Experimental study
Patients of female and male gender characterized by massive hair reduction due to various causes, and also a small number of patients of female gender of postmenopausal age, reporting hair thinning, hair reduction and loss of hair strength were selected. The clinical efficacy of preparation 4 that on previous tests displayed the best characteristics of homogeneity and stability was evaluated .
Treatments :
Lotion A, prepared according to the present example 4 ; Lotion B, comparison, prepared as described in WO 2011/095938 (example 1) and then containing PGE1 and S- equol in 1:1 ratio
Lotion C, containing 7 mg of PGE1 enclosed in liposomes as the only active substance, prepared according to method A;
Lotion D, containing 1,25 mg of DGLA enclosed in liposomes as the only active substance, prepared according to method A.
Groups of patients:
• Group 1: 10 (6 male, 4 female) patients treated for 120 days with 1 ml/day of Lotion A to be applied on a well defined area of the scalp;
• Group 2: 10 (5 male, 5 female) patients treated for 120 days with 1 ml/day of Lotion B to be applied on a well defined area of the scalp;
• Group 3: 6 female menopausal patients for about 3 years, without specific diseases related to hair reduction, treated for 120 days with 1 ml/day of Lotion A to be applied on a well defined area of the scalp.
• Group 4: 4 (2 male, 2 female) patients treated for 120 days with 1 ml/day of Lotion C to be applied on a well defined area of the scalp; • Group 5: 4 (2 male, 2 female) patients treated for 120 days with 1 ml/day of Lotion D to be applied on a well defined area of the scalp;
Evaluation was carried out at pre-determined time points by dermoscopy and direct observation with photographic detections.
Results
On day 7 : both group 1 and group 2 experience a reduction of hair loss, defined substantial by patients of group 1 and modest by those of group 2. Group 3 feels hair as more robust. Groups 4 and 5 do not report any variation;
On day 20: in group 1 all the patients have stopped losing hair and report the presence of a substantial fuzz. In group 2 hair loss has stopped in 6 patients and fuzz, where present, is more modest (in terms of number/cm2) . Group 3 reports an aesthetic improvement related to hair brightness. Group 4 reports a minimal reduction in hair loss. Group 5 does not report any variation;
On day 45: in group 1, fuzz has grown markedly stronger and takes the colour and consistency of natural hair. In group 2, as expected, all the patients have stopped losing hair, but only some of them report a certain degree of regrowth, fuzz is very weak and not completely coloured yet. Group 3 reports disappearance of split ends. Group 4 reports arrested hair loss in all the subjects and, in some of them, presence of weak fuzz. Group 5 does not report any variation;
On day 90: in group 1 all the patients report total disappearance of hair reduction areas that have been replaced by robust and shiny hair. In group 2 hair reduction is still visible, even if areas are all covered with thick fuzz. Group 3 confirms a general hair improvement. Groups 4 and 5 do not record variations from the previous evaluation;
On day 120: group 1 confirms results already seen at day 90. Group 2 continues improvement, even if in some patients of male gender the fuzz has not got the characteristics of strength and colour typical of hair yet. Group 3 confirms results previously obtained. Groups 4 and 5 do not record variations from the previous evaluation .
During the whole phase of the study the patients' skin was regularly assayed by dermoscopy, highlighting an improvement of circulation. Additionally, treated skin did not display allergic or inflammatory reactions.
From the observations reported here, first of all, it can be inferred that the formulations object of the present invention are clinically efficient in:
· stopping hair loss; • promoting hair regrowth in areas with alopecia;
• strengthening and fortifying hair, bringing it back to its original state
both in male and female subjects with forms of hair reduction or actual alopecia due to different causes, and in menopausal women.
Formulations set up here additionally:
• do not contain potentially toxic substances or that may interfere with other active ingredients;
· are not irritating for the skin: even after long term application no evidence of irritation or inflammation was reported;
• are stable in time: analysis carried out on the content of the vials 30 days after preparation detects
· significant ?? values in terms of stability, particularly for formulations containing 2% or, better, 3% stearylamine
• an unchanged content of active substances enclosed in liposomes;
· can be stored at room temperature and in a ready-to- use form;
and, surprisingly
• act more quickly and more effectively: comparison tests clearly demonstrate that group 1 has a more rapid, more substantial improvement and, mainly, it involves all the patients as compared with group 2, treated with Lotion B.
Again, it should be recalled that Lotion B contains PGE1 and equol in 1:1 ratio, while Lotion A contains 30% less of active substance (DGLA) . This means that the findings of the present invention exert an unexpectedly superior effect than what known, at markedly lower concentrations of active substances.
These results should be attributed only to the formulation set up herein. In fact, it is clear from data analysis that patients treated with PGE1 alone, even at the concentrations described in WO2011/095938, experience a very modest variation of the situation. Still different and most important is the observation of group 5, treated with DGLA alone at the same concentration employed in Lotion A: there is no reduction in hair loss and even less any regrowth, not even of fuzz.
The extraordinary effects that are displayed by the compositions of the present invention are then due to synergies between single components, promoted by the characteristics of the liposome suspensions used.
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