Skip to main content
Log in

Modification of Intestinal Absorption of Drugs by Lipoidal Adjuvants

  • Published:
Pharmaceutical Research Aims and scope Submit manuscript

Abstract

The use of various lipids for the modification of intestinal absorption of lipophilic, hydrophilic, or macromolecular drugs is reviewed. The influence of lipids on drug absorption varies with the structure and physical state of incorporated lipids. The mechanisms of drug absorption across the intestine, that involve lipids in the state of emulsions, liposomes, and micelles, are discussed. The use of fusogenic lipids in the micellar state can be most effective in enabling the absorption of poorly absorbed drugs, such as antibiotics and macromolecules. Moreover, within the gastrointestinal tract their promoting ability is greatest in the colorectal region. Fusogenic lipids are also useful for selective lymphatic delivery of drugs with a macromolecular carrier.

This is a preview of subscription content, log in via an institution to check access.

Access this article

Price excludes VAT (USA)
Tax calculation will be finalised during checkout.

Instant access to the full article PDF.

Similar content being viewed by others

References

  1. Schanker, L. S. (1959) J. Pharmacol. Exp. Ther. 126, 283–290.

    Google Scholar 

  2. Kakemi, K., Arita, T., Muranishi, S. (1965) Chem. Pharm. Bull. 13, 861–869.

    Google Scholar 

  3. Wagner, J. G., Leslie, L. G., Grove, R. S. (1969) Int. J. clin. Pharmacol. 2, 44–51.

    Google Scholar 

  4. Sjövall, J., Westerlund, D., Alván, G., Magni, L., Nord, C. E., Sörstad, J. (1984) Chemotherapy 30, 137–147.

    Google Scholar 

  5. Schanker, L. S., Tocco, D. J. (1960) J. Pharmacol. Exp. Ther. 128, 115–121.

    Google Scholar 

  6. Muranishi, S., Yoshikawa, H., Sezaki, H. (1979) J. Pharm. Dyn. 2, 286–294.

    Google Scholar 

  7. Carrigan, P. J., Bates, T. R. (1973) J. Pharm. Sci. 62, 1476–1479.

    Google Scholar 

  8. Kakemi, K., Sezaki, H., Muranishi, S., Ogata, H., Isemura, S. (1972) Chem. Pharm. Bull. 20, 708–714.

    Google Scholar 

  9. Kakemi, K., Sezaki, H., Muranishi, S., Ogata, H. (1972) Chem. Pharm. Bull. 20, 715–720.

    Google Scholar 

  10. Ogata, H., Kakemi, K., Muranishi, S., Sezaki, H. (1975) Chem. Pharm. Bull. 23, 707–715.

    Google Scholar 

  11. Ogata, H., Kakemi, K., Furuya, A., Fujii, M., Muranishi, S., Sezaki, H. (1975) Chem. Pharm. Bull. 23, 716–724.

    Google Scholar 

  12. Noguchi, T., Takahashi, C., Kimura, T., Muranishi, S., Sezaki, H. (1975) Chem. Pharm. Bull. 23, 775–781.

    Google Scholar 

  13. Noguchi, T., Jinguji, Y., Kimura, T., Muranishi, S., Sezaki, H. (1975) Chem. Pharm. Bull., 23, 782–786.

    Google Scholar 

  14. Noguchi, T., Tokunaga, Y., Ichikawa, H., Muranishi, S., Sezaki, H. (1977) Chem. Pharm. Bull. 25, 413–419.

    Google Scholar 

  15. Noguchi, T., Taniguchi, K., Muranishi, S., Sezaki, H. (1977) Chem. Pharm. Bull. 25, 434–440.

    Google Scholar 

  16. Noguchi, T., Taniguchi, K., Yoshifuji, T., Muranishi, S., Sezaki, H. (1977) Chem. Pharm. Bull. 25, 2231–2238.

    Google Scholar 

  17. Yamahira, Y., Noguchi, T., Noguchi, T., Takenaka, H., Maeda, T. (1979) Chem. Pharm. Bull. 27, 1190–1198.

    Google Scholar 

  18. Yamahira, Y., Noguchi, T., Noguchi, T., Takenaka, H., Maeda, T. (1980) Chem. Pharm. Bull. 28, 169–176.

    Google Scholar 

  19. Nakamoto, Y., Fujiwara, M., Noguchi, T., Kimura, T., Muranishi, S., Sezaki, H. (1975) Chem. Pharm. Bull. 23, 2232–2238.

    Google Scholar 

  20. Davis, S. S. (1976) J. Clin. Pharm. 1, 11–27.

    Google Scholar 

  21. Patel, H. M. (1976) FEBS Lett. 62, 60–63.

    Google Scholar 

  22. Dapergolas, G., Gregoriadis, G. (1976) Lancet 2, 824–827.

    Google Scholar 

  23. Wagner, J. G., Gerrard, E. S., Kaiser, D. G. (1966) Clin. Pharmacol. Ther. 7, 610–619.

    Google Scholar 

  24. Engel, R. H., Fahrenbach, S. J. (1978) Proc. Soc. Exp. Biol. Med. 129, 772–777.

    Google Scholar 

  25. Engel, R. H., Riggi, S. J., Fahrenbach, M. J. (1968) Nature 219, 856–857.

    Google Scholar 

  26. Engel, R. H., Riggi, S. J. (1969) J. Pharm. Sci. 58, 1372–1375.

    Google Scholar 

  27. Bean, H. S., Heman-Ackah, S. M. (1964) J. Pharm. Pharmacol. 16, Suppl. 58T–61T.

    Google Scholar 

  28. Palin, K., Davis, S. S., Phillips, A. J., Whatelay, C. G., Wilson, C. G. (1980) J. Pharm. Pharmacol. 32, 62P.

    Google Scholar 

  29. Hamilton, J. D. (1971) Biochim. Biophys. Acta 239, 1–8.

    Google Scholar 

  30. Patel, H. M., Ryman, B. E. (1977) Biochem. Soc. Trans. 5, 1739–1741.

    Google Scholar 

  31. Bridges, J. F., Millard, P. C., Woodley, J. F. (1978) Biochim. Biophy. Acta 544, 448–451.

    Google Scholar 

  32. Hemker, H. C., Muller, A. D., Hermens, W. Th., Zwaal, F. A. (1980) Lancet i, 70–71.

    Google Scholar 

  33. Anderson, P., Vilcek, J., Weissmann (1981) Infect. Immun. 31, 1099–1103.

    Google Scholar 

  34. Richard, M. H., Gardner, C. R. (1978) Biochim. Biophy. Acta 543, 508–522.

    Google Scholar 

  35. Hashida, N., Murakami, M., Yoshikawa, H., Takada, K., Muranishi, S. (1984) J. Pharm. Dyn. 7, 195–203.

    Google Scholar 

  36. Murakami, M., Masuda, Y., Fukui, H., Yoshikawa, H., Takada, K., Muranishi, S. (1984) 16th Symposium on Drug Metabolism and Action (Pharm. Soc. Japan), Gifu.

  37. Kakemi, K., Arita, T., Muranishi, S. (1965) Chem. Pharm. Bull. 13, 976–985.

    Google Scholar 

  38. Kakemi, K., Sezaki, H., Muranishi, S., Yano, A. (1970) Chem. Pharm. Bull. 18, 1563–1568.

    Google Scholar 

  39. Kaneda, A. Nishimura, K., Muranishi, S., Sezaki, H. (1974) Chem. Pharm. Bull. 22, 523–528.

    Google Scholar 

  40. Engel, R. H., Riggi, S. J. (1969) Proc. Soc. Exp. Biol. Med. 130, 879–884.

    Google Scholar 

  41. Windsor, E., Gronheim, G. E. (1961) Nature 190, 263–264.

    Google Scholar 

  42. Tidball, C. S., Lipman, R. I. (1962) Proc. Soc. Exp. Biol., Med., 111, 713–715.

    Google Scholar 

  43. Muranishi, S., Tokunaga, Y., Taniguchi, K., Sezaki, H. (1977) Chem. Pharm. Bull. 25, 1159–1161.

    Google Scholar 

  44. Tokunaga, Y., Muranishi, S., Sezaki, H. (1978) J. Pharm. Dyn. 1, 28–38.

    Google Scholar 

  45. Taniguchi, K., Muranishi, S., Sezaki, H. (1980) Int. J. Pharm. 4, 219–228.

    Google Scholar 

  46. Taniguchi, K., Miyamori, T., Muranishi, S., Sezaki, H. (1978) 98th Anu. Meet. Pharm. Soc. Jap. p. 151.

  47. Yoshikawa, H., Takada, K., Muranishi, S., Satoh, Y. (1984) J. Pharm. Dyn. 7, 56–62.

    Google Scholar 

  48. Yoshikawa, H., Takada, K., Muranishi, S. (1984) J. Pharm. Dyn. 7, 1–6.

    Google Scholar 

  49. Yoshikawa, H., Sezaki, H., Muranishi, S. (1983) Int. J. Pharm. 13, 321–332.

    Google Scholar 

  50. Muranishi, S., Muranushi, N., Sezaki, H. (1979) Int. J. Pharm. 2, 101–111.

    Google Scholar 

  51. Gibaldi, M. (1970) Fed. Proc. 29, 1343–1349.

    Google Scholar 

  52. Kimura, T., Sezaki, H., Kakemi, K. (1972) Chem. Pharm. Bull. 20, 1656–1662.

    Google Scholar 

  53. Kakemi, K., Sezaki, H., Konishi, R., Kimura, T., Ohkita, A. (1970) Chem. Pharm. Bull. 18, 1034–1039.

    Google Scholar 

  54. Muranushi, N., Kinugawa, M., Nakajima, Y., Muranishi, S., Sezaki, H. (1980) Int. J. Pharm. 4, 271–279.

    Google Scholar 

  55. Saunders, D. R., Sillery, J., McDornald, G. B. (1975) Gut 16, 543–548.

    Google Scholar 

  56. Dobbins, J. W., Binder, H. J. (1976) Gastroenterology 70, 1096–1100.

    Google Scholar 

  57. Ahkong, Q. F., Fisher, D., Tampion, W., Lucy, J. A. (1973) Biochem. J. 136, 147–155.

    Google Scholar 

  58. Maggio, B., Lucy, J. A. (1976) Biochem. J. 155, 353–364.

    Google Scholar 

  59. Kessler, M., Acuto, O., Storelli, C., Murer, H., Müller, M., Semenza, G. (1978) Biochim. Biophys. Acta 506, 136–154.

    Google Scholar 

  60. Muranushi, N., Sezaki, H., Muranishi, S. (1980) 3rd Symposium on Drug Interaction with Biomembrane (Pharm. Soc. Japan), Tokyo.

  61. Blok, M. C., van Deenen, L. L. M., de Gier, J. (1977) Biochim. Biophy. Acta 464, 509–518.

    Google Scholar 

  62. Inoue, K., Kitagawa, T. (1976) Biochim. Biophy. Acta 426, 1–16.

    Google Scholar 

  63. Muranushi, N., Nakajima, Y., Kinugawa, M., Muranishi, S., Sezaki, H. (1980) Int. J. Pharm. 4, 281–290.

    Google Scholar 

  64. Maggio, B., Lucy, J. A. (1975) Biochem. J. 149, 597–608.

    Google Scholar 

  65. Muranushi, N., Takagi, N., Muranshi, S., Sezaki, H. (1981) Chem. Phys. Lipids 28, 269–279.

    Google Scholar 

  66. Karnovsky, M. J. (1979) Am. J. Pathol. 97, 211–222.

    Google Scholar 

  67. Levine, Y. K., Birdsall, A. G., Lee, A. G., Metcalfe, J. C. (1972) Biochemistry 11, 1416–1421.

    Google Scholar 

  68. Yeagle, P. L., Martin, R. B. (1978) Membrane Transport Processes, Vol. 2, Raven Press, New York, p. 13.

    Google Scholar 

  69. Cullis, P. R., Hope, M. J. (1975) Nature 271, 672–674.

    Google Scholar 

  70. Levine, R. R., de Marco, T. J., Dizon, C. M. (1969) 4th International Congress on Pharmacology Vol. II pp. 79–107.

    Google Scholar 

  71. Helman, L., Frazell, E. L., Rosenfeld, R. S. (1960) J. Clin. Invest. 39, 1288–1294.

    Google Scholar 

  72. Fraser, R., Cliff, W. J., Courtice, F. C. (1968) Quart. J. Exper. Physiol. 53, 390–398.

    Google Scholar 

  73. Cornwell, D. G., Kruger, F. A., Robinson, H. B. (1962) J. Lipid Res. 3, 65–70.

    Google Scholar 

  74. Sieber, S. M., Cohn, V. H., Wynn, W. T. (1974) Xenobiotica 4, 265–284.

    Google Scholar 

  75. Grimus, R. C., Schuster, I. (1984) Xenobiotica, 14, 287–294.

    CAS  PubMed  Google Scholar 

  76. Kumar, R., Billimoria, J. D. (1978) J. Pharm. Pharmacol. 30, 754–758.

    Google Scholar 

  77. Takada, K., Yoshikawa, H., Muranishi, S. (1983) Res. Commun. Chem. Path. Pharmacol. 40, 99–108.

    Google Scholar 

  78. Alexander, H. L., Shirley, K., Allen, D. (1936) J. Clin. Invest. 15, 163–169.

    Google Scholar 

  79. Comline, R. S., Roberts, H. E., Titchen, D. A. (1951) Nature 167, 561–563.

    Google Scholar 

  80. Yoshikawa, H., Muranishi, S., Sugihara, N., Sezaki, H. (1983) Chem. Pharm. Bull. 31, 1726–1732.

    Google Scholar 

  81. Yoshikawa, H., Takada, K., Muranishi, S. (1983) Chem. Pharm. Bull. 31, 4070–4076.

    Google Scholar 

  82. Papp, M., Fehér, S., Folly, G., Horváth, E. J. (1977) Experientia, 33, 1191–1192.

    Google Scholar 

  83. Yoshikawa, H., Muranishi, S., Kato, C., Sezaki, H. (1981) Int. J. Pharm. 8, 291–302.

    Google Scholar 

  84. Kaji, Y., Uekama, K., Yoshikawa, H., Takada, K., Muranishi, S. (1985) Int. J. Pharm. in press.

Download references

Author information

Authors and Affiliations

Authors

Rights and permissions

Reprints and permissions

About this article

Cite this article

Muranishi, S. Modification of Intestinal Absorption of Drugs by Lipoidal Adjuvants. Pharm Res 2, 108–118 (1985). https://doi.org/10.1023/A:1016307231798

Download citation

  • Issue Date:

  • DOI: https://doi.org/10.1023/A:1016307231798

Keywords

Navigation