Percutaneous Absorption – PST05208 Pharmaceutics Theory and Compounding

NTA Level 5 • Semester 2 • PST05208

Percutaneous Absorption

Pharmaceutics Theory and Compounding • Source Session/Topic 4
Full source-text version: all educational wording from the extracted learning source is retained; only presenter/tutor metadata and web-layout noise are removed, while formatting is improved for readability.

Session 4: Percutaneous Absorption

Total Session Time: 120 minutes

Prerequisites

• None

Learning Tasks

By the end of this session students are expected to be able to:

 Explain percutaneous Absorption

 Explain factors affecting percutaneous absorption

Resources Needed:

• Flip charts, marker pens, and masking tape
• Black/white board, chalk and whiteboard markers
• LCD projector and computer

SESSION OVERVIEW

Activity/

Step Time Content

Method

1 05 Minutes Presentation Introduction, Learning Tasks

50 Minutes Presentation

2 Percutaneous Absorption

Brainstorming

55 Minutes Presentation

3 Factors Affecting Percutaneous Absorption

Buzzing

4 05 Minutes Presentation Key Points

5 05 Minutes Presentation Evaluation

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SESSION CONTENTS

STEP 1: Presentation of Session Title and Learning Tasks (5 minutes)

READ or ASK students to read the learning tasks and clarify

ASK students if they have any questions before continuing.

STEP 2: Percutaneous Absorption (50 minutes)

Activity: Buzzing (5 minutes)

ASK students to pair up and buzz on the following question for 2 minutes

• What is percutaneous absorption?

ALLOW few pairs to respond and let other pairs to add on points not mentioned

WRITE their response on the flip chart/board

CLARIFY and SUMMARIZE by using the content below

• Percutaneous absorption is the term used to describe the penetration of a substance through the

skin and subsequent movement into the systemic circulation.

• For drugs applied topically for therapeutic purpose, its necessary that:

o The medicament is released from the base

o Adequate amount of drug penetrate the skin

o Sufficient concentration of the drug is maintained at the site of action.

• In some instance, skin penetration of medicament is not necessary for a topical applied

medicament

• A surface film of the active medicament is necessary for this instance. e.g. for medicament

applied topically purposely for:

o Skin protection (against sunlight or moisture loss

o For emollient effect

o For antimicrobial activities in skin disinfection

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• When skin penetration for local activity is the aim, the active substance should be retained for as

longer as possible in the viable epidermis and dermis with minimal elimination by systemic

circulation.

• Therefore, by regarding skin as the route of drug administration, it‟s important to know the

mechanism by which medicaments penetrates the skin barrier.

• Structure of skin

o The skin is divided into three layers:

 epidermis

 dermis

 hypodermis (subcutaneous fat layer)

• Epidermis

o Is about 110µm thick

o Is pierced by hair follicles & sebaceous gland

o It is non vascular

o The outer layer of the epidermis is called stratum corneum

o The stratum corneum is transparent, tough coherent & viscoelastic properties.

o The stratum corneum is composed of dead cells each packed with keratin.

o Resistance to the diffusion of chemicals is greater in stratum corneum (sc) than in the

underlying living skin tissue.

o SC is the rate-limiting barrier to movement of materials & responsible tissue for

impenetrability of the skin.

o However the is not an absolute barriers and trace amount of penetrants can be detected; eg

nickel, chromium ions, parathion & toxic gases.

o The thickness of sc varies. It is thick on the plantar & palmar areas and thin behind the ear and

on the eyelid.

o Cells are formed through mitosis at the basale layer

o The daughter cells move up the strata changing shape and composition as they die due to

isolation from their blood source

o The cytoplasm is released and the protein keratin is inserted.

o They eventually reach the corneum and slough off (desquamation).

o This process is called keratinization and takes place within about 27 days.

o This keratinized layer of skin is responsible for keeping water in the body and keeping other

harmful chemicals and pathogens out, making skin a natural barrier to infection.

• Dermis

o The dermis is the layer of skin beneath the epidermis that consists of connective tissue and

cushions the body from stress and strain.

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o The dermis is tightly connected to the epidermis by a basement membrane.

o It also harbours many Mechanoreceptor/nerve endings that provide the sense of touch and

heat.

o It contains the hair follicles, sweat glands, sebaceous glands, apocrine glands, lymphatic

vessels and blood vessels.

o The blood vessels in the dermis provide nourishment and waste removal from its own cells as

well as from the Stratum basale of the epidermis.

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• Hypodermis

o The hypodermis lies below the dermis

o Its purpose is to attach the skin to underlying bone and muscle as well as supplying it with

blood vessels and nerves.

o The main cell types are fibroblasts, macrophages and adipocytes (the hypodermis contains

50% of body fat). Fat serves as padding and insulation for the body.

Figure: 1.4. Structure of skin

Source: Human Anatomy by Matthew Hoffman, MD (2014)

STEP 3:Factors Affecting Percutaneous Absorption (55 minutes)

Activity: Brainstorming (20 minutes)

Ask students to brainstorm on the following question:

• What are factors affecting percutaneous absorption?

ALLOW few students to respond?

WRITE their responses on the flip chart/ board

CLARIFY and SUMMARISE by using the content below

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• Factors affecting percutaneous absorption can be considered under three main heading

o Condition of the skin

o Physicochemical characteristics of the active substance

o Effect due to the vehicle.

• Condition of the skin.

o Damage and disease.

 Intact skin presents a barrier to absorption that can be reduced considerably when the skin

is damaged or is in a disease state.

 Skin can be damaged by:

• Dryness
• Irritation
• Allergic reaction
• abrasion

o Injured skin has increased percutaneous than intact skin.

• Age

o Percutaneous absorption of infants is higher than in adult to a given medicament due to

 large surface area than that of adult

 Partial developed epidermal drug metabolizing enzymes.

o Old age can also affect permeability of the skin through change in the elasticity, ultrastructure,

chemical composition & barrier properties.

• Temperature & humidity;

o Absorption is influenced by environmental factors such as skin temperature & surface

humidity,

o Diffusion can be accelerated by raising surface temperature e.g. by occlusion

• Skin site

o Fick‟s law of diffusion states that the diffusion of a solute will be inversely proportional to the

thickness of stratum corneum.

o In the plantar & palmar the SC is thick & absorption rate is low than in thin thickness like on

face & behind the ear.

• Hydration.

o Absorption of active substance is enhanced as the skin become more hydrated.

o Topical medicament with occlusive effect has high absorption rate than the non-occlusive

• Miscellaneous aspects

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o The application of vasoconstrictor such as steroids on the skins surface may slow penetration

because of the reduced blood supply.

STEP 4: Key Points (5 minutes

• Percutaneous absorption is the term used to describe the penetration of a substance through the

skin and subsequent movement into the systemic circulation.

• For drugs applied topically for therapeutic purpose, it‟s necessary that: the medicament is released

from the base, adequate amount of drug penetrate the skin and sufficient concentration of the drug

is maintained at the site of action.

• Factors affecting percutaneous absorption include condition of the skin, physicochemical

characteristics of the active substance and effect due to the vehicle.

STEP 5: Evaluation (5 minutes)

• What is percutaneous absorption?
• What are factors affecting percutaneous absorption?

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References

Bronaugh, R.L.; Stewart, R.F. (1985). "Methods for percutaneous absorption studies. IV. The flow

through diffusion cell". J. Pharm. Sci. 74: 64–7. doi:10.1002/jps.2600740117.Sudan

Mahato RA. (2006) Pharmaceutical dosage forms & drug delivery‟‟ Published by CRS press, Taylor

& Froncrs Group,6000 Broken Sound Parkway, Sute 300, Boca Raton, 196-197.New York

A. J. Winfield, J. A. R., I. Smith. (2009). Pharmaceutical Practice (4th ed.) British

Britain, R. P. S. o. G. (1994). The Pharmaceutical Codex (12 ed.). London: London

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