2160 - Controlled Drug Delivery System

CONTROLLED DRUG DELIVERY
SYSTEMS- GENERAL INTRODUCTION

NDDS-VII SEMESTER
Dr. GarimaJoshi Assistant Professor, Pharmacy, MLSU

Drug Delivery
 Drug delivery is the method of administering
pharmaceutical compound to achieve a therapeutic
effect in humans or animals.
 drug delivery can be done through various routes-
the oral (through the mouth), topical (skin), trans-
mucosal (nasal, buccal, sublingual, vaginal,
ocular,rectal), parenteral(injection into systemic
circulation) and inhalation routes.
 The drug delivery system can further be divided
into two main types: 1. Conventional drug delivery
system. 2. Novel drug delivery system
 The conventional dosage forms provide drug
release immediately and it causes fluctuation of
drug level in blood depending upon dosage form.
 Therefore to maintain the drug concentration within
therapeutically effective range need novel drug
delivery system(NDDS).
 NDDS is a combination of advanced techniques and
newer dosage form with controlled/sustained drug
release to target the at specific site.
Controlled drug delivery vs
Conventional drug delivery
Conventional drug delivery Controlled drug delivery
 Periodic administration  Drug concentration rise

 High concentration can quickly to effective
lead to undesirable level.
effects  Effective concentration
 Low concentrations can is maintained for
be ineffective longer duration
 Inconvenient
 No targeting
Sustained release drug delivery system
sustained release are drug delivery system that achieve slow release of drug over an
extended period of time after administration of single dose.
In other words, the drug release is simply extended in time i.e. the rate and duration are
not designed to achieve a particular profile. Sustained release- steadily over a long period
of time
Controlled Release Drug Delivery System
Controlled release are drug delivery system which maintain constant level of drug in
blood and tissue for extended period of time. It implies A predictability and reproducibility
in drug release kinetics
In other words, the rate and duration are designed to achieve A desired concentration.
Controlled release drug delivery system is a way of designing and formulating a
medicine so that the release of drug from it occur in a controlled manner, desirable
manner.
Pharmaceutical approaches for designing SR/CRDDS
It is further divided into matrix and reservoir type

dissolution controlled release system
Dissolution controlled release system
• Control – Dissolution of the drug from the polymer matrix
or encapsulated forms.
• The dissolution process at a steady state is described by
Noyes Whitney equation:
dc / dt = k A/V (Cs – C)
dc / dt = (D/h) A (Cs – C)
where, dC/dt = dissolution rate
V = volume of the solution
k = dissolution rate constant
D = diffusion coefficient of drug through pores
h = thickness of the diffusion layer
A = surface area of the exposed solid
Cs = saturated solubility of the drug
C = conc. of drug in the bulk solution 42
MATRIX type
• First order drug release.
• There are 2 methods:
1. Congealing &
2. Aqueous dispersion method
• The drug release is determined by dissolution rate of the polymer.
• Examples: 1. Dimetane extencaps 2. Dimetapp extentabs.
ENCAPSULATION type (Reservoir Type)
• The drug particle are coated or encapsulated by microencapsulation technique
• The pellets are filled in hard gelatin capsule, popularly called as ‘spansules’.
• Once the coating material dissolves the entire drug inside the microcapsule is immediately
available for dissolution and absorption.
• Here the drug release is determined by dissolution rate and thickness of polymer membrane
which may range from 1 to 200μ
• it is also Called as Coating dissolution controlled system.

• Dissolution rate of coat depends upon stability & thickness of coating.
• One of the microencapsulation method is used.
• Examples: 1. Ornade spansules 2. Chlortrimeton Repetabs
B)Diffusion controlled release system
INTRODUCTION
• This system is hollow containing an inner core of drug.
• The water insoluble polymeric material surrounds drug
reservoir.
• The drug partitions into the membrane and exchanges
with the surrounding
fluid by diffusion.
• The release drug from a reservoir device follows Fick’s
first law of diffusion.
J = - D dc/dx
Where, J = flux, amount/area-time
D = diffusion coefficient of drug in the polymer, area/time
dc/dx = change in conc. with respect to polymer distance
MATRIX Devices
• A matrix or monolithic device consists of an inert polymeric matrix
in
which a drug is uniformly distributed.
• Drugs can be dissolved in the matrix or the drugs can be present as
a
dispersion.
NOTE : Matrix may be HOMOGENEOUS or POROUS with water
filled
pores.
State of presentation of this form affects the various release patterns:
1. Dissolved drug (Fick’s Second law)
2. Dispersed drug (Fick’s First law)
3. Porous matrix (Higuchi’s theory for porous form)
4. Hydrophilic matrix (gelation & diffusion)
64
MATRIX Devices
• Rigid Matrix Diffusion
Materials used are insoluble plastics such as PVP & fatty acids.
• Swellable Matrix Diffusion
1. Also called as Glassy hydrogels.Popular for sustaining the release of
highly water soluble drugs.
2. Materials used are hydrophilic gums.
Examples : Natural- Guar gum, Tragacanth. Semisynthetic -HPMC, CMC, Xanthum gum.
Synthetic -Polyacrilamides.
• Examples: Glucotrol XL, Procardia XL
RESERVOIR Devices
• The drug core is encased by a water-insoluble polymeric materials.
• The mesh (i.e., the space between macromolecular chains) of these polymers,
through which drug penetrates or diffuses after partitioning, is of
MOLECULAR LEVEL.
• The rate of drug release is dependent on the rate of drug diffusion but not on
the rate of dissolution.
• In short, mass transport phenomena at molecular level occurs.
• Examples: Nico-400, Nitro-Bid
Methods of Prep. (RESERVOIR Devices)
• Mostly it involves :
o Coated Beads/Pellets
o Microencapsulation
Coated Beads/Pellets (RESERVOIR Devices)

• BEADS/PELLETS
Coating of drug solution onto preformed cores.
Covering of core by an insoluble (but permeable coat).
NOTE: Pan coating or air-suspension technique is generally used for
coating.
NOTE: Pore forming additives may be added to the coating solution
Microencapsulation (RESERVOIR Devices)

• This technique used to encapsulate small particles of drug, solution of
drug, or even gases in a coat (usually a polymer coat).
• Generally, any method that can induce a polymer barrier to deposit on
the surface of a liquid droplet or a solid surface can be used to form
microcapsules.
Design considerations of controlled
release
 Route of drug delivery
 Target site
 Patient condition
 Polymer consideration- Glass transition temperature,
Diffusion characteristics, compatibility, ease of
formulation, fabrication
 Drug considerations-Physicochemical properties,
stability, solubility, partitioning, charge protein
binding
c) Ions Exchange Based SR/CR Formulations:
Ion-exchange systems generally use resins composed of water
insoluble cross-linked polymers. These polymers contain salt-forming
functional groups in repeating positions on the polymer chain.
The drug is bound to the resin and released by exchanging with
appropriately charged ions in contact with the ion-exchange groups
d) Dissolution & Diffusion Controlled Release System:

Drug is encapsulated in partially soluble membrane, pores are
created due to soluble parts of coating film which permits entry
of aqueous medium into core and drug dissolution starts by
diffusion of dissolved drug out of system. Mixture of water
soluble PVP and water insoluble ethyl cellulose is used for this
purpose.
Osmotic Pressure Based SR/CR Formulations:
In this system, the flow of liquid into the release unit driven by a
difference in osmotic pressure between the inside and the outside of
the release unit is used as the release-controlling process.
Water penetration/Osmotic Pressure Controlled NDDS :
Drug may be osmotically active or drug may be combined with
osmotically active salts like NaCl.

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CONTROLLED DRUG DELIVERY

SYSTEMS- GENERAL INTRODUCTION

Dr. GarimaJoshi Assistant Professor, Pharmacy, MLSU

 Periodic administration  Drug concentration rise

It is further divided into matrix and reservoir type

• it is also Called as Coating dissolution controlled system.

Coated Beads/Pellets (RESERVOIR Devices)

Microencapsulation (RESERVOIR Devices)

d) Dissolution & Diffusion Controlled Release System:

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