Ophthalmic Drug Delivery Systems - part 8 docx

... analogue, 1- desamino -8 - D-arginine-vasopressin (dDAVP), in human intestinal epithelialcell line, CaCO-2, Int. J. Pharm., 64: 181 .43. Amidon, G. L., Sinko, P. J., Hu, M., and Leesman, G. D. (1 989 ). ... rhodop-sin mutation were protected from apoptosis by recombinant adeno-associated virus-mediated production of fibroblast growth factors fgf-2,fgf-5, and fgf- 18 (30,31), while lens epithelium-derived ... nearfuture. We hope that novel drug delivery systems will be developed todeliver potent polypeptide drugs through the ocular route.REFERENCES1. Lee, V. H. L. (1 987 ). Ophthalmic delivery of peptides...

... applied ophthalmic drugs,Surv. Ophthalmol., 26:207–2 18. 88 . Mikkelson, T. J. (1 984 ). Review: Ophthalmic drug delivery, Pharm. Tech., 8: 90– 98. 89 . Lee, V. H. L. (1 985 ). Review: Topical ocular drug delivery recent ... Lee, V. H. L. (19 98) . Ocular absorption ofpz-peptide and its effect on the ocular systemic pharmacokinetics of topicallyapplied drugs in the rabbit, Pharm. Res., 15: 188 2– 188 7.1 28. Peyman, G. A., ... delivery: casestudies. (7). Ocular delivery of peptide and protein drugs, Adv. Drug Delivery Rev., 8: 331–339. 81 . Chiou, G. C. Y. (1994). Systemic delivery of polypeptide drugs through ocularroute,...

... including polymer -drug complex sys-tems, erodible microspheres, responsive particulates, in situ gelling systems, ion-exchange systems, and nanoparticles (15).B. Local Injectable Systems When the ... Stenzel, K. H., andRubin, A. L. (19 78) . Soluble gentamicin ophthalmic inserts as a drug delivery system, Arch. Ophthalmol., 96 :88 5. 83 . McCoy, J. P., Jr. (1 986 ). Contemporary laboratory applications ... Inc.II. PARTICULATE SYSTEMS IN OCULAR DRUG DELIVERY A. Topical Systems The isolation of the vitreous caused by the blood-retinal and blood-aqueousbarriers creates difficulties for effective drug therapy...

... practically unaltered.The corneal and conjunctival penetration of 4-phenylazobenzyloxy-carbonyl-l-Pro-l-Leu-Gly-l-Pro-d-Arg (Pz-peptide) and its effect on thecorneal and conjunctival penetration ... nearfuture. We hope that novel drug delivery systems will be developed todeliver potent polypeptide drugs through the ocular route.REFERENCES1. Lee, V. H. L. (1 987 ). Ophthalmic delivery of peptides ... H.(1 983 ). Vasopressin effects on isolated non-pregnant myometrium and uterinearteries and their inhibition by deamino-ethyl-lysine-vasopressin and dea-mino-ethyl-oxytocin, Br. J. Obstet. Gynaecol.,...

... Na+/K+-ATPase (Usukura et al., 1 988 ; Okami et al.,1 989 ; Martin-Vasallo et at., 1 989 ), H+/K+-ATPase (Fain et al, 1 988 ) andactive ascorbate transport system (Socci and Delamere, 1 988 ) are ... of a series of 50-ester prodrugs of 5-iodo-20-deoxyuridine. Pharm.Res. 5:734–737, 1 988 .10 Macha et al.Copyright © 2003 Marcel Dekker, Inc. Ophthalmic Drug Delivery Systems Second Edition, ... Brittam96 Freeze-Drymg/Lyophilization of Pharmaceutical and Biological Prod-ucts, edited by Louis Rey and Joan C May97. Percutaneous Absorption- Drugs-Cosmetics-Mechanisms-Metho-dology,...

... consideration in topical ocular drug delivery. Clin. Exp. Pharmacol. Physiol., 27:5 58. 8. Schoenwald, R. D. (1993). Ocular pharmacokinetics/pharmacodynamics, Ophthalmic Drug Delivery Systems (A. K. Mitra, ... Ocularpharmacokineticsincludesthefeaturesofabsorption,distribu-tion,andexcretionfoundwithsystemicadministrationbutappliedtotheeye.However,owingtotheuniqueanatomyandphysiologyoftheeyeandsurroundingtissue,ocularpharmacokineticsisconsiderablymoredifficulttodescribeandpredictthanitssystemiccounterpart.Thetaskisfurthercomplicatedbythevariousformulations,routes,anddosingregimenstypi-callyencounteredinophthalmology.Pharmacodynamicsisthemeasurementofpharmacologicalresponserelativetodoseorconcentration.Thepharmacologicalresponseinducedbyadrugcanvarygreatlyfromindividualtoindividualduetodifferencesinfactorssuchaseyepigmentation,thepathologicalstateoftheeye,tearing,orblinkrate.Theapplicationofpharmacologicalendpointsisparticularlyusefulinthestudyofdrugsinthehumaneye,wheretheabilitytodeterminetheocularpharmacokineticsbasedonoculartissueconcentrationsisseverelylimited.Thischapterdiscussestheocularpharmacokineticsassociatedwithtopicalocular,intravitreal,periocular,andsystemicadministration.Inaddi-tion,thepharmacodynamicsrelatedtoophthalmicdrugsandtheroleofoculardrugmetabolismarereviewed.II.OCULARPHARMACOKINETICSApplicationofclassicalpharmacokineticstoophthalmicdrugsisprob-lematicbecauseofthecomplexitiesassociatedwitheyeanatomyandphy-siology.Asaresult,mostoftheliteratureislimitedtomeasuringconcentrationsinoculartissuesovertimefollowingsingleormultipleadministration.Thisapproach,whileinformative,doesnoteasilyyieldquantitativepredictionsforchangesinformulationordosageregimen.Compoundingtheproblemisthefactthatmoststudieshavebeenconductedinrabbiteyes,whichdiffersignificantlyfromhumaneyesinanatomyandphysiology(seeTable1).themostobviousdifferencesareinblink ... vitreous, and/or choroid-retina (8) . However, with certain topical ocu-lar drugs, such as clonidine, timolol, dapiprazole, oxymetazoline, and ketor-olac tromethamine, iris-ciliary body concentrations...

... injectionlocation and the retinal permeability of the drug. If the drug has a low retinalpermeability, then the half-life of the drug in an aphakic eye is highly depen-dent on the distance between the injection ... injection,increased as the drug diffusivity was reduced. Furthermore, the rate of drug elimination, which is inversely related to the drug s elimination half-life, decreased significantly as the drug diffusivity ... Kulkarni, P. S., and Srinvasan, B. D. (1 987 ). Nonsteroidal anti-inflammatorydrugs in ocular inflammatory conditions. In Nonsteroidal Anti-inflammatoryDrugs, A. J. Lewis, D. E. Furst, eds., Marcel...

... adenovirus encoding brain-derived neurotrophic factor (Ad-BDNF) coinjected with a free radical scavenger, N-tert-butyl-(2-sulfoph-enyl)-nitrone (S-PBN), resulted in the survival of 63% axotomized ... (19 98) .Ribozyme-targeted destruction of RNA associated with autosomal-dominantretinitis pigmentosa. Invest. Ophthamol. Vis. Sci., 39(5): 681 – 689 .213. Tombran-Tink, J., and Johnson, L. V. (1 989 ). ... Phosphorothioate-modified oli-godeoxyribonucleotides, III. NMR and UV spectroscopic studies of the Rp-Rp, Sp-SP, and Rp-Sp duplexes, [d(GGSAATTCC)]2, derived from diaster-eomeric O-ethyl phosphorothioates....

... therapeutics: drug delivery and targeting. Adv. Drug Delivery Rev., 18: 115–131.167. J. W. Jaroszewski, and J. S. Cohen. (1991). Cellular uptake of antisense oli-godeoxynucleotides. Adv. Drug Delivery ... integrins. Transplantation, 64:763–769. 87 . E. Wagner (1999). Application of membrane-active peptides for nonviral gene delivery. Adv. Drug Deliv. Rev., 38: 279– 289 . 88 . M. X. Tang and F. C. Szoka. (1997). ... Wagner. (19 98) . Application of membrane-activepeptides for drug and gene delivery across cellular membranes. Adv. Drug Deliv. Rev., 34:21–35. 85 . E. Wagner. (1999). Application of membrane-active...