Crown Ethers: Novel Permeability Enhancers for Ocular
Drug Delivery?
Version 2 2017-09-12, 04:29
Version 1 2017-08-29, 21:14
Posted on 2017-09-12 - 04:29
Crown ethers are cyclic molecules
consisting of a ring containing
several ether groups. The most common and important members of this
series are 12-crown-4 (12C4), 15-crown-5 (15C5), and 18-crown-6 (18C6).
These container molecules have the ability to sequester metal ions,
and their complexes with drugs are able to traverse cell membranes.
This study investigated 12C4, 15C5, and 18C6 for their ability to
increase solubility of ocular drugs and enhance their penetration
into the cornea. Phase solubility analysis determined crown ethers’
ability to enhance the solubility of riboflavin, a drug used for the
therapy of keratoconus, and these solutions were investigated for
ocular drug permeation enhancing properties. Atomic absorption spectroscopy
demonstrated crown ether solutions’ ability to sequester Ca2+ from corneal epithelia, and crown ether mediated adsorption
of riboflavin into the stroma was investigated. Induced corneal opacity
studies assessed potential toxicity of crown ethers. Crown ethers
enhanced riboflavin’s aqueous solubility and its penetration
into in vitro bovine corneas; the smaller sized crown ethers gave
greatest enhancement. They were shown to sequester Ca2+ ions from corneal epithelia; doing so loosens cellular membrane
tight junctions thus enhancing riboflavin penetration. Induced corneal
opacity was similar to that afforded by benzalkonium chloride and
less than is produced using polyaminocarboxylic acids. However, in
vivo experiments performed in rats with 12C4 did not show any statistically
significant permeability enhancement compared to enhancer-free formulation.
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Morrison, Peter
W. J.; Porfiryeva, Natalia N.; Chahal, Sukhmanpreet; Salakhov, Ilgiz A.; Lacourt, Charlène; Semina, Irina I.; et al. (2017). Crown Ethers: Novel Permeability Enhancers for Ocular
Drug Delivery?. ACS Publications. Collection. https://doi.org/10.1021/acs.molpharmaceut.7b00556
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AUTHORS (8)
PM
Peter
W. J. Morrison
NP
Natalia N. Porfiryeva
SC
Sukhmanpreet Chahal
IS
Ilgiz A. Salakhov
CL
Charlène Lacourt
IS
Irina I. Semina
RM
Rouslan I. Moustafine
VK
Vitaliy V. Khutoryanskiy