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Vitamin C in dermatology

April 2013
Indian Dermatology Online Journal 4(2):143-6

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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.

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Indian Dermatology Online Journal -

April-June 2013

Volume 4

Issue 2

143

Address for

correspondence:

Dr. Saokar Pumori Telang,

Embellish, the Skin and

Laser Clinic, 1stoor

Sangam Project, Opp Air

Indiaofce,atSangam

Ghat, Wellesley Road,

Pune, Maharashtra,

India.

E‑mail: drpumori@

gmail.com

Drug Prole

Consultant

Dermatologist, Joshi

Hospital Maharashtra

Medical Foundation,

Jehangir Hospital,

Apollo Group, Pune,

Maharashtra, India

ABSTRACT

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, L‑ascorbic acid, photo‑ageing, Vitamin C

INTRODUCTION

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]

BIOCHEMISTRY OF VITAMIN C

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.

MECHANISM OF ACTION OF

VITAMIN C WITH REFERENCE

TO DERMATOLOGY

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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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

expression.[2]

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]

TOPICAL FORMULATIONS OF VITAMIN C

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

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April-June 2013

Volume 4

Issue 2

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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.

ADVERSE REACTIONS OF TOPICAL

VITAMIN C

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]

FUTURE DEVELOPMENTS

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]

CONCLUSION

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.

REFERENCES

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

1999;125:1091‑8.

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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146 Indian Dermatology Online Journal-

April-June 2013

Volume 4

Issue 2

4. Wikepedia: [Home Page] Vitamin C: History, Discovery and Sources in

Available from: http://en.wikipedia.org/wiki/Vitamin_C [Last Accessed

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

2001;27:137‑42.

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

microdermabrasion enhance and control topical delivery of Vit C.

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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Feb 2001
DERMATOL SURG

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.

Temperature-Sensitive Microemulsion Gel: An Effective Topical Delivery System for Simultaneous Delivery of Vitamins C and E

Article

Full-text available

Feb 2009
AAPS PHARMSCITECH

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.

Skin penetration and retention of L-Ascorbic acid 2-phosphate using multilamellar vesicles

Article

Full-text available

Jan 2009

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.

Topical L‐ascorbic acid: percutaneous absorption studies

Article

Jan 2001

Permeation Enhancement of Ascorbic Acid by Self-Dissolving Micropile Array Tip through Rat Skin

Article

Apr 2010
CHEM PHARM BULL

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.

Electroporation-mediated topical delivery of vitamin C for cosmetic application

Article

Jun 1999
Bioelectrochem Bioenerg

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.

Use of Topical Ascorbic Acid and Its Effects on Photodamaged Skin Topography

Article

Nov 1999
ARCH OTOLARYNGOL

Steven S. Traikovich

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.

Iontophoresis promotes percutaneous absorption of L-ascorbic acid in rat skin

Article

Oct 2003
J DERMATOL SCI

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.

Lasers and Microdermabrasion Enhance and Control Topical Delivery of Vitamin C

Article

Dec 2003

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.

Skin Permeation Enhancement of Ascorbyl Palmitate by Liposomal Hydrogel (Lipogel) Formulation and Electrical Assistance

Article

Mar 2007

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.