Microencapsulation of rifampicin for the prevention of endophthalmitis: In vitro release studies and antibacterial assessment

• Published in: International journal of pharmaceutics 2016-05, Vol.505 (1-2), p.262-270
• Main Authors: Lee, Mi Yeon, Bourgeois, Sandrine, Almouazen, Eyad, Pelletier, Jocelyne, Renaud, François, Fessi, Hatem, Kodjikian, Laurent
• Format: Article
• Language: English
• Subjects: Anti-Bacterial Agents - administration & dosage; Anti-Bacterial Agents - pharmacology; Bacterial Adhesion - drug effects; Chemistry, Pharmaceutical - methods; Delayed-Action Preparations; Drug Carriers - chemistry; Drug Delivery Systems; Drug Liberation; Endophthalmitis; Endophthalmitis - microbiology; Endophthalmitis - prevention & control; Engineering Sciences; Intraocular delivery; Lactic Acid - chemistry; Materials; Microbial Sensitivity Tests; Microparticles; Microspheres; PLGA; Polyglycolic Acid - chemistry; Rifampicin; Rifampin - administration & dosage; Rifampin - pharmacology; Staphylococcal Infections - drug therapy; Staphylococcal Infections - microbiology; Staphylococcus epidermidis; Staphylococcus epidermidis - drug effects; Sustained delivery; Time Factors
• ISSN: 0378-5173; 1873-3476
• DOI: 10.1016/j.ijpharm.2016.03.026

Rifampicin encapsulated microparticles were designed for intraocular injection during cataract surgery to prevent postoperative endophthalmitis. (A) Molecular structure of rifampicin. (B) Microspheres morphology observed by scanning electron microscopic. (C) Antibacterial and antiadherent efficiencies of rifampicin loaded microparticles as percentage of control, assessed on bacterial suspension of Staphylococcus epidermidis over 24h. [Display omitted] 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.