Synthesis and characterization of an hyperbranched copolimer of polyglycidol and ε policaprolactone (PGCL) as a moxifloxacin carrier for potential ophthalmic application"

RIVAS, EI; ACEVEDO, B; OLEA A; ROMERO, VL

Rosario

Congreso; RICIFA. 4 Reunión Internacional de Ciencias Farmacéuticas; 2016

Universidad Nacional de Rosario

Synthesis and characterization of an hiperramificated copolymer of polyglycidol and ε polycaprolactone (PGCL) as a moxifloxacin carrier for potential ophthalmic applicationRivas EI, Acevedo B, Olea, A, Romero VLE-mail: veronica.romero@unab.clEscuela de Farmacia, Facultad de Medicina, Universidad Andrés Bello. Departamento de Química, Universidad Autónoma de Chile, Santiago, CHILE.Keywords: moxifloxacin, copolymer, ophthalmic applicationBacterial eye infections have generally topical antibacterial therapy and one of the most used are the fluoroquinolones, which are used with a dosing frequency for eyedrops of 3 to 4 hours for 7 to 14 days, which can lead to discomfort for the patient or breach of therapy because of the high dosing frequency. This, coupled with the difficulty and peculiarity of the pharmacokinetics and bioavailability of ophthalmic preparations presents an opportunity to seek to improve this disadvantages designing new drug delivery systems.In this work, we synthesized 3 polyglycidol hyperbranched amphiphilic molecules (PG), and from the selected PG, the copolymerization was performed in block adding to the polialcoholic terminal of the polymer units of ε-caprolactone. The copolymer obtained was purified and then was evaluated using FT-IR and RMN 1H and 13C, also using fluorometric techniques it was possible to calculate its critic aggregation concentration (CAC). In addition, hydrodynamic ratio, polidispersity index (PDI) and zeta potential was evaluated with dynamic light scattering with or without the drug. Finally loading capacity and in vitro release profiles of the drug from the aggregates was studiedOf the 3 PG synthesized, PG1 was obtained with a percentage of synthesis yield of 85,66%, so it was chosen to synthesized the copolymer. The copolymer obtained was characterized confirming its structure with FT-IR and its molecular weight (2180 g/mol, the highest of the 3 PG) with RMN. The copolymer shows an hydrodynamic ratio of 416 nm with a PDI of 0,4, both values decreases to 321 nm and 0,327 respectively when the system was loaded with the drug. Also the system shows an improvement of the apparent aqueous solubility of moxifloxacin, a loading efficacy of 30% of the drug and a prolonged release profile of the drug from the aggregates. These results, and the knowledge that both monomers of the copolymer are biodegradable, indicates that the copolymer synthesized could be a new drug delivery system for ophthalmic application of moxifloxacin.