Permeability of cornea, sclera, and conjunctiva: a literature analysis for drug delivery to the eye.

The objective of this study was to collect a comprehensive database of ocular tissue permeability measurements found in a review of the literature to guide models for drug transport in the eye. Well over 300 permeability measurements of cornea, sclera, and conjunctiva, as well as corneal epithelium, stroma, and endothelium, were obtained for almost 150 different compounds from more than 40 different studies. In agreement with previous work, the corneal epithelium was shown generally to control transcorneal transport, where corneal stroma and endothelium contribute significantly only to the barrier for small, lipophilic compounds. In addition, other quantitative comparisons between ocular tissues are presented. This study provides an extensive database of ocular tissue permeabilities, which should be useful for future development and validation of models to predict rates of drug delivery to the eye.

[1]  Irving Fatt,et al.  Physiology of the eye : an introduction to the vegetative functions , 1978 .

[2]  太田 陽一 Endothelial permeability of the living cornea to fluorescein , 1976 .

[3]  R. Schoenwald,et al.  Relationship between steroid permeability across excised rabbit cornea and octanol-water partition coefficients. , 1978, Journal of pharmaceutical sciences.

[4]  R. Schoenwald,et al.  Corneal Penetration Behavior of β-Blocking Agents I: Physicochemical Factors , 1983 .

[5]  H. Edelhauser,et al.  The corneal penetration of trifluorothymidine, adenine arabinoside, and idoxuridine: a comparative study. , 1977, Investigative ophthalmology & visual science.

[6]  Y. Sato,et al.  Studies on rabbit corneal permeability of local anesthetics (I). , 1984, Japanese journal of pharmacology.

[7]  K. Kontturi,et al.  Estimation of Pore Size and Pore Density of Biomembranes from Permeability Measurements of Polyethylene Glycols using an Effusion-like Approach , 1997 .

[8]  J. Houseman,et al.  Disposition of cyclophosphamide in the rabbit and human cornea. , 1982, Biopharmaceutics & drug disposition.

[9]  T. Maren,et al.  Permeability of human cornea and sclera to sulfonamide carbonic anhydrase inhibitors. , 1988, Archives of ophthalmology.

[10]  S. Benita,et al.  Ex-vivo permeation study of indomethacin from a submicron emulsion through albino rabbit cornea , 1997 .

[11]  K. Green,et al.  Solute permeability of the corneal endothelium and Descemet's membrane. , 1971, Experimental eye research.

[12]  S. Keipert,et al.  Influence of alpha-cyclodextrin and hydroxyalkylated beta-cyclodextrin derivatives on the in vitro corneal uptake and permeation of aqueous pilocarpine-HCl solutions. , 1997, Journal of pharmaceutical sciences.

[13]  S. Hodson,et al.  The bicarbonate ion pump in the endothelium which regulates the hydration of rabbit cornea. , 1976, The Journal of physiology.

[14]  R. Schoenwald,et al.  Corneal penetration behavior of beta-blocking agents II: Assessment of barrier contributions. , 1983, Journal of pharmaceutical sciences.

[15]  W. J. Dunn,et al.  Partition coefficient: Determination and estimation , 1986 .

[16]  S. Mishima,et al.  Permeability of the corneal endothelium to nonelectrolytes. , 1968, Investigative ophthalmology.

[17]  T. F. Patton,et al.  Physicochemical determinants of drug diffusion across the conjunctiva, sclera, and cornea. , 1987, Journal of pharmaceutical sciences.

[18]  R. Buck,et al.  Influence of ion pairing salts on the transcorneal permeability of ionized sulfonamides. , 1992, Journal of ocular pharmacology.

[19]  M. Riley A study of the transfer of amino acids across the endothelium of the rabbit cornea. , 1977, Experimental eye research.

[20]  D. Maurice,et al.  Sugar transport across the corneal endothelium. , 1969, Experimental eye research.

[21]  G. Grass,et al.  Mechanisms of corneal drug penetration. III: Modeling of molecular transport. , 1988, Journal of pharmaceutical sciences.

[22]  T. Maren,et al.  The transcorneal permeability of sulfonamide carbonic anhydrase inhibitors and their effect on aqueous humor secretion. , 1983, Experimental eye research.

[23]  G. Grass,et al.  Mechanisms of corneal drug penetration. I: In vivo and in vitro kinetics. , 1988, Journal of pharmaceutical sciences.

[24]  D. Maurice The structure and transparency of the cornea , 1957, The Journal of physiology.

[25]  A. Urtti,et al.  Permeability of pilocarpic acid diesters across albino rabbit cornea in vitro , 1991 .

[26]  D. Maurice,et al.  Diffusion across the sclera. , 1977, Experimental eye research.

[27]  Jennifer I. Lim,et al.  Human scleral permeability. Effects of age, cryotherapy, transscleral diode laser, and surgical thinning. , 1995, Investigative ophthalmology & visual science.

[28]  M. Prausnitz,et al.  Fiber matrix model of sclera and corneal stroma for drug delivery to the eye , 1998 .

[29]  D. Musson,et al.  An in vitro comparison of the permeability of prednisolone, prednisolone sodium phosphate, and prednisolone acetate across the NZW rabbit cornea. , 1992, Journal of ocular pharmacology.

[30]  T. Maren,et al.  The relations between ionic and non-ionic diffusion of sulfonamides across the rabbit cornea. , 1986, Investigative ophthalmology & visual science.

[31]  J. Topliss,et al.  Unified model for the corneal permeability of related and diverse compounds with respect to their physicochemical properties. , 1996, Journal of pharmaceutical sciences.

[32]  D. Maurice,et al.  The distribution and movement of serum albumin in the cornea. , 1965, Experimental eye research.

[33]  Kinam Park,et al.  Controlled drug delivery : challenges and strategies , 1997 .

[34]  W. Tasman,et al.  Duane’s Foundations of Clinical Ophthalmology: Ocular Anatomy, Embryology and Teratology. Physiology of the Eye and Visual System. Pathology of the Eye , 1991 .

[35]  G. Kasting,et al.  Transport across epithelial membranes , 1987 .

[36]  R. Reid,et al.  The Properties of Gases and Liquids , 1977 .

[37]  V. H. Lee,et al.  Lipophilicity influence on conjunctival drug penetration in the pigmented rabbit: a comparison with corneal penetration. , 1991, Current eye research.

[38]  D. Tang-Liu,et al.  Effects of four penetration enhancers on corneal permeability of drugs in vitro. , 1994, Journal of pharmaceutical sciences.

[39]  M. Duffel,et al.  N-Substituted sulfonamide carbonic anhydrase inhibitors with topical effects on intraocular pressure. , 1986, Journal of medicinal chemistry.

[40]  R. Schoenwald Ocular drug delivery. Pharmacokinetic considerations. , 1990, Clinical pharmacokinetics.

[41]  Studies of carbonic anhydrase inhibitors: physicochemical properties and bioactivities of new thiadiazole derivatives. , 1993, Journal of ocular pharmacology.

[42]  J. Lang Ocular drug delivery conventional ocular formulations , 1995 .

[43]  V. H. Lee,et al.  Improved corneal penetration of timolol by prodrugs as a means to reduce systemic drug load. , 1987, Investigative ophthalmology & visual science.

[44]  T. Otori,et al.  A Quantitative Study on the Relationship between Transcorneal Permeability of Drugs and Their Hydrophobicity , 1980 .

[45]  M. Eller,et al.  Topical carbonic anhydrase inhibitors. , 1984, Journal of medicinal chemistry.

[46]  K. Kobe The properties of gases and liquids , 1959 .

[47]  M. Allansmith,et al.  The dynamics of IgG in the cornea. , 1979, Investigative ophthalmology & visual science.

[48]  D. Maurice The permeability to sodium ions of the living rabbit's cornea , 1951, The Journal of physiology.