UNITEFA   23945
UNIDAD DE INVESTIGACION Y DESARROLLO EN TECNOLOGIA FARMACEUTICA
Unidad Ejecutora - UE
congresos y reuniones científicas
Título:
PREPARATION OF HUMAN SERUM ALBUMIN (HSA) NANOPARTICLES STABILIZED BY POLYMER COATING FOR THE TREATMENT OF CORNEAL NEOVASCULARIZATION
Autor/es:
LLABOT J.M; AGÜEROS M; DÁVILA CABALLERO M.J; BOIERO C; ALLEMANDI D; IRACHE J.M
Lugar:
Pamplona
Reunión:
Simposio; 19TH Simposio Internacional de Microencapsulacion; 2013
Resumen:
Topical application on to the eye´s surface is a common route for drugs administration. However, the protective mechanisms (blinking, lachrymation, and drainage) decrease the bioavailability of drug by removing rapidly the formulation1 Nanoparticles (NPs) have emerged as a suitable vehicle for drugs administration, and have yielded promising results in ophthalmic field2. There are a large variety of materials, being natural biopolymers more advantageous over synthetic materials. In this context, human serum albumin (HSA) was selected to prepare the NPs due to they are biodegradable, nontoxic and non antigenic. However, these systems requires to be stabilized to maintain their structure during its administration. HSA-NPs are typically crosslinked by glutaraldehyde3 (reacts with free amines on HSA), but could also reacts with any amines on the encapsulated drug joined the potential toxicity of glutaraldehyde. Protein crosslinking can be easily achieved by direct reaction between functional groups in HSA and diverse polymers. As an alternative, we considered the possibility of stabilizing HSA-NPs with Gantrez ES-425® by entrapping Suramine (SM) or Bevacizumab (BV). HSA-Np were prepared by a desolvation method with addition of ethanol to a 1,25% solution of HSA (1:2) under continuous stirring. Then, coacervates were hardened by crosslinking with Gantrez ES425(R) (0.5 mg/mg protein) for 5 min. After, the ethanol elimination, NPs were purified by centrifugation. SM (0,2 mg/mg protein) or BV (BV 0.13mg/mg protein) was incorporated into the HSA solution before adding ethanol. The yield of the nanoparticle formation process was determined by micro BCA, SM was quantified by UV and BV was quantifie by ELISA. The phisico-chemical characteristics was determined by measuring the particle size, polydispersity index, Z potential, yield, and drug loading. Besides, the morphology was determined by SEM. The results indicate that the interaction between the COO- groups of Gantrez ES425 and NH3+ of the protein was satisfactory to crosslink the surface of HSA-NP. The size of NPs ranged from 200-270 nm. The zeta-potential was negative (~ -35 mV) and displayed a high yield of the process (~ 80%). Both drugs were encapsulated (~ 80% for SM and ~ 90% for BV). These findings indicate that adequate particles were obtained in excellent yields what become prime candidates for use in vivo in experimental animal models of corneal neovascularization