8/12/2019 1 Skin Delivery
1/22
Skin delivery
Tommy Julianto Bustami Effendi
8/12/2019 1 Skin Delivery
2/22
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.
8/12/2019 1 Skin Delivery
3/22
8/12/2019 1 Skin Delivery
4/22
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.
8/12/2019 1 Skin Delivery
5/22
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$ +,,-.
8/12/2019 1 Skin Delivery
6/22
/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.
8/12/2019 1 Skin Delivery
7/22
&&T/1' 23'!I/4/5' /F !6I
8/12/2019 1 Skin Delivery
8/22
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.
8/12/2019 1 Skin Delivery
9/22
E2I7E%1I! !T%8CT8%E
8/12/2019 1 Skin Delivery
10/22
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.
8/12/2019 1 Skin Delivery
11/22
%oute of active penetration
8/12/2019 1 Skin Delivery
12/22
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.
8/12/2019 1 Skin Delivery
13/22
Crossing the skin
8/12/2019 1 Skin Delivery
14/22
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
8/12/2019 1 Skin Delivery
15/22
Targeted deliveries to the sebaceous gland by particle si;e
ranges
8/12/2019 1 Skin Delivery
16/22
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
8/12/2019 1 Skin Delivery
17/22
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
8/12/2019 1 Skin Delivery
18/22
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
8/12/2019 1 Skin Delivery
19/22
&/TEC3/4/5' 2%/78CT!
4iposome
Cubosome$ 3e
8/12/2019 1 Skin Delivery
20/22
T3E !I@E &7 1/%23/4/5'
8/12/2019 1 Skin Delivery
21/22
8/12/2019 1 Skin Delivery
22/22
T3&6 '/8
+ , A