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The terminologies associated with novel DDS are

sustained release
controlled release

Sustained release describes a dosage form formulated to retard the

release of a therapeutic agent such that its appearance in the systemic
circulation is delayed or prolonged and its plasma profile is sustained in
duration.

Controlled release implies a predictability and reproducibility in the

drug release kinetics.

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ate pre-programmed drug delivery systems
2 ctivation-modulated drug delivery systems
3 eed back-regulated drug delivery systems
4 Site-targeting drug delivery systems

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elease of drug from the delivery systems is activated by some physical,

chemical, or biochemical processes and facilitated by the energy supplied
externally. The rate of drug release is then controlled by regulating the
process applied or energy input.
Based on the nature of the process applied or the type of energy used,
these activation modulated DDS can be classified into,

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. Physical means
a Osmotic pressure-activated DDS
b Hydrodynamic pressure-activated DDS
c Vapour pressure-activated DDS
d Mechanically activated DDS
e Magnetically activated DDS
f Sonophoresis-activated DDS
g Iontophoresis-activated DDS
h Hydration-activated DDS
2. Chemical means
a PH activated DDS
b Ion activated DDS
c Hydrolysis activated DDS
3. Biochemical means
a Enzyme activated DDS
b Biochemical activated DDS
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Depends on osmotic pressure to activate the drug release.

The drug reservoir is contained within a semipermeable housing with
controlled water permeability.
The drug is activated to release in solution form at a constant rate through a
delivery orifice.
The rate of drug release is modulated by controlling the osmotic pressure
gradient.

The drug release is activated by osmotic pressure and controlled at a rate

determined by the water permeability and the effective surface area of the
semipermeable housing as well as the osmotic pressure gradient.

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Ex: lzet osmotic pump.

Drug reservoir is contained within a collapsible, impermeable bag
whose external surface is coated with osmotically active salt.
This reservoir is sealed inside a rigid semipermeable membrane.
Water in the tissue fluid penetrate through the semipermeable housing
and dissolve the osmotically active salt.
This creates an osmotic pressure in the spacing between the reservoir
compartment wall and the semipermeable housing.
Due to this reservoir compartment is forced to reduce its volume and
the drug solution is delivered at a controlled rate.

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It is enclosed with a collapsible, impermeable container, which

contains a liquid drug formulation, inside a rigid housing.
 composite laminate of an absorbent and a swellable, hydrophilic
polymer is sandwiched between the drug reservoir compartment and the
housing.
Laminate absorbs the GI fluid through the openings at the lower end of
the housing and becomes swollen, which generates hydrodynamic
pressure.
This pressure forces the drug reservoir to reduce in volume and causes
the drug formulation to release through the delivery orifice.
The release of drug is activated by hydrodynamic pressure and
controlled at a rate determined by the fluid permeability and effective
surface area of the wall with annular openings as well as by the
hydrodynamic pressure gradient.
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Drug reservoir in solution formulation, is contained inside the
infusion compartment. It is separated from the pumping compartment by
a partition.
The pumping compartment contains a fluorocarbon fluid that
vaporizes at body temperature and creates a vapour pressure. Due to this,
the partition moves upward. This forces the drug solution to be delivered
through flow regulators and delivery cannula into the blood circulation.
The drug release is activated by vapour pressure and controlled at a
rate determined by differential vapour pressure, formulation viscosity and
size of the delivery cannula.

Examples: Implantable infusion pump for the constant infusion of,

heparin in anticoagulation treatment(Infusaid ,
insulin in antidiabetic medication,
morphine for patients suffering from intense pain of terminal cancer.



 
   


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Vr reservoir is a sol tio for latio retai e i a co tai er
e i e it a ec a ically activate i syste .

A eas re ose of r for latio is re ro ci ly elivere i to a

o y cavity t ro t e s ray ea o a al activatio of r
elivery i syste .

e vol e of sol tio elivere is co trolla le, as s all as 10-100µl.

E a le:
etere ose e lizer for t e i tra asal a i istratio of
sereli , a sy t etic a alo of l tei izi or o e releasi or o e
(L R a i s li .

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Drug reservoir is a dispersion of peptide or protein powders in a
polymer matrix from which macromolecular drug can be delivered only
at a slow rate.

This low rate can be improved by incorporating an electromagnetically

triggered vibration mechanism into the polymeric delivery device.

Here a tiny magnet ring is placed in the core of a hemispherical drug-

dispersing polymer matrix. Then its external surface is coated with a
drug-impermeable polymer, except one cavity at the centre of the flat
surface. This uncoated cavity is positioned directly above the magnetic
ring, which permits a peptide drug to be released.

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mtilizes ultrasonic energy to activate the delivery of drugs from a

polymeric drug delivery device.

The system can be fabricated from either a nondegradable polymer or a

bio erodible polymer.

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mses electrical current to activate and to modulate the diffusion of a

charged drug molecule across a biological membrane, like skin.

Example:
n Iontophoretic drug delivery system, Phoresor, facilitate the
percutaneous penetration of anti-inflammatory drugs to surface tissues.
Transdermal periodic iontotherapeutic system (TPIS , for the
transdermal controlled delivery of insulin, in the control of hyperglycemia
in diabetic animals.

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Depends on the hydration-induced swelling process to activate the drug
release.
Drug reservoir is dispersed in a swellable polymer matrix fabricated
from a hydrophilic polymer.
The drug release is controlled by the rate of swelling of the polymer
matrix.
E.g.: Valrelease tablet.
It is prepared by a simple granulation process of homogeneous
dispersion of Valium in hydrocolloid and pharmaceutical excipients. The
granules are then compressed to form a compressed tablet. fter oral
intake the hydrocolloid in the tablet absorbs gastric fluid and forms a
colloidal gel that starts from the tablet surface and grows inward. The
release of Valium molecules is then controlled by matrix diffusion
through this gel barrier.

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This system permits targetting the delivery of a drug only in the region
with a selected pH range.

It is fabricated by coating the drug-containing core with a PH sensitive

polymer combination.

 gastric fluid-labile drug is protected by encapsulating it inside a

polymer membrane that resists the degradative action of gastric pH.

E.g.: combination of ethyl cellulose and hydroxyl methylcellulose

phthalate.

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n ionic or a charged drug can be delivered.
Prepared by first complexing an ionic drug with an ion-exchange resin
containing a counter ion.
The granules of drug-resin complex are first treated with an
impregnating agent to reduce the rate of swelling in an aqueous
environment.
It is then coated by air suspension coating, with a water insoluble but
water-permeable polymeric membrane.
This membrane serves as a rate-controlling barrier to modulate the
influx of ions as well as the release of drug. In an electrolyte medium,
such as gastric fluid, ions diffuse into the system, react with the drug-
resin complex, and trigger the release of ionic drug.
Example: Pennkinetic ² permits the formulation of liquid suspension
dosage forms with sustained drug release properties for oral
administration.

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Depends on the hydrolysis process to activate the drug release.

Drug reservoir is either encapsulated in microcapsules or dispersed in
microspheres or nanoparticles for injection.
It can also be fabricated as an implantable device.
ll these systems are prepared from a bio-erodible or biodegradable
polymer.
The release of drug from the polymer matrix is activated by the
hydrolysis-induced degradation of polymer chains and controlled by the
rate of polymer degradation.

Ex: LH
H releasing biodegradable subdermal implant, which deliver

goserelin, a synthetic LH
H analog, for the treatment of prostate
carcinoma.

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Depends on the enzymatic process to activate the drug release.

Drug reservoir is either physically entrapped in microspheres or

chemically bound to polymer chains from biopolymers, such as albumins or
polypeptides.

The release of drug is activated by the enzymatic hydrolysis of the

biopolymers by a specific enzyme in the target tissue.

Ex: lbumin microspheres that release 5-fluorouracil by protease-

activated biodegradation.

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. Novel drug delivery system ² Yie W Chien.

2. www.google.com

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