Memantine Loaded Biodegradable Polymeric Nanoparticles for Glaucoma Treatment
نویسندگان
چکیده
Extended Abstract Recent studies have shown that treatment with Memantine (MEM) protected retinal ganglion cells in monkey models of glaucoma, reducing ganglion cell loss during treatment with this drug (Hare et al, 2009). An important goal is the development of a safe and effective formulation for delivery of Memantine to the eye posterior segment. In this way, biodegradable polyesters such as poly (lactic-coglycolic acid) (PLGA) had demonstrated to be safe as drug delivery systems. Moreover, poliethilenglicol coating could increase the ocular residential time of the particles. For these reason in this work new MEM-PLGA-PEG nanoparticles had been developed in order to accomplish the quality standards for ocular drug delivery. (Vega et al, 2012) MEM-PLGA-PEG nanoparticles were prepared by double emulsion method. Briefly, the first step consisted on the preparation of a w/o emulsion and ultrasound energy was applied. Then, a second water phase was added and a second sonication was done obtaining w1/o/w2 emulsion. Finally a slight amount of surfactant was added and nanoparticles were stirred overnight in order to eliminate organic solvent. (Zambaux et al, 1998). Different factorial designs were carried out in order to determine the formulation critical factors involved in double emulsion method. In these assays, the effect of concentration of formulation compounds, sonication parameters, pH and volume phase ratios on size, polydispersion index, zeta potential and encapsulation efficiency was studied. NPs characterization was performed by dynamic light scattering (DLS), showing an average size smaller than 200 nm and a monodisperse population, both confirmed by transmission electron microscopy (TEM). Surface charge of the formulation has been found to be negative being encapsulation efficiency higher than 50 %. Short-term stability studies were carried out at 25oC during the first 3 months. Backscattering profile showed no significant modifications due to particle size agregation suggesting that nanoparticles would be stable. In vitro Hen ́s Egg Test-Chorioallantoid Membrane (HET-CAM) was carried out showing optimal ocular tolerance of the nanoparticles in contrast with the free drug which was found to be irritating. These agree with in vivo Draize test results. In conclusion, the association MEM loaded PLGA-PEG nanoparticles provides a new and stable ocular drug delivery system which had demonstrated to be less irritating than the free drug.
منابع مشابه
Paclitaxel-loaded biodegradable nanoparticles developed by direct dialysis and electrodydrodynamic atomization methods
This paper presents a new method for fabrication of biodegradable polymeric nanoparticles as carriers for anticancer drug paclitaxel. Emulsion solvent evaporation method was frequently employed to prepare polymeric nanoparticles for drug delivery systems in which the emulsifier such as PVA has to be used. In this study, direct dialysis was employed to fabricate paclitaxel-loaded biodegradable p...
متن کاملMemantine loaded PLGA PEGylated nanoparticles for Alzheimer’s disease: in vitro and in vivo characterization
BACKGROUND Memantine, drug approved for moderate to severe Alzheimer's disease, has not shown to be fully effective. In order to solve this issue, polylactic-co-glycolic (PLGA) nanoparticles could be a suitable solution to increase drug's action on the target site as well as decrease adverse effects. For these reason, Memantine was loaded in biodegradable PLGA nanoparticles, produced by double ...
متن کاملPolymeric nanoparticles containing diazepam: preparation, optimization, characterization, in-vitro drug release and release kinetic study
Nanoparticles formulated from biodegradable polymers like poly(lactic-co-glycolic acid) (PLGA) are being extensively investigated as drug delivery systems due to their two important properties such as biocompatibility and controlled drug release characteristics. The aim of this work to formulated diazepam loaded PLGA nanoparticles by using emulsion solvent evaporation technique. Polyvinyl alcoh...
متن کاملA biodegradable polymeric system for peptide–protein delivery assembled with porous microspheres and nanoparticles, using an adsorption/infiltration process
A biodegradable polymeric system is proposed for formulating peptides and proteins. The systems were assembled through the adsorption of biodegradable polymeric nanoparticles onto porous, biodegradable microspheres by an adsorption/infiltration process with the use of an immersion method. The peptide drug is not involved in the manufacturing of the nanoparticles or in obtaining the microspheres...
متن کاملSynthesis and Characterization of a Magnetically Responsive Polymeric Drug Delivery System
A magnetic target drug delivery system consisting of biodegradable polymeric microspheres (poly D, L-lactic acid) loaded with magnetite nanoparticles (10-100 nm) and anticancer drug (paclitaxel) was studied. The magnetite nanoparticles were synthesized by chemical precipitation. The as-synthesized magnetite nanoparticles were subsequently introduced into a mixture of polymer magnetic polymeric ...
متن کامل