Fat-Dissolving Injections

On April 7, 2010, the United States Food and Drug Administration sent warning letters to six spas that offered “fat-melting injections.” In the letter the FDA noted that such injections, which are provided subcutaneously, or just under the skin and are offered as an alternative to liposuction, had not been proven either safe or effective.

Liposuction is a surgical procedure in which bodyfat is literally sucked out of specific areas of the body. The fat-dissolving injections are said to remove small fat deposits around the legs, arms and stomach. Despite those claims, the FDA’s warning letter stated that the products offer “false and misleading claims not supported by any substantial evidence or clinical experience.” The FDA was prodded into that action by reports of side effects associated with the fat-dissolving injections, such as scarring, lumps and dark spots on the skin.

If such a procedure actually worked, it would be of interest to bodybuilders and others who want to lose localized fat deposits. Many small fat deposits are difficult to completely eliminate, even with consistent dieting and exercise. For example, lower-back fat in men stubbornly remains in many despite vigorous dieting and workouts. The notion of a localized injection to remove recalcitrant fat would be attractive to many—assuming that it worked as advertised. In addition, while not inexpensive, the costs of those injections would be considerably less than liposuction surgery.

Fat-dissolving injections contain a combination of phosphatidylcholine and sodium deoxycholate. The drug is manufactured in Germany and sold under the trade name Lipostabil. Its original use was for dissolving fat embolisms, or small pieces of fat in the lungs that could fatally interfere with lung function.

Phosphatidylcholine, or PC, is a natural compound consisting of the nutrient choline and polyunsaturated fatty acids. It’s a major component of lecithin, which for years was touted as a fat emulsifier. The other major ingredient of Lipostabil is sodium deoxycholate, or SD, which is a bile salt. The liver produces bile, which is stored in the gallbladder. When you eat a meal containing fat, the gallbladder contracts and releases bile salts, which emulsify the fat in the food. That reduces the surface area of the fat so that lipases, or enzymes, can break it down.

The reason Lipostabil contains both PC and SD is that the latter emulsifies the PC and makes it more soluble. In fact, one ongoing debate about Lipostabil is whether the active ingredient is PC or SD. Recent research comes down on the side of SD but not in the expected way. When injected subcutaneously, Lipostabil is said to dissolve local fat deposits safely, but when it’s used to break up pulmonary fatty embolisms, it’s always provided intravenously. Scientists view subcutaneous administration with suspicion.

Lipostabil is thought to work by facilitating lypolysis, which is the breakdown of fat cells. Normally, lipolysis involves a cascade of events. Special beta-receptors in the membranes of fat cells are activated by catecholamines, such as epinephrine and norepinephrine. That in turn activates a secondary cell messenger, most often cyclic AMP and phospholipids, which inhibit the action of phosphodiesterase, an enzyme that normally blocks lipase from breaking down fat in the fat cell.

The theory that PC has lipolytic properties was based on a Russian study of type 2 diabetics who were given large oral doses of it. The subjects showed a significant improvement in insulin resistance, a hallmark of diabetes. PC intake, they theorized, helped improve the interaction of insulin and its cell receptors. Improving insulin activity in the cellular membrane, however, would help increase fat synthesis, not fat breakdown.

Another theory was that PC helped form lipoprotein lipases—that is, enzymes that break down fat. Still another theory was that PC can be a secondary messenger for activating hormone-sensitive lipase, the main enzyme that breaks down fat in fat cells. These numerous theories help explain why a drug such as Lipostabil would help dissolve fat. In fact, however, none of the theories has been tested on animals or humans or even in a test tube.

The current idea of what really happens when Lipostabil is injected is that the detergent action associated with bile salts, such as SD, dissolves the fat-cell membrane. So what’s the problem with the destruction of fat cells?  Well, it’s not only fat cells that can be destroyed by injecting Lipostabil.

One study investigated whether injecting Lipostabil stimulated lipolytic, or fat-breakdown, pathways.¹ A special line of isolated fat cells was exposed to Lipostabil. The cells were also exposed to its ingredients, PC and SD. Neither of the two substances led to any lipolytic action in the fat cells. When used together as Lipostabil, though, even low doses resulted in the destruction of fat cells. The effect was attributed to the SD component because of its detergent action in breaking down fat-cell membranes. It can also produce such side effects as redness, pain and edema, or swelling. In addition, the destruction of membranes isn’t limited to fat cells but can also affect cells in vascular areas, such as blood vessels. Even muscle cells can be destroyed.

Another study, this time featuring both rats and a human subject, confirmed that Lipostabil brings on extreme inflammation of subcutaneous fat stores.² That leads to fibrosis, or scar tissue, and the death of fat tissue. Higher doses of the drug extend tissue death to muscle underlying the subcutaneous fat and to cell membranes in blood vessel. Using the drug can result in fat cysts that can harden or calcify, and inflammatory reactions in surrounding tissue may continue to occur even years after the injection is administered.

While the FDA is just beginning to crack down on fat-dissolving injections, other countries have already acted. Brazil suspended importation of Lipostabil in 2003 following its widespread use by nonmedical personnel for cosmetic purposes. In England, doctors don’t prescribe the drug because insurance companies won’t cover doctors who use it for fat loss.

According to Robin Ashinoff, M.D., a spokesperson for the American Academy of Dermatology, “A single injection [of Lipostabil] is giving people false hope. Everyone is looking for a quick fix. But there is no quick fix for fat deposits or cellulite.” As for the safety of Lipostabil, Naomi Lawrence, a dermatological surgeon at the Newark-based University of Medicine and Dentistry of New Jersey, says, “Phosphatidylcholine is unpredictable and causes extreme inflammation and swelling when injected. It is not a benign drug.”

While the FDA has often been criticized for its caution in relation to various drugs, including anabolic steroids and pro-hormone supplements, in the case of Lipostabil it’s doing the right thing. Lipostabil is just another example of people looking for an easy way to lose bodyfat without being willing to exert themselves in the gym or go on a diet. Lipostabil is also an example of the greed of some medical practitioners and nonmedical entrepreneurs who are willing to make a buck at the expense of the health of their patients and customers.

Editor’s note: Jerry Brainum has been an exercise and nutrition researcher and journalist for more than 25 years. He’s worked with pro bodybuilders as well as many Olympic and professional athletes. To get his new e-book, Natural Anabolics—Nutrients, Compounds and Supplements That Can Accelerate Muscle Growth Without Drugs, visit www.JerryBrainum.com.  IM

References

¹ Klein, S.M., et al. (2009). In vitro studies investigating the effect of subcutaneous phosphatidylcholine injections in the 3T3-L1 adipocyte model: Lipolysis or lipid dissolution? Plast Reconstr Surg. 124:419-27.

² Schuller-Petrovic, S., et al. (2008). Tissue-toxic effects of phosphatidylcholine/deoxycholate after subcutaneous injection for fat dissolution in rats and a human volunteer. Dermato Surg. 34:529-43.