Corneal Penetration and Ocular Bioavailability of Drugs

Journal of Ocular Pharmacology

Volumn 1, Issue 3, 1985, Pages 309-326

  Burstein, Neal L ^a   Anderson, Janet A ^a  

^a UNIVERSITY OF CALIFORNIA   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ACETAZOLAMIDE; DRUG VEHICLE; GENTAMICIN; IDOXURIDINE; METHAZOLAMIDE; PILOCARPINE; PRESERVATIVE; VIDARABINE;

ANIMAL; BIOAVAILABILITY; CORNEA; DRUG ABSORPTION; DRUG COMPARISON; DRUG FORMULATION; DRUG PENETRATION; DRUG THERAPY; EYE; PHARMACOKINETICS; REVIEW; THERAPY; TOPICAL DRUG ADMINISTRATION; VISUAL SYSTEM;

ANIMAL; BIOLOGICAL AVAILABILITY; CORNEA; HUMAN; OPHTHALMIC SOLUTIONS;

EID: 0022325722     PISSN: 87563320     EISSN: 15577732     Source Type: Journal    
DOI: 10.1089/jop.1985.1.309     Document Type: Article

References (108)

1. Benson, H. Permeability of the cornea to topically applied drugs. Arch. Ophthalmol. 91:313–326, 1974.
2. Mishima, S. Clinical pharmacokinetics of the eye. Proctor lecture. Invest. Ophthalmol. Vis. Sci. 21:504–541, 1981.
3. Adler, C.A., Maurice, D.M., Paterson, M.E. The effect of viscosity of the vehicle on the penetration of fluorescein into the human eye. Exp. Eye Res. 11:34–42, 1971.
4. Anderson, R.A., Cowle, J.B. Influence of pH on the effect of pilocarpine on aqueous dynamics. Br. J. Ophthalmol. 52:607–611, 1968.
5. Capella, J., Schaefer, I. Comparison of ophthalmic vehicles using fluorescein uptake technique. Eye Ear Nose Throat Monthly 52:23–27, 1974.
6. Conrad, J.M., Reay, W.A., Polcyn, R.E., Robinson, J.R. Influence of toxiclty and pH on lacrimation and ocular drug bioavailability. J. Parent Drug Assoc. 32:149–161, 1978.
7. Hind H, Goyan, F. A new concept of the role of hydrogen ion concentration and buffer systems in the preparation of ophthalmic solutions. J. Am. Pharm. Assoc. 36:33–41, 1947.
8. Martin, F.N., Mims, J.L. Preparation of ophthalmic solutions with special reference to hydrogen ion concentration and tonicity. Arch. Ophthalmol. 44:561–572, 1950.
9. Norn, M.S. Role of the vehicle in local treatment of the eye. Acta. Ophthalmol. 42:727–734, 1964.
10. Chrai, S.S., Makoid, M.C., Eriksen, S.P., Robinson, J.R. Drop size and initial dosing frequency problems of topically applied ophthalmic drugs. J. Pharm. Sci. 63:333–338, 1974.
11. Burstein, N.L. Corneal cytotoxicity of topically applied drugs, vehicles and preservehicles and preservatives. Surv. Ophthalmol. 25:15–30, 1980.
12. Harnisch, J.P., Hoffman, F., and Dumitrescu, L. Side-effects of local anesthetics on the corneal epithelium of the rabbit eye. Albrecht von Graefes Arch. Klin. Exp. Ophthalmol. 197:71–81, 1975.
13. Fraunfelder, F. Extraocular fluid dynamics: How best to apply topical ocular medication. Trans. Am. Ophthalmol. Soc. 74:457–487, 1976.
14. Akers, M.J. Ocular bioavailability of topically applied ophthalmic drugs. American Pharmacy 23:33–36, 1983.
15. Shell, J.W. Pharmacokinetics of topically applied ophthalmic drugs. Surv. Ophthalmol. 26:207–218, 1982.
16. Maurice, D.M. The permeability of the cornea. Ophthal. Literature 7:3–26, 1953.
17. Davis, S.S., Tomlinson, E., Wilson, C.G. The effect of ion-association on the transcorneal transport of drugs. Br. J. Pharmacol. 64:444, 1978.
18. Schoenwald, R.D., Ward, R.L. Relationship between steroid permeability across excised rabbit cornea and octanol-water partition coefficients. J. Pharm. Sci. 67:786–788, 1978.
19. Ramer, R.M. and Gasset, A.R. Ocular penetration of pilocarpine: the effect of multiple doses on the ocular penetration of pilocarpine. Ann. Ophthalmol. 7:25–26, 1975.
20. Glasser, D.B., Gardner, S., Ellis, J.G., Pettit, T.H. Loading doses and extended dosing intervals in topical gentamicin therapy. Am. J. Ophthalmol. 99:329–332, 1985.
21. Burstein, N. Preservative alteration of corneal permeability in humans and rabbits. Invest. Ophthalmol. Vis. Sci. 12:1453–1457, 1984.
22. Saetone, M.F., Savigni, B., Wirth, A. The effect of different ophthalmic vehicles on the activity of tropicamide in man. J. Pharm. Pharmacol. 32:519–521, 1980.
23. Kupferman, A., Ryan, W.J., Leibowitz, H.M. Prolongation of anti-inflammatory effect of prednisolone acetate. Influence of formulation in high-viscosity gel. Arch. Ophthalmol. 99:2028–2029, 1981.
24. Fraunfelder, F.T., Meyer, S.M. Possible cardiovascular effects secondary to topical ophthalmic 2.5% phenylephrine. Am. J. Ophthalmol. 99:362–363, 1985.
25. Lee, V.H.L., Urrea, P.T., Smith, R.E., Schanzlin, D.J. Ocular drug bioavailability from topically applied liposomes. Surv. Ophthalmol. 29:335–348, 1985.
26. Coakes, R.L., Brubaker, R.F. Methods of measuring aqueous humor flow and corneal endothelial permeability using a fluorophotometry numogram. Inv. Ophth. 18:288–302, 1979.
27. Makold, M.C. et al. Corneal drug absorption - An illustration of parallel first-order absorption and rapid loss of drug from absorption depot. J. Pharm. Sci. 65:150–152, 1976.
28. Makoid, M.C., Robinson, J.R. Pharmacokinetics of topically applied pilocarpine in the albino rabbit eye. J. Pharm. Sci. 68:435–443, 1979.
29. Patil, P.N., Jacobowitz, D. Unequal accumulation of adrenergic drugs by pigamented and nonpigmented iris. Am. J. Ophthalmol. 78:470–477, 1974.
30. Mindel, J.S., Smith, H., Jacobs, M., Kharlamb, A.B., Friedman, A.H. Drug reservoirs in topical therapy. Invest. Ophthalmol. Vis. Sci. 25:346–350, 1984.
31. Maurice, D.M. Structures and fluids involved in the penetration of topically applied drugs. Int. Ophthalmol. Clin. 20:7–29, 1980.
32. Maurice, D.M., Mishima, S. Ocular Pharmacokinetics. In Pharmacology of the Eye. Sears, M.L., ed., Springer-Verlag, Berlin, 1984, pp. 19–116.
33. Burstein, N.L. The effects of topical drugs and preservatives on the tears and corneal epithelium in dry eye. Proc. Ophthalmol. Soc. U.K. (in press).
34. Keller, N., Moore, P., Carper, D., Longwell, A. Increased corneal permeability induced by the dual effects of transient tear film acidification and exposure to benzalkonlum chloride. Exp. Eye Res. 30:203–210, 1980.
35. Woo, P., Bursteln, N.L. A Non-Invasive Technique for Determining Corneal Permeability Change with Applied Agents. Inv. Ophthalmol. Suppl. 24:119a, 1983.
36. Marsh, R.J., Maurice, D.M. The influence of non-ionic detergents and other surfactants on human corneal permeability. Exp. Eye Res. 11:43–48, 1971.
37. O'Brien, C.S. and K.C. Swan. Carbaminoyl choline chloride in the treatment of glaucoma simplex. AMA Arch. Ophthalmol. 27:253–263, 1942.
38. Leopold, I.H., Scheie, H.G. Studies with microcrystalline sulfathiazole. AMA Arch. Ophthal. 29:811–817, 1943.
39. Schoenwald, R.D., Steward, P. Effect of particle size on ophthalmic bioavailability of dexamethasone suspensions in rabbits. J. Pharm. Sci. 69:391–394, 1980.
40. Maurice, D.M. The use of fluorescein in ophthalmological research (The Jonas S. Friedenwald Memorial Lecture). Invest. Ophthalmol. 6:464–477, 1967.
41. Holland, M.G., Wei, C.P., Gupta, S. Review and evaluation of 6-Hydroxy-dopamine (6-HD): Chemical sympathectomy for the treatment of glaucoma. Ann. Ophthalmol. 5:539–558, 1973.
42. Holly, F.J. Formation and stability of the tear film. Int. Ophthalmol. Clin. 13:73–96, 1973.
43. Ehlers, N. The precorneal film. Biomicroscopical, histological and chemical investigations. Acta Ophthalmol. Suppl. 81:1–136, 1965.
44. Ehlers, N. Pharmacology of the conjunctival sac. In Drugs and Ocular Tissues, Dikstein S., ed., S. Karger, Basel, 1977, p. 23.
45. Mishima, S., Gasset, A., Klyce, S.D., Baum, J.L. Determination of tear volume and tear flow. Invest. Ophthalmol. 5:264–276, 1966.
46. Barendsen, H., Oosterhuis, J.A., van Haeringen, N.J. Concentration of fluorescein in tear fluid after instillation as eye-drops. Ophthalmic Res. 11:73–82, 1979.
47. Anderson, J.A. Systemic absorption of topical ocularly applied epinephrine and dipivefrin. Arch. Ophthalmol. 98:350–353, 1980.
48. Mikkelson, T.J., Chrai, S.S., Robinson, J.P. Altered bioavailabiiity of drugs in the eye due to drug-protein interaction. J. Pharm. Sci. 62:1648–1653, 1973.
49. Klyce, S.D. Electrical profiles in the corneal epithelium. J. Physiol. 226:407–429, 1972.
50. Swan, K. and White, N. Corneal permeability: 1. Factors affecting penetration of drugs into the cornea. Am. J. Ophthalmol. 25:1043–1058, 1943.
51. Burstein, N.L., Klyce, S.D. Electrophysiologic and morphologic effects of ophthalmic preparations on rabbit cornea epithelium. Invest. Ophthalmol. Vis. Sci. 16:899–911, 1977.
52. Pfister, R., Burstein, N. The effects of ophthalmic drugs, vehicles and preservatives on corneal epithelium: A scanning electron microscope study. Invest. Ophthalmol. 15:246–259, 1976.
53. Burstein, N.L. Corneal endothelial permeability to electron opaque tracers demonstrated by modified proprane jet cryofixation. J. Cell. Biol. Suppl. 83:300a, 1979.
54. Sieg, J.W., Robinson, J.R. Vehicle effects on ocular drug bioavailabiiity. I: Evaluation of fluorometholone. J. Pharm. Sci. 64:931–936, 1978.
55. Schoenwald, R.D., Ward, R.L., DeSantis, L.M., Roehrs, R.E. Influence of high-viscosity vehicles on miotic effect of pilocarpine. J. Pharm. Sci. 67:1280–1283, 1978.
56. Ahmed, I., Patten, T.F. Importance of the noncorneal absorption route in topical ophthalmic drug delivery. Invest. Ophthalmol. Vis. Sci. 26:584–587, 1985.
57. Doane, M.G., Jensen, A.D., Dohlman, C.H. Penetration routes of topically applied eye medications. Am. J. Ophthalmol. 85:383–386, 1978.
58. Lee, V.H., Robinson, J.R. Mechanistic and quantitative evaluation of precorneal pilocarpine disposition in albino rabbits. J. Pharm. Sci. 68:673–684, 1979.
59. Bienfang, D.C. Sector pupillary dilatation with an epinephrine strip. Am. J. Ophthalmol. 75:883–884, 1973.
60. Bito, L.Z. and Baroody, R.A. The penetration of exogenous prostaglandin and arachidonic acid into, and their distribution within, the mammalian eye. Curr. Eye. Res. 1:659–669, 1981.
61. Robinson, J.R. Personal Communication, 1983.
62. Edelhauser, H.F., Hoffert, J.R., Fromen, P.O. In vitro ion and water movement in corneas of rainbow trout. Invest. Ophthalmol. Vis. Sci. 4:290, 1965.
63. Dikstein, S., Maurice, D.M. The metabolic basis to the fluid pump in the corean. J. Physiol. 221:29–41, 1972.
64. Krohn, D.L., Breitfeller, J.M. Transport of pilocarpine by isolated rabbit cornea. Invest. Ophthalmol. 13:312–316, 1974.
65. Krohn, D.L., Breitfeller, J.M. Quantitation of pilocarpine delivery across isolated rabbit cornea by non-crosslinked high viscosity polymer gel. Invest. Ophthalmol. 15:324–327, 1976.
66. Edelhauser, H.F., Van Horn, D., Hyndiuk, R.A., Schultz, R.O. Intraocular irrigating solutions: Their effect on the corneal endothelium. Arch. Ophthalmol. 93:648–657, 1975.
67. O'Brien, W.J., Edelhauser, H.F. The corneal penetration of trifluorothymidine, adenine arabinoside, and idoturidine: A comparative study. Inv. Ophthalmol. Vis. Sci. 16:1093–1103, 1977.
68. Edelhauser, H.F. Personal Communication. 1983.
69. Anderson, J.A., Davis, W.L. and Wei, C.P. Site of ocular hydrolysis of a prodrug, dipivefrin, and a comparison of its ocular metabolism with that of the parent compound, epinephrine. Invest. Ophthalmol. Vis. Sci. 19:817–823, 1980.
70. Duzman, E., Chen, C.C., Anderson, J., Blumenthal, M., and Twizer, H. Diacetyl derivative of nadolol. Arch. Ophthalmol. 100:1916–1919, 1982.
71. Goldberg, I., Kolker, A.E., Kass, M.A., and Becker, B. Dipivefrin: Current concepts. Aust. J. Ophthalmol. 8:147–150, 1980.
72. Krieglstein, G.K. and Leydhecker, W. The dose-response relationships of dipivalyl epinephrine in open-angle glaucoma. Albrecht von Graefes Arch. Klin. Exp. Ophthalmol. 205:141–146, 1978.
73. Wei, C.P., Anderson, J.A., and Leopold, I. Ocular absorption and metabolism of topically applied epinephrine and a dipivalyl ester of epinephrine. Invest. Ophthalmol. Vis. Sci. 17:315–321, 1978.
74. Huang, H.S., Schoenwald, R.D., Lach, J.L. Corneal penetration behavior of beta blocking agents. II. Assessment of barrier contributions. J. Pharm. Sci. 72:1272–1279, 1983.
75. Ubels, J.L., Edelhauser, H.F. Retinoid permeability and uptake in corneas of normal and Vitamin A deficient rabbits. Arch. Ophthalmol. 100:1828–1831, 1982.
76. Cogan, D.G., Hirsch, E.O. The cornea VII: Permeability to weak electrolytes. Arch. Ophthalmol. 32:276–282, 1944.
77. Longwell, A., Birss, S. Effect of topically applied pilocarpine on tear film pH. J. Pharm. Sci. 65:1654–1657, 1976.
78. Smith, R.N., Hanschic, C., Ames, M.M. Selection of a reference partitioning system for drug design work. J. Pharm. Sci. 64:599–606, 1975.
79. Huang, H.S., Schoenwald, R.D., Lach, L. Corneal penetration behavior of beta blocking agents. III. In-vitro/In-vivo correlations. J. Pharm. Sci. 72:1279–1281, 1983.
80. Gambill, H.D., Ogle, K.N. and Kearns, T.P. Mydriatic effect of four drugs determined with pupillograph. Arch. Ophthalmol. 77:740–746, 1967.
81. Ishikawa, S., Oono, S., and Hikita, H. Drugs affecting the iris muscle. In Drugs and Ocular Tissues, Dikstein, S., ed., S. Karger, Basel, 1977, p. 288.
82. Ogle, K.N. Whisnaut, R.A., Hazelrig, J.B. Quantitative study of pupil response to miotic drugs. Invest. Ophthalmol. 5:176–185, 1966.
83. Ohara, K. Effects of cholinergic agonists on isolated iris sphincter muscles; a pharmacodynamic study. Jpn. J. Ophthalmol. 21:516–527, 1977.
84. Patil, P.N. Cocaine-binding by the pigmented and the non-pigmented iris and its relevance to the mydriatic effect. Invest. Ophthalmol. 11:739–746, 1972.
85. Hulem, C.D., Old, S.E., Zeleznlck, L.D., Leopold, I.H. Intraocular penetration of rosoxacin in rabbits. Arch. Ophthalmol. 100:646–649, 1982.
86. Kleinberg, J., Dea, F.J., Anderson, J.A., Leopold, I.H. Intraocular penetration of topically applied lincomycin in rabbits. Arch. Ophthalmol. 97:933–936, 1979.
87. Araie, M., Takase, M., Yokoyama, Y., and Kitagawa, M. Timolol maleate: pharmacokinetic analysis of ocular penetration in the rabbit eye and effects on human aqueous humor dynamics. Acta Soc. Ophthalmol. Jpn. 84:2139–2146, 1980.
88. Benedetto, D.A., Shah, D.O. and Kaufman, H.E. The instilled fluid dynamics and surface chemistry of polymers in the preocular tear film. Invest. Ophthalmol. 14:887–902, 1975.
89. Chrai, S.S., Robinson, J.R. Binding of sulfisoxazole to protein fractions of tears. J. Pharm. Sci. 65:437–439, March 1976.
90. Yoshida, S., Mishima, S. A pharmacokinetic analysis of the pupil response to topical pilocarpine and tropicamide. Jpn. J. Ophthalmol. 19:121–138, 1975.
91. Chen, C.C. Personal communication, 1983.
92. Anderson, J.A., Chen, C.C., Vita, J.B., Shackleton, M. Disposition of topical flurblprofen in normal and aphakic rabbit eyes. Arch. Ophthalmol. 100:642–645, 1982.
93. Kaila, T., Salminen, L., Huupponen, R. Systemic absorption of topically applied ocular timolol. J. Ocular Pharm. 1:79–83, 1985.
94. Hardberger, R.E., Hanna, C., and Goodart, R. Effects of drug vehicles on ocular uptake of tetracycline. Am. J. Ophthalmol. 80:133–138, 1975.
95. Murai, Y. Studies of tear flow using sodium pertechnetate Tc99m. Jpn. J. Ophthalmol. 20:283–289, 1976.
96. Trueblood, J.H., Rossomondo, R.M., Carlton, W.H. and Wilson, L.A. Corneal contact times of ophthalmic vehicles. Arch. Ophthalmol. 93:127–130, 1975.
97. Patil, P.N., Shimada, K., Feller, D.R. and Malspeis, L. Accumuuation of (-) 14C-eptnephrine by the pigmented and nonpigmented iris. J. Pharmacol. Exp. Ther. 188:342, 1974.
98. Schoenwald, R.D., Boltralik, J.J. A bioavailability comparison in rabbits of two steroids formulated as high-viscosity gels and reference aqueous preparations. Inv. Ophthalmol. Vis. Sci. 18:61–66, 1979.
99. Sieg, J.W., Robinson, J.R. Vehicle effects on ocular drug bioavailability II: Evaluation of pilocarpine. J. Pharm. Sci. 66:1222–1228, 1977.
100. Sieg, J.W., Robinson, J.R. Vehicle effects on ocular drug bioavailabiiity. I: Evaluation of fluorometholone. J. Pharm. Sci. 64:931–936, 1978.
101. Waltman, S.R., Buerk, K. and Foster, C.S. Effects of ophthalmic ointments on intraocular penetration of topical fluorescein in rabbits and man. Am. J. Ophthalmol. 78:262–264, 1974.
102. Bottari, F., Giannaccini, B., Peverini, D., et al. Semisolid ophthalmic vehicles II: Evaluation In albino rabbits of aqueous gel-type vehicles containing lidocaine and benzocaine. Can. J. Pharm. Sci. 14:39–44, 1979.
103. Schaeffer, H.E. and Krohn, D.L. Liposomes in topical drug delivery. Invest. Ophthalmol. Visual Sci. 22:221–227, 1982.
104. Stratford, R.E., Yang, D.C., Redell, M.A. and Lee, V.H.L. Ocular distribution of liposome-encapsulated epinephrine and insulin in the albino rabbit. Curr. Eye Res. 2:377–386, 1982/1983.
105. Salminen, L. Effect of oily vehicle on ocular pilocarpine concentration. Acta Ophthalmol. 57:633–635, 1979.
106. Smith, S.A., Smith, S.E., Lazare, R. An increased effect of pilocarpine on the pupil by appiication of the drug in oil. Br. J. Ophthalmol. 62:314–317, 1978.
107. Guss, R., Johnson, F., Maurice, D. Rhodamine, B as test molecule in intraocular dynamics. Invest. Ophthalmol. Vis. Sci. 25:758–762, 1984.
108. Gray, J. Personal communiccaion, 1982.