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Similar to Occular dds by pradipkumar rathod
Occular dds by pradipkumar rathod
- 1. PRESENTED BY :MR. PRADIPKUMAR G. RATHOD M. PHARM 1ST YEAR (1ST SEM.) (PHARMACEUTICS) UNIVERSITY DEPARTMENT OF PHARMACEUTICAL SCIENCES, R.T.M. NAGPUR UNIVERSITY, NAGPUR. 1
- 2. Introduction : Ocular administrationof drug is primarily associated with the need to treat ophthalmic diseases. Eye is the most easily accessible site for topical administration of a medication. Ideal ophthalmic drug delivery must be able to sustain the drug release and to remain in the vicinity of front of the eye for prolong period of time. Composition of eye Water - 98%, Solid -1.8%, Organic element – Protein - 0.67%, sugar - 0.65%, NaCl - 0.66% ,Other mineral element sodium, potassium and ammonia - 0.79%. 2
- 3. Routes of occulardrug delivery 3
- 4. Factors affecting intraocularbioavailability: 1. Inflow & outflow of lacrimal fluids. 2. Efficient naso-lacrimal drainage. 3. Interaction of drug with proteins of lacrimal fluid. 4. dilution with tears. 5. Corneal barriers. 6. Active ion transport at cornea. 4
- 5. IDEAL OPHTHALMIC DELIVERYSYSTEM Good corneal penetration. Prolong contact time with corneal tissue. Simplicity of instillation for the patient. Non irritative and comfortable form Appropriate rheological properties 5
- 6. 6 OCULAR DRUG DELIVERYSYSTEMS CONTROLLED DELIVERY SYSTEMS Implants Hydrogels Dendrimers Iontophorosis Contact lenses Nano suspensions Micro emulsions Mucoadhesive PARTICULATE SYSTEMS Nano particles Micro particles VESICULAR DELIVERY SYSTEMS Liposomes Neosomes Pharmacosomes discomes ADVANCED DELIVERY SYSTEMS Scleral plugs Gene therapy Stem cell CONVENTIONAL DOSAGE FORMS SOLUTIONS GELS OINTMENTS SUSPENSIONS EYE DROPS RETRO METABOLIC DELIVERY SYSTEMS Softdrug approach Chemical delivery systems
- 7. 7 LIMITATIONS OF CONVENTIONAL •Rapid precorneal elimination • Solution drainage by gravity • Frequent instillation is necessary • Conjuctival absorption ADVANTAGES OF AVANCED DUG DELIVERY • Sustained and/or controlled drug release • Site-specific targeting • Protect the drug from chemical or enzymatic hydrolysis • Increasing contact time and thus improving bioavailability • Better patient compliance.
- 8. Use of mucoadhesivesin ocular drug delivery Polymereric mucoadhesive vehicle: Retained in the eye due to non-covalent bonding with conjuctival mucine. Mucine is capable of picking of 40-80 times of weight of water. Thus prolongs the residence time of drug in the conjuctival sac. • Mucoadhesives contain the dosage form which remains adhered to cornea until the polymer is degraded or mucus replaces itself. • Types- 1. Naturally Occurring Mucoadhesives- Lectins, Fibronectins 2. Synthetic Mucoadhesives- PVA, Carbopol, carboxy methyl cellulose, cross-linked polyacrylic acid • Drugs incarporated in to this are pilocarpine, lidocaine, benzocaine and prednisolone acetate. 8
- 9. 9 • The polymerundergoes swelling in water, • Entanglement of the polymer chains with mucin on the epithelial surface. • The un-ionized carboxylic acid residues on the polymer form hydrogen bonds with the mucin. • The water-swellable yet water insoluble systems are preferred. Mechanism of mucoadhesion
- 10. Vesicular system forocular drug delivery LIPOSOMES • Vesicle composed of phospholipid bilayer enclosing aqueous compartment in alternate fashion. • Biodegradable, Non-toxic in nature. • Polar drugs are incorporated in aqeous compartment while lipophilic drugs are intercalated into the liposomemembrane •Phospholipids used- Phosphotidylcholine, Phosphotidicacid, Sphingomyline, Phosphotidyleserine, Cardiolipine. 10 Endocytosis Fusion
- 11. 11 ADVANTAGES •Drugs delivered intactto various body tissues. •Liposomes can be used for both hydrophilic and hydrophobic drug. •Possibility of targeting and decrease drug toxicity. •The size, charge and other characteristics can be altered according to drug and desired tissue. DISADVANTAGES •Their tendency to be uptaken by RI system. •They need many modification for drug delivery to special organs. •Cost
- 12. NEOSOMES Niosomes arenon-ionic surfactant based multilamellar (>0.05μm), small Unilamellar (0.025-0.05μm) or large unilamellar vesicles (>0.1μm) in which an aqueous solution of solute(s) is entirely enclosed by a membrane resulted from organization of surfactant macromolecules as bilayers STRUCTURAL COMPONENTS USED • Surfactants (dialkyl polyoxy ethylene ether non ionic surfactant) • Cholesterol. 12
- 13. 13 •ADVANTAGES: •The vesicle suspensionbeing water based offers greater patient compliance over oil based systems •Since the structure of the niosome offers place to accommodate hydrophilic, lipophilic as well as ampiphilic drug moieties, they can be used for a variety of drugs. •The characteristics such as size, lamellarity etc. of the vesicle can be varied depending on the requirement. •The vesicles can act as a depot to release the drug slowly and offer a controlled release. •They are osmotically active and stable. •They increase the stability of the entrapped drug •Improves therapeutic performance of the drug by protecting it from the biological environment and restricting effects to target cells, thereby reducing the clearance of the drug. •DISADVANTAGES: • Physical instability, Aggregation, Leaking of entrapped drug, Fusion.
- 14. 14 Advantages of vesicularsystems 1. No difficulty of insertion as in the case of ocular inserts 2. No tissue irritation and damage as caused by penetration enhancers 3. Provide patient compliance as there is no difficulty of insertion as observed in the case of inserts 4. The vesicular carriers are biocompatable and have minimum side effects 5. Degradation products formed after the release of drugs are biocompatable 6. They prevent the metabolism of drugs from the enzymes present at tear/corneal epithelium interface 7. Provide a prolong and sustained release of drug
- 15. CONTROLLED RELEASEOCULAR DEVICES 15 INSERTS: • Ophthalmic inserts are solid devices intended to be placed in the conjunctival sac and to deliver the drug at a comparatively slow rate • Increased ocular permeation with respect to standard vehicles, hence prolonged drug activity and a higher drug bioavailability; • Accurate dosing -theoretically, all of the drug is retained at the absorption site; • Capacity to provide, in some cases, a constant rate of drug release. • Nonerodible Inserts OCUSERTS: • Flexible, oval inserts • Consists of a medicated core reservior prepared out of hydrogel polymer sandwiched between two sheets of transperant lipophilic, rate controlling polymer like ethylene/vinyl acetate copolymer membrane.
- 16. 16 CONTACT LENS : •The most widely used Material is poly-2 hydroxyethylmethacrylate. • Its copolymers with PVP are used to correct eyesight , hold and deliver drugs. • Controlled release can be obtained by binding the active ingredient via biodegradable covalent linkages. Erodible Inserts LACRISERT: • It is a sterile ophthalmic insert use in treatment of dry eye syndrome. • The insert is composed of 5mg of HPC in rod-shaped form about 1.27 mm diameter by about 3.5 m long MINIDISC: • It is made up of counter disc with convex front & concave back surface in contact with eye ball. • Composition: silicon based pre polymer Hydrophillic or hydrophobic.
- 17. INTRAOCULAR INJECTIONS 17 •Micro needle used to deliver drug to posterior segment as an alternative to topical route. • It shows excellent in vitro penetration into sclera and rapid dissolution of coating solution after insertion. In-vivo drug level was found to be significantly higher than the level observed following topical drug administration. • To deliver anti-infective, corticosteroids and anesthetic product to achieve higher therapeutic condition intraocularly, FDA approved intraocular Injections includes miotics, viscoelastics, and anti-viral agents for intravitreal injection
- 18. INTRAOCULAR IMPLANTS 18 •It employed to extend the release in ocular fluids and tissues particularly in the posterior segment. It may be biodegradable and non-biodegradable. • With implants, the delivery rate could be modulated by varying polymer composition. • Implants can be in the form of solid, semi-solid or particulate based delivery systems. These implants have been applied in the treatment of diseases affecting both anterior and posterior segments of the eye. • Implant containing gancyclovir or, anti-neoplastic agents is release drug over a 5 to 8 months.
- 19. CONCLUSION 19 • Themain efforts in ocular drug delivery is to prolong the residence time of drugs • The development of ophthalmic drug delivery systems is easy because we can easily target the eye to treat ocular diseases the eye has specific characteristics such as eye protecting mechanism, which make ocular delivery systems extremely difficult. • The most widely developed drug delivery system is represented by the conventional and non- conventional ophthalmic formulations to polymeric hydrogels, nanoparticle, nanosuspensions, microemulsions, iontophorosis and ocular inserts. • In future an ideal system should be able to achieve an effective drug concentration at the target tissue for an extended period of time, while minimizing systemic exposure and the system should be both comfortable and easy to use.
- 20.