Enoxaparin (Enox) has been previously proposed as targeting ligands for tumor, due to the binding of the extracellular tumor matrix (ECM)components overexpressed in tumor tissues. Thus, in the present work we investigated the possibility to develop a parenteral Enox-coated self-emulsifying drug delivery system (SEDDS) for tumor targeting. Enox was chemically conjugated to palmitoyl chloride (PC) and then used to coat SEDDS. The formulations exhibited a size of 91-102 nm, and showed good stability in serum albumin and in plasma. Moreover, negligible hemolytic activity was found in the case of SEDDS and Enox-coated SEDDS. Furthermore, formulation coated with Enox showed a higher uptake on human breast adenocarcinoma and human epithelial colorectal adenocarcinoma cell lines, compared to uncoated SEDDS. The study provided the proof-of-principle to propose SEDDS for further investigation as novel candidate for tumor targeting by parenteral route of administration.
In vitro evaluation of tumor targeting ability of a parenteral enoxaparin-coated self-emulsifying drug delivery system
Campani V;
2019-01-01
Abstract
Enoxaparin (Enox) has been previously proposed as targeting ligands for tumor, due to the binding of the extracellular tumor matrix (ECM)components overexpressed in tumor tissues. Thus, in the present work we investigated the possibility to develop a parenteral Enox-coated self-emulsifying drug delivery system (SEDDS) for tumor targeting. Enox was chemically conjugated to palmitoyl chloride (PC) and then used to coat SEDDS. The formulations exhibited a size of 91-102 nm, and showed good stability in serum albumin and in plasma. Moreover, negligible hemolytic activity was found in the case of SEDDS and Enox-coated SEDDS. Furthermore, formulation coated with Enox showed a higher uptake on human breast adenocarcinoma and human epithelial colorectal adenocarcinoma cell lines, compared to uncoated SEDDS. The study provided the proof-of-principle to propose SEDDS for further investigation as novel candidate for tumor targeting by parenteral route of administration.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
