Polyaspartamide-g-Polylactide graft cpolymers able to form nanoparticles obtained by a novel synthetic strategy.

Interaction Between drug loaded Polyaspartamide-polylactide-polisorbate based micelles and cell membrane models: a calorimetric study

Amphiphilic biodegradable copolymers, for their ability to self-assemble into micelle-like aggregates, with a suitable loading capacity, are of emerging interest for the delivery of water-insoluble drugs. α,β-Poly[(N-hydroxyethyl)-dl-aspartamide] (PHEA) is suitable to obtain amphiphilic graft copolymers. These copolymers can be obtained starting from PHEA-ethylenediamine (PHEA-EDA) which is functionalized with polysorbate 80 (PS₈₀, like targeting residues to the brain) and polylactide (PLA, like hydrophobic chains) in order to obtain polymeric micelles of PHEA-EDA-PS₈₀-PLA potentially useful to release drugs to the central nervous system. In this paper, the interaction and absorption of PHE…

Biocompatible polymeric micelles with polysorbate 80 for use in brain targeting.

In this paper, the synthesis and characterization of novel amphiphilic graft copolymers based on an alpha,beta-poly(N-2-hydroxyethyl)-D, L-aspartamide (PHEA) backbone and D, L-polylactic acid (PLA) hydrophobic side chains are reported. These copolymers were obtained starting from PHEA-ethylenediamine (PHEA-EDA), which was functionalized with polysorbate 80 (PS(80)) and/or PLA in order to obtain the PHEA-EDA-PS(80)-PLA and PHEA-EDA-PLA samples, respectively. The degrees of derivatization, DD(PS80) and DD(PLA), of PHEA-EDA-PS80-PLA, calculated by (1)H-NMR, resulted in being 1.2 +/- 0.03 mol% and 0.54 +/- 0.05 mol%, respectively, while that of PHEA-EDA-PLA was found to be 0.60 +/- 0.05 mol%. S…

SINTESI E CARATTERIZZAZIONE DI UN NUOVO DERIVATO DEL PHEA PER IL DIREZIONAMENTO ATTIVO DI FARMACI AL SISTEMA NERVOSO CENTRALE (SNC)

POLYMERIC MICELLES FOR DRUG TARGETING TO THE BRAIN

NANOPARTICELLE POLIMERICHE OTTENUTE DA NUOVI COPOLIMERI DI UNA POLIASPARTAMIDE

NANOPARTICLES BASED ON NOVEL AMPHIPHILIC POLYASPARTAMIDE COPOLYMERS

In this article, the synthesis of two amphiphilic polyaspartamide copolymers, useful to obtain polymeric nanoparticles without using surfactants or stabilizing agents, is described. These copolymers were obtained starting from α,β-poly-(N-2-hydroxyethyl)-dl-aspartamide (PHEA) by following a novel synthetic strategy. In particular, PHEA and its pegylated derivative (PHEA-PEG2000) were functionalized with poly(lactic acid) (PLA) through 1,1′-carbonyldiimidazole (CDI) activation to obtain PHEA–PLA and PHEA-PEG2000–PLA graft copolymers, respectively. These copolymers were properly purified and characterized by 1H-NMR, FT-IR, and Size Exclusion Chromatography (SEC) analyses, which confirmed that…

NANOPARTICLES CONTAINING RIVASTIGMINE FOR THE TREATMENT OF ALZHEIMER DISEASE

Biocompatible micelles based on squalene portions linked to pegylated polyaspartamide as potential colloidal drug carriers