Effect of octreotide surface density on receptor-mediated endocytosis in vitro and anticancer efficacy of modified nanocarrier in vivo after optimization.

The objective of the present work was to investigate the optimum density of octreotide on the surface of nanostructured lipid carriers (NLC) loaded with hydroxycamptothencine (HCPT) to enhance receptor-mediated endocytosis and tumor targeting selectivity. Different amounts of octreotide-polyethylene glycol (100) monostearate (OPMS), a ligand for somatostatin receptors (SSTRs), were coupled into NLC. In vitro evaluation of OPMS modified NLCs (O-NLCs) was done by studying the physicochemical properties, drug release, cellular uptake and cytotoxicity.

Effect of octreotide-polyethylene glycol(100) monostearate modification on the pharmacokinetics and cellular uptake of nanostructured lipid carrier loaded with hydroxycamptothecine.

A new conjugate, octreotide-polyethylene glycol(100) monostearate (OPMS), was developed for the enhancement of targeting delivery of hydroxycamptothecine (HCPT) loaded in nanostructured lipid carrier (NLC). 2 × 10(-3) and 5 × 10(-3) mmol of OPMS were respectively used to modify NLC so that the targeted nanocarriers with low and high ligand density were obtained. For comparison, the pegylated NLCs without octreotide were prepared by adding equal molar amounts of polyethylene glycol(100) monostearate (PGMS).

A novel lipoprotein-mimic nanocarrier composed of the modified protein and lipid for tumor cell targeting delivery.

Ursodeoxycholic acid (UA) modified protein-lipid nanocomplex (uP-LNC) as a novel biomimetic nanocarrier was developed for tumor-targeting delivery. Bovine serum albumin (BSA) was used as a model protein and its amino groups were covalently modified by UA. Lipid nanoparticle (LNP) composed of phospholipids, triglycerides and octadecylamine was prepared by using solvent evaporation method and was used as the core.