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PEGylated nanostructured lipid carriers loaded with 10‐hydroxycamptothecin: an efficient carrier with enhanced anti‐tumour effects against lung cancer

Most drugs do not have the pharmacokinetic features required for optimal pulmonary delivery. In this study, we developed PEGylated nanostructured lipid carriers (PEG‐NLCs) to improve the delivery of anti‐tumour agents to lung tumours. PEG‐40 NLCs modified with PEG‐40 stearate (molecular weight 2000 Da), PEG‐100 NLCs modified with PEG‐100 stearate (molecular weight 5000 Da) and NLCs without PEG modification were prepared by melt‐emulsification and homogenization, and were loaded with 10‐hydroxycamptothecin (HCPT). They were investigated in terms of physiological characteristics, biodistribution, cellular uptake, and anti‐tumour effect in‐vivo. PEG‐NLCs exhibited regular morphology, with a spherical shape. The particle size (measured by laser diffraction) was approximately 100 nm. Encapsulation in PEG‐NLCs protected the active lactone form of HCPT compared with HCPT solution after incubation with plasma. In biodistribution studies, PEG‐NLCs, especially PEG‐40 NLCs, had longer circulation time and decreased uptake by the reticuloendothelial system (RES) compared with unmodified NLCs. PEG‐NLCs accumulated in the lungs after i.v. injection in mice. PEG‐NLCs showed enhanced cellular uptake by human lung adenocarcinoma epithelial A549 cells. In‐vivo experiments indicated that PEG‐NLCs loaded with HCPT have superior efficacy against A549 lung cancer compared with HCPT solution and NLCs. These results suggest that PEG‐NLCs is a promising delivery system for HCPT in the treatment of lung cancer.