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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 Dermatology Online Journal -
April-June 2013
Volume 4
Issue 2
Address for
Dr. Saokar Pumori Telang,
Embellish, the Skin and
Laser Clinic, 1stoor
Sangam Project, Opp Air
Ghat, Wellesley Road,
Pune, Maharashtra,
E‑mail: drpumori@
Drug Prole
Dermatologist, Joshi
Hospital Maharashtra
Medical Foundation,
Jehangir Hospital,
Apollo Group, Pune,
Maharashtra, India
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 difcult to deliver into the dermis in the optimum dosage, research is being directed to nd stable compounds
of Vitamin C and newer methods of delivery of Vitamin C into the dermis.
Key words: Collagen synthesis, depigmentation, drug formulations, Lascorbic acid, photo‑ageing, Vitamin C
Vitamin C (Vit. C) is one of the naturally
occurring antioxidants in nature.[1,2] Most plants
and animals are able to synthesise Vit. C in vivo
from glucose. Humans and certain other
vertebrates lack the enzyme L‑glucono‑gamma
lactone oxidase required for in vivo synthesis
of Vit. C;[3] hence, they must acquire it from
natural sources such as citrus fruits, green
leafy vegetables, strawberries, papaya and
broccoli.[3,4] The word “Ascorbus” means no
Scurvy. Traditionally, Vit. C‑rich foods like
lemons were carried by sailors on long journeys
to avoid Scurvy, a disease of bleeding gums. In
1937, Dr. Albert Szent Goyrgi was awarded the
Nobel Prize for his work in isolating the Vit. C
molecule from red peppers and identifying its
role in Scurvy.[4]
L‑ascorbic acid (LAA) is the chemically active
form of Vit. C. In nature, Vit. C is found in
equal parts as LAA and D‑ascorbic acid. These
are essentially isomeric molecules and are
mutually interchangeable.[4] However, only LAA
is biologically active and thus useful in medical
practice.[2] The absorption of Vit. C in the gut is
limited by an active transport mechanism and
hence a nite amount of the drug is absorbed
despite high oral dosage.[3] Furthermore,
bioavailability of Vit. C in the skin is inadequate
when it is administered orally.[1,2] The use of
topical ascorbic acid is therefore favored in the
practice of dermatology.[5]
Vit. C has a 5‑hydrocarbon ring similar to that
of glucose. With an attached hydrogen ion, LAA
becomes a weak sugar acid, similar to other
alfa hydroxy acids used in dermatology. With a
metal ion, it forms a mineral ascorbate. There is
a marked interest in synthesis of physiologically
active and chemically stable ascorbate molecules
as LAA is unstable in nature, especially when
exposed to light.
Vit. C as antioxidant
Vit. C, the most plentiful antioxidant in human
skin, forms a part of the complex group of
enzymatic and non‑enzymatic antioxidants that
co‑exist to protect the skin from reactive oxygen
species (ROS). As Vit. C is water soluble, it
functions in the aqueous compartments of the
cell.[4] When the skin is exposed to UV light,
ROS such as the superoxide ion, peroxide and
singlet oxygen are generated. Vit. C protects
the skin from oxidative stress by sequentially
donating electrons to neutralize the free radicals.
The oxidised forms of Vit. C are relatively
non‑reactive.[4] Furthermore, they can be
converted back to Vit. C by the enzyme dehydro
ascorbic acid reductase in the presence of
glutathione. Exposure to UV light reduces the
availability of Vit. C in the skin.
Vitamin C in dermatology
Pumori Saokar Telang
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DOI: 10.4103/2229-5178.110593
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Telang: Vitamin C in Dermatology
144 Indian Dermatology Online Journal-
April-June 2013
Volume 4
Issue 2
UV light, reactive oxygen species (ROS) and skin
damage ‑ Vit. C and photoprotection
As mentioned above, the exposure of skin to UV light generates
ROS.[3] These radicals have a potential to start chain or cascade
reactions that damage the cells. The harmful effects of ROS
occur as direct chemical alterations of the cellular DNA, the
cell membrane and the cellular proteins, including collagen.
Oxidative stress also triggers certain cellular events mediated
by transcription factors such as ROS upgrade transcription
factor activator protien‑1 (AP‑1) that increases matrix
metalloprotienase (MMP) production, leading to collagen
breakdown.[3] Oxidative stress induces nuclear transcription
factor kappa B (NFkB). This produces a number of mediators
that contribute to inammation and skin ageing.[3] ROS also
increase the elastin mRNA level in dermal broblasts. This may
explain the elastotic changes observed in photoaged skin.[2]
Antioxidants are necessary for neutralizing the ROS formed
due to UV exposure.[2] It is important to note that Vit. C is
equally effective against both UVB (290‑320 nm) and
UVA (320‑400 nm).[2,5] Repeated small doses of UVA penetrate
30‑40‑times deeper into the dermis as against UVB, which
mostly affects the epidermis. UVA mutates and destroys
collagen, elastin, proteoglycans and other dermal cellular
structures.[2] Thus, UVA causes skin ageing and possibly
melanoma formation. UVB causes sunburn, ROS, epidermal
mutations and skin cancer. Sunscreens when properly applied
prevent UV‑induced erythema and thymine dimer mutations that
contribute to cutaneous carcinogenesis. However, sunscreens
block only 55% of the free radicals produced by UV exposure.
Photoageing can be prevented by prevention of UV‑induced
erythema, sunburn cell formation and inducing collagen repair.[2]
To optimize UV protection, it is important to use sunscreens
combined with a topical antioxidant. Vit. C does not absorb
UV light but exerts an UV‑protective effect by neutralizing free
radicals, while this effect is not seen with sunscreens. Under
laboratory conditions, it has been shown that application of
10% topical Vit. C showed statistical reduction of UVB‑induced
erythema by 52% and sunburn cell formation by 40‑60%.[3]
Although Vit. C alone can provide photoprotection, it works
best in conjunction with Vitamin E (Vit. E), which potentiates
the action of Vit. C four‑fold. Hydrophilic Vit. C helps regenerate
Vit. E, a liphophilic antioxidant.[1,3,5,6] Thus, Vit. C and Vit. E
together protect the hydrophilic and lipophilic compartments
of the cell, respectively. Vit. C and Vit. E synergistically limit
chronic UV damage by signicantly reducing both cell apoptosis
and thymine dimer formation.[3,6]
A combination of 0.5% ferulic acid (a potent antioxidant of plant
origin) with 15% Vit. C and 1% Vit. E can increase the efcacy of
Vit. C eight‑fold.[3] It was noted that this triple combination was
very useful for the reduction of acute and chronic photodamage,
and could be used for prevention of skin cancer in the future.[3]
Vit. C and collagen synthesis
Vit. C is essential for collagen biosynthesis. It has been
proposed that Vit. C inuences quantitative collagen synthesis
in addition to stimulating qualitative changes in the collagen
molecule.[2] Vit. C serves as a co‑factor for the enzymes prolysyl
and lysyl hydroxylase, the enzymes that are responsible for
stabilizing and cross‑linking the collagen molecules.[2] Another
mechanism by which Vit. C inuences the collagen synthesis
is by stimulation of lipid peroxidation, and the product of this
process, malondialdehyde, in turn stimulates collagen gene
Vit. C also directly activates the transcription of collagen synthesis
and stabilizes procollagen mRNA, thereby regulating collagen
synthesis.[2,3] Signs and symptoms of Scurvy, a deciency
disease of Vit. C, are due to impaired collagen synthesis. Clinical
studies have shown that the topical use of Vit. C increases
collagen production in young as well as aged human skin.[3,6]
Vit. C as a depigmenting agent
When choosing a depigmenting agent, it is important to
differentiate between substances that are toxic to the
melanocyte and substances that interrupt the key steps
of melanogenesis. Vit. C falls into the latter category of
depigmenting agents. Vit. C interacts with copper ions at
the tyrosinase‑active site and inhibits action of the enzyme
tyrosinase, thereby decreasing the melanin formation. Vit. C
also acts on the perifollicular pigment.[5,7,8] However, Vit. C is
an unstable compound. It is therefore often combined with
other depigmenting agents such as soy and liquorice for better
depigmenting effect.[7]
Anti‑inflammatory action of Vit. C
As stated earlier, Vit. C inhibits NFkB, which is responsible for
the activation of a number of pro‑inammatory cytokines such
as TNF‑alfa, IL1, IL6 and IL8.[2,3] Therefore, Vit. C has a potential
anti‑inammatory activity and can be used in conditions like
acne vulgaris and rosacea. It can promote wound healing and
prevent post‑inammatory hyperpigmentation.[2,3]
Vit. C is available in the market as a variety of creams, serum
and transdermal patches. Of these, only the serum contains
active Vit. C in an almost colorless form. It is unstable and,
on exposure to light, gets oxidized to Dehydro Ascorbic
Acid (DHAA), which imparts a yellow color. The stability of
Vit. C is controlled by maintaining a pH of less than 3.5. At
this pH, the ionic charge on the molecule is removed and it is
transported well across the stratum corneum.[3,5,9]
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Telang: Vitamin C in Dermatology
Indian Dermatology Online Journal -
April-June 2013
Volume 4
Issue 2
From a clinical point of view, it is important to note that the
efcacy of the Vit. C serum is proportional to the concentration,
but only up to 20%.[3] The half‑life in the skin after achieving
maximum concentration is 4 days. A persistent reservoir of
Vit. C is important for adequate photoprotection, and can be
achieved by regular 8‑hourly applications.[1,5] As UV light lowers
tissue Vit. C levels, topical Vit. C is best used after exposure to
UV light and not prior.[1‑3] A combination of tyrosine, zinc and
Vit. C has been shown to increase the bioavailability of Vit. C
20‑times vis‑à‑vis using just Vit. C.[2]
A variety of creams with Vit. C derivatives are available in the
market. As a dermatologist, it is important to know that not
all preparations are physiologically effective. Some are not
delivered into the dermis in an adequate quantity, while others
do not chemically convert to the biologically active form of Vit. C
in the skin.[1,2,4]
Magnesium ascorbyl phosphate (MAP) is the most stable
and preferred ascorbyl ester. This lipophilic molecule is easily
absorbed into the skin, and the rate‑limiting step for absorption
is its release from the vehicle, and not the rate of diffusion
across the stratum corneum as one might suppose. MAP has a
hydrating effect on the skin and decreases transepidermal water
loss. It is also a free radical scavenger that is photoprotective
and increases collagen production under laboratory test
conditions.[1,3] Other useful stable esteried derivatives are:
1 Ascorbyl 6 palmitate, a lipophilic free radical scavenger that
hydrolyses to Vit. C and palmitic acid.[3,8]
2. Disodium isostearyl 2‑0 L‑ascorbyl phosphate (VCP‑IS‑Na),
another reliable and popular derivative of Vit. C with a C8
alkyl chain attached to the stable ascorbyl moiety. This
ensures increased permeability across the epidermis
3. Ascorbic acid sulfate.[1]
4. Tetraisopalmitoyl ascorbic acid, a lipophilic provitamin and
sodium ascorbate, are derivatives under research.
Topical Vit. C is largely safe to use on a daily basis for long
durations. It can safely be used in conjunction with other
common topical anti‑ageing agents such as sunscreens,
tretinoin, other antioxidants and alfa hydroxy acids such as
glycolic acid. Minor adverse reactions include a yellowish
discoloration of the skin, hypopigmented hair and staining of
clothes, which occur due to oxidative changes of Vit. C. Once
applied, Vit. C cannot be fully washed or wiped off the skin.
Rarely, stinging, erythema and dryness are observed after use
of topical Vit. C. These can easily be treated using a moisturiser.
Care must be taken while applying Vit. C around the eyes.[1,2]
Urticaria and erythema multiforme, following the use of topical
Vit. C, have been documented.[1] The toxic doses of Vit. C that
lead to cellular apoptosis under laboratory conditions are
100‑200‑times the daily recommended dose, giving Vit. C a
very high safety prole.[1]
As Vit. C is hydrophilic, there is a marked interest to nd
methods of efcient transepidermal delivery of the stable
active compound. If antioxidants could be delivered in high
concentration through the stratum corneum barrier, then a
dermal reservoir of protective antioxidant could be increased
and thus photoprotection would be enhanced.[5] As stated
earlier, the use of stable lipophilic esteried derivatives of Vit. C
is being explored for the purpose.[5,8,10‑13] Extensive research
is underway to investigate microspheres, nanoparticles and
multilayered microemulsions for graded topical delivery.
Trials have been performed with Vit. C and Vit. E in the same
multilayered emulsions together.[6] Both electroporation and
iontophoresis have been used to enhance penetration of Vit. C
into the dermis.[11,14,15] Application of Vit. C to the treated skin
surface after microdermabrasion and CO2 or Er‑Yag resurfacing
increases the transepidermal penetration of Vit. C 20‑times.[2,16]
It has also been observed that Vit. C is a good priming agent
and a post‑operative agent for the prevention of erythema
following laser resurfacing. Smokers have been found to have
low Vit. C levels in the dermis, akin to UV‑damaged skin.
Smoking‑related skin ageing is another area where efcacy of
Vit. C is being explored. Another very useful application of Vit. C
may be striae, where a study has shown that daily application
of Vit. C combined with 20% glycolic acid over 3 months can
signicantly improve striae.[9]
To summarize, Vit. C is a naturally occurring drug with
multiple desirable effects. With an excellent safety prole,
it nds increasing use in photoageing, hyperpigmentation,
tissue inammation and promotion of tissue healing. Ongoing
research has been directed toward improving its delivery into
the dermis for stimulating collagen production and scavenging
free radicals. Vit. C thus holds promise as a mainstream drug
in future dermatology practice.
1. Talakoub L, Neuhaus IM, Yu SS. Cosmeceuticals. In: Alam M,
Gladstone HB, Tung RC, editors. Cosmetic dermatology. Vol. 1.
Requisites in Dermatology. 1st ed. Gurgaon: Saunders Elsevier; 2009.
p. 13‑4.
2. Traikovich SS. Use of Topical Ascorbic acid and its effects on
Photo damaged skin topography. Arch Otorhinol Head Neck Surg
3. Farris PK. Cosmetical Vitamins: Vitamin C. In: Draelos ZD, Dover JS,
Alam M. editors. Cosmeceuticals. Procedures in Cosmetic Dermatology.
2nd ed. New York: Saunders Elsevier; 2009. p. 51‑6.
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April-June 2013
Volume 4
Issue 2
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on 2012 Aug 11].
5. Matsuda S, Shibayama H, Hisama M, Ohtsuki M, Iwaki M. Inhibitory
effects of novel ascorbic derivative VCP‑IS‑2Na on melanogenesis.
Chem Pharm Bull 2008;56:292‑7.
6. Burke KE. Interaction of Vit C and E as better Cosmeseuticals. Dermatol
Ther 2007;20:314‑9.
7. Draelos ZD. Skin lightening preparations and the hydroquinone
controversy. Dermatol Ther 2007;20:308‑13.
8. Inui S, Itami S. Perifollicular pigment is the rst target for Ascorbyl2
phosphate6palmitate. J Dermatol 2007;34:221‑3.
9. Pinnell SR, Yang HS, Omar M, Riviere NM, DeBuys HV, Walker LC.
Topical L ascorbic acid percutanous absorbtion studies. Dermatol Surg
10. Ito Y, Maeda T, Fukushima K, Sugioka N, Takada K. Permeation
enhancement of ascorbic acid by self dissolving micropile array tip
through rat skin. Chem Pharma Bull 2010;58:458‑63.
11. Lee S, Lee J, Choi YW. Skin permeation enhancement of Ascorbyl
palmitate by lipohydro gel formulation and electrical assistance. Bio
Pharma Bull 2007;30:393‑6.
12. Rozman B, Zvonar A, Falson F, Gasperlin M. Temperature sensitive
micro emulsion gel: An effective topical delivery system of Vit E, C.
AAPS Pharma Sci Tech 2009;10:54‑61.
13. Yoo J, Shanmugam S, Song CK, Kim DD, Choi HG, Yong CS, et al. Skin
penetration and retension of LAA2PO4 using multilamellar vesicles.
Arch Pharma Res 2008;31:1652‑8.
14. Ebihara M, Akiyama M, Ohnishi Y, Tajima S, Komata K, Mitsui Y.
Iontophoresis promotes percutaneous absorbtion of Lascorbic acid in
rat skin. J Dermat Sci 2003;32:217‑22.
15. Zhang L, Lerner S, Rustrum WV, Hofmann GA. Electroporation
mediated topical delivery of Vit C for cometic applications.
Bioelectrochem Bioenerg 1999;48:453‑61.
16. Lee RW, Shen CS, Wang KH, Hu CH, Fang JY. Lasers and
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J Invest Dermat 2003;121:1118‑25.
Cite this article as: Telang PS. Vitamin C in dermatology. Indian Dermatol
Online J 2013;4:143‑6.
Source of Support: Nil, Conict of Interest: None declared.
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... This controlled release mechanism enables the recommended ingredients for normal, oily, and combination skin types, such as niacinamide, vitamin C, hyaluronic acid, green tea extract, salicylic acid, tea tree oil, zinc, witch hazel, alpha hydroxy acids, jojoba oil, to exert their beneficial effects in specific areas as needed. By incorporating such advanced delivery systems, cosmeceuticals can optimise the efficacy of these ingredients, ensuring their effective penetration into the skin and enhancing their desired outcomes [30] Helps improve skin texture and tone, reduces the appearance of fine lines and wrinkles, and strengthens the skin barrier [40] Vitamin C Helps brighten and even out skin tone, promotes collagen synthesis, and protects against environmental damage [41] Hyaluronic acid Provides deep hydration and helps retain moisture in the skin, improving skin elasticity and firmness. ...
... [40] Hyaluronic acid Provides deep hydration to dry areas while being lightweight enough not to exacerbate oiliness in the Tzone [42] Vitamin C Helps brighten and even out skin tone, promotes collagen synthesis, and protects against environmental damage [41] Alpha-hydroxy acids (AHAs) ...
... Tao et al. successfully manufactured polycaprolactone/carboxymethyl chitosan/sodium alginate fibres using emulsion electrospinning with minimal organic solvents. The resulting fibres positively impacted osteoblast viability and osteogenesis [41]. ...
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... The antioxidant, vitamin C is used as an excipient in cosmetic product due to their skin brightening property. It was reported that 10-20% should be maximum concentration of vitamin C in order to perform depigmentation [29]. Whereas, it was recommended to use 1-5% for serum [30,31]. ...
... Whereas, it was recommended to use 1-5% for serum [30,31]. The concentration of vitamin C plays a vital role in skin irritation, therefore it is necessary to use it in the limit when it comes to skin application [29]. Scientific evidence has demonstrated that vitamin C contributes to the enhancement of emulsion stability without undergoing chemical degradation. ...
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... Consequently, it is more substantially reduced in the outermost strata of the epidermis. 26,27 Microneedling is an additional adjunctive therapy for melasma that involves the creation of minuscule channels in the skin. Through these channels, small quantities of localized medications are introduced into specific and predetermined layers of the skin. ...
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... Vitamin C is a powerful antioxidant that can be used topically in dermatology to treat and prevent changes associated with the photoaging of the skin. It can also be used to treat hyperpigmentation [31]. lascorbic acid is the biologically active form of vitamin C and is therefore useful in medical practice [32]. ...
Objective: The wine industry generates large quantities of by-products presenting a remarkably valuable composition in phytochemicals. The process that can significantly increase the content of bioactive compounds is fermentation by yeast and other microorganisms. The current study presents, for the first time, an evaluation of the potential of grape stems extract and its ferments using the Scoby consortium, as a cosmetic raw material for improving the skin care properties of facial cosmetics. Methods: Fermentation of grape stems using Scoby consortium was carried out for 10 and 20 days. Unfermented and fermented extracts were analyzed for their antioxidant activity and chemical composition, with a particular emphasis on biologically active substances. Additionally, the influence of the addition of the obtained ferments to the model cosmetic creams on hydration, transepidermal water loss, and skin pH were assessed. Results: The obtained results revealed that grape stems extract and its ferments are a rich source of phenolic compounds and show antioxidant activity, with the highest values observed for extracts on the 20th day of fermentation. Furthermore, the addition of the extract, as well as ferment, to the cream has a positive effect on skin hydration and reduces transepidermal water loss. Conclusion: These results suggest that grape stems extracts are a prospective source of active compounds that may be valuable ingredients for the cosmetic industry. Unfermented and fermented extracts can be used in moisturizing cosmetic formulations and also to complement the treatment of dry and sensitive skin.
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Reactive oxygen species (ROS) generated during melanogenesis make melanocytes particularly vulnerable to oxidative stress, influencing their survival and melanin synthesis. Oxidative stress, significantly present in vitiligo and recently also detected in melasma, triggers inflammatory cascades and melanogenesis, making antioxidants a promising therapeutic avenue. A systematic search was conducted on Embase and Pubmed to study the efficacy of antioxidants for treating vitiligo and/or melasma. Meta-analysis was performed to assess the difference in Melasma Severity Index (MASI) scores between baseline and follow-up. Various antioxidants like polypodium leucotomos, ginkgo biloba, catalase/superoxide dismutase, and vitamin E have potential in vitiligo. For melasma, vitamin C, silymarin, and niacinamide were among those showing promise in reducing pigmentation, with vitamin C displaying significant effects in meta-analysis. Different antioxidants improve both vitiligo and melasma, with an increased minimal erythema dose (MED) following UV exposure being significant for vitiligo and tyrosinase inhibition being crucial for melasma. However, the efficacy of individual antioxidants varies, and their exact mechanisms, especially in stimulating melanocyte proliferation and anti-inflammatory pathways, require further investigation to understand better and optimize their use.
Context Photoaging correlates with ultraviolet radiation (UVR). In addition to direct and indirect DNA damage, UVR leads to a breakdown of collagen, resulting in enlarged pores, visible wrinkles, also uneven skin tones and pigmentations. Amniotic membrane stem cell (AMSC) can be a useful modality in cell regeneration. Vitamin C has been known as an agent of depigmentation, antioxidants, and collagen synthesis. A topical combination of amniotic membrane stem cell-conditioned medium (AMSC-CM) and vitamin C is expected to improve photoaging. Fractional CO2 laser and microneedling served as transdermal drug delivery. Aims To compare between microneedling and fractional CO2 laser for the administration of AMSC-CM and vitamin C in photoaging treatment. Methods and Material Sixty Indonesian women with photoaged skins participated in this experimental analytic, controlled, matching research and were divided into two groups. Thirty women received fractional CO2 laser, and others received microneedling. All participants received a topical combination of AMSC-CM and vitamin C. Three treatment sessions were repeated at a four-week interval for fractional CO2 laser and a two-week interval for microneedling. We evaluated the progression and side effects using a skin analyzer on weeks 0, 4, and 8 for the microneedling group and for the fractional CO2 laser group on weeks 0, 4, and 12. Results Assessment of wrinkles, UV spots, skin tone, and pore revealed a statistically significant effect of a topical combination of AMSC-CM and vitamin C after fractional CO2 laser (p < 0.05). Conclusions Combination of AMSC-CM and vitamin c using fractional CO2 laser can improve photoaging and is better compared to microneedling.
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Background: Reactive oxygen species generated by ultraviolet light result in photocarcinogenic and photoaging changes in the skin. Antioxidants protect skin from these insults. Objective: This study defines formulation characteristics for delivering L-ascorbic acid into the skin to supplement the skin's natural antioxidant reservoir. Methods: L-ascorbic acid or its derivatives were applied to pig skin. Skin levels of L-ascorbic acid were measured to determine percutaneous delivery. Results: L-ascorbic acid must be formulated at pH levels less than 3.5 to enter the skin. Maximal concentration for optimal percutaneous absorption was 20%. Tissue levels were saturated after three daily applications; the half-life of tissue disappearance was about 4 days. Derivatives of ascorbic acid including magnesium ascorbyl phosphate, ascorbyl-6-palmitate, and dehydroascorbic acid did not increase skin levels of L-ascorbic acid. Conclusions: Delivery of topical L-ascorbic acid into the skin is critically dependent on formulation characteristics.
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Microemulsions (ME)--nanostructured systems composed of water, oil, and surfactants--have frequently been used in attempts to increase cutaneous drug delivery. The primary objective addressed in this work has been the development of temperature-sensitive microemulsion gel (called gel-like ME), as an effective and safe delivery system suitable for simultaneous topical application of a hydrophilic vitamin C and a lipophilic vitamin E. By changing water content of liquid o/w ME (o/w ME), a gel-like ME with temperature-sensitive rheological properties was formed. The temperature-driven changes in its microstructure were confirmed by rotational rheometry, viscosity measurements, and droplet size determination. The release studies have shown that the vitamins' release at skin temperature from gel-like ME were comparable to those from o/w ME and were much faster and more complete than from o/w ME conventionally thickened with polymer (o/w ME carbomer). According to effectiveness in skin delivery of both vitamins, o/w ME was found the most appropriate, followed by gel-like ME and by o/w ME carbomer, indicating that no simple correlation between vitamins release and skin absorption could be found. The cytotoxicity studies revealed good cell viability after exposure to ME and confirmed all tested microemulsions as nonirritant.
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Transdermal formulation of L-ascorbic acid 2-phosphate magnesium salt (A2P) was prepared using multilamellar vesicles (MLV). A2P was either physically mixed with or entrapped into three different MLVs of neutral, cationic, and anionic liposome vesicles. For the preparation of neutral MLVs, phosphatidylcholine (PC) and cholesterol (CH) were used. For cationic and anionic MLVs, dioleoyl-trimethylammonium-propane and dimyristoyl glycerophosphate were added as surface charge inducers, respectively, in addition to PC and CH. Particle size of the three A2P-loaded MLVs was submicron, and polydispersity index revealed homogenous distribution of the prepared MLVs except neutral ones. Skin penetration study with hairless mouse skin showed that both physical mixtures of A2P with empty MLVs and A2P-loaded MLVs increased penetration of the drug compared to aqueous A2P solution. During the penetration, however, significant amount of the drug was metabolized into L-ascorbic acid, which has no beneficial effect on stimulation of hair growth. Out of the physical mixtures and A2P-loaded MLVs tested, physical mixture of A2P with empty cationic MLV resulted in the greatest skin penetration and retention in hairless mouse skin.
Ascorbic acid (AA) loaded self-dissolving micropiles (SDMP) were prepared using chondroitin sulfate as the base for the percutaneous administration of AA. AA solution was added to dense solution of chondroitin solution, glue, and array tip, 1.0 cm(2), containing 100 SDMPs of which length was 500 microm and basal diameter was 300 microm, were prepared. Two kinds of AA array tips containing 1344.2+/-1.7 microg (high content ones) and 638.7+/-4.3 microg (low content ones) were used. In vitro dissolution study showed that more than 90% of AA were released from both SDMP array tips within 5 min. Stability experiment showed that 99.2-99.4% of AA was detected in SDMP array tips when stored at 23 degrees C for 1 week. When in vitro permeation experiments were performed after AA SDMP array was inserted to the isolated rat abdominal skin, extremely high amounts of AA, 1285.3+/-369.0 microg (95.3%) for high content SDMP tip and 405.6+/-84.3 microg (65.8%) for low content SDMP tip, were permeated for 6 h into the receptor compartment due to the break down of the skin barrier function. When AA SDMP array tip was administered to the rat skin under anesthetized condition with the different contact times, 10, 20 and 30 min, the permeated amount of AA was dependent on both the AA content in SDMP array tips and the contact time. When AA SDMP was contact to the skin for 30 min, permeated amounts of AA were 146.8+/-22.9 microg (10.9%) for high content-SDMP tip and 61.2+/-18.2 microg (9.6%) for low content SDMP tip. These results suggest the usefulness of SDMP array tip for the percutaneous absorption of AA.
It is now medically recognized that sagging skin and other signs of degenerative skin conditions, such as wrinkles and age spots, are caused primarily by oxy-radical damage. Vitamin C (Vit. C), in the form of L-ascorbic acid (Asc), is the one vitamin that can accelerate wound healing, protect fatty tissues from oxidation damage, and play an integral role in collagen synthesis. It is known that the lipid-rich stratum corneum (SC) is a highly resistant barrier to chemical agents penetrating into the skin. This report describes the first feasibility study of electroporation-mediated topical delivery (EMTD) of Asc for potential cosmetic applications. Both a cream formulation (20% Asc) and a crystal suspension (33% Asc) were applied respectively to human cadaver skin and fresh surgical skin. Six exponential pulses at 60 or 100 V and pulse lengths of 2.7-30 ms were selected. EMTD was more effective on fresh human skin than on human cadaver skin. For both skin models, EMTD with cream resulted in a greater enhancement of Vit. C penetration than with suspension. The distribution of electrical fields through the SC, epidermis, and dermis is demonstrated in computer simulation. Assuming that this fresh skin model and certain experimental conditions simulate projected in vivo applications, EMTD of Vit. C may represent an alternative method to ameliorate skin aging.
To determine the efficacy of topical ascorbic acid application in treating mild to moderate photodamage of facial skin using an objective, computer-assisted image analysis of skin surface topography and subjective clinical, photographic, and patient self-appraisal questionnaires. A 3-month, randomized, double-blind, vehicle-controlled study. Facial plastic surgery private practice. Nineteen evaluable volunteer sample patients aged between 36 and 72 years with Fitzpatrick skin types I, II, and III who were in good physical and mental health with mild to moderately photodamaged facial skin were considered for analysis. Coded, unmarked medications were randomly assigned to the left and right sides of each subject's face, one containing the active agent, topical ascorbic acid (Cellex-C high-potency serum; Cellex-C International, Toronto, Ontario), the other, the vehicle serum (Cellex-C International). Three drops (0.5 mL) of each formulation were applied daily to the randomly assigned hemifaces over the 3-month study period. Treatment assignments were not disclosed to subjects, clinicians, or personnel involved in analyzing skin replicas. Specific clinical parameters were evaluated and graded on a 0- to 9-point scale (0, none; 1-3, mild; 4-6, moderate; and 7-9, severe). Reference photographs were used to standardize grading criteria. Overall investigator scores were compared with baseline and graded as excellent (much improved), good (improved), fair (slightly improved), no change, or worse. Patient self-appraisal questionnaires rated the degree of improvement (much improved, improved, slightly improved, no change, or worse) and reported adverse effects (burning, stinging, redness, peeling, dryness, discoloration, itching, and rash). Standard photographs were taken at baseline, including anteroposterior and left and right oblique views to facilitate subsequent clinical evaluations, and at the end of therapy for comparison. Optical profilometry analysis was performed on the skin surface replicas of the lateral canthal (crow's feet) region, comparing baseline to end-of-study specimens. Using this computer-based system, the resulting image was digitally analyzed, and numeric values were assigned to reflect surface features. The parameters obtained included Rz, Ra, and shadows. These values provided objective data that document pretreatment and posttreatment texture changes proportional to the degree of wrinkling, roughness, and other surface irregularities. Optical profilometry image analysis demonstrated a statistically significant 73.7% improvement in the Ra and shadows north-south facial axis values with active treatment greater than vehicle control, as well as a trend for improvement in the Rz north-south facial axis parameter, showing a 68.4% greater improvement of active treatment vs vehicle control. Clinical assessment demonstrated significant improvement with active treatment greater than control for fine wrinkling, tactile roughness, coarse rhytids, skin laxity/tone, sallowness/yellowing, and overall features. Patient questionnaire results demonstrated statistically significant improvement overall, active treatment 84.2% greater than control. Photographic assessment demonstrated significant improvement, active treatment 57.9% greater than control. A 3-month daily regimen of topical ascorbic acid provided objective and subjective improvement in photodamaged facial skin. Skin replica optical profilometry is an objective method for quantification of the skin surface texture changes.
Percutaneous absorption of ascorbic acid is limited by its impermeability and instability. We attempted to improve the percutaneous absorption of ascorbic acid by use of iontophoresis after topical application of ascorbic acid. Radioactivities extracted from epidermal, dermal and blood compartments after topical application of [14C]ascorbic acid was measured in the presence or absence of iontophoresis. Autoradiography was also performed to study the histological distribution of the radioactivity of ascorbic acid. Iontophoresis greatly enhanced percutaneous absorption of [14C]ascorbic acid in the rat skin. Radioactive ascorbic acid in the dermis reached a maximum level at 1 h after application whereas, in the topical application method, the uptake of ascorbic acid in both epidermis and dermis was quite low. Autoradiography of skin specimens indicated that iontophoresis accelerated the absorption of ascorbic acid through both transepidermal and pilo-sebaceous routes. Iontophoretic delivery system of ascorbic acid may provide a more efficient tool for its percutaneous absorption than a simple topical application.
The objective of this study was to evaluate the ability of lasers and microdermabrasion, both of which are skin resurfacing modalities, to enhance and control the in vitro skin permeation and deposition of vitamin C. The topical delivery of magnesium ascorbyl phosphate, the pro-drug of vitamin C, was also examined in this study. All resurfacing techniques evaluated produced significant increases in the topical delivery of vitamin C across and/or into the skin. The erbium:yttrium-aluminum-garnet (Er:YAG) laser showed the greatest enhancement of skin permeation of vitamin C among the modalities tested. The laser fluence and spot size were found to play important parts in controlling drug absorption. An excellent correlation was observed in the Er:YAG laser fluence and transepidermal water loss, which is an estimation of skin disruption. Permeation of magnesium ascorbyl phosphate was not enhanced by the Er:YAG laser. The CO2 laser at a lower fluence promoted vitamin C permeation with no ablation of the stratum corneum or epidermal layers. Further enhancement was observed with the CO2 laser at higher fluences, which was accompanied by a prominent ablation effect. Microdermabrasion ablated the stratum corneum layers with minimal disruption of the skin barrier properties according to transepidermal water loss levels. The flux and skin deposition of vitamin C across microdermabrasion-treated skin was approximately 20-fold higher than that across intact skin. The techniques used in this study may be useful for basic and clinical investigations of enhancement of topical vitamin C delivery.
To enhance skin permeation of ascorbyl palmitate (AsP), it was encapsulated in liposomes, and formulated into liposomal hydrogel (lipogel) by dispersing the liposome into poloxamer hydrogel matrix. To improve the skin permeation of AsP, we applied electric current supplying system that mimics an electric skin massager. We evaluated the effects of composition and surface charge of the liposomes and electrical assistance on the skin permeation of AsP. In the passive transport study, the permeated amounts of AsP from all the lipogels tested were higher than that of control hydrogel which contains Transcutol used to solubilize AsP. In the cathodal delivery condition with a fixed cathodal current of 0.4 mA/cm2, the skin permeation characteristics of the negative lipogels were superior to that obtained with the neutral lipogels and the drug permeation was more increased with increased surface negative charge of the liposomes. In conclusion, the lipogel system was thought as a helpful drug delivery system to enhance skin permeation of AsP. Combined use of negative lipogel with cathodal electric assistance was found to be promising in enhancing the skin delivery of AsP.