title: Microencapsulation of rifampicin for the prevention of endophthalmitis: In vitro release studies and antibacterial assessment.
abstract: Rifampicin encapsulated microparticles were designed for intraocular injection after cataract surgery to prevent postoperative endophthalmitis. Microparticles were formulated by emulsification diffusion method using poly(lactic acid-co-glycolic acid) (PLGA) as polymer in order to propose a new form of rifampicin that overcome its limitations in intraocular delivery. Depending on processing formulation, different types of microparticles were prepared, characterized and evaluated by in vitro release studies. Two types of microparticles were selected to get a burst release of rifampicin, to reach minimal inhibitory concentrations to inhibit 90% of Staphylococcus epidermidis mainly involved in postoperative endophthalmitis, combined with a sustained release to maintain rifampicin concentration over 24h. The antibacterial activity and antiadhesive property on intraocular lenses were evaluated on S. epidermidis. Microparticles, with a rapid rifampicin release profile, showed an effect towards bacteria development similar to free rifampicin over 48h. However, slow-release profile microparticles exhibited a similar antibacterial effect during the first 24h, and were able to destroy all the S epidermidis in the medium after 30h. The association of the two formulations allowed obtaining interesting antibacterial profile. Moreover, rifampicin-loaded microparticles have shown a very efficient anti-adherent effect of S. epidermidis on intraocular lenses at 24h. These results propose rifampicin microparticles as suitable for antibioprophylaxis of the postoperative endophthalmitis.
authors.affiliation: University of Lyon, University Claude Bernard - Lyon 1, Laboratoire d'Automatique et de Génie des Procédés - LAGEP UMR CNRS 5007, F-69622 Villeurbanne, France.
authors.forename: Mi Yeon
authors.initials: MY
authors.lastname: Lee
authors.affiliation: University of Lyon, University Claude Bernard - Lyon 1, Laboratoire d'Automatique et de Génie des Procédés - LAGEP UMR CNRS 5007, F-69622 Villeurbanne, France; University of Lyon, University Claude Bernard - Lyon 1, Institut des Sciences Pharmaceutiques et Biologique ISPB - School of Pharmacy, F-69373 Lyon, France. Electronic address: sandrine.bourgeois@univ-lyon1.fr.
authors.forename: Sandrine
authors.initials: S
authors.lastname: Bourgeois
authors.affiliation: University of Lyon, University Claude Bernard - Lyon 1, Laboratoire d'Automatique et de Génie des Procédés - LAGEP UMR CNRS 5007, F-69622 Villeurbanne, France; University of Lyon, University Claude Bernard - Lyon 1, Institut des Sciences Pharmaceutiques et Biologique ISPB - School of Pharmacy, F-69373 Lyon, France.
authors.forename: Eyad
authors.initials: E
authors.lastname: Almouazen
authors.affiliation: University of Lyon, University Claude Bernard - Lyon 1, Laboratoire d'Automatique et de Génie des Procédés - LAGEP UMR CNRS 5007, F-69622 Villeurbanne, France; University of Lyon, University Claude Bernard - Lyon 1, Institut des Sciences Pharmaceutiques et Biologique ISPB - School of Pharmacy, F-69373 Lyon, France.
authors.forename: Jocelyne
authors.initials: J
authors.lastname: Pelletier
authors.affiliation: University of Lyon, University Claude Bernard - Lyon 1, MATEIS UMR-CNRS 5510, Equipe I2B "Interactions Biologiques et Biomatériaux", INSA de Lyon, F-69622 Villeurbanne, France.
authors.forename: François
authors.initials: F
authors.lastname: Renaud
authors.affiliation: University of Lyon, University Claude Bernard - Lyon 1, Laboratoire d'Automatique et de Génie des Procédés - LAGEP UMR CNRS 5007, F-69622 Villeurbanne, France; University of Lyon, University Claude Bernard - Lyon 1, Institut des Sciences Pharmaceutiques et Biologique ISPB - School of Pharmacy, F-69373 Lyon, France.
authors.forename: Hatem
authors.initials: H
authors.lastname: Fessi
authors.affiliation: University of Lyon, University Claude Bernard - Lyon 1, MATEIS UMR-CNRS 5510, Equipe I2B "Interactions Biologiques et Biomatériaux", INSA de Lyon, F-69622 Villeurbanne, France; Croix-Rousse University Hospital, Department of Ophthalmology, Hospices Civils de Lyon F-69004, Lyon, France.
authors.forename: Laurent
authors.initials: L
authors.lastname: Kodjikian
mesh_terms: D000900:Anti-Bacterial Agents / Q000008:administration & dosage* / Q000494:pharmacology; D001422:Bacterial Adhesion / Q000187:drug effects; D002626:Chemistry, Pharmaceutical / Q000379:methods; D003692:Delayed-Action Preparations; D004337:Drug Carriers / Q000737:chemistry; D016503:Drug Delivery Systems; D065546:Drug Liberation; D009877:Endophthalmitis / Q000382:microbiology / Q000517:prevention & control*; D019344:Lactic Acid / Q000737:chemistry; D008826:Microbial Sensitivity Tests; D008863:Microspheres; D011100:Polyglycolic Acid / Q000737:chemistry; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D012293:Rifampin / Q000008:administration & dosage* / Q000494:pharmacology; D013203:Staphylococcal Infections / Q000188:drug therapy / Q000382:microbiology; D013212:Staphylococcus epidermidis / Q000187:drug effects*; D013997:Time Factors
chemical_list: D000900:Anti-Bacterial Agents; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid; D012293:Rifampin
keywords: Endophthalmitis; Intraocular delivery; Microparticles; PLGA; Rifampicin; Sustained delivery