Topical Applications

Proprietary preparations containing escin have been marketed for several years in Europe as a topical therapeutic measure in the management of CVI, peripherial vascular disease and in dental practice.

Evidence for the efficacy and safety of various topical formulations of escin has been obtained in preclinical and clinical studies. Over thirteen clinical studies were performed in Europe12, 20,21. A 2% escin preparation was found to penetrate the subcutis and the underlying muscle12. In animal model studies based on the croton oil dermatitis model, the complex of escin with Β-sitosterol and phosphatidylcholine was found to be more effective than free escin20.

One clinical study21 evaluated the efficacy of a 2% W/O emulsion in the first stage of edema in cases of panniculopathy (cellulitis) of the thighs and breasts. A group of 50 female volunteers suffering from venous stasis in the thighs were included in the study. The symptoms evaluated were included skin roughness, increased skin pastiness, decreased skin elasticity, increased skin pliability, lipoedema, spontaneous pain, provoked pain, skin flaccidity and cold skin. The severity of each symptom was evaluated with score-values 0 to 4, before and after the 30-day treatment, using High Performance Contact Thermography, Infrared Photoplethysmography and Laser-Doppler flowmetry. Significant reduction in the hypothermic areas and the relative normalization of the skin temperature have been observed. The authors concluded that topical application of the escin complex improves skin and adipose tissue microcirculation, increases blood flow at the capillary level and decreases edema and stasis. A second group of 20 volunteers were similarly treated and evaluated for improvement in the symptoms of fibroblastic panniculopathy of the breast. An improvement of the thermovascular maps, with the reduction of the cold areas and an increase in circulation of the smallest skin arteries was observed22.

In the US, researchers at Bastyr University in Kenmore, Wash., conducted a double-blind, randomized, single-dose trial on 71 healthy individuals (of which 70 completed the study) to assess the effects of a topical 2 percent escin gel on experimentally induced bruises (broken blood vessels)12. The escin gel reduced inflammation and tenderness in all cases over the recorded 10-hour period. Experimental hematoma was induced in the forearm by subcutaneous injection of 2 ml of the patient’s own blood obtained immediately before from the cubital vein. 10 g of either escin (34 subjects) or a placebo gel (36 subjects) was applied 5 minutes after the injection. Tenderness measurements were recorded initially and after treatment using a calibrated tonometer that records the pressure at which there is the first perception of pain.

Tenderness change from baseline12

Figure 8 : Tenderness change from baseline12

Using a two sample t-test, the group treated with escin had a significantly higher (p < 0.001) mean area under the curve as compared to the placebo-treated group (Figure 8). Thus 2% escin gel is effective in reducing inflammation and tenderness on topical application.

Esculin, the coumarin in the extract is also useful for topical application. The main pharmacological actions of esculin include capillary protection and the inhibition of enzymes such as hyaluronidase and collagenase. Esculin improved skin vasculature and is effective in the management of cellulitis. 20 women with chronic venous stasis and cellulitis were treated for two months, twice a day with an emulsion containing 3% esculin. Topically applied esculin increased the capillary density (number of capillaries open to flow per surface unit) and the structural integrity of the blood vessels. The results of the study are shown in Figure 94.

Effect of topical treatment (60 days) with 3% esculin emulsion in chronic venous stasis in the lower limb

Figure 9 : Effect of topical treatment (60 days) with 3% esculin emulsion in chronic venous stasis in the lower limb4

A fomulation containing 1% esculin, 0.5% ximenynic acid and 0.2% lauric acid reduced hair loss in people suffering from androgenic and symptomatic alopecia. In a placebo controlled study, the formulation was applied to the scalp of male and female volunteers suffering from hair loss. The formulation induced beneficial effects on scalp microcirculation and on seborrhea, leading to improved hair vitality. Trichograms (microsopic details of plucked hair) were compared to evaluate hair vitality. The results are shown in Figure 104:

Effect of topical treatment (60 days) with 3% esculin emulsion in chronic venous stasis in the lower limb

Figure 10 : Effect of topical application of a formulation (lotion) containing esculin on the trichogram in volunteers4