ABSTRACT The parenteral administration route is the most effective and common form of delivery for active drug substances with poor bioavailability and the drugs with a narrow therapeutic index. Drug delivery technology that can reduce the total number of injection throughout the drug therapy period will be truly advantageous not only in terms of compliance, but also to improve the quality of the therapy and also may reduce the dosage frequency. Such reduction in frequency of drug dosing is achieved by the use of specific formulation technologies that guarantee the release of the active drug substance in a slow and predictable manner. The development of new injectable drug delivery system has received considerable attention over the past few years. A number of technological advances have been made in the area of parenteral drug delivery leading to the development of sophisticated systems that allow drug targeting and the sustained or controlled release of parenteral medicines.

1. PARENTRAL CONTROLLED RELEASE
DRUG DELIVERY SYSTEMS
By
P. Swapna
Department of Pharmaceutics
St. Peter’s College of Pharmacy

2. INTRODUCTION
 The application of advanced drug delivery technology to
parenteral administration lead to development of Liposomes,
Nanosuspensions, solid implants etc. to overcome limitations of
conventional parenteral delivery.

3. Advantages Disadvantages
 Reduced fluctuations in Css
levels.
 Maximum utilization of
drug.
 Localised delivery of drug.
 Possibility of dose dumping.
 Poor in-vitro in-vivo
correlations.
 Decreased systemic
availability.

4. Comparision of plasma drug levels

5. METHODS TO ACHIEVE PROLONG RELEASE OF
PARENTRALS
Pharmacological Method (IM/SC/IV/IP):
Ex: Administration Of Vasoconstrictors
Chemical Methods (use of salts, esters,
and complexes of the active ingredient
with low solubility).
Physical Methods: selection vehicle
(macro molecules, swelling agents,
adsorbents).

6. BIOPHARMACEUTICS OF PCRDDS

7. CLASSIFICATION OF PCRDDS
 INJECTABLES
 Solutions
 Coarse dispersions
 Colloidal Dispersions
 Micro Particles
 Resealed Erythrocytes

8. Different routes of administration
Different lengths of needles

9. Solutions
 Aqueous solution
 Oil solutions
Tetig Injectable solution.
(Human Blood Plasma)
Meglob Injectable solution.
(Pooled Human Venous
Plasma)

10. Coarse dispersions
 Emulsions/macro
emulsions
 Simple Emulsion
 Multiple Emulsion
 Magnetic Emulsion
 Suspension
 Factors:
 Solid Content(0.5 to5%)
 Particle size(10μs)
 Aqueous suspensions
 Oil suspensions
Ingredients: Aqua. Paraffinum liquidum.
PEG-6-stearate. Panthenol. Dimethicone.
Chlorhexidine dihydrochloride. Parfum.
Pantolactone. Disodium EDTA.

11. Colloidal dispersions
 Liposomes
 Niosomes
 Polymeric/ mixed micelles
 Nano particles
Liposomes
Why liposomes offer great potential in parentral therapy?
 Encapsulate both hydrophillic and lipophillc drugs.
Ex: Delivery Of Immuno Modulators.
 Effective Solubilising vehicle for drugs with poor soulbility.
Ex: Alphaxalone, Tacroline, Paclitaxel, Camphothecin.

12. Contd…..
Niosomes
Advantages over liposomes:
More flexibility.
Low toxicity(non ionic nature)
More chemical stability.
Advanced forms:
Discomes (12-60μm)
Capable of entrapping water
soluble solutes.
Ex: Opthalmics.

13. Marketed Products Of Niosomes

14. Contd….
 Polymeric/mixed micelles
 Polymeric micelles are nano
carriers generated by the self-assembly
of amphiphilic
polymers in water.
 Hydrophobic core is excellent
host for anti cancer drugs.

15. Contd….
 Nano particles
 Nano Suspensions/Nano Crystals
 Nano Emulsions
 Polymeric nano particles/ nanospheres
 Nano capsules
 Solid lipid nano particles
 Nano structured lipid carrier
 Lipid drug conjugate nano particles
Nano suspensions
Nanonised drug is dispersed in water
Advantage: More drug loading(upto 90%)

16. Contd….
Nano Emulsions/Micro
Emulsions (5-50nm)
R= 5-10nm
Transparent
R=10-50nm
Translucent
o/w emulsion
• The dispersed phase
droplets are nanonized.

17. Contd…
 Polymeric nano particles/ nanospheres
 Drug in nano particles dispersed in polymer matrix.
 Polymers used cellulose derivatives.
 Solid lipid nano particles:(100- 400 nm):
 Potentially applied dermally, IntraVenously.
 Nano structured lipid carrier:
 oil loaded solid lipid nano particles.
 Advantages over SLN:
 Decreased burst release.
 better controlled release.

18. Contd….
 Lipid conjugate drug carrier
 Enhance stabilty.
 Increase membrane permeability.
 Nano capsules
Drug is dispersed in core and separated by polymer matrix from
the surroundings

19. Micro particles
Microspheres
Magnetic microspheres
Micro capsules
 Size: <125μs
 Injected by using 18 or 20 number
Table-needle
1: List of Marketed Products of Microspheres
Drug
Commercial name Company
Risperidone Risperdal® Consta® Janseen®/Alkermes,
Inc
Naltrexone Vivitrol® Alkermes
Bromocriptine Parlodel LAR ™ Novartis

20. Contd…
Micro capsules
 Size:50nm-20mm.
 Release the medicaments at a zero
order rate.
 Ex: Steroids, Peptides and Anti
neoplastic agents
Magnetic microspheres:
Used for target drug delivery of anti
cancer agents

21. Resealed Erythrocytes
Longer life span in circulation.
 Drug protected from enzymatic inactivation.
 Ability to target the organs of the RES.
Drug loading can be done by immersing the cell in
buffered hypotonic solution.

22. IMPLANTS
1. In-situ Forming Implant (In-situ
Depot forming system)
 In-situ precipitating implants
 In situ gel forming implants
 In situ micro particle implants
In situ cross linked gels
2. Solid Implants
 Atrigel® In Situ Implant System
Controlled release pattern of Artigel

23. INFUSION DEVICES
1. Osmotic pressure activated drug delivery systems
 ALZET OSMOTIC
PUMP
 DUROS Infusion Implant

24. Contd…
2. VAPOUR PRESSURE POWERED PUMPS
3. BATTERY POWERED PUMPS
• Peristaltic Pumps
• Solenoid Driven Reciprocating Pumps

25. CONCLUSION
The final specifications need to ensure the safety,
identity, strength, performance, and quality of the drug
product at release and during storage through the end of
its shelf-life.

26. REFERENCES
1. Patel RP: Niosomes: An Unique Drug Delivery System.
Pharmainfo.net. 2007.
2. Brahmankar D.M: Biopharmaceutics and Pharmacokinetics.
Vallabh prakashan, 2nd edition 2010.
3. J.R. Robinson, V. L. Lee; Controlled Drug Delivery:
Fundamental and Applications, Marcel dekker, USA, 2003.
4. Milan Agrawal, Mahesh Limbachiya, Amit Sapariya and Girish
Patel, IJPSR, 2012; Vol. 3(10): 3657-3669.