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PARENTERAL CONTROLLED DRUG
DELIVERY SYSTEM EMPHASIS ON
INJECTABLE SYSTEM
Presented By
SOVAN KAYAL
M.PHARM[PHARMACEUTICS]
INTRODUCTION
Parenteral is the introduction of nutrition, a medication, or other
substance into the body via a route other than the mouth, especially
via infusion, injection or implantation.
The aim of controlled release drug delivery systems is to maintain
plasma concentration of drugs within the therapeutic window for a
longer period of time.
The parenteral administration route is the most common and efficient
for delivery of active drug substance with poor bio-availability and
the drug with a narrow therapeutic index.
OBJECTIVES
1.Site-Specific delivery
2.Reduce side effects
3.Increase Bio-availability
4.Increase therapeutic effectiveness
ROUTES OF ADMINISTRATION OF PDDS
Common Routes:
 Intravenous
 Intramuscular
 Subcutaneous
 Transdermal
Other routes:
 Intra-arterial
 Intraarticular
 Intracardiac
 Intradermal
 Intravaginal
 Transmucosal
CLASSIFICATION OF PARENTERAL
CONTROLLED DRUG DELIVERY SYSTEM
Injectable Drug Delivery System
Implantable Drug Delivery System
INJECTABLE DRUG DELIVERY SYSTEM
1. In situ forming drug delivery system
2. Solutions
3. Microspheres
4. Liposomes
5. Suspension
6. Solid liquid nanoparticles
In situ forming drug delivery system:
1. THERMOPLASTIC PASTES:
Semisolid polymers which injected as a melt and form a depot upon cooling to
body temperature.
2. IN SITU CROSS LINKED POLYMER SYSTEMS:
Cross-linked polymer network can be found in situ by free radical reactions
initiated by heat/absorption of photon/ionic interactions between small cation &
polymer anions.
3. IN SITU POLYMER PRECIPITATION:
Water-insoluble and biodegradable polymer in biocompatible organic solvent.
Phase separation and precipitation of the polymer forming the depot at the site of
injection.
4. THERMALLY INDUCED GELLING SYSTEM:
Gelation at body temperature when highly concentrated polymer solution.
5. IN SITU SOLIDIFYING ORGANOGELS:
Water insoluble amphiphilic lipids, which swell in water and forms various
types of lyotropic liquid crystals.
SOLUTIONS:
 Aqueous solution
 High viscosity solution
 For water soluble drugs.
 Gelling agents or viscosity enhancers are used.
 Complex formulations
 Drug forms dissociable complex with macromolecules
 Fixed amount of drug gets complexed
 Given by I.M route
 Oil suspension
 Given by I.M route
 Process of drug availability consists of dissolution of drug particles followed by partitioning
of drug from oil solution to aqueous medium.
 More prolong drug action as compared to oil solution and aqueous suspension.
 E.g., Penicillin G procaine in vegetable oil.
MICROSPHERES:
 Each microsphere is basically a matrix of drug dispersed in a polymer from
which release occurs by first order process.
 Polymers used are biocompatible and biodegradable
E.g., Polylactic acid, Polylactide coglycolide etc.
 Drug release is controlled by dissolution degradation of matrix.
 Small matrices release drug at a faster rate.
 For controlled release of peptide/protein drugs have short half lives.
 Magnetic microspheres are developed for promoting drug targeting which are
infused into an artery.
LIPOSOMES:
 Lipid most commonly used are phospholipids, sphingolipids,
glycolipids and sterols.
 Water soluble drugs are trapped in aqueous compartment.
 Lipophilic ones are incorporated in the lipid phase of liposomes.
 Can be given by I.M, SC routes for controlled rate release.
 Can be given by I.V for targeted delivery.
SUSPENSION:
 Aqueous suspension:
 Given by I.M or SC routes
 Concentration of solids should be 0.5 to 5%
 Particle size should be <10µm
 Drug is continuously dissolving to replenish the lost
 For oil soluble drugs
 Only crystalline and stable polymorphic drugs are given by this forms
 Viscosity builders can be used
 E.g., Crystalline zinc insulin
Oil suspension:
 Given by I.M route
 Process of drug availability consists of dissolution of drug particles followed by
partitioning of drug from oil solution to aqueous medium.
 More prolong drug action as compared to oil solution and aqueous suspension
E.g., Penicillin G procaine in vegetable oil.
SOLID-LIQUID NANOPARTICLES:
 Nanoparticles are called as nanospheres or nano capsules depending upon the
position of drugs
 Polymer used are biodegradable ones
E.g., Polyacrylic acid, Polyglycolic acid
 For selective targeting therapy
PROPERTIES OF IDEAL PCDDS:
1. Simple to administer and remove
2. Inert
3. Biocompatible
4. Comfortable for the patient
5. Capable of achieving high drug loading
6. Readily processable
ADVANTAGES:
 Improve patient convenience and compliance
 Reduction in fluctuation in steady state levels
 Increase safety margin of high potency drugs
 Maximum utilization of drug
 Reduction in health care costs through improved therapy, shorter
treatment period, less frequency of dosing.
DISADVANTAGES:
 Decrease systemic availability
 Poor in vivo-in vitro correlation
 Retrieval of drug is difficult in case of toxicity, poisoning, or
hypersensitivity reactions
 Higher cost of formulation.
THANK YOU

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PARENTERAL CONTROLLED DRUG DELIVERY SYSTEM(PCDDS)

  • 1. PARENTERAL CONTROLLED DRUG DELIVERY SYSTEM EMPHASIS ON INJECTABLE SYSTEM Presented By SOVAN KAYAL M.PHARM[PHARMACEUTICS]
  • 2. INTRODUCTION Parenteral is the introduction of nutrition, a medication, or other substance into the body via a route other than the mouth, especially via infusion, injection or implantation. The aim of controlled release drug delivery systems is to maintain plasma concentration of drugs within the therapeutic window for a longer period of time. The parenteral administration route is the most common and efficient for delivery of active drug substance with poor bio-availability and the drug with a narrow therapeutic index.
  • 3. OBJECTIVES 1.Site-Specific delivery 2.Reduce side effects 3.Increase Bio-availability 4.Increase therapeutic effectiveness
  • 4. ROUTES OF ADMINISTRATION OF PDDS Common Routes:  Intravenous  Intramuscular  Subcutaneous  Transdermal Other routes:  Intra-arterial  Intraarticular  Intracardiac  Intradermal  Intravaginal  Transmucosal
  • 5. CLASSIFICATION OF PARENTERAL CONTROLLED DRUG DELIVERY SYSTEM Injectable Drug Delivery System Implantable Drug Delivery System
  • 6. INJECTABLE DRUG DELIVERY SYSTEM 1. In situ forming drug delivery system 2. Solutions 3. Microspheres 4. Liposomes 5. Suspension 6. Solid liquid nanoparticles
  • 7. In situ forming drug delivery system: 1. THERMOPLASTIC PASTES: Semisolid polymers which injected as a melt and form a depot upon cooling to body temperature. 2. IN SITU CROSS LINKED POLYMER SYSTEMS: Cross-linked polymer network can be found in situ by free radical reactions initiated by heat/absorption of photon/ionic interactions between small cation & polymer anions. 3. IN SITU POLYMER PRECIPITATION: Water-insoluble and biodegradable polymer in biocompatible organic solvent. Phase separation and precipitation of the polymer forming the depot at the site of injection.
  • 8. 4. THERMALLY INDUCED GELLING SYSTEM: Gelation at body temperature when highly concentrated polymer solution. 5. IN SITU SOLIDIFYING ORGANOGELS: Water insoluble amphiphilic lipids, which swell in water and forms various types of lyotropic liquid crystals.
  • 9. SOLUTIONS:  Aqueous solution  High viscosity solution  For water soluble drugs.  Gelling agents or viscosity enhancers are used.  Complex formulations  Drug forms dissociable complex with macromolecules  Fixed amount of drug gets complexed  Given by I.M route  Oil suspension  Given by I.M route  Process of drug availability consists of dissolution of drug particles followed by partitioning of drug from oil solution to aqueous medium.  More prolong drug action as compared to oil solution and aqueous suspension.  E.g., Penicillin G procaine in vegetable oil.
  • 10. MICROSPHERES:  Each microsphere is basically a matrix of drug dispersed in a polymer from which release occurs by first order process.  Polymers used are biocompatible and biodegradable E.g., Polylactic acid, Polylactide coglycolide etc.  Drug release is controlled by dissolution degradation of matrix.  Small matrices release drug at a faster rate.  For controlled release of peptide/protein drugs have short half lives.  Magnetic microspheres are developed for promoting drug targeting which are infused into an artery.
  • 11. LIPOSOMES:  Lipid most commonly used are phospholipids, sphingolipids, glycolipids and sterols.  Water soluble drugs are trapped in aqueous compartment.  Lipophilic ones are incorporated in the lipid phase of liposomes.  Can be given by I.M, SC routes for controlled rate release.  Can be given by I.V for targeted delivery.
  • 12. SUSPENSION:  Aqueous suspension:  Given by I.M or SC routes  Concentration of solids should be 0.5 to 5%  Particle size should be <10µm  Drug is continuously dissolving to replenish the lost  For oil soluble drugs  Only crystalline and stable polymorphic drugs are given by this forms  Viscosity builders can be used  E.g., Crystalline zinc insulin
  • 13. Oil suspension:  Given by I.M route  Process of drug availability consists of dissolution of drug particles followed by partitioning of drug from oil solution to aqueous medium.  More prolong drug action as compared to oil solution and aqueous suspension E.g., Penicillin G procaine in vegetable oil.
  • 14. SOLID-LIQUID NANOPARTICLES:  Nanoparticles are called as nanospheres or nano capsules depending upon the position of drugs  Polymer used are biodegradable ones E.g., Polyacrylic acid, Polyglycolic acid  For selective targeting therapy
  • 15. PROPERTIES OF IDEAL PCDDS: 1. Simple to administer and remove 2. Inert 3. Biocompatible 4. Comfortable for the patient 5. Capable of achieving high drug loading 6. Readily processable
  • 16. ADVANTAGES:  Improve patient convenience and compliance  Reduction in fluctuation in steady state levels  Increase safety margin of high potency drugs  Maximum utilization of drug  Reduction in health care costs through improved therapy, shorter treatment period, less frequency of dosing.
  • 17. DISADVANTAGES:  Decrease systemic availability  Poor in vivo-in vitro correlation  Retrieval of drug is difficult in case of toxicity, poisoning, or hypersensitivity reactions  Higher cost of formulation.