetics form a microemulsion formulation. J. Pharm. Sci. 1994; 83: 444–446
  • Trull A. K., Tan K. K.C., Tan L., Alexander G. J.M., Jamieson N. J. Absorption of cyclosporin from conventional and new microemulsion oral formulations in liver transplant recipients with external biliary diversion. Br. J. Clin. Pharmacal. 1995; 39: 627–631
  • Mueller E. A., Kovarik J. M., van Bree J. B., Grevel J., Lucker P. W., Kutz K. Influence of a fat rich meal on the pharmacokinetics of a new oral formulation of cyclosporine in a crossover comparison with the market formulation. Pharm. Res. 1994; 11: 151–155
  • Milton K. A., Edwards G., Ward S. A., Orme M. L., Breckenridge A. M. Pharmacokinetics of halofantrine in man: effects of food and dose size. Br. J. Clin. Pharmacol. 1989; 28: 71–77
  • Humberstone A. J., Porter C. J.H., Charman W. N. A physicochemical basis for the effect of food on the absolute oral bioavailability of halofantrine. J. Pharm. Sci. 1996; 85: 525–529
  • Khoo S.-M., Humberstone A. J., Porter C. J.H., Edwards G. A., Charman W. N. Formulation design and bioavailability assessment of lipidic self-emulsifying formulations of halofantrine. Int. J. Pharmaceut. 1998; 167: 155–164
  • Benet L. Z., Wu C.-Y., Hebert M. F., Wacher V. J. Intestinal drug metabolism and antitransport processes: a potential paradigm shift in oral drug delivery. J. Cont. Rel. 1996; 39: 139–143
  • Wacher V. J., Salphati L., Benet L. Z. Active secretion and enterocytic drug metabolism barriers to drug absorption. Adv. Drug Deliv. Rev. 1996; 20: 99–112
  • Thummel K. E., Kunze K. L., Shen D. D. Enzyme-catalised processes of first pass hepatic and intestinal drug extraction. Adv. Drug Deliv. Rev. 1997; 27: 99–127
  • Thummel K. E., O'Shea D., Paine M. F., Shen D. D., Kunze K. L., Perkins J. D., Wilkinson G. R. Oral first pass elimination of midazolam involves both gastrointestinal and hepatic CYP3A-mediated metabolism. Clin. Pharmacol. Ther. 1996; 59: 491–502
  • Hebert M. F. Contributions of hepatic and intestinal metabolism and P-glycoprotein to cyclosporine and tacrolimus oral drug delivery. Adv. Drug. Del. Rev. 1997; 27: 201–214
  • Vickers A. E.M., Fischer V., Connors S., Fisher R. L., Baldeck J. P., Maurer G., Brendel K. Cyclosporin A metabolism in human liver, kidney and intestinal slices. Drug Metab. Dispos. 1992; 20: 802–809
  • Wu C.-Y., Benet L. Z., Hebert M. F., Gupta S. K., Rowland M., Gomez D. Y., Wacher V. J. Differentiation of absorption and first-pass gut and hepatic metabolism in humans: studies with cyclosporine. Clin. Pharmacol. Ther. 1995; 58: 492–497
  • Lampen A., Christians U., Guengerich F. P., Watkins P. B., Kolars J. C., Bader A., Gonschior A.-K., Dralle H., Hackbarth I., Sewing K. F. Metabolism of the immunosuppressant tacrolimus in the small intestine: cytochrome P450, drug interactions, and interindividual variability. Drug Metab. Dispos. 1995; 23: 1315–1324
  • Watkins P. B. The barrier function of CYP3A4 and P-glycoprotein in the small bowel. Adv. Drug Deliv. Rev. 1997; 27: 161–170
  • Fitzsimmons M. E., Collins J. M. Selective biotransformation of the human immunodeficiency virus protease inhibitor saquinavir by human small intestinal cytochrome P4503A4. Drug Metab. Dispos. 1997; 25: 256–266
  • Koudriakova T., Iatsimirskaia E., Tulebaev S., Spetie D., Utkin I., Mullet D., Thompson T., Vouros P., Gerber N. In vivo disposition and metabolism by liver and enterocyte microsomes of the antitumour drug rifabutin in rats. J. Pharmacol. Exp. Therap. 1996; 279: 1300–1309
  • Lown K. S., Mayo R., Blake D. S., Benet L. Z., Watkins P. B. Interpatient variation in intestinal Pgp expression contributes to variable oral kinetics of cyclosporin A. Clin. Pharmacol. Ther. 1997; 62: 1–13
  • Hunter J., Jepson M. A., Tsuruo T., Simmons N. L., Hirst B. H. Functional expression of p-glycoprotein in apical membranes of human intestinal Caco-2 cell layers: kinetics of vinblastine secretion and interaction with modulators. J. Biol. Chem. 1993; 268: 14991–14997
  • Saitoh H., Aungst B. J. Possible involvement of multiple P-glycoprotein-mediated efflux systems in the transport of verapamil and other organic cations across the rat intestine. Pharm. Res. 1995; 12: 1304–1310
  • Karlsson J., Kuo S. M., Ziemniak J., Artusson P. Transport of celiprolol across human intestinal epithelial (Caco-2) cells: mediation of secretion by multiple transporters including p-glycoprotein. Br. J. Pharm. 1993; 110: 1009–1016
  • Leu B. L., Huang J. Inhibition of intestinal P-glycoprotein and effects on etoposide absorption. Cancer Chemother. Pharmacol. 1995; 35: 432–436
  • Wacher V. J., Wu C.-Y., Benet L. Z. Overlapping substrate specificities and tissue distribution of Cytochrome P450 3A and P-glycoprotein: implications for drug delivery and activity in cancer chemotherapy. Mol. Carcinog 1995; 13: 129–134
  • Benet L. Z., Wacher V. J., Bener R. M. Use of essential oils to increase bioavailability of oral pharmaceutical compounds. United States Patent No 5,665,386, Sep 9, 1997
  • Nerurkar M. M., Burton P. S., Borchardt R. T. The use of surfactant to enhance the permeability of peptides through Caco-2 cells by inhibition of an apically polarised efflux system. Pharm. Res. 1996; 13: 528–534
  • Choc M. G., Robinson W. T. Gastrointestinal variables and water insoluble compounds in normal and disease states. Presentation to the AAPS/CRS/FDA workshop on scientific foundation and applications for the biopharmaceutics classification and in vitro–in vivo correlations, Arlington, VA, April, 14–161997
  • Porter C. J.H., Charman S. A., Charman W. N. Lymphatic transport of halofantrine in the triple-cannulated anaesthetized rat model: effect of lipid vehicle dispersion. J.Pharm. Sci. 1996; 85: 351–356
  • Porter C. J.H., Charman S. A., Charman W. N. Lymphatic transport of halofantrine in the conscious rat when administered as either the free base or the hydrochloride salt: effect of lipid class and lipid vehicle dispersion. J. Pharm. Sci. 1996; 85: 357–361
  • Pantaleo G., Graziosi C., Butini L., Pizzo P. A., Schnittman S. M., Kotler D. P., Fauci A. S. Lymphoid organs as major reservoirs for human immunodeficiency virus. Proc. Natl. Acad. Sci. USA 1991; 88: 9838–9842
  • Pantaleo G., Graziosi C., Demarest J. F., Butini L., Montroni M., Fox C. H., Orenstein J. M., Kotler D. P., Fauci A. S. HIV infection is active and progressive in lymphoid tissue during the clinically latent stage of disease. Nature 1993; 362: 355–358
  • Casley-Smith J. R. The fine structure and functioning of tissue channels and lymphatics. Lymphology 1980; 12: 177–183
  • Casley-Smith J. R. Are the initial lymphatics normally pulled open by the anchoring filaments?. Lymphology 1980; 13: 120–129
  • Yang V. V., O'Morchoe P. J., O'Morchoe C. C. Transport of protein across lymphatic endothelium in the rat kidney. Microvasc. Res. 1981; 21: 75–91
  • O'Morchoe P. J., Yang V. V., O'Morchoe C. C. Lymphatic transport during volume expansion. Microvasc. Res. 1980; 20: 275–294
  • O'Morchoe C. C., Albertine K. H., O'Morchoe P. J. The rate of translymphatic endothelial fluid movement in the canine kidney. Microvasc. Res. 1982; 23: 180–187
  • Porter C. J.H. Drug delivery to the lymphatic system. Crit. Rev. Drug Carrier Syst. 1997; 14: 333–393
  • Charman W. N., Stella V. J. Estimating the maximal potential for intestinal lymphatic transport of lipophilic drug molecules. Int. J. Pharmaceut 1986; 34: 174–178
  • Kuksis A. Absorption of fat soluble vitamins. Fat Absorption, A. Kuksis. CRC Press, Boca Raton 1987; 2: 65–86
  • Palin K. J., Wilson C. J. The effect of different oils on the absorption of probucol in the rat. J. Pharm. Pharmacol. 1984; 36: 641–643
  • Grimus R. C., Schuster I. The role of the lymphatic transport in the enteral absorption of naftifine by the rat. Xenobiotica 1984; 14: 287–294
  • Katayama K., Fujita T. Studies on lymphatic absorption of 1′, 2′-(3H)-Coenzyme Q10 in rats. Chem. Pharm. Bull. 1972; 20: 2585–2592
  • Ueda C. T., Lemaire M., Gsell G., Nussbaumer K. Intestinal lymphatic absorption of cyclosporin A following oral administration in an olive oil solution to rats. Biopharm. Drug Dispos. 1983; 4: 113–124
  • Sieber S. M. The lymphatic absorption of p,p-DDT and some structurally-related compounds in the rat. Pharmacology 1976; 14: 443–454
  • Charman W. N., Noguchi T., Stella V. J. An experimental system designed to study the in situ intestinal lymphatic transport of drugs in anaesthetized rats. Int. J. Pharmaceut. 1986; 33: 155–164
  • Charman W. N., Stella V. J. Effect of lipid class and lipid vehicle volume on the intestinal lymphatic transport of DDT. Int. J. Pharmaceut. 1986; 33: 165–172
  • Sieber S. M., Cohn V. H., Wynn W. T. The entry of foreign compounds into the thoracic duct lymph of the rat. Xenobiotica 1974; 4: 265–284
  • Laher J. M., Rigler M. W., Vetter R. D., Barrowman J. A., Patton J. S. Similar bioavailability and lymphatic transport of benzo(a)pyrene when administered to rats in different amounts of dietary fat. J. Lipid. Res. 1984; 25: 1337–1342
  • Busbee D. L., Yoo J.-S. H., Norman J. O., Joe C. O. Polychlorinated biphenyl uptake and transport by lymph and plasma components. Proc. Soc. Exp. Biol. Med. 1985; 179: 116–122
  • Hauss D. J., Mehta S., Radebaugh G. W. Targeted lymphatic transport and modified systemic distribution of CI-976, a lipophilic lipid-regulator drug, via a formulation approach. Int. J. Pharmaceut. 1994; 108: 85–93
  • Nankervis R., Davis S. S., Day N. H., Shaw P. N. Intestinal lymphatic transport of three retinoids in the rat after oral administration: effect of lipophilicity and lipid vehicle. Int. J. Pharmaceut. 1996; 130: 57–64
  • Kwei G. Y., Novak L. B., Hettrick L. H., Reiss E. R., Fong E. K., Olah T. V., Loper A. E. Lymphatic uptake of MK-386, a sterol 5α-reductase inhibitor, from aqueous and lipid formulations. Int. J. Pharm. 1998; 164: 37–44
  • Takada K., Yoshimura H., Yoshikawa H., Muranishi S., Yasumura T., Oka S. Enhanced selective lymphatic delivery of cyclosporin A by solubilisers and intensified immunosuppressive activity against mice skin allograft. Pharm. Res. 1986; 3: 48–51
  • Myers R., Stella V. J. Factors affecting the lymphatic transport of penclomedine (NSC-338720), a lipophilic cytotoxic drug: comparison to DDT and hexachlorobenzene. Int. J. Pharm. 1992; 80: 51–62
  • Charman W. N., Porter C. J.H. Lipophilic prodrugs designed for intestinal lymphatic transport. Adv. Drug Deliv. Rev. 1996; 19: 149–169
  • Stella V. J., Pochopin N. L. Lipophilic prodrugs and the promotion of intestinal lymphatic drug transport. Lymphatic Transport of Drugs, W. N. Charman, V. J. Stella. CRC Press, Boca Raton 1992; 181–210
  • Nishigaki R., Awazu S., Hanano M., Fuwa T. The effect of dosage form on absorption of vitamin A into lymph. Chem. Pharm. Bull. 1976; 24: 3207–3211
  • Kuksis A. Effect of dietary fat on formation and secretion of chylomicrons and other lymph lipoproteins. Fat Absorption, A. Kuksis. Chap. 6, CRC Press, Boca Raton 1987; 2
  • Blomhoff R., Helgerud P., Dueland S., Berg T., Pederson J. I., Norum K. R., Drevon C. A. Lymphatic absorption and transport of retinol and vitamin D-3 from rat intestine—evidence for different pathways. Biochim. Biophys. Acta 1984; 772: 109–116
  • Vost A., Maclean A. Hydrocarbon transport in chylomicrons and high density lipoproteins in rat. Lipids 1984; 19: 423–435
  • Ichihashi T., Kinoshita H., Takagishi Y., Yamada H. Effect of oily vehicles on absorption of mepitiostane by the lymphatic system in rats. J. Pharm. Pharmacol. 1992; 44: 560–564
  • Geigy Scientific Tables. 8th Ed., Ciga-Geigy Ltd, BasleSwitzerland 1984
  • Naito H. K. Disorders of lipid metabolism. Clinical Chemistry Theory Analysis and Correlation, L. A. Kaplan, A. J. Pesce. Mosby, St. Louis, Missouri 1989; 454–483
  • Mayes P. A. Lipid transport and storage. Harper's Biochemistry, R. K. Murray, D. K. Granner, P. A. Mayes, V. W. Rodwell. Prentice Hall, New Jersey 1996; 254–269
  • Urien S. Interaction of drugs with human plasma lipoproteins. Proceedings of the Symposium on Protein Binding and Drug Transport, J. P. Tillement, E. Lindenlaub. F. K. Schattauer Verlag, Stuttgart-New York 1986; 63–75
  • Wasan K. W., Cassidy S. M. Role of plasma lipoprotiens in modifying the biological activity of hydrophobic drugs. J. Pharm. Sci. 1998; 87: 411–424
  • Shu H. P., Nichols A. V. Uptake of lipophilic carcinogens by plasma lipoproteins. Structure activity studies. Biochim. Biophys. Acta 1981; 665: 376–384
  • Urien S., Albengres E., Comte A., Kiechel J. R., Tillement J. P. Plasma protein binding and erythrocyte partitioning of nicardipine in vitro. J. Cardiovasc. Pharmacol. 1985; 7: 891–898
  • Glasson S., Zini R., D'Athis P., Tillement J. P., Boissier J. R. The distribution of bound propranolol between the different human serum proteins. Mol. Pharmacol. 1980; 17: 187–191
  • Chassany O., Urien S., Claudepierre P., Bastian G., Tillement J. P. Binding of anthracycline derivatives to human serum lipoproteins. Anticancer Res. 1994; 14: 2353–2355
  • Bard J. M., Urien S., Fruchart J.-C., Tillement J.-P. Location of probucol in lipoproteins inferred from compositional analysis of lipoprotein particles. An in-vitro study. J. Pharm. Pharmacol. 1994; 46: 797–800
  • Urien S., Albengres E., Comte A., Kiechel J., Tillement J. P. Plasma protein binding and erythrocyte partitioning of nicardipine in vitro. J. Cardio. Pharmacol. 1985; 7: 891–898
  • Urien S., Zini R., Lemaire M., Tillement J. P. Assessment of cyclosporine A interactions with human plasma lipoproteins in vitro and In vivo in the rat. J. Pharm. Exp. Ther. 1990; 253: 305–309
  • Wasan K. M., Pritchard P. H., Ramaswamy M., Wong W., Donnachie E. M., Brunner L. J. Differences in lipoprotein lipid concentration and composition modify the plasma distribution of cyclosporine. Pharm. Res. 1997; 4: 1613–l620
  • Urien S., Claudepierre P., Meyer J., Brandt R., Tillement J. P. Comparative binding of etretinate and acitretin to plasma proteins and erythrocytes. Biochem. Pharmacol. 1992; 44: 1891–1893
  • Simon N., Dailly E., Jolliet P., Tillement J.-P., Urien S. pH dependent binding of ligands to serum lipoproteins. Pharm. Res. 1997; 14: 527–532
  • Glasson S., Zini R., Tillement J.-P. Multiple human serum binding of two thienpyridinic derivatives, ticlopidine and PCR 2362, and their distribution between HSA, a-acid glycoprotein and lipoproteins. Biochem. Pharmacol. 1982; 31: 831–135
  • Sgoutas D., MacMahon W., Love A., Jerunika I. Interaction of cyclosporin A with human lipoproteins. J. Pharm. Pharmacol. 1986; 38: 583–588
  • Verrill H. L., Girgis R. E., Easterling R. E., Malhi B. S., Mueller W. F. Distribution of cyclosporine in blood of a renal transplant recipient with type V hyperlipoproteinemia. Clin. Chem. 1987; 33: 423–428
  • Danon A., Chen Z. Binding of imipramine to plasma proteins: effect of hyperlipoproteinemia. Clin. Pharmacol. Ther. 1979; 25: 316–321
  • Eder H. A. The effect of diet on the transport of probucol in monkeys. Artery 1982; 10: 105–107
  • Legg B., Gupta S. K., Rowland M. A model to account for the variation in cyclosporin binding to plasma lipids in transplant patients. Ther. Drug Monit. 1988; 10: 20–27
  • Humberstone A. J., Porter C. J.H., Edwards G. A., Charman W. N. Association of halofantrine with post-prandially derived plasma lipoproteins decreases its clearance relative to administration in the fasted state. J. Pharm. Sci. 1998; 87: 936–942
  • Gupta S. K., Benet L. Z. High fat meals increase the clearance of cyclosporin. Pharm. Res. 1990; 7: 46–48
  • Brajtberg J., Elberg S., Bolard J., Kobayashi G. S., Levy R. A., Ostlund R. E., Jr., Schlessinger D., Medoff G. Interaction of plasma proteins and lipoproteins with amphotericin B. J. Infect. Dis. 1984; 149: 986–997
  • Wasan K. M., Vadiei K., Lopez-Berenstein G., Luke D. R. Pharmacokinetics, tissue distribution and toxicity of free and liposomal amphotericin B in diabetic rats. J. Infect. Dis. 1990; 161: 562–566
  • Lopez-Berenstein G. Liposomes as carriers of antifungal drugs. Ann. N.Y. Acad. Sci. 1988; 544: 590–597
  • Pontani D. R., Sun D., Brown J. W., Shahied S. I., Plescia O. J., Schaffner C. P., Lopez-Berestein G., Sarin P. S. Inhibition of HIV replication by liposomal-encapsulated amphotercin B. Antiviral Res. 1989; 11: 119–125
  • Chabot G. G., Pazdur R., Valeriote F. A., Baker L. H. Pharmacokinetics and toxicity of a continuous infusion of amphotericin B in cancer patients. J. Pharm. Sci. 1989; 78: 307–310
  • Wasan K. M., Conklin J. S. Evaluation of renal toxicity and antifungal activity of free and liposomal amphotericin B following a single intravenous dose to diabetic rats with systemic candidiasis. Antimicrob. Agents Chemother. 1996; 40: 1806–1810
  • Koldin M. H., Kobayashi G. S., Brajtburg J., Medoff G. Effects of elevation of serum cholesterol and administration of amphotericin B complexed to lipoproteins on amphotericin B-induced toxicity to rabbits. Antimicrob. Agents Chemother. 1985; 28: 144–145
  • Chavanet P., Joly V., Rigaud D., Bolard J., Carbon C., Yeni P. Influence of diet on experimental toxicity of amphotericin B deoxycholate. Antimicrob. Agents Chemother. 1994; 38: 963–968
  • Souza L. C., Maranhao R. C., Schrier S., Campa A. in vitro and In vivo studies of the decrease of amphotericin B toxicity upon association with a triglyceride rich emulsion. J. Antimicrob. Agents 1993; 32: 123–132
  • Lemaire M., Tillement J.-P. Role of lipoproteins and erythrocytes in the in vitro binding and distribution of cyclosporin in the blood. J. Pharm. Pharmacol. 1982; 34: 715–718
  • Lithell H., Odlind B., Selinus I., Lindberg A., Lindstrom B., Frodin L. Is the plasma lipoprotein pattern of importance for treatment with cyclosporine? Transplant. Proc. 1986; 18: 50–51
  • De Kippel N., Sennesael J., Lamote J., Ebinger G., Keyser J. Cyclosporine leukoencephalopathy induced by intravenous lipid solution. Lancet 1992; 339: 1114–1115
  • Nemunaitis J., Deeg H. J., Yee G. C. High cyclosporin levels after bone marrow transplantation associated with hypertriglyceridemia. Lancet 1986; 2: 744–745
  • Amadottir M., Thysell H., Nilsson-Ehle P. Lipoprotein levels and post heparin lipase activities in kidney transplant recipients: ciclosporin-versus nonciclosporin-treated patients. Am. J. Kidney Dis. 1991; 17: 700–717
  • Gardier A. M., Mathe D., Guedeney X., Barre J., Benvenutti C., Navarro N., Vernillet J., Loisance D., Cachera J. P., Jacotot B., Tillement J.-P. Effects of plasma lipid-levels on blood distribution and pharmacokinetics of cyclosporin A. Ther. Drug Monit. 1993; 15: 274–280
  • Lemaire M., Partridge W. M., Chaudhuri G. Influences of blood components on the tissue uptake indices of cyclosporin in rats. J. Pharmacol. Exp. Ther. 1988; 244: 740–743
  • Partridge W. M. Carrier mediated transport of thyroid hormones through the rat blood brain barrier. Primary role of albumin bound hormone. J. Clin. Invest. 1979; 64: 145–154

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