Aqueous-core PEG-coated PLA nanocapsules for an efficient entrapment of water soluble anticancer drugs and a smart therapeutic response

• Aqueous-core PLA nanocapsules allowed to efficiently entrap hydrophilic compounds.
• Gemcitabine chloride was entrapped in order to increase its anticancer properties.
• The physicochemical stability of nanocapsules was preserved up to 6 months.
• The colloids favored a decrease of the drug efficacious dosage.
• The nanocapsules evidenced a great localization in the tumor masses.

Novel PEGylated PLA nanocapsules (PEG-AcPLA nanocapsules), loading high percentage of water soluble drugs have been formulated by using multiple emulsion technique without using conventional stabilizers. In particular, sodium deoxycholate hydrate has been used to obtain nanocapsules having a mean diameter of about 200 nm and a polydispersity index of ∼0.1. Gemcitabine hydrochloride (GEM) was used as a model of hydrophilic drug. GEM-loaded PEG-AcPLA nanocapsules demonstrated a high encapsulation efficacy and the drug-release followed a zero-order kinetic. MTT-assay evidenced an increased antitumor effect of GEM-loaded PEG-AcPLA nanocapsules compared to the free drug on different cancer cell lines and confocal laser scanning microscopy showed a significant improvement of cell interaction at 6 h of incubation. In vivo anticancer activity of GEM-loaded PEG-AcPLA nanocapsules using two xenograft murine models of human solid tumors further supported the efficacy of this nano-drug, thus providing preliminary results about the potential clinical application of this innovative nanotherapeutic.

Novel PEGylated aqueous core PLA-nanocapsules were realized with the aim of efficiently entrapping water-soluble compounds. Gemcitabine hydrochloride was chosen as model drug and it was demonstrated that encapsulating it in the nanosystems allowed the increase of its anticancer efficacy in both in vitro and in vivo tests. This new formulation could represent a valuable innovative nanomedicine to be used in clinical trials.Figure optionsDownload high-quality image (108 K)Download as PowerPoint slide