Carrageenan based microspheres for oral controlled release of Enrofloxacin in biomedical applications

CACICEDO MAXIMILIANO L.; ISLAN GERMAN A.; BOSIO VALERIA E.; CAUERHFF ANA; CASTRO GUILLERMO R.

Taipei

Congreso; The 5th International Conference on Industrial Bioprocesses; 2012

National Taiwan University of Science and Technology

Enrofloxacin (ENRO) is a third generation fluoroquinolone which has a broad spectrum of anti-microbial activity mainly used in veterinary medicine. Current oral administration of ENRO is commonly associated to gastric and intestinal problems, in addition to its toxicity at high concentrations. In this work a biopolymeric matrix based on natural and non toxic biopolymers was developed in order to improve the ENRO release profile for oral administration and reduce the undesirable drug side effects. For this purpose, several biopolimeric matrices were assayed, finding that the more stable interaction with ENRO was obtained with carrageenan (70 % at 1 hour). Carrageenan-ENRO interaction at different pHs were studied, at pH 4.0 a degree of interaction close to 70% was reached. Based on that, carrageenan was mixed with other biopolymers as pectin and alginate, to make blended microspheres by ionic gelation. Although, these systems have an encapsulation capacity of the drug around 40 %, the release profile reached the 100 % at two hours in simulated intestinal media. Several optimization assays were performed: particles coated with HM pectin and oleic acid showed a decrease of 20 % in the amount of ENRO release. Additionally, hybrid microparticles (hMPs) of Calcium Carbonate and carrageenan (at 0.5 and 1 % wt/vol in reaction media) were synthesized. Microspheres of 5 micrometers average diameter, measured by Optical Microscopy, loaded with ENRO, showed a sustainable release profile in simulated intestinal fluids, reaching a 65 and 59 % of ENRO release at 3 hours for carrageenan at 0.5 and 1 % wt/vol, respectively. The improvement in the ENRO release kinetics suggests that this system could be a possible candidate for biomedical applications, minimizing the toxic effects of antibiotic treatment.