PHEA-PLA biocompatible nanoparticles by technique of solvent evaporation from multiple emulsions

Abstract

Nanocarriers of amphiphilic polymeric materials represent versatile delivery systems for poorly water soluble drugs. In this work the technique of solvent evaporation from multiple emulsions was applied to produce nanovectors based on new amphiphilic copolymer, the α,β-poly(N-2-hydroxyethyl)-DL-aspartamide-polylactic acid (PHEA-PLA), purposely synthesized to be used in the controlled release of active molecules poorly soluble in water. To this aim an amphiphilic derivative of PHEA, a hydrophilic polymer, was synthesized by derivatization of the polymeric backbone with hydrophobic grafts of polylactic acid (PLA). The achieved copolymer was thus used to produce nanoparticles loaded with α tocopherol (vitamin E) adopted as lipophilic model molecule. Applying a protocol based on solvent evaporation from multiple emulsions assisted by ultrasonic energy and optimizing the emulsification process (solvent selection/separation stages), PHEA-PLA nanostructured particles with total α tocopherol entrapment efficiency (100%), were obtained. The drug release is expected to take place in lower times with respect to PLA due to the presence of the hydrophilic PHEA, therefore the produced nanoparticles can be used for semi-long term release drug delivery systems.

Keywords: 1,1′-Carbonyldiimidazole—CDI: PubChem CID: 68263; Amphiphilic polymer; Biocompatible polymer; Diethylamine—DEA: PubChem CID: 8021; Drug delivery; Emulsions; Ethanolamine: PubChem CID: 700; N,N′-dimethylformamide—DMF: PubChem CID: 6228; Nanoparticles; PHEA–PLA; Poly-lactic acid—PLA: PubChem CID: 612; Polysuccinimide—PSI: PubChem CID: 5960; Polyvinyl alcohol—PVA: PubChem CID: 11199; Ultrasonic energy; α,β-Poly(N-2-hydroxyethyl)-dl-aspartamide—PHEA: PubChem CID: 155399; α-Tocopherol: PubChem CID: 14985.