Injectable sustained-release formulations based on polyesters: from small molecule solutions to protein delivery to the eye

Diplôme Thèse Injectable sustained-release formulations based on polyesters: from small molecule solutions to protein delivery to the eye eng 2012-02-03 author Asmus Lutz 657909 director Gurny Robert 24779 director Moeller Michael 534286 director Allémann Eric 0000-0002-6598-9521 26730 10.13097/archive-ouverte/unige:18571 urn:nbn:ch:unige-185716 Sc. 4403 The liquid polyester hexylsubstituted poly(lactic acid) (hexPLA) was investigated toward its suitability as an excipient for parenteral sustained-release formulations. HexPLA can be synthesized in pharmaceutical quality by a direct polycondensation method. The resulting small molecular weight polymers fulfill the basic requirements for a parenteral excipient, like sterilizability and injectability. Small lipophilic molecules are soluble in the hexPLA polymer matrix to a high extent, while hydrophilic peptides and proteins form suspension formulations, which can be prepared by a one-step cryo-milling-mixing method. The degradation and release characteristics of these formulations are controllable via the polymer molecular weight and drug loading. Small molecule solutions released the active substance over several days and for suspension formulations release periods of up to 6 months in vivo were achieved. Furthermore, the matrix protected the incorporated therapeutic protein from the environment and released it in its bioactive form, rendering hexPLA interesting as parenteral sustained-release excipient. Dewey 615 31 Section des sciences pharmaceutiques 17 false 4c430ac3-ae94-4093-816e-a9596ad77272 Thesis Restricted Thesis manuscript.pdf 3811506 application/pdf Private 2012-08-20 92593837c708cf3ac6411142fd3f1ae851db43cd376cdeaa4fe976bfaf51e87e restrictedAccess Faculté des sciences / Section des sciences pharmaceutiques

Title	Published in	Access level	OA Policy	Year	Views	Downloads

Injectable sustained-release formulations based on polyesters: from small molecule solutions to protein delivery to the eye				2012	958	18

Archive ouverte UNIGE

Asmus, Lutz