RT Journal Article
T1 Novel biodegradable polyesteramide microspheres for controlled drug delivery in Ophthalmology
A1 Andrés Guerrero, Vanessa
A1 Zong, Mengmeng
A1 Ramsay, Eva
A1 Rojas López, Blanca
A1 Sarkhel, Sanjay
A1 Gallego Collado, Beatriz Isabel
A1 Hoz Montañana, Rosa de
A1 Ramírez Sebastián, Ana Isabel
A1 Salazar Corral, Juan José
A1 Triviño Casado, Alberto
A1 Ramirez Sebastian, Jose Manuel
A1 Amo, Eva M. del
A1 Cameron, Neil
A1 Las Heras Polo, Beatriz de
A1 Urtti, Arto
A1 Mihov, George
A1 Dias, Aylvin
A1 Herrero Vanrell, Rocío
AB Most of the posterior segment diseases are chronic and multifactorial and require long-term intraocular medication. Conventional treatments of these pathologies consist of successive intraocular injections, which are associated with adverse effects. Successful therapy requires the development of new drug delivery systems able to release the active substance for a long term with a single administration. The present work involves the description of a new generation of microspheres based on poly(ester amide)s (PEA), which are novel polymers with improved biodegradability, processability and good thermal and mechanical properties. We report on the preparation of the PEA polymer, PEA microspheres (PEA Ms) and their characterization. PEA Ms (~ 15 μm) were loaded with a lipophilic drug (dexamethasone) (181.0 ± 2.4 μg DX/mg Ms). The in vitro release profile of the drug showed a constant delivery for at least 90 days. Based on the data from a performed in vitro release study, a kinetic ocular model to predict in vivo drug concentrations in a rabbit vitreous was built. According to the pharmacokinetic simulations, intravitreal injection of dexamethasone loaded PEA microspheres would provide release of the drug in rabbit eyes up to 3 months. Cytotoxicity studies in macrophages and retinal pigment epithelial cells revealed a good in vitro tolerance of the microsystems. After sterilization, PEA Ms were administered in vivo by subtenon and intravitreal injections in male Sprague–Dawley rats and the location of the microspheres in rat eyes was monitored. We conclude that PEA Ms provide an alternative delivery system for controlling the delivery of drugs to the eye, allowing a novel generation of microsphere design.
PB Elsevier
SN 0168-3659
YR 2015
FD 2015-08-10
LK https://hdl.handle.net/20.500.14352/23243
UL https://hdl.handle.net/20.500.14352/23243
LA eng
NO Received 3 March 2015, Revised 18 May 2015, Accepted 19 May 2015, Available online 21 May 2015
NO Unión Europea. FP7
NO NMP Theme of the Cooperation Programme
DS Docta Complutense
RD 17 jul 2024