<p>Functionalized docetaxel-loaded lipid-based-nanosuspensions to enhance antitumor efficacy in vivo</p>

Abstract

Purpose: To further enhance the antitumor efficacy through targeted delivery, DTX loaded lipid-based-nanosuspensions (DTX-LNS) were prepared and functionalized by PEGylation or NGR modification to develop DSPE-PEG 2000 modified DTX-LNS (P-DTX-LNS) or DSPE-PEG 2000 -NGR modified DTX-LNS (N-DTX-LNS), respectively. Methods: Based on our previous work, functionalized DTX-LNS including P-DTX-LNS and N-DTX-LNS were prepared using thin-film hydration, and then characterized. Release behavior, stability in vitro, cytotoxicity and cellular uptake of functionalized LNS were observed. To demonstrate tumor targeting efficiency of functionalized DTX-LNS, in vivo real-time and ex vivo imaging study were conducted. Furthermore, therapeutic efficacy in vivo was evaluated in an H22-bearing mice model. Results: Functionalized DTX-LNS 100–110 nm in diameter were successfully prepared and exhibited good stability under various conditions. In vitro release studies demonstrated that DTX was released from functionalized DTX-LNS steadily and reached approximately 95% at 48 hrs. Functionalized DTX-LNS showed dose-dependent cytotoxicity and time-dependent internalization in human hepatocellular liver carcinoma cells (HepG2) cells. In vivo real-time and ex vivo imaging results indicated that tumor targeting efficiencies of P-DiR-LNS and N-DiR-LNS were 29.9% and 34.3%, respectively. Moreover, evaluations of in vivo antitumor efficacy indicated that functionalized DTX-LNS effectively inhibited tumor growth with low toxicity. Conclusion: The functionalized LNS exhibited suitable particle size, nearly spherical structure, enough drug loading and great potentials for large-scale production. The results in vitro and in vivo demonstrated that functionalized LNS could realize tumor targeting and antitumor efficacy. Consequently, functionalized DTX-LNS could be expected to be used for tumor targeting therapy.

Biomimetic Gold Nanostructure with a Virus-like Topological Surface for Enhanced Antigen Cross-Presentation and Antitumor Immune Response

“…Lymphoid organs, in which DCs are in the proximity of T cells, are the ideal microenvironments for efficient priming, activation, and expansion of T cells. , To measure the ability of AuNV to migrate to draining lymph nodes (LNs), Cy7-labeled gold nanostructures (Figure S2) were subcutaneously injected into the right flank of C57BL/6 mice, and the fluorescence at the injection site was imaged with a Lumina II imaging system at different time points. All gold nanostructures remained in the injection site for a long time, which will be beneficial for the continuous delivery of antigens and the persistent activation of DCs.…”

Combined Biomimetic MOF-RVG15 Nanoformulation Efficient Over BBB for Effective Anti-Glioblastoma in Mice Model

“…The collected samples were centrifuged (18000 rcf, 10 min), and the supernatant was analyzed for DTX content using a previously established HPLC method. 53 Finally, the cumulative release of DTX was calculated and an in vitro release curve was plotted.…”

Lipid based nanoparticles as a novel treatment modality for hepatocellular carcinoma: a comprehensive review on targeting and recent advances

“…Regular, pegylated and NGR modified nanosuspensions showed higher accumulation in HepG2 cells compared to human normal liver cells (HL-7702). NGR modification greatly enhanced nanosuspension accumulation in the tumor tissue compared to pegylated and regular nanosuspensions in H22 tumor bearing mice [ 269 ].…”