1 Skin Delivery

8/12/2019 1 Skin Delivery

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Skin delivery

Tommy Julianto Bustami Effendi


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Topical

Topical administration of active ingredients is

targeted to deliver actives across the skin to

either permeate into the epidermis and

dermis or beyond the skin by itsaccumulation in blood circulation.


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IT%I!IC &CTIVIT'

The intrinsic activity of active ingredient

dictates its functional profile$ but does not

guarantee that every product containing this

active ingredient "ill indeed be functional. Toensure functionality$ it must be delivered to

the site of action at relevant concentration for

a sufficient period of time to do its action.


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The overall efficacy of a product containing

an active ingredient for skin application is

given by both its intrinsic activity and its

delivery$ according to follo"ing e(uation)*iechers$ +,,-.


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/bstacle in skin penetration

& ma0or obstacle in skin delivery is the

permeation characteristics of the epidermis$

especially the stratum corneum$ "hich limits

active ingredient penetration intu skin.


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E2I7E%1I!

The epidermis is a human tissue "ithout any

blood vessels and therefore the nutrients and

"aste products must diffuse across the dermal

and epidermal 0unction to maintain its vitality. Theepidermis consists of five layers as described in$

"hich from inside to outside are the stratum

germinativum )basal layer$ stratum spinosum

)spinous layer$ stratum granulosum )granularlayer$ stratum lucidum and stratum corneum

)!C.


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E2I7E%1I! !T%8CT8%E


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Skin barrier and routes for active ingredient permeation

&fter the application of topical products on the skin$ active

molecules are ready to permeated into skin epidermis. There are

t"o main routes of skin permeation that have been defined# first

is the transappendageal and the other is transepidermal

The transappendageal routes are also kno"n as the shunt

routes and include permeation through the s"eat glands and

across the hair follicles "ith their associated sebaceous glands.


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%oute of active penetration


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Trans epidermal route

The trans9epidermal route can be defined as

the path"ay "here active ingredients

permeate across the epidermis$ unbroken

!C. There are t"o micro9path"ays$ theintercellular and the transcellular routes.

The recommended molecular "eight for skin

delivery is around :,, 7alton$ but in manycases there are much larger molecules.


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Crossing the skin


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Targeting sebaceous gland

There are t"o "ays of targeting the

sebaceous gland by means of active delivery

through skin.

First$ is the principle of si;e e


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Targeted deliveries to the sebaceous gland by particle si;e

ranges


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Strategies to overcome barriers OF skin delivery

2enetration enhancer The first approach is by the perturbation of the intercellular domains

"ith fatty acids$ pyrrolidones$ surfactants$ and a;ones.

The second approaches is to change the active ingredient=ssolubility in the stratum corneum and thus influencing the

concentration gradient "ith e


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anoparticulates delivery system

2article si;e reductions of drugs has the potential to>

Increase surface area

Enhance solubility

Increase rate of dissolution

Increase oral bioavailability

1ore rapid onset of therapeutic action

7ecrease the dose needed

7ecrease fed?fasted variability

7ecrease patient to patient variability

7elivery of drug directly to target of action

7ecrease adverse effect to patient


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4I2/!/1E!

Viral VectorsANTIBODIS

!ON"#$ATS

%O&'()(I!&&S

anoparticles

2olymer9

protein Con0

8nimolecular2olymer Con0ugates

7E7%I1E%con0ugates

&/T8BE

Buckyball

9fullerenes

NANOT!*NO&O$'

Cubosome

s

3e


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4iposome

Cubosome$ 3e


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T3E !I@E &7 1/%23/4/5'


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1 Skin Delivery