BENEFITS OF LIPOSOMES

What science tells us

The advantages of liposome technology are being discovered by research teams all over the world. We present a broad selection of this research below. The numbers refer to the sources cited at the bottom of this page.

Biological availability

Research has shown that when an active substance is encapsulated in a liposome, it is protected from rapid breakdown in the body. The substance is therefore able to circulate inside the body for a longer period of time. Because its biological availability is greater, there is also an increasing likelihood that the active substance will enter the target cells. Research has also shown that more than one substance can be loaded into a liposome [1].

Administration

There are many different ways to administer an active substance liposomally, including directly into the bloodstream and by mouth. The latter is clearly easier than the former. While the administration of liposomal medicines into the bloodstream is the most effective, oral administration may be preferable in many situations as the less invasive option. The disadvantage of the oral route is that the liposomes have to pass through the stomach and intestine, and this can affect the stability of the liposomal product. A great deal of research has been done into ways of allowing liposomes to pass through the lining of the stomach and intestine, and this has shown that encapsulating the active substance in lipids increases the biological availability of orally administered active substances [1].

Greater impact

Liposomes are made entirely out of natural materials. They are non-toxic and biologically degradable. Research has shown that they have the unique ability to hold active substances – including medicines – in both an aqueous and a lipid phase. This makes liposomes an attractive drug delivery system. Research indicates that ongoing improvements to liposomal formulations are also benefiting targeted delivery, thereby improving the pharmaceutical effect of the drugs involved. It has also been demonstrated that the liposomal encapsulation of a drug reduces its potential toxicity, while its therapeutic efficacy is retained or even improved [2,3,4].

Protection

After extensive studies, other researchers have discovered that liposomes – as ultra-small vesicles for the transport of active substances such as medicines – ensure their higher biological availability of these substances in the body. This effect has been attributed to:

  • liposomal protection of the active substance as it passes through the stomach and intestine;
  • liposomes have increased cellular contact, increasing the likelihood that the active substance will enter the target cells;
  • the ‘residence time’ of a liposomally encapsulated active substance is greater. The residence time is the period of time that is needed for a substance to interact with its target;
  • liposomes protect the active substance from breaking down too rapidly. Many active substances that are administered in the traditional manner are simply lost because they are absorbed too quickly through the stomach or intestinal wall and pass into a bloodstream leading straight to the liver (the ‘hepatic portal system’). The liver breaks down the active substance before it has the chance to reach the target cells. Liposomal encapsulation prevents this loss [5,6].

Vitamin C

Another study has shown that the intravenous administration of liposomal vitamin C leads to the highest rise in vitamin C levels in the blood. The oral administration of liposomal vitamin C leads to slightly lower blood levels of vitamin C, but even these are still much higher than after the oral administration of non-liposomal vitamin C [7].

Improved uptake

Lipophilic active substances, including medicines, have poor solubility in water. Many new drugs are lipophilic, which reduces their biological availability and intestinal absorption. In order to be absorbed into the body through the intestine, medical drugs need to be highly soluble. Reduced uptake in the intestine can lead to a reduced therapeutic effect. It has been shown that lipid formulations can improve the uptake of active substances [8].

Sources

  • 1. Kraft, J.C., Freeling, J.P., Wang, Z., & Ho R.J.Y. (2014). Emerging research and clinical development trends of liposome and lipid nanoparticle drug delivery systems. Journal of Pharmaceutical Sciences, 103(1), 29–52.
  • 2. Kulkarni, P.R., Yadav, J.D., & Vaidya, K.A. (2011). Liposomes: a novel drug delivery system. International Journal of Current Pharmaceutical, 3(2), 10-18.
  • 3. Samad, A., Sultana, Y., & Aqil, M. (2007). Liposomal drug delivery systems: an update review. Current Drug Delivery, 4(4), 297-305.
  • 4. Allen, T.M., & Cullis, P.R. (2013). Liposomal drug delivery systems: from concept to clinical applications. Advanced Drug Delivery Reviews, 65, 36-48.
  • 5. Rogers, J.A., & Anderson K.E. (1998). The potential of liposomes in oral drug delivery. Critical Reviews in Therapeutic Drug Carrier Systems, 15(5), 421–480.
  • 6. Daeihamed, M., Dadashzadeh, S., Haeri, A., & Akhlaghi, F.M. (2017). Potential of liposomes for enhancement of oral drug absorption. Current Drug Delivery, 14(2), 289-303.
  • 7. Davis, J.L., Paris, H.L., Beals, J.W., Binns, S.E., Giordano, G.R., Scalzo, et al. (2016). Liposomal-encapsulated ascorbic acid: Influence on vitamin C bioavailability and capacity to protect against ischemia–reperfusion injury. Nutrition and Metabolic Insights, 9, 25-30.
  • 8. Fricker, G., Kromp, T., Wendel, A., Blume, A., Zirkel, J., Rebmann, H., et al. (2010). Phospholipids and lipid-based formulations in oral drug delivery. Pharmaceutical Research, 27(8), 1469-1486.

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