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BY
Mr. Debasis Gantayat
SAP ID- 1000018087
M Pharm Pharmaceutics
 INTRODUCTION
 GENERAL ANATOMY OF EYE
 DRUG DELIVERY SYSTEM TO EYE
 TYPES OF ODDS
 ADVANTAGES
 DISADVANTAGES
 CONCLUSION
INTRODUCTION
 DRUG DELIVERY SYSTEM-
It is a formulation or a device which brings the drug to a specific site of the body at a certain
rate to achieve an effective concentration at the site of drug action.
Mainly used to carry the drug components to the targeted part of the body without
reaching non target tissues and organs.
 OBJECTIVES-
 Increase patient compliance
 Enhance drug efficacy
 Cornea(Transparent part of the eye)
 Iris(coloured part of the eye)
 Pupil(the round opening at the centre of the
eye)
 Lens(serves to transmit light to retina)
 Vitreous body(clear gel fills the space
between the lens and retina)
 Retina(contains millions of light sensitive
cells)
 Optic nerve(a bundle of nerve carries visual
images)
OCULAR DRUG DELIVERY
SYSTEM
 Definition-
 Ocular drug delivery system (ODDS) is a dosage form or system intended for
installing and administering the drug /medicine to eye against any disease or
disorder.
 The most common disease or disorders that require ODDS are glaucoma, cataract,
infection on the ocular surface, inflammation, dry eye syndrome etc..
 By the ODDS either the drug can be curable or provide a short term relief to various
diseases.
 Non irritative and non-toxic
 Prolong contact time with corneal tissue
 Non greasy
 Patient compliance
 Must have good corneal penetration
 Eye drops
 Eye ointments
 Eye lotions
 Ocuserts
 Hydrogel contact lens
TYPES
 CONVENTIONAL DRUG DELIVERY SYSTEM
 Eye drops
 Ointments and gels
 Ocuserts
 VESICULAR SYSTEM
 Liposomes
 CONTROLL DRUG DELIVERY SYSTEM
 Implants
 Dendrimer
 Nanosuspension
 microneedles
 NANOPARTICLES AND MICROPARTICLES
CONVENTIONAL DRUG DELIVERY SYSTEM-
EYEDROPS-
 Applied directly to the surface of the eye
 Contains saline and one or more medications
 Less risk of side effects
 Shelf life- no longer then three months after opening
 Drawbacks- redness of eye, widened pupils
OINTMENTS AND GELS-
 Prolonged drug contact time with external ocular surface can be achieved
 Shelf life- 1 to 3 months
 Drawbacks- blurring vision, matting of eyelids
OCUSERTS
 Sterile preparations placed in conjunctival sac
 Delivers drug at constant rate by diffusion mechanism
 The device consist of three layers
1. Outer layer
2. Inner core
3. A retaining ring
 Two types-
 Insoluble Ocuserts
 Soluble Ocuserts
RESERVOIR SYSTEM
 The reservoir system can release drug
either by diffusion or by an osmotic
process.
 It mainly contains a liquid, a gel, a
colloid, a semisolid, a solid matrix and
a carrier containing drug.
 The carriers are made up of
hydrophobic, hydrophilic, organic,
natural or synthetic polymers.
MATRIX SYSTEM
 The matrix system can be represented
by contact lens.
 It comprises of a covalently cross-
linked polymer that forms a three
dimensional network capable of
retaining water, aqueous drug solution
or solid components.
 The hydrophilic or hydrophobic
polymers swells by absorbing water.
 Offers the advantages of being entirely soluble
 Need not to be removed from the site of application
 Natural polymer-
 Collagen is mainly used
 As the collagen dissolves, the drug binds between the collagen is gradually released.
 Synthetic and semi-synthetic polymer-
 Semi-synthetic polymers such as cellulose derivatives are mainly used.
VESICULAR SYSTEM
 LIPOSOMES-
 It is used for the effective drug delivery to the posterior chamber of the eye.
 These are biodegradable and biocompatible lipid vesicles made up of natural lipids
and about 25-10000 nm in diameter.
 They are having an intimate contact with the corneal and conjunctival surfaces which
is desirable for drugs that are
 poorly absorbed
 With low partition coefficient
 Poor solubility
 With high molecular weights
 They can contain a wide range of both hydrophilic and hydrophobic therapeutic
agents.
Continue…
 Liposomes have good effectiveness for
both the anterior and posterior segment
of eye.
 LIMITATIONS-
 Chemical instability
 Oxidative degradation of phospholipids
 The cost of natural phospholipids
Continue…
 NIOSOMES-
 Non ionic surfactant vesicles that have potential
applications in the delivery of hydrophobic and
amphiphilic drugs.
 They are chemically as stable as liposomes and can
entrap both hydrophobic and hydrophilic drugs.
 Non toxic and don't require any special handling
technique.
CONTROL DRUG DELIVERY SYSTEM
 IMPLANTS-
• It is of two types
• Biodegradable implants
• Non-biodegradable implants
• Biodegradable implants- Implants containing biodegradable polymers and here the
drug is released during polymer degradation.
• Non-biodegradable implants- Can be presented in form of matrix and reservoir
system.
• Matrix system- here the drug is dispersed homogenously in the polymeric matrix.
• Reservoir system-here the drug is surrounded by a non degradable membrane which can control
the diffusion of drug.
 The dendrimer generally means a synthetic
polymer with a structure of repeatedly
branching chains.
 It can enhance the drugs water solubility and
bioavailability.
 They also have permeable enhancer
properties.
 Here is a schematic representation of drug
entrapped in dendrimers.
 NANO-SUSPENSIONS
 They basically enhance the rate and extent of drug
absorption and also increase the duration of drug effect.
 There are various techniques used for the commercial
preparation of the nanosuspensions.
 MICRONEEDLES
 They had shown prominent in-vitro penetration in to sclera
and rapid dissolution of coating solution after insertion.
NANOPARTICLES AND
MICROPARTICLES
 The maximum size limit for nanoparticles are 5-10mm above which itching occurs
upon installation.
 The nanoparticles are prepared by using various bio adhesive polymers to provide
sustained effect to the entrapped drugs.
 These are mainly designed to
 Overcome the barriers
 Increase the drug penetration at the target site
 Increase the drug retention for controlled delivery.
EVALUATION OF ODDS
Thickness of the film
Drug content uniformity
Uniformity of weight
Percentage moisture absorption
Percentage moisture loss
INVITRO EVALUATION METHODS-
 Bottle method
 Diffusion method
Accelerated stability study
 THICKNESS OF THE FILM-
Measured the thickness at different points and the mean value is calculated.
 DRUG CONTENT UNIFORMITY-
The cast film cut at different places and tested for drug as per monograph.
 UNIFORMITY OF WEIGHT-
Three patches are weighed.
 PERCENTAGE MOISTURE ABSORPTION-
Here the ocular films were weighed and placed in a desiccator containing
1. 100ml of saturated solution of aluminum chloride
2. 75% of humidity was maintained.
After 3 days the ocular films were reweighed and percentage moisture absorbed is
calculated.
initial weight –final weight
Percentage moisture absorbed= x 100
initial weight
 PERCENTAGE MOISTURE LOSS-
Ocular films are weighed and kept in desiccator containing anhydrous calcium
chloride.
After 3 days, the film were reweighed and percentage loss in moisture is calculated
using ..
initial weight – final weight
Percentage moisture loss= x 100
initial weight
 BOTTLE METHOD-
Here the dosage forms are placed in a bottle containing dissolution medium
maintained at specified temperature and pH.
The bottle is then shaken and sample is taken at appropriate intervals and analyzed.
 DIFFUSION MEHOD-
Drug solution is placed in donor compartment and buffer medium is placed in
between donor and receptor compartment.
Drug diffused in receptor compartment is measured in different time intervals.
 Carried out to predict the breakdown that may occur over period of time.
 Here the dosage form is kept at elevated temperature or humidity or intensity of light
or oxygen.
 Then after regular interval of time the sample is taken and analyzed for drug content.
 From the result graphical data is plotted and self life and expiry date are determined.
ADVANTAGES OF ODDS
Improve bioavailability by increasing ocular resistance
Providing a prolonged drug release
Increase self life with respect to aqueous solutions
Less visual and systemic side effects
Better patient compliance
Having quick absorption and effect
DISADVANTAGES
Foreign body sensation
High cost
Unwanted migration of the implants inside the eye
Interference with vision
Difficulty in the insertion of ocular implants
Necessity of using preservative
CONCLUSION
 The controlled ocular drug delivery systems increase the efficacy of the drug
by reducing its wastage and by enhancing absorption by increasing contact
time of drug to the absorbing surface.
 This improve patient compliance by reducing the frequency of dosing.
 As they reduce the frequency of dosing, the adverse effect of the drug is
minimalized.
 How vision works-
 https://www.youtube.com/watch?v=s0B_CiOEXSI
 Detailed explanation of ocular drug delivery system-
 https://www.youtube.com/watch?v=46luf1uwwfE&t=3s
 https://www.youtube.com/watch?v=4L8kUNdtRnM
 https://www.youtube.com/watch?v=Vd2zRLWQ1sg
 Ocuserts-
 https://www.youtube.com/watch?v=_OOFuyjuW6s
OCCULAR DRUG DELIVERY SYSTEM.pptx

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OCCULAR DRUG DELIVERY SYSTEM.pptx

  • 1. BY Mr. Debasis Gantayat SAP ID- 1000018087 M Pharm Pharmaceutics
  • 2.  INTRODUCTION  GENERAL ANATOMY OF EYE  DRUG DELIVERY SYSTEM TO EYE  TYPES OF ODDS  ADVANTAGES  DISADVANTAGES  CONCLUSION
  • 3. INTRODUCTION  DRUG DELIVERY SYSTEM- It is a formulation or a device which brings the drug to a specific site of the body at a certain rate to achieve an effective concentration at the site of drug action. Mainly used to carry the drug components to the targeted part of the body without reaching non target tissues and organs.  OBJECTIVES-  Increase patient compliance  Enhance drug efficacy
  • 4.  Cornea(Transparent part of the eye)  Iris(coloured part of the eye)  Pupil(the round opening at the centre of the eye)  Lens(serves to transmit light to retina)  Vitreous body(clear gel fills the space between the lens and retina)  Retina(contains millions of light sensitive cells)  Optic nerve(a bundle of nerve carries visual images)
  • 5.
  • 6. OCULAR DRUG DELIVERY SYSTEM  Definition-  Ocular drug delivery system (ODDS) is a dosage form or system intended for installing and administering the drug /medicine to eye against any disease or disorder.  The most common disease or disorders that require ODDS are glaucoma, cataract, infection on the ocular surface, inflammation, dry eye syndrome etc..  By the ODDS either the drug can be curable or provide a short term relief to various diseases.
  • 7.  Non irritative and non-toxic  Prolong contact time with corneal tissue  Non greasy  Patient compliance  Must have good corneal penetration
  • 8.  Eye drops  Eye ointments  Eye lotions  Ocuserts  Hydrogel contact lens
  • 9. TYPES  CONVENTIONAL DRUG DELIVERY SYSTEM  Eye drops  Ointments and gels  Ocuserts  VESICULAR SYSTEM  Liposomes  CONTROLL DRUG DELIVERY SYSTEM  Implants  Dendrimer  Nanosuspension  microneedles  NANOPARTICLES AND MICROPARTICLES
  • 10. CONVENTIONAL DRUG DELIVERY SYSTEM- EYEDROPS-  Applied directly to the surface of the eye  Contains saline and one or more medications  Less risk of side effects  Shelf life- no longer then three months after opening  Drawbacks- redness of eye, widened pupils OINTMENTS AND GELS-  Prolonged drug contact time with external ocular surface can be achieved  Shelf life- 1 to 3 months  Drawbacks- blurring vision, matting of eyelids
  • 11. OCUSERTS  Sterile preparations placed in conjunctival sac  Delivers drug at constant rate by diffusion mechanism  The device consist of three layers 1. Outer layer 2. Inner core 3. A retaining ring  Two types-  Insoluble Ocuserts  Soluble Ocuserts
  • 12. RESERVOIR SYSTEM  The reservoir system can release drug either by diffusion or by an osmotic process.  It mainly contains a liquid, a gel, a colloid, a semisolid, a solid matrix and a carrier containing drug.  The carriers are made up of hydrophobic, hydrophilic, organic, natural or synthetic polymers. MATRIX SYSTEM  The matrix system can be represented by contact lens.  It comprises of a covalently cross- linked polymer that forms a three dimensional network capable of retaining water, aqueous drug solution or solid components.  The hydrophilic or hydrophobic polymers swells by absorbing water.
  • 13.  Offers the advantages of being entirely soluble  Need not to be removed from the site of application  Natural polymer-  Collagen is mainly used  As the collagen dissolves, the drug binds between the collagen is gradually released.  Synthetic and semi-synthetic polymer-  Semi-synthetic polymers such as cellulose derivatives are mainly used.
  • 14. VESICULAR SYSTEM  LIPOSOMES-  It is used for the effective drug delivery to the posterior chamber of the eye.  These are biodegradable and biocompatible lipid vesicles made up of natural lipids and about 25-10000 nm in diameter.  They are having an intimate contact with the corneal and conjunctival surfaces which is desirable for drugs that are  poorly absorbed  With low partition coefficient  Poor solubility  With high molecular weights  They can contain a wide range of both hydrophilic and hydrophobic therapeutic agents.
  • 15. Continue…  Liposomes have good effectiveness for both the anterior and posterior segment of eye.  LIMITATIONS-  Chemical instability  Oxidative degradation of phospholipids  The cost of natural phospholipids
  • 16. Continue…  NIOSOMES-  Non ionic surfactant vesicles that have potential applications in the delivery of hydrophobic and amphiphilic drugs.  They are chemically as stable as liposomes and can entrap both hydrophobic and hydrophilic drugs.  Non toxic and don't require any special handling technique.
  • 17. CONTROL DRUG DELIVERY SYSTEM  IMPLANTS- • It is of two types • Biodegradable implants • Non-biodegradable implants • Biodegradable implants- Implants containing biodegradable polymers and here the drug is released during polymer degradation. • Non-biodegradable implants- Can be presented in form of matrix and reservoir system. • Matrix system- here the drug is dispersed homogenously in the polymeric matrix. • Reservoir system-here the drug is surrounded by a non degradable membrane which can control the diffusion of drug.
  • 18.  The dendrimer generally means a synthetic polymer with a structure of repeatedly branching chains.  It can enhance the drugs water solubility and bioavailability.  They also have permeable enhancer properties.  Here is a schematic representation of drug entrapped in dendrimers.
  • 19.  NANO-SUSPENSIONS  They basically enhance the rate and extent of drug absorption and also increase the duration of drug effect.  There are various techniques used for the commercial preparation of the nanosuspensions.  MICRONEEDLES  They had shown prominent in-vitro penetration in to sclera and rapid dissolution of coating solution after insertion.
  • 20. NANOPARTICLES AND MICROPARTICLES  The maximum size limit for nanoparticles are 5-10mm above which itching occurs upon installation.  The nanoparticles are prepared by using various bio adhesive polymers to provide sustained effect to the entrapped drugs.  These are mainly designed to  Overcome the barriers  Increase the drug penetration at the target site  Increase the drug retention for controlled delivery.
  • 21. EVALUATION OF ODDS Thickness of the film Drug content uniformity Uniformity of weight Percentage moisture absorption Percentage moisture loss INVITRO EVALUATION METHODS-  Bottle method  Diffusion method Accelerated stability study
  • 22.  THICKNESS OF THE FILM- Measured the thickness at different points and the mean value is calculated.  DRUG CONTENT UNIFORMITY- The cast film cut at different places and tested for drug as per monograph.  UNIFORMITY OF WEIGHT- Three patches are weighed.
  • 23.  PERCENTAGE MOISTURE ABSORPTION- Here the ocular films were weighed and placed in a desiccator containing 1. 100ml of saturated solution of aluminum chloride 2. 75% of humidity was maintained. After 3 days the ocular films were reweighed and percentage moisture absorbed is calculated. initial weight –final weight Percentage moisture absorbed= x 100 initial weight
  • 24.  PERCENTAGE MOISTURE LOSS- Ocular films are weighed and kept in desiccator containing anhydrous calcium chloride. After 3 days, the film were reweighed and percentage loss in moisture is calculated using .. initial weight – final weight Percentage moisture loss= x 100 initial weight
  • 25.  BOTTLE METHOD- Here the dosage forms are placed in a bottle containing dissolution medium maintained at specified temperature and pH. The bottle is then shaken and sample is taken at appropriate intervals and analyzed.  DIFFUSION MEHOD- Drug solution is placed in donor compartment and buffer medium is placed in between donor and receptor compartment. Drug diffused in receptor compartment is measured in different time intervals.
  • 26.  Carried out to predict the breakdown that may occur over period of time.  Here the dosage form is kept at elevated temperature or humidity or intensity of light or oxygen.  Then after regular interval of time the sample is taken and analyzed for drug content.  From the result graphical data is plotted and self life and expiry date are determined.
  • 27. ADVANTAGES OF ODDS Improve bioavailability by increasing ocular resistance Providing a prolonged drug release Increase self life with respect to aqueous solutions Less visual and systemic side effects Better patient compliance Having quick absorption and effect
  • 28. DISADVANTAGES Foreign body sensation High cost Unwanted migration of the implants inside the eye Interference with vision Difficulty in the insertion of ocular implants Necessity of using preservative
  • 29. CONCLUSION  The controlled ocular drug delivery systems increase the efficacy of the drug by reducing its wastage and by enhancing absorption by increasing contact time of drug to the absorbing surface.  This improve patient compliance by reducing the frequency of dosing.  As they reduce the frequency of dosing, the adverse effect of the drug is minimalized.
  • 30.  How vision works-  https://www.youtube.com/watch?v=s0B_CiOEXSI  Detailed explanation of ocular drug delivery system-  https://www.youtube.com/watch?v=46luf1uwwfE&t=3s  https://www.youtube.com/watch?v=4L8kUNdtRnM  https://www.youtube.com/watch?v=Vd2zRLWQ1sg  Ocuserts-  https://www.youtube.com/watch?v=_OOFuyjuW6s