Implantable Preparation

Skin

• largest of the body organs

• an average adult’s skin has a surface area of about 2
m2
• heaviest organ of the body
• for local, regional, or systemic effects.
 Drug Effects

Drug are applied to the skin to elicit one or more of four general
effects:
• an effect on the skin surface
• an effect within the stratum corneum
• a more deep-seated effect requiring penetration into the
epidermis and dermis
• a systemic effect resulting from delivery of sufficient drug through
the epidermis and the dermis to vasculature to produce
therapeutic systemic concentrations.
 Implants

• solid dosage forms which are inserted under the skin by a

small surgical incision.
• used for hormone replacement therapy
• implant containing a progestogen has been developed for
use as a contraceptive.
• slow and long-term therapy
• contraceptive implant the effect continues up to 5 years.
• A testosterone implant used in the treatment of male
hypogonadism will maintain adequate hormone levels in the
patient for 4-5 months. Implants must be sterile.
• most commonly use for parenteral administration over a
significantly prolonged period of time.
• Norplant (Wyeth-Ayerst) is a commercially available
levonorgestestrel implant system, indicated for the
preventions of pregnancy for as long as 5 years.
Transdermal drug delivery
system
 Transdermal Drug Delivery System

Transdermal Patches
• stratum corneum, presents a barrier to most drug absorption, it
provides a large (1-2 m2)
• accessible surface area for drug diffusion.
• transdermal administration, as compared to other routes, is fairly
noninvasive.
• quite willing to accept the use of simple-looking “patch” as it can
be conveniently applied and removed.
• A transdermal patch or skin patch is a medicated adhesive
patch that is placed on the skin to deliver a time released
dose of medication through the skin and into the
bloodstream.
• A wide variety of pharmaceuticals can be delivered by
transdermal patches. The first commercially available
prescription patch was approved by the U.S. Food and Drug
Administration in December 1979, which administered
scopolamine for motion sickness.
 Current transdermal patches can be classified into four types:

1. Membrane-modulated system represented by Transderm-Scop (Scopolamine, Novartis)

• drug reservoir is totally encapsulated in a shallow compartment molded from a drug-
impermeable backing and a rate-controlling polymeric membrane.
• The drug molecules are released only through the rate-controlling polymeric
membrane.
• The rate-limiting membrane can be microporous or nonporous.
• external surface of the membrane, a thin layer if drug-compatible, hypoallergenic,
adhesive polymer (e.g. silicone or polyacrylate adhesive) may be applied to achieve
intimate contact of the transdermal system with the skin.
• The rate of drug release from this type of drug-delivery
system can be tailored by varying the polymer composition,
permeability coefficient, or thickness of the rate-limiting
membrane and adhesive.
2. Adhesive dispersion-type system
• lacks the permeation-controlling membrane
• drug reservoir is formulated by directly dispersing the drug in an
adhesive polymer and then spreading the medicated adhesive, by
solvent casting, onto a flat sheet of drug-impermeable backing
membrane to form a thin drug-reservoir layer.
• On top of the drug-reservoir layer, layers of nonmedicated, rate-
controlling adhesive polymer of constant thickness are applied to
produce an adhesive diffusion-controlled drug delivery system.
3. Matrix dispersion-type system
• The drug reservoir is formed by homogeneously dispersing the
drug in a hydrophilic or lipophilic polymer matrix, and then the
medicated polymer is molded into a medicated disc with a defined
surface area and controlled thickness.
• The disc is then glued onto an occlusive base plate in a
compartment fabricated from drug-impermeable backing.
• The adhesive polymer is spread along the circumference to form a
strip of adhesive rim around the medicated disc. Release rate is
controlled by diffusion from the matrix.
4. Micro reservoir System
• drug reservoir is formed by first suspending the drug particles
in an aqueous solution of water-soluble polymer and then
dispersing it homogeneously in a lipophilic polymer by s high-
shear mechanical force to form a large number of
unleachable, microscopic spheres of drug reservoir.
 Method of use

Novel method of drug delivery it is very important that patients are

informed how to use these devices correctly. All patients who
purchase or are prescribed patches should be given the following
information about their use.
• To ensure adequate adhesion the patch must be applied to a
clean, dry area of skin.
• The old patch must always be removed before applying a new one.
• When a patch is replaced area of skin. The area of skin from
which a patch has just been removed will be soft and possibly
moist. This alters the permeability of the skin. In order to
maintain the same level of drug absorption a different, intact
area of skin must be used.
• The patch must be disposed of carefully. It should be folded
together to prevent it being struck onto another person’s skin.
Particular care should be taken to keep patches away from
children.
 Penetration Enhancers

• Substances that facilitates absorption through the skin.

• Penetration enhancers with a direct effect on skin
permeability include solvents, surfactants, and
miscellaneous chemicals such as urea and N,N-diethyl-m-
toluamide.
 Penetration Enhancers
1. Solvents
- Water
- Alcohols
Methanol
Ethanol
2-propanol
- Alkyl-methyl sulfoxide
Dimethyl sulfoxide
Decylmethyl sulfoxide
Tetradecylmethyl sulfoxide
- Pyrrolidones
2-pyrrolidones
N-Methyl-2-pyrrolidone
- Leurocapram
- Miscellaneous solvents
Acetone
Dimethyl acetamide
Dimethyl formamide
2. Amphiphiles
• Amino acids
• anionic surfactants
• cationic surfactants
• amphoteric surfactants
• nonionic surfactants
• fatty acids and alcohols
3. Miscellaneous
• Clofibric acid amides
• Hexamethylene lauramide
• Proteulytic enzymes
• Urea
Cosmetics
Cosmetics are substances used to enhance or protect the
appearance or odor of the human body.
• The U.S. FDA which regulates cosmetics defines cosmetics as:
"intended to be applied to the human body for cleansing,
beautifying, promoting attractiveness, or altering the
appearance without affecting the body's structure or
functions."
• Cosmetics include skin-care creams, lotions, powders,
perfumes, lipsticks, fingernail polishes, eye and facial makeup,
permanent waves, hair colors, deodorants, baby products,
bath oils, bubble baths, bath salts, butters and many other
types of products.
• A subset of cosmetics is called "make-up", which refers
primarily to colored products intended to alter the user’s
appearance.
Lipstick
 Lipstick

• cosmetic product containing pigments, oils, waxes, and emollients that

applies color and texture to the lips.
• Lipstick is known to have been used around 5000 years ago in ancient
Mesopotamia, when semi-precious jewels were crushed and applied to
the lips and occasionally around the eyes. Women in the ancient Indus
Valley Civilization applied lipstick to their lips for face decoration. Ancient
Egyptians extracted purplish-red dye from fucus-algin, 0.01% iodine, and
some bromine mannite, which resulted in serious illness.
• Cleopatra had her lipstick made from crushed carmine
beetles, which gave a deep red pigment, and ants for a base.
Lipsticks with shimmering effects were initially made using a
substance found in fish scales called pearlescence
Shampoo
 Shampoo

• Shampoo is a common hair care product used for the removal of oils,
dirt, skin particles, environmental pollutants and other contaminant
particles that gradually build up in hair.
• The goal is to remove the unwanted build-up without stripping out so
much as to make hair unmanageable.
• Shampoo, when lathered with water, is a surfactant, which, while
cleaning the hair and scalp, can remove the natural oils (sebum) which
lubricate the hair shaft.
• Shampooing is frequently followed by conditioners which increase the
ease of combing and styling.
• Shampoo cleans by stripping sebum from the hair. Sebum is an oil
secreted by hair follicles that is readily absorbed by the strands of hair,
and forms a protective layer. Sebum protects the protein structure of hair
from damage, but this protection comes at a cost. It tends to collect dirt,
styling products and scalp flakes. Surfactants strip the sebum from the hair
shafts and thereby remove the dirt attached to it.
• While both soaps and shampoos contain surfactants, soap bonds to oils
with such affinity that it removes too much if used on hair. Shampoo uses
a different class of surfactants balanced to avoid removing too much oil
from the hair.
• The chemical mechanisms that underlie hair cleansing are similar to that
of traditional soap. Undamaged hair has a hydrophobic surface to which
skin lipids such as sebum stick, but water is initially repelled. The lipids do
not come off easily when the hair is rinsed with plain water. Shampoo
applied to wet hair is absorbed into the oil/hair interfaces.
• The anionic surfactants substantially reduce the interfacial surface tension
and allow for the removal of the sebum from the hair shaft. The non-polar
oily materials on the hair shaft are solubilised into the surfactant micelle
structures of the shampoo and are removed during rinsing. There is also
considerable removal through a surfactant and oil "roll up" effect.
Shampoo formulations seek to maximize the following qualities:
• Easy rinsing
• Good finish after washing hair
• Minimal skin/eye irritation
• No damage to hair
• Feels thick and/or creamy
• Pleasant fragrance
• Low toxicity
• Good biodegradability
• Slightly acidic pH, since a basic environment weakens the hair
by breaking the disulfide bonds in hair keratin.
• Many shampoos are pearlescent. This effect is achieved by
addition of tiny flakes of suitable materials, eg. glycol
distearate, chemically derived from stearic acid, which may
have either animal or vegetable origins. Glycol distearate is a
wax.
 Surfactants

Surfactants, also known as wetting agents, lower the surface tension of a

liquid, allowing easier spreading, and the interfacial tension between
two liquids. The term surfactant is a contraction of "Surface active
agent".
The major types of surfactants used in shampoos include:
• Anionic
• Cationic
• Nonionic
• Amphoteric
 Specialized shampoos

a. Dandruff
• Cosmetic companies have developed shampoos specifically
for those who have dandruff. These contain fungicides such
as zinc pyrithione and selenium sulfide which reduce loose
dander by killing Malassezia furfur. Coal tar and salicylate
derivatives are often used as well.
b. All-natural
Some companies use "all-natural", "organic", "botanical", or "plant-
derived" ingredients (such as plant extracts or oils), combining
these additions with one or more typical surfactants. The
effectiveness of these organic ingredients is disputed.
c. Alternative
Alternative shampoos, sometimes labeled SLS-free, have fewer harsh
chemicals - typically none from the sulfate family. They are claimed
to be gentler on human hair.
d. Infant
Shampoo for infants is formulated so that it is the same pH level
as the eye, thus less irritating if it were to get into the eyes.
Most contain sodium laureth sulfate and/or sodium lauryl
sulfate, the mildest surfactant of the sulfate family.
Alternatively, infant shampoos may be formulated using other
classes of surfactants, most notably non-ionics which are much
milder than any charged anionics used.
e. Animal
• Shampoo for animals (such as for dogs or cats) should be
formulated especially for them, as their skin has fewer cell
layers than human skin.
• Cats' skin is 2-3 cell layers thick, while dogs' skin is 3-5 layers.
• Human skin, by contrast, is 10-15 cell layers thick. This is a
clear example of why one should never use even something
as mild as baby shampoo on a cat, dog, or other pet.
• Shampoo intended for animals may contain insecticides or other
medications for treatment of skin conditions or parasite infestations such
as fleas or mange.
• These must never be used on humans! It is equally important to note that
while some human shampoos may be harmless when used on animals,
any haircare products that contain active ingredients/drugs (such as zinc in
antidandruff shampoos) are potentially toxic when ingested by animals.
• Special care must be taken not to use those products on pets. Cats are at
particular risk due to their instinctive method of grooming their fur with
their tongues
Powder
• Face Powders. A cosmetic made from coloured talc, applied to
the face
• Body powder is the generic name for alternatives to talcum
powder. It is usually made from a combination of tapioca
flour, rice flour, cornstarch, kaolin, arrowroot powder, and/or
orrisroot powder, but other powders may be used.
Soap
• Soap is a surfactant used in conjunction with water for washing and
cleaning.
• It usually comes in a solid molded form, termed bars due to its
historic and most typical shape.
• The use of thick liquid soap has also become widespread, especially
from soap dispensers in public washrooms. Applied to a soiled
surface, soapy water effectively holds particles in suspension so the
whole of it can be rinsed off with clean water. In the developed
world, synthetic detergents have superseded soap as a laundry aid.
• Many soaps are mixtures of sodium (soda) or potassium
(potash) salts of fatty acids which can be derived from oils or
fats by reacting them with an alkali (such as sodium or
potassium hydroxide) at 80 – 100 °C in a process known as
saponification. The fats are hydrolyzed by the base, yielding
glycerol and crude soap. Historically, the alkali used was
potassium hydroxide made from the deliberate burning of
vegetation such as bracken, or from wood ashes.
USES:
• Soaps are useful for cleaning because soap molecules attach readily to
both nonpolar molecules (such as grease or oil) and polar molecules (such
as water).
• Although grease will normally adhere to skin or clothing, the soap
molecules can attach to it as a "handle" and make it easier to rinse away.
Allowing soap to sit on any surface (skin, clothes etc) over time can
imbalance the moisture content on it and result in the dissolving of fabrics
and dryness of skin.
• (fatty end) :CH3-(CH2)n - COONa: (water soluble end)
• The hydrocarbon ("fatty") portion dissolves dirt and oils, while the ionic
end makes it soluble in water. Therefore, it allows water to remove
normally-insoluble matter by emulsification.
Toothpaste
 Toothpaste

• Toothpaste is a paste or gel dentifrice used to clean and improve the

aesthetic appearance and health of teeth. It is almost always used in
conjunction with a toothbrush.
• Toothpaste use can promote good oral hygiene: it can aid in the removal
of dental plaque and food from the teeth, it can aid in the elimination
and/or masking of halitosis, and it can deliver active ingredients such as
fluoride to prevent tooth and gums (Gingiva) disease. Most people in
developed countries consider toothpaste a necessity and use it at least
once a day.
• Sodium fluoride (NaF) is the most popular active ingredient in
toothpaste to prevent cavities; some brands use sodium
monofluorophosphate (Na2PO3F). Nearly all toothpaste sold in
the United States has 1000 to 1100 parts per million fluoride
ion from one of these active ingredients. This consistency
leads some to conclude that cheap toothpaste is just as good
as expensive toothpaste. When the magazine Consumer
Reports rated toothpastes in 1998, 30 of the 38 were judged
excellent.
• Many, though not all, toothpastes contain sodium lauryl sulfate (SLS) or
another of the sulfate family. SLS is found in other personal care products
as well, such as shampoo, and is largely a foaming agent. SLS may cause a
greater frequency of mouth ulcers in some people as it can dry out the
protective layer of oral tissues causing the underlying tissues to become
damaged. Some brands include powdered white mica. This acts as a mild
abrasive to aid polishing of the tooth surface, and also adds a
cosmetically-pleasing glittery shimmer to the paste. Many may include
frustules of dead diatoms, as a mild abrasive.
• Ingredients such as baking soda, enzymes, vitamins, herbs, calcium, calcium
sodium phosphosilicate, mouthwash, and/or hydrogen peroxide are often
combined into base mixes and marketed as being beneficial. Some
manufacturers add antibacterial agents, for example triclosan or zinc
chloride.
• Toothpaste comes in a variety of flavors, most often being some variation on
mint (spearmint, peppermint, regular mint, etc). Other more exotic flavors
include: anise, apricot, bubblegum (marketed mostly to children), cinnamon,
fennel, neem, ginger, vanilla, lemon, orange, pine. Flavors which have been
introduced but discontinued due to poor reception include peanut butter,
iced tea, and even whisky. Some pastes are unflavored.
• Many toothpastes contain colorings for better visual acceptance.
• Toothpaste is not intended to be swallowed. Some types of
toothpaste may cause nausea or diarrhea if swallowed in excess
quantity. Extended consumption while the teeth are forming can
result in fluorosis. This is why young children should not use
toothpaste except under close supervision. There are several non-
fluoride toothpaste options available in the market for those with
no tolerance to fluoride.
Finish
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