RT Journal Article
T1 Optimising the controlled release of dexamethasone from a new generation of PLGA-based microspheres intended for intravitreal administration
A1 Rodríguez Villanueva, Javier
A1 Bravo Osuna, Irene
A1 Herrero Vanrell, María Del Rocío
A1 Molina Martínez, Irene Teresa
A1 Guzmán Navarro, M.
AB Successful therapy for chronic diseases affecting the posterior segment of the eye requires sustained drug concentrations at the site of action for extended periods of time. To achieve this, it is necessary to use high systemic doses or frequent intraocular injections, both associated with serious adverse effects. In order to avoid these complications and improve patient`s quality of life, an experimental study has been conducted on the preparation of a new generation of biodegradable poly D-L(lactide-co-glycolide (50:50) (PLGA) polymer microspheres (MSs) loaded with Dxm, vitamin E and/or human serum albumin (HSA). Particles were prepared according to a S/O/W encapsulation method and the 20-40μm fraction was selected. This narrow size distribution is suitable for minimally invasive intravitreal injection by small calibre needles.Characterisation of the MSs showed high Dxm loading and encapsulation efficiency (> 90%) without a strong interaction with the polymer matrix, as revealed by DSC analysis. MSs drug release studies indicated a small burst effect (lower than 5%) during the first five hours and subsequently, drug release was sustained for at least 30 days, led by diffusion and erosion mechanisms. Dxm release rate was modulated when solid state HSA was incorporated into MSs formulation. SDS-PAGE analysis showed that the protein maintained its integrity during the encapsulation process, as well as for the release study. MSs presented good tolerance and lack of cytotoxicity in macrophages and HeLa cultured cells. After 12 months of storage under standard refrigerated conditions (41ºC), MSs retained appropriate physical and chemical properties and analogous drug release kinetics. Therefore, we conclude that these microspheres are promising pharmaceutical systems for intraocular administration, allowing controlled release of the drug.
PB Elsevier
SN 0928-0987
YR 2016
FD 2016-09-20
LK https://hdl.handle.net/20.500.14352/18742
UL https://hdl.handle.net/20.500.14352/18742
LA eng
NO Rodríguez Villanueva, J., Bravo Osuna, I., Herrero Vanrell, M. R. et al. «Optimising the Controlled Release of Dexamethasone from a New Generation of PLGA-Based Microspheres Intended for Intravitreal Administration». European Journal of Pharmaceutical Sciences, vol. 92, septiembre de 2016, pp. 287-97. DOI.org (Crossref), https://doi.org/10.1016/j.ejps.2016.03.012.
NO Fundación General de la Universidad de Alcalá
NO Grupo de Investigación UCM 920415
DS Docta Complutense
RD 9 abr 2025