118
Views
112
CrossRef citations to date
0
Altmetric
Original Article

Lipophilicity influence on conjunctival drug penetration in the pigmented rabbit: A comparison with corneal penetration

, , &
Pages 571-579 | Received 25 Feb 1991, Accepted 22 Apr 1991, Published online: 02 Jul 2009

References

  • Walsky M. A., Jablonski M. M., Edelhauser H. F. Comparison of conjunctival and corneal surface areas in rabbit and human. Curr. Eye Res. 1988; 2: 483–486
  • Lee V. H.L., Robinson J. R. Mechanistic and quantitative evaluation of precorneal pilocarpine disposition in albino rabbits. J. Pharm. Sci. 1979; fig: 673–684
  • Lee V. H.L. Mechanisms and facilitation of corneal drug penetration. J. Contr. Rel. 1990; 11: 79–90
  • Woodward D. F., Hawley S. B., William L. S., Ralston T. R., Protzman C. E., Spada C. S., Nieves A. L. Studies on the ocular pharmacology of prostaglandin D2. Invest. Ophthalmol. Vis. Sci. 1990; 31: 138–146
  • Chang S. C., Lee V. H.L. Nasal and conjunctival contributions to the systemic absorption of topical timolol in the pigmented rabbit: implications in the design of strategies to maximize the ratio of ocular to systemic absorption. J. Ocular Pharmacol. 1987; 3: 159–169
  • Chang S. C., Bundgaard H., Burr A., Lee V. H.L. Improved corneal penetration of timolol by prodrugs as a means to reduce systemic drug load. Invest. Ophthalmol. Vis. Sci. 1987; 28: 487–491
  • Chang S. C., Chien O. S., Bundgaard H., Lee V. H.L. Relative effectiveness of prodrug and viscous solution approaches in maximizing the ratio of ocular to systemic absorption of topically applied timolol. Exp. Eye Res. 1988; 46: 59–69
  • Schoenwald R. D., Huang H.-S. Corneal penetration behavior of β-blocking agents I: Physicochemical factors. J. Pharm. Sci. 1983; 72: 1266–1272
  • Hafkenscheid T. L., Tomlinson E. Correlations between alkane/water and octan-1-ol/water distribution coefficients and isocratic reversed-phase liquid chromatographic capacity factors of acids, bases and neutrals. Int. J. Pharm. 1983; 16: 225–229
  • Lee V. H.L., Chien D. S., Sasaki H. Ocular ketone reductase distribution and its role in the metabolism of ocularly applied levobunolol in the pigmented rabbit. J. Pharmacol. Exp. Ther. 1988; Mfe: 871–878
  • Dixon W. J., Brown M. B., Engelman L., Hill M. A., Jennrich R. I. BMDP Statistical Software Manual. University of California Press, Berkeley, California 1988; Vol. 1: 389–418
  • Van Bree J. B., DeBoer A. G., Danhof M., Ginsel L. A., Breimer D. D. Characterization of an “in vitro” blood-brain barrier: effects of molecular size and lipophilicity on cerebrovascular endothelial transport rates of drugs. J. Pharmacol. Exp. Ther. 1988; 24Z: 1233–1239
  • Tavakoli-Saberi M. R., Audus K. L. Physicochemical factors affecting β-adrenergic antagonist permeation across cultured hamster pouch buccal epithelium. Int. J. Pharm. 1989; 56: 135–142
  • Nichols B., Dawson C. R., Togni B. Surface features of the conjunctiva and cornea. Invest. Ophthalmol. Vis. Sci. 1983; 64: 570–576
  • Huang A. J.W., Tseng S. C.G., Kenyon K. R. Paracellular permeability of corneal and conjunctival epithelia. Invest. Ophthalmol. Vis. Sci. 1989; 3Q: 684–689
  • Flynn G. L., Yalkowsky S. H., Roseman T. J. Mass transport phenomena and models: theoretical concepts. J. Pharm. Sci. 1974; 63: 479–510
  • Neutra M. R., Forstner J. F. Gastrointestinal mucus: synthesis, secretion, and function. “Physiology of the Gastrointestinal Tract,”, L. R. Johnson. Raven Press, New York 1987; 975–1009
  • Nichols B. A., Chiappino M. L., Dawson C R. Demonstration of the mucous layer of the tear film by electron microscopy. Invest. Ophthalmol. Vis. Sci. 1985; 26: 464–473
  • Schoenwald R. D., Ward R. L. Relationship between steroid permeability across excised rabbit cornea and octanol-water partition coefficients. J. Pharm. Sci. 1978; 67: 786–788
  • Mosher G. L., Mikkelson T. J. Permeability of the n-alkyl p-aminobenzoate esters across the isolated corneal membrane of the rabbit. Int. J. Pharm. 1979; 2: 239–243
  • Kishida K., Otori T. A quantitative study on the relationship between transcorneal permeability of drugs and their hydrophobicity. Jpn. J. Ophthalmol. 1980; 24: 251–259
  • Chien D. S., Sasaki H., Bundgaard H., Buur A., Lee V. H.L. Role of enzymatic lability in the corneal and conjunctival penetration of timolol ester prodrugs in the pigmented rabbit. Pharm. Res. 1991; 8: 728–733
  • Anderson B. D., Raykar P. V. Solute structure-permeability relationships in human stratum corneum. J. Invest. Dermatol. 1989; 93: 280–286
  • Shi B., Tien H. T. Action of calcium channel and beta-adrenergic blocking agents in bilayer lipid membranes. Biochim. Biophys. Acta 1986; 859: 125–134
  • Elena P. P., Kosina-Boix M., Moulin G., Lapalus P. Autoradiographic localization of beta-adrenergic receptors in rabbit eye. Invest. Ophthalmol. Vis. Sci. 1987; 2S: 1436–1441
  • Elena P. P., Moulin G., Lapalus P. Characterization of /) adrenergic receptors in bovine pigmented ciliary processes. Curr. Eye Res. 1984; J: 743–750
  • Wood A. J.J. Pharmacokinetics and pharmacodynamics of beta-blockers. “The Evaluation of Beta Blockers and Calcium Antagonist Drugs,”, J. Morgenroth, E. N. Moore. Martinas Njihoff Publishers, AmsterdamThe Netherlands 1981; 41–61
  • Bonanno J. A., Machen T. E. Intracellular pH regulation in basal corneal epithelial cells measured in corneal explants: Characterization of Na/H exchange. Exp. Eye Res. 1989; 49: 129–142
  • Renner E. L., Lake J. R., Persico M., Scharschmidt B. F. Na+-H+ exchange activity in rat hepatocytes: role in regulation of intracellular pH. Am. J. Physiol. 1989; 256: G44–52
  • Dudeja P. K., Foster E. S., Brasitus T. A. Na+-H+ antiporter of rat colonic basolateral membrane vesicles. Am. J. Physiol. 1989; 217: G624–632
  • Zadunaisky J. A., Kinne-Saffran E., Kinne R. A Na/H exchange mechanism is apical membrane vesicles of the retinal pigment epithelium. Invest. Ophthalmol. Vis. Sci. 1989; 30: 2332–2340
  • Orsenigo M. N., Tosco M., Zoppi S., Faelli A. Characterization of basolateral membrane Na/H antiport in rat jejunum. Biochim. Biophys. Acta 1990; 1026: 64–68
  • Felder C. C., Campbell T., Albrecht F., Jose P. A. Dopamine inhibits Na+-H+ exchanger activity in renal BBMV by stimulation of adenylate cyclase. Am. J. Physiol. 1990; 259: F297–303
  • Manganel M., Turner R. J. Agonist induced activation of Na+/H+ exchange in rat parotid acinar cells. J. Membr. Biol. 1989; HI: 191–198
  • Rajendran V. M., Binder H. J. Characterization of Na-H exchange in apical membrane vesicles of rat colon. J. Biol. Chem. 1990; 265: 8408–8414
  • Stiles G. L., Caron M. G., Lefkowitz R. J. β-Adrenergic receptors: biochemical mechanisms of physiological regulation. Physiol. Rev. 1984; 64: 661–743
  • Watson E. L., Jacobson K. L., Singh J. C. Monovalent ion enhancement of beta-adrenergic-stimulated adenylate cyclase activity in mouse parotid gland. Biochem. Pharmacol. 1989; 38: 1069–1074
  • Harvey B. J., Ehrenfeld J. Epithelial pH and ion transport regulation by proton pumps and exchangers. Ciba Found. Symp. 1988; 132: 139–164

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.