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PARENTERAL CONTROLLED DRUG
DELIVERY SYSTEM
Miss. SNEHAL K. DHOBALE
M-PHARMACY (2ND SEMISTER)
ROLL NO-02
PADM. Dr. D. Y. PA...
INTRODUCTION
 Parenteral is the introduction of nutrition, a medication, or
other substance into the body via a route oth...
OBJECTIVES of PARENTERAL
CONTROLLED DRUG DELIVERY
SYSTEM
1) Site-specific delivery
2) Reduced side effects
3) Increased bi...
Properties of ideal PCDDS
1.
• Simple to administer and remove
2.
• Inert
3.
• Biocompatible
4.
• Comfortable for the pati...
Advantages & Disadvantages of PCDDS
Advantages
• Improved patient
convenience and
compliance.
• Reduction in fluctuation i...
Routes of administration of PCDDS
1) Intramuscular
2) Subcutaneous
3) Intradermal
4) Intraarticular
5) Intraspinal
6) Intr...
• Drug absorption is controlled by slow dissolution of
drug particle.
• Eg. Formation of salt or complexes with low
aqueou...
DISSOLUTION TYPE DEPOT
FORMULATIONS
• Drug absorption is controlled by slow dissolution of drug
particles.
• Rate of disso...
DISSOLUTION TYPE DEPOT
FORMULATIONS
Formation of salts or
Complexes with Low
solubility.E.g.,
Aqueous
suspensions of
benza...
ADSORPTION-TYPE DEPOT
PREPARATION
• Formed by binding of drug molecules to adsorbents.
• Only unbound, free species of dru...
ENCAPSULATION-TYPE DEPOT
PREPARATIONS
• Prepared by encapsulating drug solids within a permeation
barrier or dispersing dr...
ESTERIFICATION-TYPE DEPOT
PREPARATION
• Esterifying a drug to form a bioconvertible prodrug-type ester.
• Forms a reservoi...
CLASSIFICATION OF PARENTERAL
CONTROLLED DRUG DELIVERY
SYSTEM
INJECTABLE DRUG
DELIVERY
IMPLANTABLE DRUG DELIVERY SYSTEM
1) ...
INJECTABLE DRUG DELIVERY: 1) In situ
forming drug delivery systems (ISFD)
1) THERMOPLASTIC PASTES
Semisolid polymers which...
INJECTABLE DRUG DELIVERY:
2) Solutions
• HIGH VISCOSITY SOLUTIONS
• For comp. with mol. wt. more than 750
• For water sol....
INJECTABLE DRUG DELIVERY:
3) Microspheres
 Each microsphere is basically a matrix of drug dispersed in a
polymer from whi...
INJECTABLE DRUG DELIVERY:
4) Liposomes
 Spherule/vesicle of lipid bilayers enclosing an aqueous
compartment.
 Lipid most...
INJECTABLE DRUG DELIVERY: 5)
Suspension
AQUEOUS SUSPENSIONS
• Given by I.M. or S.C. routes
• Conc. of solids should be 0.5...
INJECTABLE DRUG DELIVERY:
6) Solid liquid nanoparticles
 Nanoparticles are called as nanospheres or nanocapsules
dependin...
IMPLANTABLE DRUG DELIVERY
SYSTEM
1) In-situ forming implant
i. Thermoplastic pastes
ii. In-situ polymer precipitation
2) S...
CLASSIFICATION OF IMPLANTABLE
DRUG DELIVERY SYSTEM
A) Controlled
drug release by
diffusion
1) Membrane
permeation-controll...
A. Controlled drug release by diffusion
Approach Mechanism example
Membrane permeation-
controlled release
Drug encapsulat...
1) Polymer membrane permeation
controlled DDS
 Reservoir is solid drug or dispersion of solid drug in liquid or
solid med...
2) Polymer Matrix diffusion controlled
DDS
 Drug is homogeneously dispersed throughout polymer matrix.
 Polymers used ar...
3) Membrane-Matrix Hybrid type Drug
Delivery Device
 Hybrid of first two
 Minimizes the risk of dose dumping
 Drug rese...
4) Microreservoir Partition Drug Delivery
Device
 Drug reservoir is a
suspension of drug crystals
in an aqueous solution ...
B. Controlled drug release by activation
Approach Mechanism Examples
Osmotic pressure activated Drug reservoir solution or...
1) Osmotic pressure activated
 Osmotic pressure is
used as energy source
 Drug reservoir is either
a solution or semisol...
2) Vapor pressure activated
 Vapor pressure is used as
the power source.
 Drug reservoir is a
solution formulation.
 Fl...
3) Magnetically activated
 Electromagnet is used as power source.
 Drug can be triggered to release at varying rates dep...
C. Controlled drug delivery by feedback
regulated mechanism
Approach Mechanism
Bioerosion regulated Drug dispersed bioerod...
1) Bioerosion regulated
 Releases drug upon activation by hydration of device by tissue
fluid at the implantation site.
...
2) Bioresponse activated
 Release drug upon hydrolysis of polymer base by tissue fluid
at implantation site.
 Polymer us...
RECENT DEVELOPMENTS:
CYCLODEXTRIN
 Lipophilic drug solubilisation for
parenteral use
 These compounds form inclusion
com...
RECENT DEVELOPMENTS:ADEPT
 Active tumour targeting
 It is an Antibody Directed
Enzyme Prodrug Therapy
 An antibody enzy...
RECENT DEVELOPMENTS:POLYMER
DRUG CONJUGATES
 Passive tumour targeting
 These include soluble
polymeric prodrugs of
dauno...
RECENT DEVELOPMENTS: Needle free
injections
 Decreased pain on injection
 Increased bioavailability of intradermal vacci...
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parenteral drug delivery systemsSnehal pdds ppt

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parenteral drug delivery system

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parenteral drug delivery systemsSnehal pdds ppt

  1. 1. PARENTERAL CONTROLLED DRUG DELIVERY SYSTEM Miss. SNEHAL K. DHOBALE M-PHARMACY (2ND SEMISTER) ROLL NO-02 PADM. Dr. D. Y. PATIL COLLEGE OF PHARMACY, AKURDI
  2. 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.  Controlled Release drug delivery systems aim 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 substances with poor bio- availability and the drugs with a narrow therapeutic index  Para: outside  Enteron: intestine (i.e. beside the intestine)
  3. 3. OBJECTIVES of PARENTERAL CONTROLLED DRUG DELIVERY SYSTEM 1) Site-specific delivery 2) Reduced side effects 3) Increased bio-availability 4) Increased therapeutic effectiveness
  4. 4. 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
  5. 5. Advantages & Disadvantages of PCDDS Advantages • Improved patient convenience and compliance. • Reduction in fluctuation in steady-state levels. • Increased 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 • Decreased systemic availability • Poor in vitro-in vivo correlation • Possibility of dose dumping. • Retrieval of drug is difficult in case of toxicity, poisoning or hypersensitivity reactions. • Reduced potential for dosage adjustments. • Higher cost of formulations.
  6. 6. Routes of administration of PCDDS 1) Intramuscular 2) Subcutaneous 3) Intradermal 4) Intraarticular 5) Intraspinal 6) Intrathecal 7) Intracardiac 8) Intrasynovial 9) Intravaginal 10) Intraarterial
  7. 7. • Drug absorption is controlled by slow dissolution of drug particle. • Eg. Formation of salt or complexes with low aqueous solubility, Suspension of Macrocrystals. DISSOLUTION CONTROLLED DEPOT • Binding of drug molecules to adsorbent [Al(OH)3] • Eg. Vaccine preparations ADSORPTION TYPE DEPOT • Encapsulating drug within permeation barrier /dispersing drug particles in a diffusion matrix • Eg. Naltrexone pamoate-releasing biodegradable microcapsule, liposome, & Norethindrone- releasing biodegradable beads. ENCAPSULATION TYPE DEPOT • Esterifying drug to form bioconvertible Prodrug- type ester & then into injection. • Eg. Fluphenazine enanthate, nandrolone decanoate in oleaginous solution. ESTERIFICATION TYPE DEPOT Mechanism:On the basis of different mechanism, depot formulation categorize into four types
  8. 8. DISSOLUTION TYPE DEPOT FORMULATIONS • Drug absorption is controlled by slow dissolution of drug particles. • Rate of dissolution is given by ; where, Sa – Surface area of drug particles Ds – Diffusion coefficient of drug Cs – Saturation solubility of drug hd – Thickness of hydrodynamic diffusion ( Q t )d = SaDsCs hd
  9. 9. DISSOLUTION TYPE DEPOT FORMULATIONS Formation of salts or Complexes with Low solubility.E.g., Aqueous suspensions of benzathine penicillin G. Suspension of macro crystals. E.g., aqueous suspension of testosterone isobutyrate for I.M. administration. Approaches Release of drug molecules is not of zero order kinetics as expected from the theoretical model. Surface area Sa of drug particles diminishes with time. The saturation solubility Cs of the drug at the injection site cannot be easily maintained. Drawbacks
  10. 10. ADSORPTION-TYPE DEPOT PREPARATION • Formed by binding of drug molecules to adsorbents. • Only unbound, free species of drug is available for absorption. • Equilibrium conc. of free, unbound drug species (C)f is determined by the Langmuir relationship. • E.g., - Vaccine preparations 1 a(C)b.m (C)f (C)b = + (C)f (C)b,m
  11. 11. ENCAPSULATION-TYPE DEPOT PREPARATIONS • Prepared by encapsulating drug solids within a permeation barrier or dispersing drug particles in a diffusion matrix. • Membrane – biodegradable or bioabsorbable macromolecules • Gelatin, Dextran, polylactate, lactide-glycolide copolymers, phospholipids, and long chain fatty acids and glycerides. • E.g., Naltrexone pamoate-releasing biodegradable microcapsules. • Release of drug molecules is controlled by i. Rate of permeation across the permeation barrier ii. The rate of biodegradation of the barrier macromolecules
  12. 12. ESTERIFICATION-TYPE DEPOT PREPARATION • Esterifying a drug to form a bioconvertible prodrug-type ester. • Forms a reservoir at the site of injection. • Rate of absorption is controlled by 1) Interfacial partitioning of drug esters from reservoir to tissue fluid. 2) Rate of bioconversion of drug esters to regenerate active drug molecules. • E.g., Fluphenazine enanthate, nandrolone decanoate, and testosterone 17B-cyprionate in oleaginous solution.
  13. 13. CLASSIFICATION OF PARENTERAL CONTROLLED DRUG DELIVERY SYSTEM INJECTABLE DRUG DELIVERY IMPLANTABLE DRUG DELIVERY SYSTEM 1) In situ forming drug delivery systems (ISFD) i) Thermoplastic pastes ii) In situ cross linked systems iii) In situ polymer precipitation iv) Thermally induced gelling system v) In situ solidifying organogels. 2) Solutions 3) Microspheres 4) Liposomes 5) Suspension 6) Solid liquid nanoparticles 1) In-situ forming implant i. Thermoplastic pastes ii. In-situ polymer precipitation 2) Solid Implants i. ALZET osmotic pump ii. DUROS infusion implant
  14. 14. INJECTABLE DRUG DELIVERY: 1) In situ forming drug delivery systems (ISFD) 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 (thermosets) /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 >15% w/w were injected 5) IN SITU SOLIDIFYING ORGANOGELS Water insoluble amphiphilic lipids, which swell in water and forms various types of lyotropic liquid crystals.
  15. 15. INJECTABLE DRUG DELIVERY: 2) Solutions • HIGH VISCOSITY SOLUTIONS • For comp. with mol. wt. more than 750 • For water sol. drugs • Gelling agents or viscosity enhancers are used • COMPLEX FORMULATIONS • Drug forms dissociable complex with macromolecule • Fixed amount of drug gets complexed • Given by I.M. route Aqueous solutions • 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 dug action as compared to oil solution and aqueous suspension. • E.g., Penicillin G procaine in vegetable oil Oil suspensi ons
  16. 16. INJECTABLE DRUG DELIVERY: 3) 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. 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 such as LHRH which have short half-lives.  Magnetic microspheres are developed for promoting drug targeting which are infused into an artery.  Magnet is placed over the area to localize it in that region.
  17. 17. INJECTABLE DRUG DELIVERY: 4) Liposomes  Spherule/vesicle of lipid bilayers enclosing an aqueous compartment.  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., S.C., for controlled rate release.  Can be given by I.V. for targeted delivery.
  18. 18. INJECTABLE DRUG DELIVERY: 5) Suspension AQUEOUS SUSPENSIONS • Given by I.M. or S.C. routes • Conc. of solids should be 0.5 to 5 % • Particle size should be < 10 μm • Drug is continuosly dissolving to replenish the lost. • For oil soluble drugs • Only crystalline and stable polymorphic drugs are given by this form • Viscosity builders can be used. • E.g., Crystalline zinc insulin OIL SUSPENSIONS • 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 dug action as compared to oil solution and aqueous suspension. • E.g., Penicillin G procaine in vegetable oil
  19. 19. INJECTABLE DRUG DELIVERY: 6) Solid liquid nanoparticles  Nanoparticles are called as nanospheres or nanocapsules depending upon the position of drugs  Polymer used are biodegradable ones.  Polyacrylic acid, polyglycolic acid  For selective targeting therapy
  20. 20. IMPLANTABLE DRUG DELIVERY SYSTEM 1) In-situ forming implant i. Thermoplastic pastes ii. In-situ polymer precipitation 2) Solid Implants i. ALZET osmotic pump ii. DUROS infusion implant
  21. 21. CLASSIFICATION OF IMPLANTABLE DRUG DELIVERY SYSTEM A) Controlled drug release by diffusion 1) Membrane permeation-controlled release system 2) Matrix diffusion- controlled release system 3) Micro-reservoir dissolution-controlled release system 4) Membrane matrix hybrid type-controlled release system B) Controlled drug release by activation 1) Osmotic pressure activated eg.- Alzet pump 2) Vapour pressure activated eg.- Infusaid pump 3) Magnetically activated 4) Phonophoresis 5) Hydrolysis activated eg.- for control release of levonorgestrel (poly ortho esters used) 6) Hydration activated eg.- Hydron implant C) Controlled drug delivery by feedback regulated mechnism 1) Bioerosion regulated drug delivery system 2) Bioresponse activated drug delivery system
  22. 22. A. Controlled drug release by diffusion Approach Mechanism example Membrane permeation- controlled release Drug encapsulated in capsule / spherical compartment Norplant subdermal implant Matrix diffusion-controlled release Homogenous dispersion of drug in lipophilic/ hydrophilic polymer matrix Compudose implant Micro-reservoir dissolution- controlled release Drug in suspension in aqueous solution of water miscible polymer forms dispersion of drug reservoir in polymer matrix Syncro mate implant Membrane matrix hybrid type-controlled release Hybrid of polymer membrane permeation controlled DDS and Polymer matrix diffusion controlled DDS Norplant II
  23. 23. 1) Polymer membrane permeation controlled DDS  Reservoir is solid drug or dispersion of solid drug in liquid or solid medium.  Drug enclosed in reservoir and reservoir is enclosed in rate limiting polymeric membrane.  Encapsulation of drug in reservoir can be done by encapsulation, microencapsulation, extrusion, molding or any other technique.  E.g., Norplant Subdermal Implant Polymeric membrane nonporous microporous semipermeable
  24. 24. 2) Polymer Matrix diffusion controlled DDS  Drug is homogeneously dispersed throughout polymer matrix.  Polymers used are :  Lipophilic polymers  Hydrophilipic polymers  Porous  Decreasing release with time  E.g., Compudose implant
  25. 25. 3) Membrane-Matrix Hybrid type Drug Delivery Device  Hybrid of first two  Minimizes the risk of dose dumping  Drug reservoir is homogeneous dispersion of drug solids throughout a polymer matrix, and is further encapsulated by polymeric membrane  E.g., Norplant II Subdermal Implant
  26. 26. 4) Microreservoir Partition Drug Delivery Device  Drug reservoir is a suspension of drug crystals in an aqueous solution of polymer.  Device is further coated with layer of biocompatible polymer.  Polymer used for matrix : water soluble polymers  Polymer used for coating : semipermeable polymer
  27. 27. B. Controlled drug release by activation Approach Mechanism Examples Osmotic pressure activated Drug reservoir solution or semisolid placed within semipermeable housing with controlled water permeability Alzet osmotic pump Vapour pressure activated Drug reservoir is solution is placed inside infusate chamber Infusaid pump Magnetically activated Magnetic wave triggering mechanism is incorporated into drug delivery device Hydrolysis activated Solid drug is homogenously dispersed throughout polymer matrix of bioerodible or biodegradable polymer Levonorgestrel using Poly ortho esters biodegradable polymer Hydration activated Solid drug is coated by hydrophilic polymer Hydron implant
  28. 28. 1) Osmotic pressure activated  Osmotic pressure is used as energy source  Drug reservoir is either a solution or semisolid formulation  Cellulosic outer membrane  Polyester internal membrane
  29. 29. 2) Vapor pressure activated  Vapor pressure is used as the power source.  Drug reservoir is a solution formulation.  Fluid which vaporizes at body temperature is used such as fluorocarbon. E.g., Infusaid Pump for Heparin.
  30. 30. 3) Magnetically activated  Electromagnet is used as power source.  Drug can be triggered to release at varying rates depending upon the magnitude and the duration of electromagnetic energy applied.  A tiny donut shaped magnet at the centre of medicated polymer matrix that contains a homogeneous dispersion of drug  It has low polymer permeability
  31. 31. C. Controlled drug delivery by feedback regulated mechanism Approach Mechanism Bioerosion regulated Drug dispersed bioerodible matrix fabricated with polymer coated with immobilised urease Bioresponse activated Drug enclosed in bioresponsive polymer whose permeability is controlled by concentration of biochemical agent in tissue
  32. 32. 1) Bioerosion regulated  Releases drug upon activation by hydration of device by tissue fluid at the implantation site.  Hydrohilic polymer is used for formulation which becomes swollen upon hydration.  Drug gets released by diffusing through the water saturated pore channels in the swollen polymer matrix.  E.g., Norgestomet releasing Hydron Implant
  33. 33. 2) Bioresponse activated  Release drug upon hydrolysis of polymer base by tissue fluid at implantation site.  Polymer used is bioerodible or biodegradable polymer.  Pellet or bead shaped implant.  Rate of drug release is determined by rate of biodegradation, polymer composition and mol. Wt., drug leading and drug polymer interactions.  Erosion rate is controlled by using a buffering agent.
  34. 34. RECENT DEVELOPMENTS: CYCLODEXTRIN  Lipophilic drug solubilisation for parenteral use  These compounds form inclusion complexes with hydrophobic guest molecule  Modfied cyclodextrins such as hydroxypropyl b-cyclodextrin and sulphobutyl b-cyclodextrins are regardedas safe for parentral use
  35. 35. RECENT DEVELOPMENTS:ADEPT  Active tumour targeting  It is an Antibody Directed Enzyme Prodrug Therapy  An antibody enzyme conjugate is administered intravenously , localises in tumour tissue and subsequently activates an administered prodrug predominantly within such tumours
  36. 36. RECENT DEVELOPMENTS:POLYMER DRUG CONJUGATES  Passive tumour targeting  These include soluble polymeric prodrugs of daunorudicin, doxorubicin, cisplatin and 5- flurouracil  These PDC accumulate selectively within tumour tissues
  37. 37. RECENT DEVELOPMENTS: Needle free injections  Decreased pain on injection  Increased bioavailability of intradermal vaccines

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