Biodisponibility of Ciprofloxacin encapsulated on alginate/pectin coacervates

ISLAN GA; CASTRO GR

Trivandrum

Conferencia; New Horizonts in Biotechnology; 2011

Ciprofloxacin (Cip) is the fifth largest generic antibiotic produced in the world keeping 24 % of the therapeutic prescription market (about US$ 2.3 million dollars).Cip (1-cyclopropyl-6-fluoro-1,4-dihydro-4-ox-o-7-(1-piperazinyl)-3-quinoline carboxylic acid) belong to the fluoroquinolone antibiotic family, a wide class of antibiotics with broad antibacterialspectrum.Cip is currently used in many Infections such as clinical respiratory, urinary tract and intestinal, intra-abdominal, gynecologic, infections of bones and joints .However, ciprofloxacin administration is currently associated with many undesirable and diverse physiological side effects. Many of the reported problems could be associated to a poor drugbiodisponibility because Cip posses poor solubility in physiological media. Cip is a "sticky" drug interacting with many molecules and stacking phenomena can surpass drug solubility and becominghighly toxic.In order to avoid undesirable secondary effects, controlled release techniques can be a feasible alternative for drug delivery. Biopolymeric-based formulations are atoxic, safe, can be tailored and targeted; posses well known loading capabilities,high stability and well-established release kinetics. Alginate is a linear polysaccharide of ß-D-mannuronic (M) and α-L-guluronic (G) acids found in algae and some bacteria that can be gelled by multivalent cations making a gel structure know asegg-box. Pectins are water-soluble polysaccharides present in the plant cell wall and are not degradable by intestinal enzymes. Pectins are composed of linear polysaccharides of partially metoxylated poly α-(1,4)-D-galacturonic acids. Theesterification degree (DE) of pectins has strong influence on biopolymer properties. Pectins are grouped into Low Methoxylated (LM) with DE below of 40 %, Medium Metoxylated (MM) with DE range between 40 to 60 %, and High Methoxylatedpectins (HM) with DE higher than 60 %.Biopolymer blends is an alternative strategy to increase the formulation stability, the amount of the cargo and target organ to be deliver the drug. Alginates and pectins showed interesting synergistic properties forming mixed gels.The aim of the present work is to study the encapsulation of Cip in biopolymeric blend gel matrices for oral drug delivery.