Doctoral thesis
English

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

ContributorsAsmus, Lutz
Defense date2012-02-03
Abstract

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.

Citation (ISO format)
ASMUS, Lutz. Injectable sustained-release formulations based on polyesters: from small molecule solutions to protein delivery to the eye. Doctoral Thesis, 2012. doi: 10.13097/archive-ouverte/unige:18571
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Creation20/02/2012 15:37:00
First validation20/02/2012 15:37:00
Update time14/03/2023 17:09:05
Status update14/03/2023 17:09:05
Last indexation29/10/2024 19:03:19
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