HYDROXYPINACOLONE RETINOATE

Description

A derivative of the most potent form of vitamin A, retinoic acid. The ingredient can be sold under name Granactive Retinoid. Note that if a skincare brand discloses the concentration of Granactive Retinoid in a product, the concentration refers to a diluted form of Hydroxypinacolone Retinoate: 1% of Granactive Retinoid corresponds to 0.1% of Hydroxypinacolone Retinoate. Hydroxypinacolone Retinoate (HPR) is a unique derivative of retinoic acid because it can directly work in the skin and does not require additional conversion steps. According to studies done by the manufacturer on models of human skin (not real people), this derivative is more effective than other cosmetic versions of retinoids (such as retinol, retinaldehyde, and retinyl palmitate), and, at the same time, causes less irritation. It has been also demonstrated to be more stable than retinol which makes formulating with easier and increases the chances that a product with it will maintain its effectiveness after opening. The packaging should still ideally be air-tight. HPR is available over the counter in the EU, UK, Asia, Australia and New Zealand, but is only with a prescription in Canada.

Scientific paper review

Safety and Efficacy of Retinsphere® Technology and Biopep-15 in the treatment of Acne in Asian Population
n Participants Interventions Punchline
30 Filipino patients diagnosed with mild-moderate acne (Grades 0-3 by Leeds Acne Grading System Revised correlated with grades 1-2 on Plewig scale and Kligman, 1975). Patients having undergone treatment for acne including cosmeceuticals within 3 weeks previous to the start of the study. Exclusion criteria: patients with concomitant systemic conditions, receiving systemic treatments and with other concomitant dermatoses at the time of study; pregnant or breast-feeding women. Biretix Duo (active ingredients: Hydroxypinacolone Retinoate, Retinol, Salicylic Acid) was applied to the whole face in the morning and night after washing with hypoallergenic bar soap. A broad spectrum sunscreen was also applied in the morning and patients were advised to avoid sun exposure. The results were assessed at baseline, day 45, day 90 and day 120 The number of open comedones, closed comedones and papules showed statistically significant decrease over time. Closed comedones responded faster than open comedones with significant difference seen as early as day 45. Both open and closed comedones continued to decrease in lesion count throughout the entire study period. The number of papules decreased throughout the treatment period with significant difference between baseline and days 90 and 120. Median sebumeter values showed significant decrease over time. Mild itching was experienced by 3-13% of patients from days 15 to 120, with highest percentage at day 45. Mild burning occurred in 7% of patients at day 45 but was absent at days 90 and 120. No edema was reported by any of the patients throughout the study period.
Clinical evaluation of the efficacy of a new retinoic-complex (Retinsphere®) product for the treatment of skin photoaging
n Participants Interventions Punchline
10 Female patients (age 28-81 years) with photoaged skin classified with the Glogau scale Product: product containing a new retinoic complex (hydroxypinacolone retinoate and retinol, associated with papain, Maca andina, Cupressus sempervirens, moisturizing complex, folic acid and vitamin E). Treatment consisted of applying the product twice daily for 8 weeks together with a topical photoprotector. No sun-exposure or artificial-UV exposure was admitted. a significative improvement of all the observed characteristics has been recorded. Also the global skin photoaging evaluation, performed at the times T0 and T12 with the Glogau scale, showed a significative improvement (P<0.001).
Treatment of mild to moderate acne with a fixed combination of hydroxypinacolone retinoate, retinol glycospheres and papain glycospheres
n Participants Interventions Punchline
98 Caucasian patients (28 males and 70 females), with an age ranging from 15 to 40 years Product: A fixed combination of 0.1% hydroxypinacolone retinoate (synthetic esther of 9-cis-retinoic acid), 1% retinol in glycospheres and 2% papain in glycospheres in aqueous gel. Participants were treated with the product once daily for 12 weeks A 41% mean reduction in the GAGS score was observed; a 40.8% mean reduction of total lesions was recorded; 15.3% of patients experienced mild to moderate local side effects (dryness, peeling, erythema, burning). No patients stopped the treatment because of these side effects.
Evaluation of efficacy and safety of the combinated use of two topic retinoids to treat mild / moderate acne.
n Participants Interventions Punchline
20 (9F/11M) (mean age: 30, range. 18-40 yrs) with mild to moderate acne Participants were treated with an association of hydroxypinacolone retinoate, a new retinoid, allowed in cosmetic formulas, and Retinol entrapped into Glycospheres Technology, containing Papain, R-NMF (Rebuilt-Natural Moisturizer Factor), tocopherol (Vit. E), glycerol, Treolase, Aloe Barbadenis. During the course of the study, no other topical or systemic treatment was allowed Most of patients had satisfactory therapeutic response with a reduction of GAGS global score of 70%. Digital images confirmed clinical improvement (Figure 1). Micro-comedones and macro-comedones showed respectively a reduction of 38% and of 65%. Follicular biopsy proved a reduction about 60% in the density of micro and macro- comedones. No patients dropped out the study because of side effects and tolerability was very good in 90% of our sample.
Assessment of the efficacy and tolerance of a new combination of retinoids and depigmenting agents in the treatment of melasma
n Participants Interventions Punchline
28 Inclusion criteria: Aged over 18 years; Absence of treatment for melasma in the last 3 months; No desire to get pregnant in the forthcoming months and use of contraceptives; No concomitant diseases; No administration of another topical or systemic product that may interfere or affect the process; No allergy to the product ingredients. 67% of patients cited a history of sensitive skin. The product included retinol glycospheres and hydroxypinacolone retinoate, as well as N-acetylglucosamine, kojic acid, Cromabright and Natriquest, copper and iron ions, albatin & alistin, and niacinamide. The formulation contains 10% of hydrating active ingredients and 3% anti-irritant, anti-inflammatory active ingredients. The treatment protocol included the application of the active cream with sun protection factor SPF 50 (Neoretin discrom control gel cream—IFC Pharmaceuticals) during the day and active serum (Neoretin discrom control serum booster fluid—IFC Pharmaceuticals) at night on one side of the face vs. vehicle gelcream with SPF 50 during the day and vehicle serum during the night on the other side of the face; thus, the patient was also the control group. The vehicle had the same photoprotector as the study product. In percentage terms, the reduction of the MASI at the end of the study on the side treated with the product was 74% (31%) vs. a reduction of 55% (36%) on the side that received the vehicle with SPF, with this being a significant difference (P = 0.009).

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