Kiriiri Geoffrey

University Of Nairobi ,School of Pharmacy

Objectives
 Define sunscreens and the scientific of UV rays
 Reasons for using sunscreens
 Detail the various formulation of sunscreens available
 Determination of the efficacy parameters
 Regulatory requirements for sunscreens
Sunscreens
 These are formulations applied onto the skin surface to
protect against detrimental changes arising from the
exposure to ultra violet rays.
 Repeated exposure to sunlight causes sunburns, loss of
elasticity and wrinkling of the skin.(photoaging)
 Ultra violet rays have been associated with increased
incidence of melanomas
 Main cause of sunburns is UVB ,effects are acute and
present with pain and erythema.
 UVA causes delayed effects including wrinkling, elasticity
loss and melanomas.
Ultraviolet Rays
 They form part of the visible light.
 UV spans of wavelength 200-400nm, UVC(180nm>), UVA(200-
320nm), UVA( 320-400nm)
 The UVC section of the band is not significant as the waves are
filtered out by the ozone layer in the stratosphere.
 UVB triggers production of melanin pigment and stimulates
epidermal thickening resulting in a permanent skin tan.
 UVA stimulates melanin already on the skin to produce short
term tans. It however penetrates much deeper into the skin
causing long term skin damage including mutations that
precede cancers as well as skin aging.
 The mutations result from DNA damage by free radicals
produced when molecules on the skin surface are irradiated
Effects of UV rays
Observable effects of sunrays
 Sun burns
 Erythema
 Loss of elasticity( loose or hanging skin)
 Increased wrinkling
 Melanomas in the long term
Determinants of extent of skin
damage
 Skin colour- Light skinned individuals are more
susceptible to UV induced skin damage compared to
those who are dark skinned .
 Duration of exposure- The longer the exposure to
sunlight the higher the magnitude of damage
 Age- Children are more susceptible as their skins are
undeveloped ( thin Stratum corneum)
 Health status- Persons with existing skin disorders are
more susceptible
 Behavioral factors; Sun bathing, Tanning, Light
clothing
History and modern use of
sunscreens
 Awareness of the damaging effects of the sunrays dates
to prehistoric days. Egyptians, Greeks, chinese and
Indians
 Evidence of use include writings, wall carvings.
 Modern use and production began in the early 1900’s
coinciding with the scientific description of UV
spectrum.
 Earliest formulations were reported in USA(1928),
PABA followed by Australia in 1934
 More formulations became available after 1950s’
Classification
 Based on mechanism of action
 Chemical sunscreens: They absorb UV rays and
converting it into heat energy that is reflected away
from the skin.
 Mineral sunscreens: They form an occlusive barrier
that blocks, reflects or scatters the UV light
 Classification based on mode of administration;
Topical & Systemic
 Sun protection factor: UVA, UVB, Broad spectrum
Organic sunscreens
 These are organic chemical derived from natural sources
and synthesis
 Are further classified depending on the UV spectrum in
which they afford the best protection.
 UVB protectants;
 PABA derivatives-
 Cinnamates- Octisalate, Homosalate, Trolamine salicylate
 Octocrylene
 Ensulizole
 Ethylhexyl triazone
UVA Filters
 Benzophenones- e.g Oxybenzone,
Sulibenzone,Dioxybenzone
 Avobenzone
 Meradimate
 Bidisulizone disodium
 Diethylaminohydroxyl benzoyl hexyhydrate
 Ecanisole
 Methylacralinate
Broad Spectrum sunscreen
They afford protection against both UVA and UVB
 Ecamsule
 Silatriazole
 Bemotrizinol
 Besotricozole
Inorganic Sunscreens
 Main constituents- Zinc oxide, Titanium oxide
 Others
 Talc
 Iron oxide
 Red veterinary petrolatum
 Kaolin
 Calamine
 Ichthamol
Systemic sunscreens
 These are taken orally and are absorbed systemically to
afford protection. The act as antioxidants to scavenge
radicals from the skin . Include
 β- carotene, α- tocopherol, ascorbic acid,
antimalarials( quinolines), Retinol, Selenium, green
tea polyphenols, PABA, Antihistamines ,Aspirin,
Indomethacin, Corticosteroids
Mechanism of action of sunscreens
 Inorganic sunscreens
 Afford skin protection by scattering and reflection of
UV energy from the skin surface
 Organic Sunscreens
 Absorption of the UV energy by converting it to heat
energy thus reducing its harmful effects and reduce
the depth through which it can penetrate the skin.
Features of an ideal sunscreen
 Chemical properties
 Chemically inert
 Non irritating
 Photo stable
 Compatible with other ingredients and formulation
excipients
 Soluble in appropriate solvents vehicles
 Non odorous
Ideal features of sunscreen
 Physical;
 Non viscous to promote good spreadability
 Aesthetically appealing to promote usage
 Small particle size
 Waterproof
 Appropriate solubility in either aqueous or organic
solvents
Ideal characteristics cont’
 Functional attributes
 Should afford protection against UV across a wider
range of wavelength
 Limited systemic absorption through the skin to
minimize sensitization.

 Others
 Readily available
 Inexpensive
 Contaminant and microbe free
Other considerations
 Convenience to the user
 Patentability
 Regulatory considerations
 Special requirements for different target populations
Formulation
 Sunscreens can be formulated as ;
 Gels
 Ointments
 Lotions
 Sprays
 Sticks
 Powders
Formulation
 Traditionally Inorganic sunscreens were formulated as
creams that were sticky and unpleasant.
 Nanomization and micronization has allowed them to
be formulated as pastes, emulsions and ointments
 The aesthetic value is important to promote use.
Formulation
 Various sunscreens are usually combined in formulation
to afford higher photo protection
 They can also be included in other formulations such as
makeup, bathing soap, hand sanitizers, and
moisturizers
 Suitable propellants are used in the case where the
sunscreen is intended for use as a spray.(CFC, HC
HCFC)
 Emulsifying agents ( Eg.Agar, alginates, glycerol),
Other excipients
 Surfactants
 Buffering agents
 Preservatives
 Suspending agents
 Moisturizers
Quality Control measures
 Physical analysis. Includes organoleptic tests to check the
appearance and feel of the product
 Stability tests; Colour, phase separation and liquefaction.
There should be no colour changes nor separation of
phases in sunscreen formulations in the stability tests if
they are to pass the quality tests. The absence of
liquefaction provides strong evidence for the stability of
the emulsions.
 PH determination over time The PH value of sunscreen
stored at different conditions is determined using a digital
pH Meter. The pH tests are repeated for multiple emulsions
or formulations after a defined period of storage
Quality Control cont’
 Determination of SPF in vitro using
spectrophotometry
 Level of water resistance for UVB: This test is
conducted by immersion of a subject in a pool or spa
for 40 minutes with a five minute rest in between(20-
5-20). A sunscreen is considered to be water resistant if
it retains no less than 50% of its SPF following
immersion.
Quality control cont’
 Microbiological stability For streptococcus aureus,
psuedomonas aeroginosa, yeast and mould.
Sunscreens like other topical formulations must be
free from any microbial contamination that may
render them deleterious to the users.
Measurement of photoprotection
1)Sun protection factor; refers to the ability of the
sunscreen to prevent development of erythema upon
exposure to UVB radiation
 SPF = MED of protected skin/MED of unprotected skin
(MED = minimal erythemal dose)
 Application 2mg/cmsq
 Grading
 Low: SPF 2 - 15
 Medium: SPF 15 - 30
 High: SPF 30 - 50
 Highest: SPF >50
Examples
Measurement of Photoprotection
2)Persistent pigment darkening.
 This measures establishes the ability of the sunscreen
to protect against UVA light. The method is similar to
that of establishing SPF Where the erythemic dose in a
healthy subject covered with the sunscreen is
compared to that obtained without using the
sunscreen
Measurement of photoprotection
 3. Immune Protection Factor
 Ability of sunscreen products to prevent UV-induced
immunosuppression.
 IPF is considered to correlate better with the UVA-
protectiveness of a sunscreen than with its SPF
 4) Clothing Factor
 Fabric SPF is similar to SPF, except that fabric is used
to protect the skin while testing, instead of a
sunscreen.
Regulatory control
 Regulation of sunscreen is variable across different
jurisdictions.
 In the USA, they are considered as OTC drugs
 In European union and Japan sunscreens are
considered to be cosmetics.
 In Australia they are considered therapeutic goods
and regulated as such.
 Regulation in other countries in not well defined, most
countries follow the USA or EU guidelines.
Labelling requirements
 Label must include
 Manufacturers name and physical address
 List of ingredients in order of predominance from the
highest
 Indication of the SPF
 Optimal storage conditions
 Cautionary information for patients who may be
allergic to any of the ingredients
Challenges
 Documented sensitivity to sunscreens
 Some orgnanic sunscreens are absorbed through the
skin resulting in systemic effects
 Association with cancer induction especially when
kaolin and talc is sourced from unverified sources(
contamination with asbestos)
 Inappropriate application methods that render the
sunscreens ineffective
References
 WHO
 FDA website
 EMA website
 Australia therapeutic drug agency website
 Dermatological association of Brazil