by Bryan Moskow
Chief Science Officer Blackstone Labs, MS Organic and Biochemistry
Cellulite is predominantly a condition of poor microcirculation that can cause damage to adipose tissue under the skin. It is the result of cellular impairment to the framework by which the body stores subcutaneous fat cells and can affect up to 98% of women after puberty. When microcirculation is poor, fluid leaks into the surrounding spaces of the framework, which allows for fat cells to grow in size, blocks the flow of oxygen and nutrients carried into the area, and can prevent the drainage of toxins that may accumulate. This process repeatedly damages the connective tissue, such as collagen and elastin, and eventually leads to scarring and an uneven distribution damaged tissue and fat cells. The net result is non-aesthetically pleasing, “orange-peel” skin that can be embarrassing to some women.1
Over the last decade, there have been many topical “cellulite reducing creams” that have made very bold claims but with very little science behind them. Everyone wants something that works great and is very effective, however until recently the science hasn’t been too sound. In the last few years however, liposomal technology has dramatically improved the efficacy of therapeutics by enhancing delivery of the active compounds. It has also been shown to reduce the toxicity and increase targeted delivery in several types of molecules/therapeutics.2
Since cellulite is the result of excess fat and damage to cellular framework, a 2-pronged approach is needed to effectively fight cellulite: improving local circulation and increasing lipolysis (fat burning).
This is the exact mechanism by which the liposomal formula Liporeductyl®, included in Body Shaping, the contour-refining cream by Celestial Bodies works. Liporeductyl® is a specific blend of natural herbal extracts and a unique compound called Tripeptide-1 that together have been shown to fight and reverse the effects of cellulite buildup, both in vitro and in vivo!
Let’s talk about the first prong of fighting cellulite: improving local circulation. Liporeductyl® contains several ingredients that can improve circulation to the damaged area. Butcher’s Broom (Ruscus aculeatus) extract contains several flavonoids, fatty acids, and plant sterols that have all been shown to increase circulation locally when applied topically. In a recent randomized, double-blind study, it was shown that the active ingredients in Butcher’s Broom extract can reduce venous capacity, exerts protective effects on capillaries, strengthen blood vessels and maintain healthy circulation.3 Ivy (Hedera helix) extract contains chemicals called saponins, phenolic acids and flavonoids that all aid in the improvement of circulation, reduce inflammation, and can induce the drainage of liquid and tissue responsible for cellulite. Ivy extract may lead to reconstruction of the cellular matrix.4 Escin, found naturally in horse chestnut, is a triterpene saponin that has been shown to decrease fluid leakage from small blood vessels, and block the action of thrombin, a blood-clotting agent. In studies, escin has been shown to decrease the activity of lysosomal enzymes (which may be elevated in cases of cellulitis) by up to 30%.5
While all of these ingredients have really good data and work synergistically to help fight the root cause of cellulite, the real revolutionary ingredient is Tripeptide-1 (GHK). GHK is a tripeptide made up of 3 amino acids: glycine, hisitidine, and lysine stabilized with a copper atom. GHK’s main mechanism of action is that it scavenges specific by-products of a process called lipid peroxidation, which damages cell membranes and creates instability. These by-products are highly reactive and have been shown to decrease the effectiveness of all the anti-cellulite compounds in Liporeductyl® by interfering with the processes by which they work. Think of GHK has the ingredient that makes every other ingredient work even better. A recent study demonstrated GHK to quench 75% of these by-products within 2 hours of administration.6
Now, that was just the first prong to fighting cellulite. The second prong is all about increasing lipolysis, or fat burning. The first ingredient in Liporeductyl® that aids in increasing fat breakdown is caffeine. Caffeine works by increasing the breakdown of fatty acids by increasing concentrations of cyclic AMP (cAMP). Up until recently, caffeine has not been well absorbed topically. However, Liporeductyl® was shown to increase absorption of caffeine by almost 5-fold.6 The next ingredient, the amino acid L-carnitine works very well together with caffeine to increase fatty acid breakdown. L-carnitine is required for the transport of fatty acids into the mitochondrial matrix, where they are burned as fat for energy. Without L-carnitine, fat burning would be severely hindered.7
On paper, a product can look great, but many times what looks good on paper doesn’t live up to what the data claims. Liporeductyl® has real in vitro and in vivo data to back up its potency. Some key in vitro data shows that Liporeductyl®’s liposomal formulation enhances the absorption of the active ingredients. Liporeductyl® significantly increased the absorption of two key compounds: induction of caffeine and escin into the affected cells increased by 5-fold and 8-fold, respectively. Typically, escin bioavailability is very poor. Studies have shown it to range between 0.25% and 12.5%.8 With escin being such an integral ingredient to improving microcirculation and repairing damage caused by cellulite, it’s easy to see this 8-fold in absorption makes the product stand out from the competition. To test for cellulite prevention, Liporeductyl® was added to preadipocytes (cells that will differentiate to become fat cells) in a dose-dependent manner. Liporeductyl® was shown to decrease only the fat cells and not total cells. What this means is that Liporeductyl® specifically targets the process of fat cell maturation, and is not cytotoxic to other healthy cells. At its highest dose, Liporeductyl® reduced the number of fat cells by 275% percent vs the placebo.6
In a 2013 in vivo study, 20 female volunteers between the ages of 18 and 70 used Liporeductyl® daily for 60 days to test its anti-cellulite properties. The first experiment was designed to test for reduction of buttock and thigh circumference. The group using Liporeductyl® lost, on average almost 1cm of buttock circumference, including 15% of the subjects losing between 2 to3 cm. Average thigh circumference decreased by 0.5cm, with 85% of all subjects showing a reduction between 0.5-1cm. Body fat and extracellular water changes were also measured. On average, participants lost 0.7kg (1.54lbs), with 50% of the volunteers losing between 0.6 and 1.4kg (1.32-3.08lbs). As for extracellular water, subjects averaged a 0.6L decrease, with 60% of participants displaying a decrease between 0.5 to 1.6L. This is extracellular water, so the loss of this water doesn’t cause dehydration. In fact, subjects from this study showed an average of 9.5% increase in skin moisture and a 24.4% increase in skin elasticity. One of the major health issues associated with cellulite is loss of skin elasticity, so this is not only an aesthetic improvement, but functional as well.
Subjects also went through a dermatological evaluation, in which a dermatologist evaluated improvements in certain criteria such as smoothness, appearance of “orange-peel” skin (lumps of cellulite) and nodules, as well as, elasticity and complexion. The most staggering improvement noted was 95% of subjects displayed a reduction in nodules, or little bumps on the skin. Equally as important, was that 75% of participants showed improvement in the “orange-peel” appearance and 65% showed an improvement in Rosy complexion, meaning there was truly a reversal in the damage caused by microcirculation.6
- Rossi, Ana Beatris R., and André Luiz Vergnanini. "Cellulite: a review."Journal of the European Academy of Dermatology and Venereology 14.4 (2000): 251-262.
- Samad, Abdus, Y. Sultana, and M. Aqil. "Liposomal drug delivery systems: an update review." Current drug delivery 4.4 (2007): 297-305.
- Redman, Deborah A. "Ruscus aculeatus (butcher's broom) as a potential treatment for orthostatic hypotension, with a case report." The Journal of Alternative and Complementary Medicine 6.6 (2000): 539-549.
- Hexsel, Doris, Cecilia Orlandi, and Debora Zechmeister do Prado. "Botanical extracts used in the treatment of cellulite." Dermatologic surgery 31.s1 (2005): 866-873.
- Pittler MH, Ernst E. Horse-chestnut seed extract for chronic venous insufficiency. A criteria-based systematic review. Arch Dermatol. 1998 Nov;134(11):1356-60.
- Unpublished data from Lipotec, 2013.
- Foster, Daniel W. "The role of the carnitine system in human metabolism."Annals of the New York Academy of Sciences 1033.1 (2004): 1-16.
- Wu XJ, et al Comparative pharmacokinetics and bioavailability of escin Ia and isoescin Ia after administration of escin and of pure escin Ia and isoescin Ia in rat .J Ethnopharmacol. (2012)