New generation of poly(ortho esters): synthesis, characterization, kinetics, sterilization and biocompatibility

Article Article scientifique Article New generation of poly(ortho esters): synthesis, characterization, kinetics, sterilization and biocompatibility eng 1997 author Zignani Monia 42214 author Merkli Alain 27497 author Sintzel Martina Barbara 30099 author Bernatchez Stéphanie 27154 author Kloeti Werner 25694 author Heller Jorge author Tabatabay Cyrus A. 28691 author Gurny Robert 24779 115-129 10.1016/S0168-3659(97)00050-3 0168-3659 After a brief historical overview of the development of three families of poly(otho esters) (POEs), the physico-chemical characteristics, drug release properties and biocompatibility of the third generation is discussed. Its synthesis is based on a transesterification reaction between 1,2,6-hexanetriol and trimethylorthoacetate. This viscous hydrophobic polymer has been used for the sustained release of 5-fluorouracil (5-FU) or mitomycin C (MMC) in glaucoma filtering surgery. It shows a good correlation between drug release and polymer erosion and can be injected using a hydraulic syringe. Drug release can be modulated by using different molecular weights of the polymer, or by adding basic or acidic excipients. Because conventional sterilization methods using gamma or electron beam-irradiation can not used due to changes in molecular weight and dynamic viscosity resulting from backbone cleavage, an aseptic fabrication procedure has been developed and validated. POE biocompatibility has been established after subconjunctival injections of POE, monomers and degradation products in rabbits. Better control of the microenvironmental pH during polymer degradation has been achieved by using an in situ formed buffer system. Poly(ortho esters) Sterilization Biocompatibility Release kinetics Ophthalmology 5-Fluorouracil Mitomycin C Dewey 540 Dewey 615 38 Département de chimie physique 142 31 Section des sciences pharmaceutiques 17 false Journal of controlled release 48 2 b79426cf-28c1-4a41-ba46-2c6ff40418f3 Article (Published version) Restricted ZIGNANI_JCR_1997129.pdf 323543 application/pdf restrictedAccess Faculté des sciences / Section de chimie et biochimie / Département de chimie physique Faculté des sciences / Section des sciences pharmaceutiques

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New generation of poly(ortho esters): synthesis, characterization, kinetics, sterilization and biocompatibility	Journal of controlled release			1997	284	0

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Kloeti, Werner