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A.A. Silva, B. Wanczinski, A.G. Oliveira, J.A. Cardillo, F. Paganelli, R.A. Costa, M. Skaf, A.A. Souza–Filho, R. Belfort, Jr, B.D. Kuppermann; In vitro and in vivo Release Profile of a New Ciprofloxacin Hydrochloride Biodegradable Controlled Release Microspheres System Optimized for Sub–Tenon’s Capsule Delivery . Invest. Ophthalmol. Vis. Sci. 2005;46(13):5395.
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© ARVO (1962-2015); The Authors (2016-present)
Purpose: To study the in vitro and in vivo release profile of a ciprofloxacin (CP) biodegradable controlled release microspheres system developed for ocular sub–Tenon’s capsule application. Methods: CP and polylactic–co–glycolic acid (PLGA) were dissolved in acetone in order to obtain the relationship CP/PLGA 1:1 and 1:2. The drug loading was determined dissolving both, the PLGA and CP in glacial acetic acid. The CP loading efficiency and quantitative analysis were determined by high performance liquid chromatography and the morphology assessed by scanning electronic microscopy. In vitro, 1mg of CP microspheres was incubated in phosphate buffer and serial CP measurements performed. In vivo, 1mg/0.1mL CP loaded microspheres were injected in the sub–Tenon’s capsule space of 30 albino rabbits and the overtime released CP concentration determined in the aqueous and vitreous humors up to 10 days. Results: The PLGA microspheres showed roughly spherical shape and uniform particle size distribution around 2µm. The encapsulation efficiency was in the range of 90.5 + 4.5%. The in vitro release time from the CP/PLGA 1:1 microsphere was 24 hours and 15 minutes for the free CP form. In vivo, the free CP form remained in therapeutic levels for 12 hours in both, aqueous and vitreous humors. The CP/PLGA 1:1 microesphere system reached therapeutic levels within 12 hours following the sub–Tenon’s capsule injection and remained in this range up to 7 days. Conclusions: This micro sphere biodegradable system demonstrated in vitro and in vivo the potential to proportionate a more sustained and steady CP release profile than the CP free form after sub–Tenon’s capsule application. This is a rational approach for extra–ocular controlled drug delivery and may have broad applications in clinical ophthalmology
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