Biomed. Papers 145(2), 17-26 (2001) | DOI: 10.5507/bp.2001.008
LIPID-BASED VEHICLE FOR ORAL DRUG DELIVERY
- Research, Development and Clinical Department, IVAX-CR a.s., Ostravská 29, 747 70 Opava 9, Czech Republic,
With an increasing number of lipophilic drugs under development, homolipids and heterolipids have gainedrenewed interests as excipients for oral drug delivery systems. Oral administration has many advantages for chronicdrug therapy. It is relatively safe, convenient for the patient and allows self administration.This article is notintended to review the broad area of lipid-based vehicle for oral drug delivery comprehensively. The rationalebehind choosing lipids materials for pharmaceutical dosage forms and their applications is discussed. It alsocomments on the methods for monitoring the physicochemical properties of vehicles and formulations anddescribes a range of pharmacopoeial excipients suitable for these purposes. The excipients selected here arepharmacopoeial in European Pharmacopoeia 4th Ed.,United States Pharmacopoeia 24th Ed./National Formulary19th Ed. and Japanese Pharmacopoeia 13th Ed. or are drafted in Pharmaeuropa and Pharmacopoeial Forum.Widening availability of lipidic excipients with specific characteristics offer flexibility of application with respectto improving the bioavailability of poorly water-soluble drugs and manipulating release profiles.
Keywords: Lipids, Lipophilic drugs, Oral drug delivery systems
Received: October 18, 2001; Published: December 1, 2001 Show citation
References
- Charman, W. N., Porter, C. J. H., Mithani, S., Dressman, J. B. (1997) Physicochemical and physiological mechanisms for the effects food on drug absorption: The effect of lipids and pH. J. Pharm. Sci., 86, 269-282 .
Go to original source...
Go to PubMed...
- Fleischer, D., Li, C., Zhou, Y., Pao, L-H., Karim, A. (1999) Drug, meal and formulations influencing drug absorption after oral administration. Clin. Pharmacokinet., 36, 233-254.
Go to original source...
Go to PubMed...
- Constantinides, P. P. (1995) Lipid microemulsions for improving drug dissolution and oral absorption: Physical and biopharmaceutical aspects. Pharm. Res., 11, 1561-1572.
Go to original source...
Go to PubMed...
- Lawrence, M. J. (1996) Microemulsion as drug delivery vehicles. Curr. Opin. Colloid. Interface Sci., 1, 826-832.
Go to original source...
- Humberstone, A. J., Charman, W. N. (1997) Lipid-based vehicles for the oral delivery of poorly water-soluble drugs. Adv. Drud. Del. Rev., 25, 103-128.
Go to original source...
- Serajuddin, A. T. M. (1999) Solid dispersion of poorly watersoluble drugs: Early promises, subsequent problems and recent breakthroughs. J. Pharm. Sci., 88, 1058-1066.
Go to original source...
Go to PubMed...
- Amidon, G. L., Lennernas, H., Shah, V. P., Crison, J. R. (1995) A theoretical basis for a biopharmaceutical drug classification: The correlation of in-vitro drug product dissolution and in-vivo bioavailability. Pharm. Res., 12, 413-419.
Go to original source...
Go to PubMed...
- Brunner, L. J., Bai, S. (2000) Effect of dietary oil intake on hepatic cytochrome P 450 activity in the rat. J. Pharm. Sci., 89, 1022-1027.
Go to original source...
Go to PubMed...
- Tsevegsuren, N., Aitzetmuller, K., Bruhl, L., Werner, G. (2000) Seed oil fatty acids of mongolian Compositae: The trans- fatty acids of Heteropappus hispidus, Asterothamnus centrali-asiaticus and Artemisia palustris. J. High Resol. Chromatogr., 23, 360-366.
Go to original source...
- Bell, S. J., Bradley, D., Forse, R. A., Bistrian, B. R. (1997) The new dietary fats in health and disease. J. Am. Diet. Assoc. 97, 280-286.
Go to original source...
Go to PubMed...
- Lee, K. T., Akoh, C. C. (1996) Immobilized lipase-catalyzed production of structured Lipids with eicosapentaenoic acid at specific positions. J. Am. Oil Chem. Soc., 73, 611-615.
Go to original source...
- Huang, K. S., Akoh, C. C. (1996) Enzymatic synthesis of structured lipids - Transesterification of of triolein and capryliuc acidethylester. J. Am. Oil Chem. Soc., 73,245-250 .
Go to original source...
- Másson, M., Loftsson, T., Haraldsson, G. G. (2000) Marine lipids for prodrugs, soft compounds and other pharmaceutical applications. Pharmazie, 55, 172-177.
Go to PubMed...
- Hallgren, B. (1983) in: Ether Lipids. Biochemical and biomedical aspects, (Mangold H. K.,Paltauf F., eds.), Academic Press, New York, pp. 261-275.
Go to original source...
- Pérez-Camino, M. C., Moreda, W., Cert, A. (1996) Determination of diacylglycerol isomers in vegetable oils by solid-phase extraction followed by gas chromatography on a polar phase. J. Chromatogr., A721, 305-314.
Go to original source...
- Schneider, M. (1997) Industrial production of phospholipids - lecithin processing. Lipid Technology, September 109-116.Technology, September 109-116.
- Anonym (1994) Sojae Lecithinum. Pharmaeuropa, 6, 279.
- Verleysen, K., Sandra, P. (1997) Analysis of phospholipids in lecithins. Separation According to hydrophobicity by lowering the temperature. J. High Resol. Chromatogr. 20, 337-339.
Go to original source...
- Bijsterbosch, M. K., Van Berkel, T. J. C. (1990) Uptake of lactosylated low-density lipoprotein by galactose-specific receptors in rat liver. Biochemical Journal (London), 270, 233-239.
Go to original source...
Go to PubMed...
- Pitas, R. E., Boyles, J., Mahley, R.V., Bissel, D. M. (1985) Uptake of chemically modified low density lipoproteins in vivo is mediated by specific endothelial cells. J. Cell Biol., 100, 103-117.
Go to original source...
Go to PubMed...
- Ashwell, G., Morell, A. G. (1974) The role of surface carbohydrates in the hepatic recognition and transport of circulating glycoproteins. Adv. Enzymol., 41, 99-128.
Go to original source...
- Peyrot, M., Sautereau, A. M., Rabanel, T. M., Nguyen, F., Tocanne, J. F., Samain, D. (1994) Int. J. Pharm., 102, 25.
Go to original source...
- Bach, A. C., Babayan, V. K. (1982) Medium chain triglycerides. Amer. J. Clin. Nutrit., 36, 950-962 .
Go to original source...
- Borgström, B. (1988) in: Boekus Gastroenterology, 4th ed. (Berk J. E., Saunders W. B., eds.), Saunders W. B., Philadelphia, pp. 1510-1519.
- Yhi-Fu, S. (1987) in: Physiology of the Gastrointestinal Tract, 2 nd ed. (Johnson L. R., ed.), Raven Press, New York, pp. 1527-1556.
- Behrens, D., Fricker, R., Bodoky, A., Drewe, J., Harder, F., Heberer, M. (1996) Comparison of cyclosporin A absorption from LCT and MCT solutions following intrajejunal administration in conscious dogs. J. Pharm. Sci., 85, 666-668.
Go to original source...
Go to PubMed...
- Larsson, K. (1994) Lipids - Molecular organisation, Physical functions and Technical applications. The Oily Press Ltd., Dundee, p. 2.
- Vyas, S. P., Jaitely, V., Kanaujia, P. (1997) Self-assembling supramolecular biovectors: a new dimension in novel drug delivery systems. Pharmazie, 52, 259-267.
Go to PubMed...
- Velíšek, J. (1999) Fats and other lipids in Chemie potravin 1, Ossis, Tábor, p. 91.
- Charman, W. N. (2000) Lipids, lipophilic drugs and oral delivery - Some emerging Concepts. J. Pharm. Sci., 89, 967-978.
Go to original source...
Go to PubMed...
- Bowtle, W. (2000) Lipid formulations for oral drug delivery. Pharmaceutical Technology Europe, 12 (9), 20-30.