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

CACICEDO ML; ISLAN GA; BOSIO VE; CAUERHFF A; CASTRO GR

Taipei, Taiwan

Conferencia; 5th International Conference on Industrial Bioprocesses; 2012

National Taiwan University of Science and Technology - National Taiwan University - National Cheng Kung University - National Chung Hsing University

Enrofloxacin (Enro) is a third generation fluoroquinolone which has a broad spectrum ofantimicrobial activity mainly used in veterinary medicine. Current oral administration of Enro iscommonly associated to gastric and intestinal problems, in addition to its toxicity at highconcentrations. In this work a biopolymeric matrix based on natural and non toxic biopolymers wasdeveloped in order to improve the Enro oral release profile for oral administration and reduce theundesirable drug side effects. For this purpose, several biopolymeric matrices were assayed, Thecarrageenan-Enro complex showed the higher stability related to other tested marices (70% in 1 hour).Carrageenan-Enro interaction at different pHs were studied. The interaction was close to 70% at pH4.0. Based on that, carrageenan was blend with other biopolymers such as pectin and alginate, and inorder to make microspheres by ionic gelation. Although, the Enro-blends encapsulation capacitieswere around 40%, and the release profile reached the 100 % in two hours under simulated intestinalmedia. Several optimization assays were performed: particles coated with HM pectin and oleic acidreducing 20 % of Enro release. Additionally, hybrid microparticles (hMPs) of CaCO3 andcarrageenan (0.5-1.0 %) were synthesized and tested. Microspheres loaded with Enro displayed 5 μmdiameter average determined by microscopy. The hMPs showed a sustainable release profile insimulated intestinal fluids, reaching a 65 and 59 % of Enro release in 3 hours for 0.5 and 1.0%carrageenan respectively. The improvement in Enro release kinetics suggests that this system could bea possible candidate for biomedical applications, minimizing undesirable side effects of the antibiotictreatment.