We commissioned an independent, simple yet comprehensive report on the bioavailability of 1g of liposomal Vitamin C (Lipolife® Gold) compared to 1g of non-liposomal oral Vitamin C.
Vitamin C plays a vital role in human health with some of its key functions including wound healing and neurotransmitter and carnitine synthesis. Vitamin C also functions as an important physiological antioxidant (Carr and Frei, 1999; Li and Schellhorn, 2007).
Unlike the majority of land animals, humans have not evolved to bio-synthesise Vitamin C and therefore it is an essential nutrient which can only be obtained from dietary intake (Drouin et al 2001).
Serum ascorbate levels are considered to be an appropriate reflection of bioavailability (Brubacher et al., 2000).
The bioavailability of Vitamin C has long been a controversial topic. It once was incorrectly assumed by the National Institute of Health (NIH) that oral Vitamin C intakes >200mg resulted in an absorption threshold of 220µM/L (Ods.od.nih.gov) until recently disproved by Hickey et al (2008) in a pilot-study that showed concentrations of >235µM/L could be achieved with 5g liposomal and non-liposomal Vitamin C.
This was a significant finding for Vitamin C as a therapeutic agent since ascorbate concentrations at 300µM/L have resulted in 30% necrosis and apoptosis in cancer cells and concentrations at 400µM/L increased cell death to approximately 50% (Chen et al 2005).
Only one other study has validated the bioavailability of liposomal Vitamin C which showed 4g of liposomal Vitamin C achieved a peak concentration of approximately 181.7µM/L compared to 130µM/L with non-liposomal Vitamin C (Davis et al., 2016).
The focus of this paper herein is to test and report on the bioavailability of 1g of liposomal Vitamin C (Lipolife Gold) compared to 1g of non-liposomal Vitamin C.
Twenty-four healthy subjects (n=24) took part in an open-label, randomized, single dose, 2 x 2 (2 dosing periods and 2 treatments) cross-over study to determine the bioavailability of a single oral dose of 1g of liposomal Vitamin C suspension compared to 1g of non-liposomal Vitamin C liquid.
The study consisted of two treatment periods and subjects were randomly divided into two treatment groups. In the first treatment period, group 1 (n=12) received 5ml of liposomal Vitamin C containing 1g and group 2 (n=12) received 5ml of non-liposomal Vitamin C containing 1g.
In the second treatment, period group 1 received the non-liposomal Vitamin C whilst group 2 received liposomal Vitamin C.
By the end of the study both groups had been exposed to both treatments.
A seven-day washout period separated both treatment periods.
A baseline blood sample was drawn at 0 hours, the first treated sample was drawn 15 minutes later, followed by; 15-minute intervals until 1 hour; 30-minute intervals until 3 hours; hourly until 12 hours; 2-hourly until 16 hours; and the final sample was taken at 24 hours from baseline. Plasma levels of Vitamin C are measured as ascorbate (µM/L).
The liposomal and non-liposomal vitamin C were provided by Lipolife (Lipolife, Unit 1 Drakes Lane Industrial Estate, Essex, UK).
The design and protocol set out in this study complied with ICH GCP regulatory guidelines issued by CDSCO, Ministry of Health.
Results from figures 1 show the oral bioavailability of 1g of liposomal Vitamin C compared to 1g of non-liposomal Vitamin C across a twenty-four and seven-hour period. At two hours post-treatment, liposomal Vitamin C reached plasma concentrations that were two-fold the concentration of non-liposomal Vitamin C at 205.1µM/L and 102.6µM/L, respectively.
Tmax was achieved in both groups at four hours post-treatment with liposomal Vitamin C showing a 2.4-fold greater plasma response than non-liposomal Vitamin C with concentrations of 297.5 µM/L and 123.2 µM/L, respectively.
After twenty-four hours plasma concentrations of liposomal Vitamin C remained above baseline, however, plasma concentrations of non-liposomal Vitamin C had fallen below baseline measurements.
A single oral dose of liposomal Vitamin C showed greater absorption and peak plasma levels of ascorbate compared to non-liposomal oral Vitamin C.
Furthermore, liposomal Vitamin C resulted in quicker increases in ascorbate concentration and also sustained higher blood levels of ascorbate over a greater period of time than non-liposomal Vitamin C.
The data presented here shows oral liposomal Vitamin C is superior to non-liposomal oral Vitamin C across multiple measures.
Liposomal Vitamin C lends itself as a promising therapeutic tool in the pursuit of targeting chronic disease with nutraceuticals agents.
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Chen Q. Espey M.G. Krishna M.C. Mitchell J.B. Corpe C.P. Buettner G.R. Shacter E. Levine M. (2005). Pharmacologic ascorbic acid concentrations selectively kill cancer cells: action as a pro-drug to deliver hydrogen peroxide to tissues. Proc Natl Acad Sci USA. 102(38), 13604-13609
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Ods.od.nih.gov. (n.d.). Office of Dietary Supplements - Vitamin C. [online] Available at: https://ods.od.nih.gov/factsheets/VitaminC-HealthProfessional/ [Accessed 13 Nov. 2018].