Antibiotics in local therapy of eye infections: Current aspects of drug products formulation

Abstract

In local therapy of ocular infections (bacterial conjunctivitis, bacterial keratitis, endophthalmitis) commonly used antibiotics are those with bactericidal effect: penicillins, cephalosporins, aminoglycosides and fluoroquinolones. Tetracycline, erythromycin, chloramphenicol and sulfonamide are bacteriostatic drugs administrating in less severe infections. A proper selection of final dosage form is of paramount importance for achieving the satisfying therapeutic effect of these drugs. For the reason of simple application and acceptable price conventional pharmaceutical forms of antibiotics (eye drops and ointments) are the most available at the market The disadvantage of the conventional dosage forms is relatively poor drug bioavailability in the eye, which is out to enhance either by promoting drugs’ biopharmaceutical properties or by development of novel drug delivery systems.

U lokalnoj terapiji infekcija oka (bakterijski keratitis, bakterijski konjunktivitis i endoftalmitis) najčešće se koriste antibiotici sa baktericidnim delovanjem (kod jakih bakterijskih infekcija): penicilini, cefalosporini, aminoglikozidi i fluorohinoloni. Tetraciklin, eritromicin, hloramfenikol i sulfonamidi pokazuju bakteriostatsko delovanje i primenjuju se kod infekcija slabijeg inteziteta. Za postizanje zadovoljavajućeg terapijskog delovanja ovih aktivnih supstanci veoma je važan izbor i formulacija finalnog preparata. Konvencionalni farmaceutski oblici antibiotika (kapi i masti za oči) su najviše zastupljeni na tržištu zbog jednostavnosti primene i prihvatljive cene. Nedostatak ovih oblika je relativno loša raspoloživost lekovite supstance u oku, koja se nastoji poboljšati unapređenjem njihovih biofarmaceutskih osobina i razvojem novih "nosača" lekovite supstance (eng. new drug delivery systems).