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Prostate Cancer, Magnesium, and Vitamin C Topical

June 2016

By Life Extension

Vitamin C topical

Efficacy of cosmetic formulations containing dispersion of liposome with magnesium ascorbyl phosphate, alpha-lipoic acid and kinetin.

The present study aimed to evaluate the photoprotective effects of cosmetic formulations containing a dispersion of liposome with magnesium ascorbyl phosphate (MAP), alpha-lipoic acid (ALA) and kinetin, as well as their effects on the hydration and viscoelastic skin properties. The photoprotection was determined in vitro (antioxidant activity) and in vivo on UV-irradiated hairless mouse skin. The hydration effects were performed with the application of the formulations under study on the forearm of human volunteers and skin conditions were analyzed before and after a single application and daily applications during 4 weeks in terms of transepidermal water loss (TEWL), skin moisture and viscoelastic properties. The raw material under study possessed free-radical scavenging activity and the formulation with it protected hairless mouse skin barrier function against UV damage. After 4 weeks of application on human skin, the formulation under study enhanced stratum corneum skin moisture and also showed hydration effects in deeper layers of the skin. Thus, it can be concluded that the cosmetic formulation containing a dispersion of liposome with MAP, ALA and kinetin under study showed photoprotective effects in skin barrier function as well as pronounced hydration effects on human skin, which suggests that this dispersion has potential antiaging effects.

Photochem Photobiol. 2012 May-Jun;88(3):748-52

In vitro antioxidant activity and in vivo efficacy of topical formulations containing vitamin C and its derivatives studied by non-invasive methods.

BACKGROUND/PURPOSE: Vitamins C and its derivatives, mainly due to their antioxidant properties, are being used in cosmetic products to protect and to reduce the signs of ageing. However, there are no studies comparing the effects of vitamin C [ascorbic acid (AA)] and its derivatives, magnesium ascorbyl phosphate (MAP) and ascorbyl tetra-isopalmitate (ATIP), when vehiculated in topical formulations, mainly using objective measurements, which are an important tool in clinical efficacy studies. Thus, the objective of this study was to determine the in vitro antioxidant activity of AA and its derivatives, MAP and ATIP, as well as their in vivo efficacy on human skin, when vehiculated in topical formulations. METHODS: The study of antioxidant activity in vitro was performed with an aqueous and a lipid system. The in vivo methodology consisted of the application of these formulations on human volunteers’ forearm skin and the analysis of the skin conditions after 4-week period daily applications in terms of transepidermal water loss (TEWL), stratum corneum moisture content and viscoelasticity using a Tewameter, Corneometer and Cutometer, respectively. RESULTS: In vitro experiments demonstrated that in an aqueous system, AA had the best antioxidant potential, and MAP was more effective than ATIP, whereas in the lipid system ATIP was more effective than MAP. In in vivo studies, all formulations enhanced stratum corneum moisture content after a 4-week period daily applications when compared with baseline values; however, only the formulation containing AA caused alterations in TEWL values. The formulations containing MAP caused alterations in the viscoelastic-to-elastic ratio, which suggested its action in the deeper layers of the skin. CONCLUSION: AA and its derivates presented an in vitro antioxidant activity but AA had the best antioxidant effect. In in vivo efficacy studies, only the formulation containing AA caused alterations in TEWL values and the formulation containing MAP caused alterations in the viscoelastic-to-elastic ratio. This way, vitamin C derivatives did not present the same effects of AA on human skin; however, MAP showed other significant effect-improving skin hydration, which is very important for the normal cutaneous metabolism and also to prevent skin alterations and early ageing.

Skin Res Technol. 2008 Aug;14(3):376-80

Postadministration protective effect of magnesium-L-ascorbyl-phosphate on the development of UVB-induced cutaneous damage in mice.

The effects of stable vitamin C, magnesium-L-ascorbyl-2-phosphate (MAP), administered after acute and chronic exposure to UVB irradiation were investigated using hairless mice. Intraperitoneal administration of 100 mg/kg of MAP immediately after acute exposure to 15 kJ/m2 of UVB significantly prevented increases of UVB-induced lipid peroxidation in skin and sialic acid in serum, an inflammation marker. Administration of 50 mg/kg of MAP immediately after each exposure significantly delayed skin tumor formation and hyperplasia induced by chronic exposure to 2 kJ/m2 of UVB. Intraperitoneal administration of 200 mg/kg of MAP produced an increase in ascorbic acid (As) levels in the serum, liver and skin within 15 min. Serum As levels quickly returned to normal, but hepatic and cutaneous levels remained elevated before returning to normal after 24 h, suggesting that MAP was converted to As in the serum and in those tissues. Ultraviolet B-induced hydroxyl radical generation in murine skin homogenates was scavenged by As-Na addition, which was directly detected by electron spin resonance (ESR). These results suggest that postadministration of MAP delays progression of skin damage induced by UVB irradiation. It is presumed that MAP, once converted to As, exhibits such inhibitory effects by scavenging hydroxyl and lipid radicals generated as a direct or indirect result of UVB exposure.

Photochem Photobiol. 1998 Jun;67(6):669-75

Protective effects of sodium-L-ascorbyl-2 phosphate on the development of UVB-induced damage in cultured mouse skin.

The protective effect of sodium-L-ascorbyl-2 phosphate (As-2P), a stable form of ascorbic acid (AsA), against photodamage induced by a single dose of UVB exposure (290-320 nm, Max 312 nm) was investigated using cultured mouse skin. When the cultured skin was treated with various As-2P concentrations, the cutaneous AsA level increased in proportion to the As-2P concentration. After 3 h of incubation, the AsA level in the cultured skin treated with 2, 20 and 100 mM As-2P increased 1.03-, 2.17- and 6.27-fold, respectively, compared with that of the control skin. These results suggest that As-2P was transported into the cultured mouse skin where it was converted to AsA. After 3 h, the cutaneous AsA level in irradiated (20 kJ/m2) skin was depleted to a half of that in the control skin. However, the level in skin pretreated with 20 mM As-2P was maintained within normal limits, even after 24 h. Pretreatment with 20 mM As-2P significantly prevented such photodamage as sunburn cell formation, DNA fragmentation and lipid peroxidation, which were caused by a single dose of UVB irradiation. These results suggest that the protective effect of 20 mM As-2P on UVB-induced cutaneous damage is due to the maintenance of a normal As level by conversion of As-2P to As in skin tissue.

Biol Pharm Bull. 1999 Dec;22(12):1301-5

Sodium ascorbyl phosphate shows in vitro and in vivo efficacy in the prevention and treatment of acne vulgaris.

Acne vulgaris is the most common inflammatory skin disorder and jeopardizes seriously the facial impression of a person. Development of acne involves a complex relation among several causes. Treatment and prevention success can be archived by affecting the main contributors positively like Proprionibacterium acnes or lipid oxidation leading to inflammatory reactions and follicular keratinization. Vitamin C tends to break down in cosmetic formulations resulting in a brownish discoloration. Sodium ascorbyl phosphate (SAP) represents a stable precursor of vitamin C that ensures a constant delivery of vitamin C into the skin. We were able to show that 1% SAP has a strong antimicrobial effect with a log reduction of 5 after 8 h on P. acnes in a time-kill study. Further on in a human in vivo study with 20 subjects an SAP O/W formulation significantly prevents the UVA-induced sebum oxidation up to 40%. Finally, we performed an open in vivo study with 60 subjects with a 5% SAP lotion over 12 weeks. The efficacy ranked as excellent and good of SAP was 76.9%, which was superior compared with a widely prescribed acne treatment. In conclusion, these data show that SAP is efficient in the prevention and treatment of acne vulgaris. SAP can be used in a non-antibiotic and effective treatment or co-treatment of acne with no side effects, which makes it particularly attractive for cosmetic purposes.

Int J Cosmet Sci. 2005 Jun;27(3):171-6

Mechanisms regulating skin pigmentation: the rise and fall of complexion coloration.

Skin pigmentary abnormalities are seen as aesthetically unfavorable and have led to the development of cosmetic and therapeutic treatment modalities of varying efficacy. Hence, several putative depigmenting agents aimed at modulating skin pigmentation are currently being researched or sold in commercially available products. In this review we will discuss the regulation of processes that control skin complexion coloration. This includes direct inhibition of tyrosinase and related melanogenic enzymes, regulation of melanocyte homeostasis, alteration of constitutive and facultative pigmentation and down-regulation of melanosome transfer to the keratinocytes. These various processes, in the complex mechanism of skin pigmentation, can be regulated individually or concomitantly to alter complexion coloration and thus ameliorate skin complexion diseases.

Int J Mol Sci. 2009 Sep 15;10(9):4066-87

Ferulic acid stabilizes a solution of vitamins C and E and doubles its photoprotection of skin.

Ferulic acid is a potent ubiquitous plant antioxidant. Its incorporation into a topical solution of 15%l-ascorbic acid and 1%alpha-tocopherol improved chemical stability of the vitamins (C+E) and doubled photoprotection to solar-simulated irradiation of skin from 4-fold to approximately 8-fold as measured by both erythema and sunburn cell formation. Inhibition of apoptosis was associated with reduced induction of caspase-3 and caspase-7. This antioxidant formulation efficiently reduced thymine dimer formation. This combination of pure natural low molecular weight antioxidants provides meaningful synergistic protection against oxidative stress in skin and should be useful for protection against photoaging and skin cancer.

J Invest Dermatol. 2005 Oct;125(4):826-32

Topical vitamin C: a useful agent for treating photoaging and other dermatologic conditions.

BACKGROUND: Cosmeceuticals containing antioxidants are among the most popular antiaging remedies. Topically applied antioxidants exert their benefits by offering protection from damaging free radicals produced when skin is exposed to ultraviolet light or allowed to age naturally. Vitamin C is a naturally occurring potent water-soluble antioxidant. Accordingly, it has been incorporated into a variety of cosmeceuticals designed to protect and rejuvenate photoaged skin. OBJECTIVE: This article reviews the scientific data and clinical studies supporting the use of topically applied vitamin C for treating
photoaged skin. Other innovative uses for vitamin C cosmeceuticals are also discussed. CONCLUSION: A significant body of scientific research supports the use of cosmeceuticals containing vitamin C. Cutaneous benefits include promoting collagen synthesis, photoprotection from ultraviolet A and B, lightening hyperpigmentation, and improvement of a variety of inflammatory dermatoses. Because of the diverse biologic effects of this compound, topical vitamin C has become a useful part of the dermatologist’s armamentarium.

Dermatol Surg. 2005 Jul;31(7 Pt 2):814-7

Vitamin C in dermatology.

Vitamin C is a potent antioxidant drug that can be used topically in dermatology to treat and prevent changes associated with photoageing. It can also be used for the treatment of hyperpigmentation. Because it is unstable and difficult to deliver into the dermis in the optimum dosage, research is being directed to find stable compounds of Vitamin C and newer methods of delivery of Vitamin C into the dermis.

Indian Dermatol Online J . 2013 Apr;4(2):143-6.

Ferulic acid stabilizes a solution of vitamins C and E and doubles its photoprotection of skin.

Ferulic acid is a potent ubiquitous plant antioxidant. Its incorporation into a topical solution of 15% l-ascorbic acid and 1% alpha-tocopherol improved chemical stability of the vitamins (C+E) and doubled photoprotection to solar-simulated irradiation of skin from 4-fold to approximately 8-fold as measured by both erythema and sunburn cell formation. Inhibition of apoptosis was associated with reduced induction of caspase-3 and caspase-7. This antioxidant formulation efficiently reduced thymine dimer formation. This combination of pure natural low molecular weight antioxidants provides meaningful synergistic protection against oxidative stress in skin and should be useful for protection against photoaging and skin cancer.

J Invest Dermatol. 2005 Oct;125(4):826-32

Sodium L-ascorbyl-2-phosphate 5% lotion for the treatment of acne vulgaris: a randomized, double-blind, controlled trial.

BACKGROUND: Antioxidants are becoming increasingly important in the treatment of skin disease. In addition to their known anti-inflammatory effects, antioxidants may act to prevent the oxidation of sebum which has been proposed to be comedogenic in acne patients. Sodium L-ascorbyl-2-phosphate (APS) is a stable vitamin C derivative and highly effective antioxidant that has demonstrated efficacy in acne in open label studies. OBJECTIVE: To evaluate the efficacy and safety of APS 5% lotion for the treatment of acne in a blinded controlled study. METHODS: A total of 50 subjects were randomized in a double-blind controlled trial to receive APS 5% lotion or vehicle for 12 weeks. Evaluation included an Investigator’s Global Assessment Score, a Subjects’ Global Assessment Score, lesion counts, cutaneous tolerability, and adverse events. RESULTS: APS 5% lotion demonstrated statistically significant improvement when compared to vehicle in all of the parameters measured. The adverse event frequency and cutaneous tolerability profile for APS 5% lotion were similar to vehicle. LIMITATIONS: Adjunctive topical or oral agents and their impact on acne were not studied in this trial. CONCLUSIONS: This study demonstrates that 5% sodium L-ascorbyl-2-phosphate is efficacious as monotherapy for the treatment of acne. APS 5% lotion offers a novel addition to our current acne armamentarium.

J Cosmet Dermatol. 2010 Mar;9(1):22-7

The prevalence of acne in adults 20 years and older.

BACKGROUND: Acne, one of the most common skin diseases, is often mistakenly thought to affect exclusively the teenaged group. However, a significant number of patients either continue to experience acne or develop new-onset acne after the teenaged years. OBJECTIVE: A survey was designed to assess the prevalence of acne in the teenaged years, and aged 20 to 29 years, 30 to 39 years, 40 to 49 years, and 50 years and older. METHODS: Adults aged 20 years and older were asked to complete surveys distributed at various sites on our university campus and medical complex. RESULTS: Of 1013 participants aged 20 years and older, 73.3% (n = 744) reported ever having acne. After the teenaged years, women were more likely to report having acne than men, with the difference being statistically significant in all age groups. The prevalence of acne reported in women versus men was as follows: 20 to 29 years, 50.9% (n = 276) versus 42.5% (n = 201) (P = .0073); 30 to 39 years, 35.2% (n = 152) versus 20.1% (n = 73) (P < .0001); 40 to 49 years, 26.3% (n = 93) versus 12.0% (n = 36) (P < .0001); and 50 years and older, 15.3% (n = 41) versus 7.3% (n = 18) (P = .0046). LIMITATIONS: Our results are based on the participant’s own perception of the presence or absence of acne rather than a clinical evaluation. CONCLUSIONS: Acne continues to be a common skin problem past the teenaged years, with women being affected at higher rates than men in all age groups 20 years or older.

J Am Acad Dermatol. 2008 Jan;58(1):56-9

Ultrasound enhanced skin-lightening effect of vitamin C and niacinamide.

BACKGROUND/PURPOSE: Cutaneous hyperpigmentation occurs in multiple conditions. There is a strong need for the improvement of hyperpigmentation especially among Asian women. However, the effect of existing skin-lightening agents is not sufficient. One reason attributes to the limited capability of active agents to be delivered transepidermally. Ultrasound is one promising approach to enhance transepidermal transport. In this work, we investigate the effect of the use of high-frequency ultrasound together with coupling gel containing skin-lightening agents (ascorbyl glucoside and niacinamide) on facial hyperpigmentation in vivo in Japanese women. METHODS: The effect of ultrasound on the absorption of skin-lightening agents into the stratum corneum was evaluated in a tape-stripping method on human forearms in vivo. The skin efficacy was assessed in a facial clinical trial involving 60 subjects with hyperpigmentation in a paired design. Subjects were assigned to two groups, each group using two treatments (one on each facial cheek): (1) skin-lightening gel with ultrasound vs. no treatment or (2) skin-lightening gel with ultrasound vs. skin-lightening gel treatment. Changes in facial hyperpigmentation were objectively quantified by computer analysis and visual grading of high-resolution digital images of the face in addition to the subjective assessment via questionnaire. RESULTS: Ultrasound radiation enhanced the absorption of skin-lightening agents in the stratum corneum in a radiation-time-dependent manner. In the facial clinical trial, use of ultrasound radiation together with the skin-lightening gel significantly reduced facial hyperpigmented spots compared with both no treatment and skin-lightening gel alone after 4 weeks. CONCLUSIONS: The data suggest that use of high-frequency ultrasound radiation together with skin-lightening gel is effective to reduce hyperpigmentation via enhancing transepidermal transport of skin-lightening agents.

Skin Res Technol. 2006 May;12(2):105-13

Successful short-term and long-term treatment of melasma and postinflammatory hyperpigmentation using vitamin C with a full-face iontophoresis mask and a mandelic/ malic acid skin care regimen.

BACKGROUND: Treatment of melasma and postinflammatory hyperpigmentation is often challenging. No ideal short-term and long-term treatment is available. Vitamin C alone and in combination with iontophoresis has been studied and found to be useful; however, no long-term studies have been published. METHODS: In this study, 35 patients (34 female, 1 male) were treated with a novel full-face iontophoresis mask (FFIM) and a proprietary vitamin C (ascorbyl glucoside) preparation. Patients received one in-office treatment and 12 to 24 at-home treatments over 1 to 2 months in conjunction with a strict maintenance regimen consisting of a mandelic/malic acid skin care regimen, broad-spectrum ultraviolet A/ultraviolet B sunblock, a wide-brimmed hat, and sun-avoidance behavior. Follow-up after the initial in-office treatment ranged from 1 to 54 months (mean, 26 months). Four independent observers graded improvement of melasma and PIH using a 4-point scale. Before the study, high-performance liquid chromatography was used to verify iontophoretic penetration of vitamin C into the skin to a level of 0.2 cm in healthy volunteers (2 male, 2 female). RESULTS: A mean 73% improvement in abnormal pigmentation was observed at the end of FFIM/vitamin C treatment. Greater than 25% improvement was observed in 32 of 35 patients, and greater than 50% improvement in 22 of 35 patients. Melasma Area and Severity Index scores demonstrated substantial improvement from baseline for all patients, with a mean improvement of 15.7. CONCLUSIONS: Full-face iontophoresis of vitamin C appears to be an effective short-term treatment for melasma and postinflammatory hyperpigmentation. A protocol of strict sun avoidance in combination with a mandelic/malic acid skin care regimen appears to be useful in maintaining the improvement.

J Drugs Dermatol. 2013 Jan;12(1):45-50