ascorbate-2-phosphate and Melanosis

Ascorbic acid (vitamin C) is an antioxidant that is widely used in cosmetics in skincare products. Due to the excessive low stability of ascorbic acid in cosmetic formulations, the stabilized ascorbic acid derivative, magnesium ascorbyl phosphate (MAP) was formulated as vesicular carriers; ethosomes and niosomes. The aim was to deliver MAP at the intended site of action, the skin, for sufficient time with enhanced permeation to get an effective response. Ethosomes were formulated using a full 3

Topics: Administration, Cutaneous; Adult; Animals; Antineoplastic Agents; Ascorbic Acid; Chemistry, Pharmaceutical; Dose-Response Relationship, Drug; Drug Carriers; Drug Liberation; Drug Stability; Female; Gels; Humans; Liposomes; Male; Melanosis; Middle Aged; Neurocutaneous Syndromes; Rats; Surface Properties

Melasma is an acquired disorder of hypermelanosis of great psychosocial concern. The treatments with various conventional therapies are often unsatisfactory. Lasers and light sources have been used to treat pigmented lesions, but in Asian skin with higher melanin content, such treatments may be challenging.. To determine the effectiveness of treating melasma with a combination of topical 5% magnesium ascorbyl phosphate (MAP) and fluorescent pulsed light (FPL).. Patients of skin types III-V with refractory melasma were treated for 12 weeks with topical application of 5% MAP and three sessions of FPL (570-950 nm) at 3, 6, and 9 weeks (fluence 12-14 J/cm(2) , pulse width 15 ms, and spot size 3 cm(2) ). They were followed up for another 12 weeks to assess the persistence of treatment benefit. Digital photographs of the patients were taken at each visit. Treatment efficacy was determined by calculating mean melasma area and severity index (MASI) at the beginning and then at weeks 6, 12, and 24. The subjective assessment was done by comparing pre-treatment and post-treatment photographs by an independent observer and self-assessment by patients using four-point scoring scale (1, poor, 2, fair, 3, good, and 4, excellent).. Sixty-five patients completed the study. The baseline mean MASI score of 14.80 decreased to 4.53 at the 12th week (end of treatment) and 6.35 at the 24th week (end of follow-up). The overall regression of mean MASI at these end-points was 69.3% and 57% (P < 0.01). The pre- and post-treatment photographic evaluation by independent observer and patients' self-assessment at the 12th week showed good to excellent response (scores 3 and 4) in 52.3% and 44.6% cases, respectively. No significant adverse effects of treatment were noted.. Combination of 5% MAP with FPL is effective, well tolerated, and safe in treating refractory melasma in Asian patients but for persistent improvement, maintenance treatments would be required.

Topics: Administration, Topical; Adolescent; Adult; Antineoplastic Agents; Ascorbic Acid; Asian People; Combined Modality Therapy; Female; Fluorescence; Follow-Up Studies; Humans; Male; Melanosis; Phototherapy; Treatment Outcome; Young Adult

Vitamin C (L-Ascorbic acid) has many favourable effects on the skin such as antioxidant, anti-aging and whitening effects. Its instability and low permeability limit its pharmaceutical use in cosmetic and dermatological products. Instead, Mg ascorbyl phosphate (MAP), an ascorbic acid derivative, has the same effect with higher stability is being used. In this work, a vesicular system, aspasomes, containing MAP was developed and evaluated. Aspasomes are multilayered vesicles formed by amphiphiles molecules, Ascorbyl palmitate (ASP), in combination with cholesterol and charged lipids for drug encapsulation. Here, we investigated the use of lecithin instead of the charged lipid dicetyl phosphate for aspasomes development. Nine formulations were prepared and evaluated for their entrapment efficiency, particle size, polydispersity index (PDI) and zeta potential. Their entrapment efficiency ranged from 33.00 ± 2.27 to 95.18 ± 1.06, while their particle size was from 373.34 ± 60.85 to 464.37 ± 93.46 nm with acceptable PDI (from 0.212 ± 0.068 to 0.351 ± 0.061) and zeta potential (from -37.52 ± 2.42 to -50.36 ± 1.82). Three formulations were selected and evaluated for their drug release, permeation and retention into skin. One formulation was selected to be formulated as aspasomal topical cream and gel. The aspasomal cream was found to have enhanced drug permeation and skin retention over the aspasomal gel as well as the aspasomes formulation. MAP aspasomal cream was evaluated clinically as an effective treatment for melasma against 15% trichloroacetic acid (TCA) and the results recorded that the aspasomal cream showed the greatest degree of improvement regarding the hemi-MASI scores with 35% of patients rating it as excellent treatment. The study showed that MAP aspasomal cream can be considered a novel treatment of melasma which is free of side effects. Its efficacy as a monotherapy is superior to that of chemical peeling using 15% TCA.

Topics: Administration, Cutaneous; Animals; Antineoplastic Agents; Ascorbic Acid; Biological Transport; Cholesterol; Drug Compounding; Drug Liberation; Drug Stability; Humans; Lecithins; Liposomes; Magnesium; Male; Melanosis; Rats, Wistar; Skin; Skin Absorption; Treatment Outcome

An inhibitory effect of ascorbic acid (AsA) on melanogenesis has been described. However, AsA is quickly oxidized and decomposed in aqueous solution and thus is not generally useful as a depigmenting agent.. Our purpose was to examine the effect on pigmentation of magnesium-L-ascorbyl-2-phosphate (VC-PMG), a stable derivative of AsA.. Percutaneous absorption of VC-PMG was examined in dermatomed human skin, and its effect on melanin production by mammalian tyrosinase and human melanoma cells in culture was also measured. A 10% VC-PMG cream was applied to the patients.. VC-PMG suppressed melanin formation by tyrosinase and melanoma cells. In situ experiments demonstrated that VC-PMG cream was absorbed into the epidermis and that 1.6% remained 48 hours after application. The lightening effect was significant in 19 of 34 patients with chloasma or senile freckles and in 3 of 25 patients with normal skin.. VC-PMG is effective in reducing skin hyperpigmentation in some patients.

Topics: Ascorbic Acid; Female; Humans; In Vitro Techniques; Melanins; Melanoma, Experimental; Melanosis; Monophenol Monooxygenase; Skin Absorption; Skin Neoplasms; Tumor Cells, Cultured