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 m 2)

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