title: Improved delivery of angiogenesis inhibitors from PLGA:poloxamer blend micro- and nanoparticles.
abstract: Clinical studies have demonstrated the efficacy of new strategies in cancer therapy, such as chemotherapy and radiotherapy, associated to the administration of tumour vascularization inhibitors. A critical limitation for the clinical application of angiogenesis inhibitors relies in their instability in biological environment and high-dose requirements. This work has attempted to overcome this limitation by designing an adequate delivery vehicle consisting of PLGA:poloxamer blend micro- and nanoparticles. The potential of this delivery system was investigated for a new synthetic angiogenesis inhibitor named polyaminoacid JS-2892b. PLGA:poloxamer (ratio 10 : 1) blend microparticles were prepared by the oil-in-oil emulsion technique, while PLGA:poloxamer (ratio 1 : 1) blend nanoparticles were obtained by a modified solvent diffusion technique. The results showed that, by adjusting the formulation conditions, it was possible to efficiently encapsulate the polyaminoacid JS-2892b within PLGA:poloxamer micro- (particle size of 20 microm and encapsulation efficiency higher than 90%) and nanoparticles (particle size of less than 280 nm and encapsulation efficiency of 52%). In addition, the delivery of the polyaminoacid JS-2892b from the particles could be controlled, without altering its stability, for extended periods of time (from a few days to over a month). The release of the encapsulated compound was significantly affected by the particle size and the way the drug is dispersed into the polymeric matrix. Therefore, this study provides information about the formulation conditions and potential of biodegradable particles for the controlled release of polyaminoacid JS-2892b.
authors: Department of Pharmaceutical and Toxicological Chemistry, University of Naples Federico II, Naples, Italy.
authors: Ivana
authors: I
authors: d'Angelo
authors: Yolanda
authors: Y
authors: Parajó
authors: Anikó
authors: A
authors: Horváth
authors: György
authors: G
authors: Kéri
authors: Maria Immacolata
authors: MI
authors: La Rotonda
authors: María José
authors: MJ
authors: Alonso
mesh_terms: D020533:Angiogenesis Inhibitors / Q000008:administration & dosage*; D003692:Delayed-Action Preparations / Q000737:chemistry*; D007700:Kinetics; D019344:Lactic Acid / Q000737:chemistry*; D053758:Nanoparticles / Q000737:chemistry*; D010316:Particle Size; D020442:Poloxamer / Q000737:chemistry*; D011100:Polyglycolic Acid / Q000737:chemistry*; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer
chemical_list: D020533:Angiogenesis Inhibitors; D003692:Delayed-Action Preparations; D020442:Poloxamer; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid