Design of cosmeceutical products: Sun protection, Sunscreens Classification and Regulatory

aspects

INTRODUCTION :

 The UV radiation reaching the Earth’s surface is largely composed of UVA

(approximately 95%) with a small UVB component (approximately 5%)
 All UVC and approximately 90% of UVB radiation are absorbed by ozone, water vapor,
oxygen, and carbondioxide

Sunlight reaching the surface of the earth contains :

 Ultra-violet rays
 Visible rays
 Infra-red rays

UV Rays (particularly wave-length below 320mµ) are responsible for most of the
therapeutic as well as noxious effects that we attribute to sun-light.

Sun exposure & SKIN – DAMAGE

 Sun exposure can lead to reddening, irritation, and eventually tanning

 possible cause of premature wrinkling and various types of skin cancer
 Sun protection has become a very important issue today.

SKIN – DAMAGE :
The UV Spectrum is broken into three parts:
 Very High Energy (UVC)
 High Energy (UVB)
 Low Energy (UVA)
 Visible and IR radiation don’t harm the skin.
 Very High Energy (UVC) ranges from 100 to 280 nm and is blocked out by the ozone
layer
 High Energy (UVB) ranges from 280 to 320 nm mainly penetrate the superficial skin
layers, i.e., epidermis causes sunburn, redness and also contributes to photoaging,
tanning and immunosuppressive effects.
 Advantageous effect of the UVB radiation is that it is responsible for the synthesis of
vitamin D in the skin
 Low Energy (UVA) ranges from 320 to 400 nm can penetrate deeper into the skin, down
to the dermis (Figure 3.24) further subdivided into
 UVA II (320–340 nm) and
 UVA I (340–400 nm).
 radiation leads to skin tanning

Difference between UVA and UVB

 “A” (UVA) as standing for aging and “B” (UVB) as standing for burning. Both UV
radiations can cause skin cancer.
 UVA has the same damaging effect in the morning or in late afternoon and during
winter or summers
 UVA can penetrate glass and UVB can not.
 UVC radiation is recognized as the most carcinogenic. Fortunately, almost all UVC
radiation approaching the Earth is filtered out by the protective ozone layer.
 The only source of UVC on the surface of Earth is germicidal lamps, which are used to kill
germs on surfaces or in the air.
 WHY USE SUN-SCREEN?

Too much unprotected sun exposure leads to:

 Premature skin ageing
 Sun-burn
 Skin-Cancer

Sunscreen: Definition

 Sunscreen also known as sunblock or suntan lotion is a lotion, spray, gel or other topical
product that absorbs or reflects the sun's ultraviolet (UV) radiation and protects the
skin.

PRINCIPLE OF EFFECTIVENESS OF SUN SCREENS

 A protective layer can be provided to the skin that prevents the UV-rays to reach the
skin either by absorbing or by reflecting them.
 Zinc oxide and titanium dioxide both have such tendency.
 Preparations reflecting UV-rays are very effective and used widely.

IDEAL SUN-SCREEN CHARACTERS

 Provide protection against both UVB and UVA radiation
 Absorb light preferentially over the range of 280 - 320mµ.
 Resistance to water
 Be stable to heat, light and perspiration.
 Preferably odorless, if mild odor: accepted by user.
 Be non-toxic, non-irritant, non- sensitizing
 Capable of retaining sunscreening property for several hours.
 Stable under condition of use.
 Non-stain
 Not be rapidly absorbed.
 Be neutral.
 Be rapidly soluble in suitable vehicles.

Sunscreen ingredients
 UV filters
 Additional ingredients in sunscreen products are listed as inactive ingredients
UV Filters : Classification
Classified into two groups based on their mechanism of action:
 Physical Sunscreens
 Chemical Sunscreens
 A single product usually contains more than one active ingredient, both physical and
chemical filters, to achieve the desired SPF value and broad-spectrum protection.

Physical sunscreens/ Inorganic UV Filters

 also known as inorganic UV filters,

 reflect and scatter UV radiation
 The two approved physical filters are titanium dioxide (TiO2) and zinc oxide (ZnO).
 Both of these ingredients are white powders that are insoluble in the sunscreen product
base therefore are suspended in such products.
 SUNSCREEN CLASSIFICATIONS
 Physical
 Opaque formulations containing:
 titanium dioxide
 talc, kaolin
 zinc oxide
 ferric chloride
 icthyol, red petrolatum
 Mechanism: scatters or reflects UV radiation due to large particle size

Physical sunscreens/ Inorganic UV Filters

 They can only penetrate the outer layer of the skin therefore, they have an excellent
safety
 They are photostable, independent of the sunscreen base and other ingredients
 provide a broad-spectrum protection since they reflect and scatter both UVA and UVB
radiations
 TiO2offers UVB and UVA II protection, while
 ZnOprovides protection against UVB, UVA II, and UVA I radiations

Physical sunscreens/ Inorganic UV Filters: Disadvantage

 They reflect and scatter UV radiation into the visible spectrum (>400 nm), which provide
a white appearance on the skin after application and therefore cosmetically less
appealing
 Today, TiO2 and ZnO are commonly used in micronized (1–100 μm) and nanonized (1
100 nm) forms for an aesthetically more appealing cosmetic look.
 Sunscreen Products contain nanoparticles no longer reflect visible light and, therefore,
do not appear white but transparent on the skin.

Chemical sunscreens/ Organic UV filters

 Also known as organic UV filters that are aromatic compounds.

 Their molecular structure is responsible for absorbing UV energy.
 They absorb UV rays, which produce excitation of the sunscreen chemical to a higher
energy state. Then, they return to the ground state and convert the absorbed energy
into longer, lower energy wavelengths (heat)
 SUNSCREEN CLASSIFICATIONS

 Chemical
 Formulations containing one or more:
 PABA, PABA esters
 Benzophenones
 Cinnamates
 Salicylates
 Digalloyltrioleate
 Anthranilates
 Mechanism: absorbs UV radiation

Chemical sunscreens/Organic UV filters

 15 organic sunscreen ingredients approved in the US.
 Examples for organic UVB absorbing filters include octinoxate, octisalate, and padimate
O.
 Examples for organic UVA filters include avobenzone, oxybenzone & meradimate.
 Organic filters are often combined with one another to achieve the desired broad-
spectrum protection.

Chemical sunscreens/Organic UV filters Disadvantage

 Organic sunscreens can penetrate the skin due to their lipophilic nature, which may
cause safety issues
 issues with photostability.Upon exposure to UVradiation, the structure of UVfilters may
be negatively affected and/or destructed. They lose their absorption capacity.
 Therefore, most formulations contain photostabilizers

Additional Ingredients of Sunscreens

Inactive ingredients generally found in sunscreen products depend on the dosage form.

 Waterproofing agents
 Photostabilizers
 Emollients
 Water
 Emulsifiers
 Thickeners
 Film-forming ingredients
 Antioxidants
 Preservatives
 Humectants
 Chelating agents
 Propellants

Sunscreen Products
 O/W or W/O emulsions
 anhydrous systems, such as ointments, sticks, oils, and
 silicone-based aerosols
 wipes; and gels
 Sun Protection Factor (SPF)

 was adopted by the FDA to describe the effectiveness of sunscreens.

 SPF is a measure that indicates how long it takes for UV rays to redden protected skin
(i.e., skin with a sunscreen) compared to unprotected skin (i.e., skin without a
sunscreen).
 The concentration and combination of UV filters determine the efficacy of sunscreens as
measured by Sun Protection Factor (SPF)

Sun Protection Factor (SPF)

 As the SPF value increases, sunburn protection increases.

 The effectiveness of a given SPF is measured in terms of redness (medically termed
“erythema”) that appears on the skin after sun exposure
 The amount of UV energy required to produce the first visible redness on the skin is
referred to as the minimal erythema dose (referred to as “MED”).
 As SPF values are determined from the test that measures protection against sunburn
caused by UVB radiation, SPF values only indicate a sunscreen’s UVB protection

SUNSCREENS :
 Sun Protection Factor(SPF) = MED of PhotoprotectedSkin
------------------------------------
MED of Unprotected Skin
 MED is minimum dose of radiation which produces erythema
 SPFs are determined indoors using xenon lamps which approximate the spectral quality
of UV radiation

How to determine SPF

 In a controlled indoor laboratory eliminating any effects of environmental change, e.g.,

wind, heat and cold, untanned test subjects are put through a two day test.
 On the first day, the lower back is protected except for the test site and exposed to UVB
light until mildly red.
 On the second day, a sunscreen is applied to a new test site and exposed to UVB light
until the same mild redness occurs.
 The amount of time to achieve redness with the applied sunscreen determines the SPF.
As people vary so will the sun protection of products…results vary with individuals.

SUNSCREENS

 Factors which influence effectiveness of SPFs

 Difference in skin types.
 Thickness of the applied sunscreen.
 Time of day.
 Altitude: each 1,000 ft increase adds 4% to the intensity of erythema producing UV
radiation; thus intensity is about 20% greater in Pocatello than at sea level.
 Environment: snow/white surfaces reflect 70-90%, and when directly overhead water
reflects nearly 100% of UVR.
 Vehicle: determines skin penetration of sunscreen.

Skin Types Based on Sensitivity to Ultraviolet Light (skin phototype)

 Fitzpatrick classified skin (1975) based on how the skin behaves to UV radiation
exposure
 It correlates the skin color (i.e., its melanin content) with its ability to tan or burn with
UV light exposure. It has six categories
 SUNSCREENS

SUNCREEN AGENTS
PABA (Para-aminobenzoic acid)

 Very effective in the UVB range (200-320 nm).

 Most effective in conc of 5% in 70% ethanol.
 Maximum benefit when applied 60 min prior to exposure (to ensure penetration and
binding to stratum corneum).
 Does NOT prevent drug/chemical-induced photosensitivity rxn.
 Contact dermatitis can develop.
 May produce transient drying/stinging from alcohol content (may be alleviated by
adding 10-20% glycerol).
 May stain clothing.

SUNCREEN AGENTS
PABA Esters (Padimate A, Padimate O, Glyceryl PABA)
 Also very effective in UVB range (280-320)
 Most effective in conc. 2.5-8% in 65% alcohol
 May penetrate less effectively than PABA
 Similar application and adverse effect
 Less staining

SUNCREEN AGENTS
 Benzophenones (oxybenzone, dioxybenzone, sulisobensone)
 Slightly less effective than PABA.
 Absorbs from 250-400 nm spectrum
 Combined , UVA & UVB). with PABA or PABA ester improves penetration and is superior
to either agent used alone (200-400 nm wavelength coverage).
 Beneficial in preventing photosensitivity rxns.
 Contact dermatitis is rare.

SUNCREEN AGENTS

Cinnamates and Salicylates

 Minimally effective, absorb UVB spectrum.
 Generally used in combination with one of the above.
 Minimally effective, absorbs UVA spectrum 250-322 nm.
 Usually combined with UVB agent to broaden spectrum.

Regulatory aspects

 Sunscreen chemicals and products are regulated as cosmetic or drug depending upon
the regulation of the country in which it is manufactured.
 Adverse effects due to sunscreen chemicals are of concern all over the world.
 Variation in the regulation affects the safetyassessment of UV filters and its products
 The list of substances classified as UV filters and the maximum allowable concentration
are established by each country,
 for example, European Union (EU), United States of America (USA), Australia, Canada,
ASEAN and India. UV filters approved in India and other nations are
 summarised as Table I.
 In the EU, sunscreen chemicals (UV filters) are classified as cosmetics
 In the USA, sun products are classified as over-the-counter drugs, a class for which it is
necessary to indicate active ingredients demonstrated to be effective and safe.
Production and marketing of these products is regulated by US FDA monographs
published in the Federal Register.
 In Canada, Sunscreen products are classified as prescription drugs and must meet the
requirements set out in Canada's Food and Drugs Act before they may be imported,
advertised, or sold in Canada. Sunscreens are classified as natural health products
(NHPs) if they contain ingredients like titanium oxide, zinc oxide and para amino benzoic
acid.. Sunscreens are classified as drugs if they contain at least one ingredient from
Avobenzon.
 In India, Bureau of Indian Standards (BIS) has listed permitted UV filters which cosmetic
products may contain