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Topical Agents
Definition
• Topical : Place the use of these drugs or
compounds on the surface
• Ex: Antiseptic
• Systemic: The drugs are absorbed into
circulatory system and distributed to various
organs or tissues.
Types of inorganic topical agents
• The compounds used topically will be divided
into broad categories based on their usual
action or uses.
• There are TWO types:
• 1- Protective agents.
• 2- Antimicrobial agents.
Protective agents
• Are substances which may be applied to skin
to protect certain areas from irritation.
• Properties of protective agents are insoluble
in water ( H2O), and chemically inert (
unreactive), in order to prevent interactions
between the protective substance and the
tissue.
• Also, small fine partials(large surface area).
Classification of protective agents
• 1- Dusting powders.
• 2-Suspensions.
• 3- Ointments
Talc
• MgO.4SiO2.H2O
• Hydrous magnesium silicate, very fine white
powder, smoothly, greasy feeling to the touch(
soapstone).
• Talc is characterized as fine powder ( 80/100)
mesh particle size, odorless, insoluble in water
,dil HCl, bases.
Uses of Talc
• 1- It is useful in lubricating, protective dusting,
• Can be prevent any friction.
• 2-Used for wound & surgical incision because
can produce sterile abscesses
• 3- Used in medical gloves.( plastic disposable)
• 4- Used in cosmetic may be perfumed
• Medical Talc by mixing boric acid with talc as
antimicrobial agents.
Zinc Oxide
• The chemical formula for Zinc oxide is ZnO
• Is a very fine, oderless, amorphous , white or
fait yellow powdwer, can heated 400-500 ∙C
• Zno is insoluble in water, alcohol, but react
with dil HCl
• ZnO + HCl --------- ZnCl2 + H2O
Uses of Zinc Oxide
• 1- Is a mild astringent and weak antimicrobial
agents. Used as powder, ointments to protect
the skin.
• 2- Dusting powder used in the treatment of
skin ulceration & other dermatological
problems.
• Medicated zinc oxide by mixing with boric acid
as antimicrobial agents.
Calamine
• The formula is ZnO.xFe2O3
• Can be synthesized by mixing ZnO with ferric
oxide.
• It is a fine powder, water insoluble, alcohols
,adhering to the skin.
Uses of Calamine
• Calamine can be used as topical protective
agent.
• 1- It is USP product used as dust powder,
calamine lotion ( applied to skin )pink color.
• Calamine is applied to the skin for its
adsorbent, protective properties, used in
dermatological problems.
• The calamine lotion contain ZnO and ferric
oxide equally mixed Bentonite magma in the
solution of Calcium hydroxide.
• Phenolated calamine lotion( USP ) contains 1%
liquid which provide a local anesthetic and
anti- itching action.
Titanium Dioxide
• TiO2 as topical protective agent, it is
characterized by off white powder color,
tasteless, odorless. A 1 to 10 aqueous suspension
of the solution is neutral to litmus paper.
• It is insoluble in water , HCl. HNO3, dil H2SO4.
• It is soluble in HF, Conc. H2SO4.Also, in H2O2
• TiO2 + H2O2 -------• Tritium dioxide
TiO3
Titanium trioxide
Uses of TiO2
• TiO2 is a protective agent, topically, used as
Sun screen light ( UV light radiation) due to its
highly refractive index.
• Many pharmaceutical preparation as TiO2
cream, 5, 10, ..25% ointments.
• Other organic sun screen agent p- aminobenzoic acid ( PABA).
• TiO2 used in cosmetic and paints.
Aluminum
• Aluminum ( Al ) is a silver- white metal as
protective agents , highly affinity to O2
forming Al2O3as protective layer.
• It is insoluble in water, alcohols, and
uncreative towards HNO3,H2SO4
• It react rapidly with dil HCl
• HCl + Al ------ AlCl3. 6H2O
• Aluminum, paste ( ZnO with base ) used for
prevent irritation.
Silicon Polymer
• There are inert protective substances
occurring in liquid form known as Silicon oils;
e.g.dimethyl silicon ( Dimethicon,or
Simethicone )
•
CH3
CH3
CH3
• CH3 Si-O- ( - Si - O ) ------Si - CH3
•
CH3
CH3
CH3
• Very well adhere to skin, but not wound, be
avoided contact to the eyes.
Topical Agents
3rd Year Pharmacy
2016 - 2017
Outline
• Classification a- protective b- antimicrobial agents
• A- protective products
• Talc , Zinc oxide ZnO, Calamine, Titinum oxide TiO2,
Al products& silicon polymer
• Antimicrobials
• Mechanism 1-oxidation H2O2,ZnO,KMnO4, Iodine
• 2- Halogenations NaOCl
• 3- protein ppt AgNO3.
Protective Agents
• Protective
• Any agent that isolates the exposed surface
from harmful or annoying stimuli
• Properties of protective agents:
• Insoluble in water
Chemical Inertness
Adsorbent
• Deeper penetration of topical agents are also seen in
many cases which are beneficial. (Penetration of
antiseptics into the tissue
• below the skin prevents the possibility of deeper in
fections-)
•
Protective Agents
Talc
• Talc (Mg3Si4O10(OH)2
• protective: native hydrous magnesium silicate,
common name and chemical formula.
• Soapstone can be grinding in 80/100 mesh particle
size.
• As grease touch., insoluble in water,
• Uses as protective agents , as lubricants and
in pharmaceuticals, as cosmetics, ceramics, for
plastic cloves,
Zinc Oxide ( ZnO )
• White or fait yellow color powder, insoluble in water.
Other formulation as Zinc Oxide ointment for adult,
& Zinc Oxide in Glycerin for children.
• Dusting powder, used astringent and protective
topical agent, mild antiseptic, used in the acne
preparation, eczema,& psoriasis
• It is usually used in the manufacture of plasters.
Calamine ZnO and Fe2O3
• It used as dusting powder, lotions, ointments,
as smoothing agents, for sunburn, eczema,
urticaria. Calamine lotion is very popular.
Boric Acid H3BO3
• Is a weak acid, used as antiseptic, and as
chemical precursor for many reactions.
• Uses:
• 1- Antiseptic
• 2- dilute solution for eye wash
• 3-Acne
• 4- Vaginal douche against bacteria.
• 5-It used as protective against athlete foot.
Titanium dioxide TiO2
• Topical protective agents as cream is used
against sunscreen to protect the skin aganist
ultra-violet light ( U.V.).
• The organic topical protective agents is
• P-aminobenzoic acid ( PABA) .
Antimicrobial Agents
• Antiseptic:
• Any agent which kills or inhibits the growth of
microorganisms found in living tissue.
• Disinfectant:
• Any agent which kills or inhibits the growth of
microorganisms found in inanimate objects.
• Germicide:
• General term for fungicide, bactericide, amoebicide
Mechanisms of action of antimicrobials
• There are THREE proposal mechanisms:
• 1-Oxidation
2-Halogenation
Protein Precipitation3-
Oxidation
cell membrane of bacteria
• SH
SH
S---S
Halogenation the protein of the cell
membrain
• H2N CHR CO NH CHR1--(HOCl)
NaOCl
H2NCHRCONCl CHR!...
Protein pption that kill the microbe
• H2NCHR1CONHCHR2---• AgNO3
• H2NCHR1CONHCHR2--•
•
Ag
Hydrogen Peroxide H2O2
• liquid not store in glass bottles because it
decompose ,it store in white plastic container,
keep in cold dark place to prevent
decomposition.
• There are many uses :
• 1- Antiseptic for wash wound , teeth and ear
• 2-Bleaching color ( hair ).
• 3- Laundry for cloths.
• Sodium Perborate
• Antimicrobial :
Composite of H2O2, NaBO2 and NaOH
Used as bleaching agent in non-chlorine
laundry bleaches
Potassium Permanganate KMnO4
• Chemically is a strong oxidizing agent, solid
purple crystalline , odorless.
• Store in well closed container.
• Uses:
• 1- Oxidizing agent for skin disease in different
concentrations 1: 5000, 1:15000
• 2- used in swimming pool for athlete foot.
• 3- Strong oxidizing for many organic reactions.
Iodine I2
• It is dark violet ,insoluble in water , but the
• I2 + KI = I3 – Complex soluble in water as iodine solution,
soluble in alcohol known as tincture iodine
• Iodine solution weak solution ( 25g I2 + 25g KI ) in 100ml
• And strong solution ( 50g I2 + 50g KI ) in 100 ml.
• Iodine preparations and compounds
• Antimicrobial property due to oxidation and Iodination
disinfectants
• A chemical reagents in analytical reagent.
• In drug synthesis.
• In Povidin iodine as new product.
Povidone Iodine ( PVP – I)
• is a stable chemical complex of poly vinyl
pyrrolidine iodide. It is broad spectrum
antiseptic for wounds. It is used disinfectant .
2- Halogenation
• Dakin's Solution
• Sodium hypochlorite solution, (usp)
Contains 4-6% of NaOCl,
• It is made from bleach that has been diluted
and treated to decrease irritation. Chlorine,
the active ingredient in Dakin's solution, is a
strong antiseptic that kills most forms of
bacteria and viruses. .
3- Protein ppt (Silver Nitrate AgNO3)
• Prepare as 1% AgNO3 , protective from light
due to oxidation. Effective against gonococcal
organism.
• Antimicrobial activity of these compounds is
due to protein precipitant action.
• 1% used eye newborn babies.