Corneal Critical Barrier against the Penetration of Dexamethasone and Lomefloxacin Hydrochloride: Evaluation by the Activation Energy for Drug Partition and Diffusion in Cornea

Autor:	Masayo Higashiyama, Shinichi Yasueda, Akiharu Isowaki, Akira Ohtori, Masazumi Yamaguchi
Rok vydání:	2007
Předmět:	Male Anti-Inflammatory Agents Pharmaceutical Science In Vitro Techniques Dexamethasone Permeability Cornea Diffusion Anti-Infective Agents Drug Discovery medicine Animals Lomefloxacin Hydrochloride Chromatography High Pressure Liquid Antibacterial agent Corneal epithelium Pharmacology Chromatography Chemistry Preservatives Pharmaceutical Organic Chemistry Temperature Biological Transport Penetration (firestop) Permeation medicine.anatomical_structure Permeability (electromagnetism) Thermodynamics Lomefloxacin Rabbits sense organs Ophthalmic Solutions Benzalkonium Compounds Fluoroquinolones medicine.drug
Zdroj:	Drug Development and Industrial Pharmacy. 33:805-811
ISSN:	1520-5762 0363-9045
DOI:	10.1080/03639040701377995
Popis:	The cornea is a solid barrier against drug permeation. We searched the critical barrier of corneal drug permeation using a hydrophobic drug, dexamethasone (DM), and a hydrophilic drug, lomefloxacin hydrochloride (LFLX). The activation energies for permeability of DM and LFLX across the intact cornea were 88.0 and 42.1 kJ/mol, respectively. Their activation energies for permeability across the cornea without epithelium decreased to 33.1 and 16.6 kJ/mol, respectively. The results show that epithelium is the critical barrier on the cornea against the permeation of a hydrophobic drug of DM as well as a hydrophilic drug of LFLX. The activation energy of partition for DM (66.8 kJ/mol) was approximately 3-fold larger than that of diffusion (21.2 kJ/mol). The results indicate that the partition for the hydrophobic drug of DM to the corneal epithelium is the primary barrier. Thermodynamic evaluation of activation energy for the drug permeation parameters is a good approach to investigate the mechanism of drug permeability.
Databáze:	OpenAIRE
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