The effect of drug charge type and charge density on corneal transport

Jiahorng Liaw, Yongyut Rojanasakul, Joseph R. Robinson

Research output: Contribution to journalArticle

43 Citations (Scopus)

Abstract

In order to understand the effect of charge type on corneal transport of peptides, it is useful to first investigate the mechanism of transport of amino acids across corneal tissue. The transport characteristics of l-[14C]lysine and l-[14C]glutamic acid were based on in vitro flux measurements. Net flux of l-lysine occurs via a sodium-dependent cotransport mechanism (with a coupling ratio of 1:1). The transport of l-lysine involves the Na+-K+-ATPase pump and requires a stereospecific carrier-mediated transport system. The permeability coefficient (P) of l-lysine was decreased from 10.1 ± 0.80 to 2.34 ± 0.75 × 10-6 (cm/s by blocking the active pump and carrier-mediated system. However, l-glutamic acid was apparently absorbed by a passive aqueous transport mechanism which was oubain-insensitive, [Na+]-independent, temperature-insensitive and non-stereospecific. Overall, the cornea was 2-3-fold more permeable to a cation (l-lysine) than an anion (l-glutamic acid). In addition, the negatively charged drug, salicylic acid, was 2.3 times less permeable than the cationic drug, benzylamine.

Original languageEnglish
Pages (from-to)111-124
Number of pages14
JournalInternational Journal of Pharmaceutics
Volume88
Issue number1-3
DOIs
Publication statusPublished - Dec 8 1992
Externally publishedYes

Fingerprint

Lysine
Glutamic Acid
Pharmaceutical Preparations
Salicylic Acid
Cornea
Anions
Cations
Permeability
Sodium
Amino Acids
Peptides
Temperature

Keywords

  • Active transport
  • Charge density
  • Charge type
  • Hill coefficient
  • l-Glutamic acid
  • l-Lysine
  • Na dependence
  • Permselectivity

ASJC Scopus subject areas

  • Pharmaceutical Science

Cite this

The effect of drug charge type and charge density on corneal transport. / Liaw, Jiahorng; Rojanasakul, Yongyut; Robinson, Joseph R.

In: International Journal of Pharmaceutics, Vol. 88, No. 1-3, 08.12.1992, p. 111-124.

Research output: Contribution to journalArticle

Liaw, Jiahorng ; Rojanasakul, Yongyut ; Robinson, Joseph R. / The effect of drug charge type and charge density on corneal transport. In: International Journal of Pharmaceutics. 1992 ; Vol. 88, No. 1-3. pp. 111-124.
@article{14c41257188f4612b35f7adb72901422,
title = "The effect of drug charge type and charge density on corneal transport",
abstract = "In order to understand the effect of charge type on corneal transport of peptides, it is useful to first investigate the mechanism of transport of amino acids across corneal tissue. The transport characteristics of l-[14C]lysine and l-[14C]glutamic acid were based on in vitro flux measurements. Net flux of l-lysine occurs via a sodium-dependent cotransport mechanism (with a coupling ratio of 1:1). The transport of l-lysine involves the Na+-K+-ATPase pump and requires a stereospecific carrier-mediated transport system. The permeability coefficient (P) of l-lysine was decreased from 10.1 ± 0.80 to 2.34 ± 0.75 × 10-6 (cm/s by blocking the active pump and carrier-mediated system. However, l-glutamic acid was apparently absorbed by a passive aqueous transport mechanism which was oubain-insensitive, [Na+]-independent, temperature-insensitive and non-stereospecific. Overall, the cornea was 2-3-fold more permeable to a cation (l-lysine) than an anion (l-glutamic acid). In addition, the negatively charged drug, salicylic acid, was 2.3 times less permeable than the cationic drug, benzylamine.",
keywords = "Active transport, Charge density, Charge type, Hill coefficient, l-Glutamic acid, l-Lysine, Na dependence, Permselectivity",
author = "Jiahorng Liaw and Yongyut Rojanasakul and Robinson, {Joseph R.}",
year = "1992",
month = "12",
day = "8",
doi = "10.1016/0378-5173(92)90308-O",
language = "English",
volume = "88",
pages = "111--124",
journal = "International Journal of Pharmaceutics",
issn = "0378-5173",
publisher = "Elsevier",
number = "1-3",

}

TY - JOUR

T1 - The effect of drug charge type and charge density on corneal transport

AU - Liaw, Jiahorng

AU - Rojanasakul, Yongyut

AU - Robinson, Joseph R.

PY - 1992/12/8

Y1 - 1992/12/8

N2 - In order to understand the effect of charge type on corneal transport of peptides, it is useful to first investigate the mechanism of transport of amino acids across corneal tissue. The transport characteristics of l-[14C]lysine and l-[14C]glutamic acid were based on in vitro flux measurements. Net flux of l-lysine occurs via a sodium-dependent cotransport mechanism (with a coupling ratio of 1:1). The transport of l-lysine involves the Na+-K+-ATPase pump and requires a stereospecific carrier-mediated transport system. The permeability coefficient (P) of l-lysine was decreased from 10.1 ± 0.80 to 2.34 ± 0.75 × 10-6 (cm/s by blocking the active pump and carrier-mediated system. However, l-glutamic acid was apparently absorbed by a passive aqueous transport mechanism which was oubain-insensitive, [Na+]-independent, temperature-insensitive and non-stereospecific. Overall, the cornea was 2-3-fold more permeable to a cation (l-lysine) than an anion (l-glutamic acid). In addition, the negatively charged drug, salicylic acid, was 2.3 times less permeable than the cationic drug, benzylamine.

AB - In order to understand the effect of charge type on corneal transport of peptides, it is useful to first investigate the mechanism of transport of amino acids across corneal tissue. The transport characteristics of l-[14C]lysine and l-[14C]glutamic acid were based on in vitro flux measurements. Net flux of l-lysine occurs via a sodium-dependent cotransport mechanism (with a coupling ratio of 1:1). The transport of l-lysine involves the Na+-K+-ATPase pump and requires a stereospecific carrier-mediated transport system. The permeability coefficient (P) of l-lysine was decreased from 10.1 ± 0.80 to 2.34 ± 0.75 × 10-6 (cm/s by blocking the active pump and carrier-mediated system. However, l-glutamic acid was apparently absorbed by a passive aqueous transport mechanism which was oubain-insensitive, [Na+]-independent, temperature-insensitive and non-stereospecific. Overall, the cornea was 2-3-fold more permeable to a cation (l-lysine) than an anion (l-glutamic acid). In addition, the negatively charged drug, salicylic acid, was 2.3 times less permeable than the cationic drug, benzylamine.

KW - Active transport

KW - Charge density

KW - Charge type

KW - Hill coefficient

KW - l-Glutamic acid

KW - l-Lysine

KW - Na dependence

KW - Permselectivity

UR - http://www.scopus.com/inward/record.url?scp=0026685311&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=0026685311&partnerID=8YFLogxK

U2 - 10.1016/0378-5173(92)90308-O

DO - 10.1016/0378-5173(92)90308-O

M3 - Article

VL - 88

SP - 111

EP - 124

JO - International Journal of Pharmaceutics

JF - International Journal of Pharmaceutics

SN - 0378-5173

IS - 1-3

ER -