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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

When an active substance is encapsulated in a liposome, it can be protected from rapid degradation and elimination in the body. The substance is therefore able to circulate inside the body for a longer period of time. This will increase the likelihood that the active substance will enter the target tissues and cells. Research has also shown that more than one substance can be loaded into a liposome to make them work synergistically [1].

Enhanced delivery

There are many different ways to administer a liposomal form of an active substance, for instance by intravenous infusion, local injection, inhalation but also by simple oral intake. While the administration of liposomal medicines into the bloodstream can be a very clear and direct way to target diseased sites in the body, oral administration is often preferable as a less invasive administration route. The disadvantage of the oral route is that the liposomes have to pass through the stomach and intestine, which form a relatively hostile environment affecting the stability of liposomal products. A great deal of research effort has been undertaken to engineer liposomes that pass through the stomach and intestine in an intact form, showing that in some cases the biological availability of orally administered active substances can indeed be enhanced [1].

Better efficacy – less toxicity

Liposomes are usually made of naturally-derived starting materials. They are essentially non-toxic and biologically degradable. They have the unique ability to hold active substances – including medicines and supplements – both in their aqueous interior as well as their lipid bilayer. This makes liposomes attractive as drug delivery systems. Drug delivery selectively at diseased sites in the body increases the local concentration of the drug improving its pharmacologic effect. It has also been demonstrated that the liposomal encapsulation of a drug can significantly reduce its toxicity by the tendency of liposomes to avoid healthy organs and protect these from exposure to the encapsulated drug [2,3,4].

Protection

Studies reveal that liposomes – harnessing their ability to encapsulate and transport active ingredients – can increase the bioavailability and target delivery of these ingredients in the body. This effect has been attributed to:

liposomal protection of the active substance against enzymatic or hydrolytic degradation as it passes through the stomach and intestine;
enhanced enterocyte interaction in the intestine, increasing the concentration of the active substance at the site where it has to be taken up;
prolongation of the ‘residence time’ of a liposomal encapsulated active substance in the body and at the target site;
liposomal redirection of the actives after uptake, protecting the active substance from rapid clearance. Many active substances that are administered in the traditional manner are simply lost because after absorption they are led 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 can help prevent 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

However, even if intact passage through the stomach and intestine is not achieved, liposome products such as liposome vitamin supplements can be of great benefit. Especially lipophilic active substances that have low solubility in water, show poor absorption and thus inferior efficacy. It has been shown that lipid formulations can significantly improve the intestinal uptake of such difficult-to-formulate lipophilic actives [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.
[9] Carlson, R. P., Hartman, D. A., Ochalski, S. J., Zimmerman, J. L., & Glaser, K. B. (1998). Sirolimus (rapamycin, Rapamune ® ) and combination therapy with cyclosporin A in the rat developing adjuvant arthritis model: Correlation with blood levels and the effects of different oral formulations. Inflammation Research, 47(8), 339–344.
[10] Chen, Y., Lu, Y., Chen, J., Lai, J., Sun,. et al. (2009). Enhanced bioavailability of the poorly water-soluble drug fenofibrate by using liposomes containing a bile salt. International Journal of Pharmaceutics, 376(1–2), 153–160.
[11] Değim, I. T., Gümüşel, B., Değim, Z., Özçelikay, T., Tay, A., et al. (2006). Oral Administration of Liposomal Insulin. Journal of Nanoscience and Nanotechnology, 6(9), 2945–2949.
[12] Fahr, A., Hoogevest, P. van, May, S., Bergstrand, N., & S. Leigh, M. L. (2005). Transfer of lipophilic drugs between liposomal membranes and biological interfaces: Consequences for drug delivery. European Journal of Pharmaceutical Sciences, 26(3–4), 251–265.
[13] Guo, J., Ping, Q., & Chen, Y. (2001). Pharmacokinetic behavior of cyclosporin A in rabbits by oral administration of lecithin vesicle and sandimmun neoral. International Journal of Pharmaceutics, 216(1–2), 17–21. https://doi.org/10.1016/s0378-5173(00)00680-3
[14] Juenemann, D., Jantratid, E., Wagner, C., Reppas, C., Vertzoni, M., et al. (2011). Biorelevant in vitro dissolution testing of products containing micronized or nanosized fenofibrate with a view to predicting plasma profiles. European Journal of Pharmaceutics and Biopharmaceutics, 77(2), 257–264.
[15] Ling, S. S. N., Yuen, K. H., Magosso, E., & Barker, S. A. (2009). Oral bioavailability enhancement of a hydrophilic drug delivered via folic acid-coupled liposomes in rats. Journal of Pharmacy and Pharmacology, 61(4), 445–449.
[16] Masuda, K., Horie, K., Suzuki, R., Yoshikawa, T., & Hirano, K. (2002). Oral Delivery of Antigens in Liposomes with Some Lipid Compositions Modulates Oral Tolerance to the Antigens. Microbiology and Immunology, 46(1), 55–58.
[17] Sun, M., Gao, Y., Pei, Y., Guo, C., Li, H., et al.(2010). Development of Nanosuspension Formulation for Oral Delivery of Quercetin. Journal of Biomedical Nanotechnology, 6(4), 325–332.
[18] Takahashi, M., Uechi, S., Takara, K., Asikin, Y., & Wada, K. (2009). Evaluation of an Oral Carrier System in Rats: Bioavailability and Antioxidant Properties of Liposome-Encapsulated Curcumin. Journal of Agricultural and Food Chemistry, 57(19), 9141–9146.
[19] Thirawong, N., Thongborisute, J., Takeuchi, H., & Sriamornsak, P. (2008). Improved intestinal absorption of calcitonin by mucoadhesive delivery of novel pectin–liposome nanocomplexes. Journal of Controlled Release, 125(3), 236–245.
[20] Werle, M., & Takeuchi, H. (2009). Chitosan–aprotinin coated liposomes for oral peptide delivery: Development, characterisation and in vivo evaluation. International Journal of Pharmaceutics, 370(1–2), 26–32.
[21] Xu, H., He, L., Nie, S., Guan, J., Zhang, et al. (2009). Optimized preparation of vinpocetine proliposomes by a novel method and in vivo evaluation of its pharmacokinetics in New Zealand rabbits. Journal of Controlled Release, 140(1), 61–68.

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