Phosphatidylcholine in the treatment of localized fat

Journal of Drugs in Dermatology, Oct, 2003 by Doris Hexsel, Marcio Serra, Rosemari Mazzuco, Taciana Dal'Forno, Debora Zechmeister

Abstract

Phosphatidylcholine was initially used in emergencies and in the treatment of atheroma plaques in cardiac diseases. Recently, it has also been used in the treatment of localized fat deposits. We report on the authors' clinical experience of the use of 250 mg/ml phosphatidylcholine injections in the treatment of subcutaneous fat deposits, showing the clinical response and side-effects. Volunteers received phosphatidylcholine injections in several areas of localized fat deposits, with a minimum interval of one week and mean interval of 15 days between applications. Laboratory tests were performed during the period of the drug use. Clinical results reflect that phosphatidylcholine was efficacious in reducing the fatty pads in the treated areas, with few side effects. From the authors' point of view, the off-label use of phosphatidylcholine in the treatment of fatty pads and small areas of localized fat is safe, low cost, and effective.

Introduction

Phosphatidylcholine is a phospholipid extracted from soybean lecithin present in abundance in cell membranes, actively participating in the structure and transport between the cells (1).

This substance can alter cholesterol and other triglyceride metabolisms. It seems to be able to increase cholesterol solubility, alter the composition of fat deposits, and inhibit plaque aggregation (1). For these reasons, phosphatidylcholine is used in the intravenous treatment of lipid atheromas, hypercholesterolemia, fat embolism, fatty deposits or plaque adhering to arterial walls, mental disturbances, hepatic and cardiac conditions induced by medication, alcohol, pollution, virus, and toxins (2-10).

The cosmetic use of phosphatidylcholine originated in Italy. Its first use for such purposes was reported by an Italian physician named Sergio Maggiori, at the Fifth International Meeting of Mesotherapy in 1988, held in Paris, France. He presented his work with phosphatidylcholine in the treatment of xanthelasmas (11). In Brazil, the cosmetic use of phosphatidylcholine began at the end of the 1990s on an off-label basis.

Although the injectable form of phosphatidylcholine has not been approved for cosmetic purposes in Brazil, there is clinical evidence of its efficacy in treating localized fat. It has been widely used in Brazil in various clinical conditions where there are fat deposits in the subcutaneous tissue. These conditions are treated conventionally by liposuction or dermolipectomy. Phosphatidylcholine seems to be efficacious and effective in these cases, representing a new, less invasive, and potentially promising treatment for conditions which include "buffalo-hump" (an unaesthetic condition related with HIV fat redistribution syndrome, or FRS), lipomas, eye bulging (12), and xanthelasmas. Other possible therapeutic applications include localized fat on the thighs, hips, abdomen, flanks, neck, and lower third of the face.

Cautious about the use of phosphatidylcholine in the treatment of localized fat deposits, the Brazilian National Agency of Health Inspection (ANVISA), which regulates the use of medication in Brazil, published a resolution on January 9, 2003 prohibiting the use of this medication at the national level (13). Recently, this product has been used in Brazil not only by physicians, but also by laypersons, in non-medical locations such as gyms, beauty salons, etc.

The lack of research and publication on the subject and the apparent disinterest of the manufacturer (Aventis Pharma[R]) represent additional factors that have contributed to the non-regulation of cosmetic use of phosphatidylcholine in Brazil and, perhaps, the world. To date, there are no published articles or research studies reporting clinical, histopathological and laboratory data that prove the effectiveness of phosphatidylcholine in the treatment of localized fat areas. A study by Rittes shows photographs of pre and post phosphatidylcholine application in fat pad cases (12) but does not report either the doses used or side effects. Another study, presented by one of the present authors (Serra) in a poster at the Workshop on Lipodystrophy in Athens in 2001 (14), showed this treatment on two HIV/AIDS patients with buffalo-hump and fatty pads, with good results. Temporary edema and erythema were the only side effects presented.

Action Mechanism

The action mechanisms of phosphatidylcholine injections in the subcutaneous tissue have not yet been explained. It is supposed that the medication penetrates the adipocyte through the double lipid layer, acting as an emulsifying/tensoactive agent (15). The physical-chemical characteristics of the stored lipids would therefore be altered, making them water soluble. This would permit their elimination due to their non-compatibility with the material stored in the adipocyte which is liposoluble. However, there are no histological and/or pharmacodynamic studies that ratify such a supposition.

Toxicity

The authors' experience in the cosmetic use of phosphatidylcholine has been short. However, the long-term safety of a drug may be assessed by drawing a comparative parallel to the safety of the drug itself, in this case phosphatidylcholine, when used for other, non-cosmetic ends. The doses used by the present authors do not exceed those considered safe for those therapeutic ends described above.

 

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