Amphiphilic poly(hydroxyethylaspartamide) derivative-based micelles as drug delivery systems for ferulic acid

Self-assembling micelles, potentially useful as drug delivery systems for ferulic acid (FA), were obtained in aqueous media from amphiphilic alpha,beta-poly(N-2-hydroxyethyl)-dl-aspartamide (PHEA) copolymers bearing at the polyamino acidic backbone both poly(ethyleneglycol) (2000 or 5000 Da) and hexadecylamine (C(16)) moieties, at a concentration of 7 x 10(- 3) and 4 x 10(- 3) g/l, respectively, with nanometre size and negative zeta potential. These micelles were able to entrap FA and to release it in a prolonged way in phosphate buffer solution at pH 7.4 and human plasma. These systems were also stable in storage conditions and have no cytotoxic effects on Caco-2, 16 HBE, HuDe and K562 cel…

Nanostructured formulations for the delivery of silibinin and other active ingredients for treating ocular diseases

Folate-targeted gold nanorods for effective combined photothermal-chemotherapy of osteosarcoma

Osteosarcoma (OS) is the most common primary malignant neoplasm of bone. The annual incidence of osteosarcoma is 8-11 per million in the age group of 15-19 years. Despite its rarity, it has been reported to be the second leading cause of cancer-related deaths in children and young adults. In particular with regard to OS therapy, a variety of nanostructures have been exploited in the areas of OS imaging. Among them, Gold nanorods (AuNRs) have unique optical and chemical-physical properties that make them appealing for biomedical applications such as photothermal therapy, drug delivery and imaging of solid tumors. The noble metal core is biologically inert, contributing to low toxicity and go…

Folate-mediated targeting of polymeric conjugates of gemcitabine.

The synthesis of two new macromolecular prodrugs for active tumor targeting was set up. Gemcitabine (2'-deoxy-2',2'-difluorocytidine) was conjugated to alpha,beta-poly(N-2-hydroxyethyl)-DL-aspartamide (PHEA) through succinyl or diglycolyl hydrolysable spacers. The targeting agent folic acid was attached to the macromolecular backbone through the aminocaproic spacer. The two conjugates [PHEA-(5'-succinylgemcitabine)-1'-carboxypentyl-folamide and PHEA-(5'-diglycolyl-gemcitabine)-1'-carboxypentyl-folamide], were purified and extensively characterised by spectroscopic (UV, IR and NMR) and chromatographic analyses to determine the correct chemical structure, the purity degree and the reaction yi…