Research on Lipsomes for increased bioavailability
Liposomes protect products from digestion in the GI tract, but that is only the first step. The improved bioavailability varies greatly, depending on the molecule itself and the quality of the liposome.
Water solubility. Molecules with very poor water solubility usually have the worst bioavailability and can benefit the most from liposomal delivery. Fisetin is one example shown below up to 27x more bioavailable.
Liposome Stability. Liposomes need modification to increase stability so they do not break apart and release their payload when exposed to the GI tract and bloodstream. Recent advances in Liposomal technology enables skilled manufacturers to adjust the stability so the payload is protected for several hours. Different manufacturing techniques result in significant variation in stability and bioavailability.
Liposome size. As noted above, size of the liposome is crucial. Larger Lipsomes are quickly filtered out by the liver and other parts of the RES. Smaller liposomes (below 50 nanometers) can circulate much longer. The study on B-12 below shows the larger size liposome formula increased bioavailability of 3xvs 5x for the smaller sized liposomal formula.
Liposomal Fisetin 1.6 to 27x more bioavailable
This study in mice found a 2.7-fold increase (in Cmax) with Liposomal Fisetin, with a dose 10 times lower than that of the free fisetin when given by IP.
With IV, the Cmax of liposomal fisetin was 10, vs 6 for free fisetin.
Liposomal Vitamin B-12 formulas 3-5x more bioavailable than tablet.
This study compared five formulations for bioavailabilty in humans over 6 hours.A standard table (iii) was compared against an emulsion (ii), a chewabletablet (iv), an oral spray comprised of larger liposomes (v) and an oral spray comprised of very small (20 nanometer) liposomes.(I)NANOCELLE 1000UG -28% – A NANO LIPOSOMAL FORMULATION OF B12SUBLINGUAL SPRAY WITH AN AVERAGE PARTICLE SIZE OF ABOUT 20 NM
(ii) Emulsion 1000ug – 10% -An emulsion formulation of B12 sublingual
(iii) Tablet 1000ug – 5% – A standard tablet formulation of B12 that is absorbed through the gastrointestinal tract.
(iv) Chewable 5000ug – 27% – A dissolvabletablet of B12 that is absorbed through the sublingual mucosa
(v) Liposome1000ug – 14% – A liposome oral spray of B12 with particle sizes of approximately 100 nm.
The chewable showed similar increase as nano liposomal, but a 5x higher dosage was used.
The standard liposomal product was 3x more bioavailable than tablet.
The nano liposomal spray exhibitedsustained release with more than 5x increased bioavailability over standard tablets.READ MORE
Liposomal Berberine increases circulation time 23-46x
Preparation, Pharmacokinetics and Tumour-Suppressive Activity of Berberine Liposomes (Zheng, 2017)
Administration of standard Liposomal Berberine increased retention time in circulation from .42 to 10 hours. Use of PEG modified Liposomes further increased retention to to 14 hours.
Administration of Berberine solution injection is hindered by unsatisfactory pharmacokinetics and, more importantly, the risk of lethal cardiovascular adverse reactions due to rapid uptake into heart and lung. This study validated common and long-circulating liposomes as safe and effective method for sustained release of Berberine.
Liposomal Curcumin & Resveratrol capsules 10-20x more bioavailable in circulation and prostate tissue vs standard capsules
Liposome capsules of resveratrol and curcumin may inhibit prostate problems by increasing their bioavailability synergistically.
In this study, we determined the bioavailability of liposome encapsulated curcumin and resveratrol, individually and in combination and evaluated the inhibitory effects of these agents against prostate growth and progression.
Serum and prostate tissue samples harvested at different time points of 30 min to12 hr with plain liposome (0.1%), curcumin (50 mg/kg/bw), lipo-curcumin (50 mg/kg/bw),lipo-resveratrol (50 mg/kg/bw) and lipo-curcumin co administered with lipo-resveratrol (25 mg/kg/bw for each)
figure a – Levels of curcumin and resveratrol recorded in the serum
figure b – Levels of curcumin and resveratrol recorded in the prostate
figure d – Quantification of tumor growth inhibition. Total number of adenocarcinomas observed under 10 high-power fields of control vs. treatment groups.
Liposomal Glutathione: Key to Oxidative Stress
Glutathione is a diverse nutrient that can be used as a nutritional supplement to support many areas of health – from the lungs to the liver and more. The Free Radical Theory of Aging mechanistically links oxidative stress to aging. 1
Known as the “Master Antioxidant,” its levels decrease as a result of aging, stress and toxin exposure. Boosting glutathione may provide many health benefits, including reduction of oxidative stress. 2
Because glutathione can be broken down rapidly in the digestive tract, it is important to select a glutathione supplement that is formulated to survive exposure to digestive enzymes and be well absorbed.
The liposomes surround each molecule and protect the core ingredients from the digestive system while increasing its transport and uptake by your cells.
What Exactly Is Glutathione?
Glutathione, also referred to as GSH, is a tripeptide composed of three amino acids – glycine, cysteine, and glutamic acid.1 Glutathione is a naturally occurring intracellular antioxidant found abundantly in nearly every cell in your body. This potent molecule plays such a crucial role in our bodies, it’s even been dubbed “the mother of all antioxidants.” There is increasing awareness of its utility in mitigating body toxin load. 3
Glutathione is a biomarker associated with disease risk and health status that has potential to translate to an important target relevant to health optimization, disease prevention, and treatment. As a result, it is possible that supporting the body’s endogenous levels of glutathione would be important for maintaining health and mitigating disease. 4
Some of the critical roles glutathione plays in your body include:
- Scavenging and neutralizing harmful free radicals
- Acting as a signaling molecule and modulating your immune response
- Regenerating other important antioxidants like Vitamins C and E
- Supporting mitochondrial function (the powerhouse of your cells)
- Transporting toxic heavy metals, like mercury, out of your cells
- Regulating cellular proliferation and apoptosis (programmed cell death)
Glutathione depletion is indicative of oxidative stress and occurs in various pathological conditions and following extreme exercise activity. Raising blood glutathione concentration has potential to attenuate and prevent chronic disease and also to improve recovery from exercise. 5
EFFECTS OF LIPOSOMAL GLUTATHIONE
The results of a recent study demonstrated increased body stores of Glutathione (GSH) after oral administration of Liposomal GSH humans. 1
Liposomes have been used as an effective means of drug delivery allowing for more efficient absorption and delivery of both hydrophilic and lipophilic substances and greater protection against oxidation and degradation. Since GSH is subject to destruction in the acid environment of the stomach, researchers tested that oral liposomal GSH might be an effective means of GSH delivery in vivo.
The results of this pilot study demonstrate for the first time increased body stores of GSH after oral administration of liposomal GSH humans. Liposomal GSH appeared to be effective at two doses (500 and 1000 mg/d) and effects were seen as early as 1 week. In addition, liposomal GSH had positive effects on several GSH-related parameters including decreases in biomarkers of oxidative stress and enhancements in immune functions. Finally, liposomal GSH was highly tolerated and its administration was not associated with any signs of adverse effects. 2
The results from this study provide support for the potential use of oral liposomal Glutathione as an intervention strategy for enhancing tissue Glutathione levels for use in disease therapy or prevention.
In addition, they provide a rationale for additional larger placebo-controlled trials in both healthy and diseased individuals aimed at assessing the potential therapeutic efficacy of liposomal Glutathione. These results are consistent with previous findings where oral supplementation with non-liposomal glutathione was effective at enhancing body stores of GSH in laboratory animals and humans 2, 3, 4.
Liposomal Glutathione effects were often greater that previously observed for non-liposomal Glutathione 5.
LIPOSOMAL GLUTATHIONE ENHANCES IMMUNE FUNCTION
The immune system works best if the lymphoid cells have a delicately balanced intermediate level of glutathione. Even moderate changes in the intracellular glutathione level have profound effects on lymphocyte functions. Certain functions, such as the DNA synthetic response, are exquisitely sensitive to reactive oxygen intermediates and, therefore, are favoured by high levels of the antioxidant glutathione. 1
Recent findings support the effectiveness of daily liposomal GSH administration at elevating stores of GSH and impacting immune function and levels of oxidative stress. 2