Supercharged: Liposomal D3 and K3

Vitamin D3, often referred to as the ‘sunshine vitamin’, plays a crucial role in various physiological processes that can impact longevity and healthspan—the period of life spent in good health, free from significant chronic diseases or disabilities. Some of the most noted benefits include bone health, cardiovascular wellbeing, and healthy immune function. 

However, in recent years, we have learnt that to get the full benefits of vitamin D3 you need adequate amounts of vitamin K2. These two fat-soluble vitamins work in tandem to regulate calcium metabolism, ensuring it is efficiently utilised in the body while preventing its deposition in undesirable locations.

However, there are some significant challenges when it comes to the absorption and utilisation of vitamin D3 and K2. Both D3 and K2 require dietary fat for absorption, and deficiencies in fat absorption or issues like malabsorption disorders can hinder their effectiveness. Additionally, obesity, gastrointestinal issues, genetic factors, and age can all play a role in influencing the efficiency of absorption.

Recent advances in a technology called liposomal encapsulation have now overcome these absorption challenges.

What are liposomes?

Liposomes are composed of a double layer of phospholipids, which are the same material that makes up our cells. And, just like our cells, they can self-organise into microscopic spheres. 

These phospholipids have a water-loving head and a water-repellent tail, which allow them to safely transport both fat-soluble and water-soluble nutrients through the gut wall, into the bloodstream and then release them directly into cells where they are needed. 1

This form of encapsulation ensures that nutrients are protected from degradation and destruction in the harsh environment of the gastrointestinal tract and creates a stable delivery system with enhanced absorption and improved bioavailability.2

Because they are made up of the same components as our cells, once a liposome has been passively absorbed into the bloodstream, it can then fuse with the cell membrane and deliver its contents directly into the cell.3

Vitamin D

When vitamin D was first discovered, it was primarily understood to be responsible for the absorption and mobilisation of calcium and phosphorus and its contribution to bone health.

However, over the last several decades, vitamin D3 has been recognised as an essential nutrient required for a range of critical biological functions including normal immune function, regulating mood and nervous system function as well as gut health.

As a result, deficiency is associated with a range of disease states including autoimmune diseases, allergies, osteoporosis, rickets, various cancers, infections, schizophrenia and depression. 4

To ensure adequate levels of vitamin D3 are achieved for these broad functions, the Australian government recommends between 200iu and 600iu of vitamin D3 per day. However, there is growing evidence that this dose may be too low and that doses above 1,000 iu per day should be considered for maintenance and up to 6,000 iu per day as therapy. 5

The most natural way to get vitamin D3 is through sun exposure, but the risks and practicalities associated with regular, full-body exposure can make this difficult and problematic.

Supplementation is the next best option, but absorption challenges often result in an inability to improve deficiency states. 6

Nevertheless, recent research has shown that liposomal vitamin D3 causes a rapid increase in the blood concentration of vitamin D3 compared to standard forms. This effect was especially pronounced for people with severe vitamin D3 deficiency.7

Vitamin K2

Vitamin K2, also known as menaquinone, is an important fat-soluble vitamin that has only recently begun to gain the recognition it deserves. 

Unlike vitamin K1, which is found in plants and plays a role in blood coagulation, vitamin K2 is a product of bacterial fermentation and is required for the healthy function of calcium in the body. 8

Vitamin K2 activates proteins that help regulate calcium distribution, directing it towards the bones and teeth where it is needed and away from arteries and other tissues. Specifically, vitamin K2 activates osteocalcin, a protein responsible for binding calcium to the bone matrix, and matrix Gla-protein, which helps prevent arterial calcification.

Availability of vitamin K2 from dietary sources is low globally except in a few geographic regions such as Japan due to the consumption of natto and in western Europe from fermented dairy products.9 Given this, it is likely that deficiency is common, and many people could benefit from more vitamin K2. What’s more, there is evidence that broad-spectrum antibiotics can destroy the gut bacteria that produce vitamin K2 further contributing to vitamin K2 deficiency.10

The health benefits of vitamin K2 extend to osteoporosis, cardiovascular disease, inflammation, cancer, Alzheimer’s disease, diabetes and peripheral neuropathy. 

Clinical studies have unequivocally demonstrated the utility of vitamin K2 supplementation in ameliorating peripheral neuropathy, reducing bone fracture risk and improving cardiovascular health.11

Although vitamin D3 has been known as the bone vitamin, vitamin K2 has been recognised as being just as important for bone maintenance. That’s because vitamin K2 plays a pivotal role in calcium metabolism and therefore, not only promotes the calcification of bone but also prevents calcium from accumulating in soft tissues, such as the kidneys and blood vessels. 12

As a result, the combination of vitamin D3 and K2 in a single formula is considered highly worthwhile as a way of providing bone support, promoting heart health, and helping boost immunity. 13

A recent study found that liposomal vitamin K2 can significantly ameliorate vitamin K2 status in people with insufficient levels.14

Summing it all up

In the past, vitamins D3 and K2 were shown to have positive health benefits but typically had poor uptake and bioavailability. With the development of new liposomal technologies, these nutrients can now be readily absorbed and utilised.

The benefits of liposomes are numerous:

High bioavailability  

• Protects against degradation in the harsh environment of the GI tract
• Increases gastrointestinal uptake and absorption
• Increases intracellular delivery
• Reduced risk of gut irritation or digestive sensitivity
• Non-invasive 
• Can hold and deliver both fat-soluble and water-soluble compounds

Non-toxic, biocompatible and biodegradable

Offers flexible dosing and administration

 

References:

1. Akbarzadeh A, Rezaei-Sadabady R, Davaran S, Joo SW, Zarghami N, Hanifehpour Y, Samiei M, Kouhi M, Nejati-Koshki K. Liposome: classification, preparation, and applications. Nanoscale Res Lett. 2013 Feb 22;8(1):102. doi: 10.1186/1556-276X-8-102. PMID: 23432972; PMCID: PMC3599573.
2. He H, Lu Y, Qi J, Zhu Q, Chen Z, Wu W. Adapting liposomes for oral drug delivery. Acta Pharm Sin B. 2019 Jan;9(1):36-48. doi: 10.1016/j.apsb.2018.06.005. Epub 2018 Jun 20. PMID: 30766776; PMCID: PMC6362257.
3. Sharif Mohammad Shaheen, Fazle Rabbi Shakil Ahmed , Md. Nazir Hossen , Maruf Ahmed , Md. Shah Amran and Md. Anwar-UL-Islam , 2006. Liposome as a Carrier for Advanced Drug Delivery. Pakistan Journal of Biological Sciences, 9: 1181-1191.
4. Holick MF. Vitamin D: a d-lightful solution for health. J Investig Med. 2011 Aug;59(6):872-80. doi: 10.2310/JIM.0b013e318214ea2d. PMID: 21415774; PMCID: PMC3738435.
5. Bleizgys A. Vitamin D Dosing: Basic Principles and a Brief Algorithm (2021 Update). Nutrients. 2021 Dec 10;13(12):4415. doi: 10.3390/nu13124415. PMID: 34959969; PMCID: PMC8709011.
6. Ramasamy I. Vitamin D Metabolism and Guidelines for Vitamin D Supplementation. Clin Biochem Rev. 2020 Dec;41(3):103-126. doi: 10.33176/AACB-20-00006. PMID: 33343045; PMCID: PMC7731935.
7. Dałek P, Drabik D, Wołczańska H, Foryś A, Jagas M, Jędruchniewicz N, Przybyło M, Witkiewicz W, Langner M. Bioavailability by design - Vitamin D3 liposomal delivery vehicles. Nanomedicine. 2022 Jul;43:102552. doi: 10.1016/j.nano.2022.102552. Epub 2022 Mar 26. PMID: 35346834; PMCID: PMC8957331.
8. Manouchehr Saljoughian, PharmD, PhD, The Emerging Role of Vitamin K2 Department of Pharmacy, Alta Bates Summit Medical Center, Berkeley, California US Pharm. 2012;37(1):HS-12-HS-14. 
9. Fox, P., McSweeney, P., Cogan, T., and Guinee, T. (2004). Cheese: Chemistry, Physics and Microbiology. 3rd Edition, 1. Available at: https://www.elsevier.com/books/cheese-chemistry-physics-and-microbiology-volume-1/fox/978-0-12-263652-3 (Accessed November 25, 2021).
10. Jadhav Nikita, Ajgaonkar Saiprasad, Saha Praful, Gurav Pranay, Pandey Amitkumar, Basudkar Vivek, Gada Yash, Panda Sangita, Jadhav Shashank, Mehta Dilip, Nair Sujit, Molecular Pathways and Roles for Vitamin K2-7 as a Health-Beneficial Nutraceutical: Challenges and Opportunities, Frontiers in Pharmacology, Volume 13, 2022,  https://www.frontiersin.org/articles/10.3389/fphar.2022.896920  DOI:10.3389/fphar.2022.896920    
11. Elbossaty WF. Significant influence for vitamin K on different metabolic diseases according to positive effect on levels of both vitamin D, and calcium. Arch Biotechnol Biomed. 2018; 2: 008-011. DOI: 10.29328/journal.abb.1001010
12. Dalmoro, A., Bochicchio, S., Lamberti, G., Bertoncin, P., Janssens, B., & Barba, A. A. (2019). Micronutrients encapsulation in enhanced nanoliposomal carriers by a novel preparative technology. RSC Advances, 9(34), 19800–19812. https://doi.org/ 10.1039/c9ra03022k
13. Nowak JK, Krzyżanowska-Jankowska P, Drzymała-Czyż S, et al. Fat-Soluble Vitamins in Standard vs. Liposomal Form Enriched with Vitamin K2 in Cystic Fibrosis: A Randomized Multi-Center Trial. J Clin Med. 2022;11(2):462. Published 2022 Jan 17. doi:10.3390/jcm11020462
14. Lai Yujiao, Masatoshi Hori, Ma Yanbo, Guo Yuming, Zhang Bingkun, Role of Vitamin K in Intestinal Health, Frontiers in Immunology, Volume 12, 2022,  https://www.frontiersin.org/articles/10.3389/fimmu.2021.791565,    DOI=10.3389/fimmu.2021.791565