A presentation on the basic elements and concept of controlled drug delivery systems.

1. CONTROLLED
RELEASE
DRUG DELIVERY SYSTEMS
Al Ameen College of Pharmacy
BY:
SURAJ CHOUDHARY
M.PHARM (PHARMACEUTICS)
DEPT. OF PHARMACEUTICS

2. 2
PPT. PACKAGE
CONTENTS:-
THEME QUESTION -1
THEME QUESTION -2
FLASHBACK
COMPARISON - 1
COMPARISON - 2
MOVEMENT RESTRICTIONS
CRDDS DESIGN CONSIDERATIONS
PRE-REQUISITES
CLASSIFICATION
CONCEPT-BASED ON CLASSES
RECENT INNOVATIONS

3. 3
THEME QUESTION - 1

4. 4
What is DRUG DELIVERY SYSTEM?

5. 5
THEME QUESTION - 2

6. • Definition covers : …..
Controlled rate
Localize drug action
Target drug action
6
What is CONTROLLED RELEASE DDS?

7. FLASHBACK
7

8. 8
HISTORY
¤ The history of controlled release technology is divided into three time
periods:
 1950 to 1970 - Period of SUSTAINED DRUG RELEASE
 1970 to 1990 - NEEDS of the control drug delivery
 1990 (post era) - MODERN ERA of controlled release technology

9. COMPARISON - 1
CONTROLLED RELEASE DRUG DELIVERY SYSTEMS (CRDDS)
Vs.
CONVENTIONAL DRUG DELIVERY SYSTEMS (CONVENTIONAL)
9

10. 10
CRDDS VS CONVENTIONAL

11. CRDDS VS CONVENTIONAL
• Conventional
Periodic administration
Non-specific administration
High systemic concentrations
can be toxic, causing side
effects or damage to organs.
Low concentrations can be
ineffective.
• CRDDS
11
Drug Concentration rises
quickly to effective level.
Effective concentration is
maintained for extended time.

12. • Conventional
 Inconvenient
 Difficult to monitor
 Careful calculation necessary to prevent overdosing
 Large amounts of drug can be “lost” when they don’t get to the
target organ
 Drug goes to non-target cells and can cause damage
 Expensive (using more drug than necessary)
12
DISADVANTAGES OF
CONVENTIONAL

13. COMPARISON - 2
CONTROLLED RELEASE DRUG DELIVERY SYSTEMS (CRDDS)
Vs.
SUSTAINED RELEASE DRUG DELIVERY SYSTEMS (SR)
13

14. 14
CRDDS VS SR

15. • Sustained Release
Controlled drug delivery
Well - characterized and
reproducible dosage form
Controls entry to the body
according to the specifications of
the required drug delivery profile.
(rate and duration of delivery are
designed to achieve desired
concentration)
CRDDS VS SR
• CRDDS
15
Release of drug is extended in
time
Rate and duration are not
designed to achieve a particular
profile.

16. MOVEMENT
RESTRICTIONS
16

17.  Cost of formulation
 Fate of CRDDS
 Biocompatibility
 Fate of polymer,etc.
17
CHALLENGES IN CRDDS
Drug absorption,
distribution and
metabolism vary
among individuals
Individualized
therapy
Controlled
release

18. CRDDS
DESIGN CONSIDERATIONS
18

19.  Route of delivery
 Target sites
1. Desired site for efficacy
2. Sites to avoid to minimize side effects
 Type of therapy
1. Acute or chronic – rate and duration
e.g., 1 yr duration implant vs. antibiotic for acute infection
 Patient condition
1. Cognitive ability and memory
2. Physical condition – ambulatory, bedridden, etc.
19
DESIGN CONSIDERATIONS

20.  Polymer design considerations
1. Physical properties
 Glass transition temperature
 Diffusion characteristics
2. Compatibility with active
3. Stability – must not decompose
in storage
4. Biocompatibility of polymer and
degradation products
5. Ease of formulation and
fabrication
6. Mechanical properties are stable
when drug is added
7. Cost
Agent
1. Physicochemical properties
2. Stability
3. Solubility
4. Partitioning
5. Charge
6. Protein binding properties
20
DESIGN CONSIDERATIONS

21. PRE-REQUISITES
21

22. 22
PRE-REQUISITES ……
OF A RESPONSIVE DRUG DELIVERY SYSTEM

23. 23
BASIC MECHANISMS

24. 24
MECHANISMS
PARTITION
DISSOLUTION
DIFFUSION
OSMOSIS
EROSION
SWELLING TARGETTIN
G COMBINATION

25. CLASSIFICATION
25

26. Based on the……………
26
CLASSIFICATION CRITERIA

27. 27
BASED ON THE
TECHNICAL SOPHISTICATION
Rate-
Preprogrammed
DDS
Activation-
Modulated DDS
Feedback-Regulated
DDS Site-Targeting DDS

28.  Rate of release of the drug has been PRE-PROGRAMMED at specific rate
profiles.
 Fick’s law of diffusion are often followed.
28
RATE-PREPROGRAMMED
DRUG DELIVERY SYSTEMS
Drug Reservoir
Rate-Controlling
surface
Drug

29. 1. Polymer Membrane Permeation
Ex: i. Norplant subdermal implant (levonorgestrol, encap/sd)
ii. Occusert system (Pilocarpine – Ethylene acetate mem)
iii. Transderm-Nitro (disp. Of Nitroglycerine-lactose triturate)
2. Polymer Matrix Diffusion Controlled
Ex: i. Nitro-Dur (Nitroglycerin)
ii. Compudose subdermal implant (Estradiol)
3. Polymer Micro-reservoir Partition
Ex: i. Nitrodisc (Nitroglycerin)
ii. Subdermal Synvro-Mate-C implant (Norgestomet-PEG 400)
29
RATE-PREPROGRAMMED
DRUG DELIVERY SYSTEMS

30.  Rate of release of the drug has been ACTIVATED by some physical,
chemical or Bio-chemical processes.
 Or it may be activated even by the energy supplied externally.
30
ACTIVATION-MODULATED
DRUG DELIVERY SYSTEMS
Drug Reservoir
Rate-Controlling
surface
Drug
Energy Sensor

31. 1. Physical Means
 Osmotic pressure activated
Ex: Acutrim Tab (PPA HCl)
 Hydrodynamic pressure activated
 Vapor pressure activated
Ex: Infusaid pump (Heparin)
 Mechanically activated
Ex: M.D.Nebulizer (Buserelin)
 Magnetically activated
Ex: Hemisphere (Bovine serum
albumin)
 Sonophoresis activated
 Iontophoresis activated
Ex: Phoresor by Motion Control (for
anti-inflammatory drugs)
 Hydration activated
Ex: Valrelease Tab (Valium)
2. Chemical Means
 pH-activated
 Ion-activated
 Hydrolysis-activated
3. Biochemical Means
 Enzyme-activated
Ex: Albumin microspheres (5-
Fluorosil)
 Biochemical-activated
31
ACTIVATION-MODULATED
DRUG DELIVERY SYSTEMS

32. 32
FEEDBACK-REGULATED
DRUG DELIVERY SYSTEMS
 Rate of release of the drug has been activated by a triggering agent, such
as biochemical substance (in the body) & also regulated by it’s
concentration via some FEEDBACK mechanisms.
Drug Reservoir
Rate-Controlling
surface
Drug
Biochemical
responsive/Energy
Sensor

33. 1. Bioerosion regulated
Ex: Urea activated Hydrocortisone
2. Bioresponsive
Ex: Glucose triggered Insulin
3. Self-regulating
Ex: Glycosylated Insulin- Concanavalin A
33
FEEDBACK-REGULATED
DRUG DELIVERY SYSTEMS

34.  Proposed by Ringsdorf. Consists of following parts attached to the non-immunogenic
& biodegradable polymer:
1. Site-specific targeting moiety 3. Drug moiety with spacer
2. Solubilizer
34
SITE TARGETTING
DRUG DELIVERY SYSTEMS
Drug Reservoir
Rate-Controlling
surface
Drug
Biochemical
responsive/Energy
Sensor
Site-Targetting
Moiety

35. 35
BASED ON THE
ROUTE OF ADMINISTRATION

36. • Osmotic Pressure
• Hydrodynamic Pressure
• Membrane Permeation
 Microporous MP
 Gastric Fluid-Resistant Intestine-Targeted
• Gel Diffusion
• pH
• Ion-Exchange
36
BASED ON THE
ORAL DRUG DELIVERY

37. • Nasal delivery of…………..
- Organic based Pharmaceuticals
- Peptide based Pharmaceuticals
• Development of……………
- Epinephrine-Releasing
- Hydrophilic Contact lenses
37
NASAL DRUG DELIVERY
OCULAR DRUG DELIVERY
NON-INVASIVE

38. • Transdermal delivery of…………..
- Polymer Membrane Permeation
- Polymer Matrix Diffusion
- Drug Reservoir Gradient
- Micro reservoir Dissolution
• Development of……………
- Dissolution-Controlled Depot
- Adsorption-type Depot
- Encapsulation-type Depot
- Esterification-type Depot
38
TRANSDERMAL DRUG DELIVERY
PARENTAL DRUG DELIVERY

39. 39
RECENT TRENDS

40. 40
REFERENCES
1. Chien Y W; Novel Drug Delivery Systems; Informa Healthcare, 2nd
Edition, 2009.
2. Siegel R A and Rathbone M J; Overview of Controlled Release
Mechanisms; Advances in Delivery Science and Technology, 2012.
3. Bhowmik D, et.al; Recent trends in scope and opportunities of control
release oral drug delivery systems; Critical review in pharmaceutical
sciences, (1): 2012.
4. Ummadi S, Shravani B; Overview on Controlled Release Dosage Form;
International Journal of Pharma Sciences, 3(4); 2013.