Research and development of an anti-cellulite product from Thai herbal compress

Abstract

Cellulite is associated with a complex array of adipocytes under the skin and the vascular system. Herbal compresses previously developed from Thai traditional medicines have been proven to have an anti-cellulite effect in healthy volunteers within 2 weeks of treatment. One particular herbal compress had previously been identified as having specific anti-cellulite properties, and the objectives in this research study were 1) to investigate the mechanisms of the cellulite reducing chemical components of that herbal compress, 2) develop a topical preparation containing the essential oils found in extracts obtained from the ingredients of that herbal compress, 3) investigate the stability and quality control methods of the formulation developed and 4) study the effectiveness on cellulite reduction and safety of the developed formulation in female participants. Eight essential oils in, and two water extracts from, the ingredients of the herbal compress, together with nine monoterpenoid constituents, were tested on the 3T3-L1 adipocytes. The vasodilatory effect on rat aortae was also studied. The adipocytes were induced by dexamethasone, 3-isobutyl-1- methylxanthine and insulin. At all concentrations tested, all essential oils, water extracts and their monoterpenoid constituents significantly inhibited lipid accumulation activity (p < 0.05) and decreased the number of triglycerides when compared to untreated cells (p < 0.01). In addition, our results showed that the mixed oil distilled from the mixed ingredients of the herbal compress could relax the isolated rat aorta (EC50 = 14.74 ± 2.65 µg/mL). Overall, all essential oils, extracts, and chemical constituents tested showed adipogenesis inhibition and lipolysis induction effects on the cultured adipocytes with the mixed oil demonstrating vasorelaxation activity, successfully demonstrating the anti-cellulite effects of the extracts from the herbal compress.

To formulate a more convenient dosage form for administering the extracts, a gelled emulsion or an ‘emgel’ was prepared. The caffeine bio-active marker was characterized by HPLCs and the monoterpenes (camphene, camphor, 3-carene, α-citral, β-citral, limonene, β-myrcene, α-pinene, β-pinene and terpinene-4-ol) were characterized by headspace GCMS. The stability study was carried over a 12-week period. Changes in the compositions were monitored every 2-weeks during storage at 4, 25 and 50°C. The anti-cellulite herbal emgel that was developed was physically stable under accelerated testing. The shelf-life of the emgel, when kept at room temperature, was estimated to be 31 months, using the Q10 method.

The emgel was tested in a double-blind, placebo-controlled trial with 18 women aged 20–50yr with severe cellulite. The emgel was applied to the thigh skin twice daily for 12 weeks, and the appearance of cellulite (the primary outcome), thigh circumferences, skin firmness, and cutaneous blood flow (secondary outcomes) were assessed at baseline, 2, 4, 8 and 12 weeks with a 2-week follow-up. Reduced cellulite severity scores were seen at each testing time point, from 13.4±0.3 (baseline) to 12.1±0.3 (week 2) and 9.9±0.6 (week12). All secondary outcomes improved with both the placebo and the herbal emgels suggesting that the ingredients in the base-formulation might be responsible. During the testing period participant were queried, their diaries were analysed, and they underwent physical monthly inspections. No adverse events were reported or identified during this period. The herbal emgel safely improved the appearance of cellulite, while the base emgel may play a role for other endpoints. In conclusion, the research and development of anti-cellulite product containing extracts and volatile oils from Thai herbal compress completed successfully and the efficacy and safety of the ingredients of the formulation were demonstrated in both in vitro and in vivo tests.

-