How an increase in the carbon chain length of the ester moiety affects the stability of a homologous series of oxprenolol esters in the presence of biological enzymes

Journal of Pharmaceutical Sciences
C G Jordan

Abstract

beta-Blockers including timolol and propranolol are administered in eye-drops for the treatment of glaucoma. Due to high incidence of cardiovascular and respiratory side-effects, their therapeutic value is limited. As a result of poor ocular bioavailability, many ocular drugs are applied in high concentrations, which give rise to both ocular and systemic side-effects. Therefore, some methods have been employed to increase ocular bioavailability such as (a) the development of drug delivery devices designed to release drugs at controlled rates, (b) the use of various vehicles that retard precorneal drug loss, and (c) the conversion of drugs to biologically reversible derivatives (prodrugs) with increased corneal penetration properties, from which the active drugs are released by enzymatic hydrolysis. A series of structurally related oxprenolol esters were synthesized and investigated as potential prodrugs for improved ocular use. The stability of each ester was studied in phosphate buffer (pH 7.4), also in the presence of (a) 30% human plasma, (b) aqueous humor, and (c) corneal extract at pH 7. 4 and at 37 degreesC. An account is given of how the stability of a homologous series of oxprenolol esters in the presence of biological ...Continue Reading

References

Jan 1, 1988·Journal of Ocular Pharmacology·D S ChienV H Lee
Nov 15, 1986·American Journal of Ophthalmology·W L NelsonJ N Kuritsky
Feb 1, 1985·Drug Intelligence & Clinical Pharmacy·W P MunroeR M Kershner
Mar 1, 1983·Journal of Pharmaceutical Sciences·V H Lee
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Oct 1, 1982·Biopharmaceutics & Drug Disposition·V H LeeR E Stratford
Jan 1, 1982·Current Eye Research·V H LeeK A Takemoto

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Citations

May 27, 2011·Pharmaceutical Research·Melissa D HowardYounsoo Bae
May 7, 2005·International Journal of Pharmaceutics·Li DiHong Chen
Aug 29, 2014·Expert Opinion on Drug Discovery·Rafik Karaman
Sep 16, 2003·Biopharmaceutics & Drug Disposition·D WerdenbergP Langguth
Aug 9, 2019·Current Topics in Medicinal Chemistry·Lídia M LimaDaniel N do Amaral
Feb 19, 2019·Chemical Science·Hannah M BrittJohn M Sanderson
May 18, 2021·Asian Journal of Pharmaceutical Sciences·Jagpreet KourBharti Sapra

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