Cabazitaxel liposomes with aptamer modification enhance tumor‑targeting efficacy in nude mice

Abstract

The present study investigated the feasibility of improving the tumor-targeting efficacy and decreasing the toxicity of liposomal cabazitaxel (Cab) with aptamer modification. The process involved preparing aptamer (TLS1c)-modified liposomes and studying the behavior of the liposomes in vitro and in vivo. TLS1c as an aptamer, which has high specificity for BNL 1ME A.7R.1 (MEAR) cells, was conjugated with Cab liposomes (Cab/lipo) to enhance MEAR tumor tissue targeting. Confocal laser scanning microscopy and flow cytometry analyses demonstrated that the fluorescence of the liposomes modified with the aptamer was notably stronger compared with that of the unmodified liposomes. Furthermore, the biodistribution data of the modified liposomes tested in tumor-bearing mice revealed high specificity of biotinylated TLS1c-modified Cab/lipo (BioTL-Cab/lipo) for tumor tissues. Furthermore, the modified liposomes demonstrated decreased cytotoxicity and simultaneously retained potent inhibition against tumor growth. It is likely that the specific binding of the aptamer (TLS1c) to the targeted cells (MEAR) facilitates the binding of the liposomes to the targeted cells. Therefore, BioTL-Cab/lipo may be considered as a promising delivery system to improve cell targeting and reduce drug toxicity in the treatment of cancer.

RGD peptide-mediated liposomal curcumin targeted delivery to breast cancer cells

“…19 Grafting liposomes with a variety of targeting ligands [e.g. hormones, 20 antibodies, 21 peptides, 22 aptamers 23 ] has proved successful in enhancing their specificity and targeting efficiency.…”

<p>Aptamers as Versatile Ligands for Biomedical and Pharmaceutical Applications</p>

“…In another study, tumoral delivery of cabazitaxel was improved using aptamer-modified liposomal delivery system (apt-liposomes) . 61 In this study, apt-liposomes increased the accumulation of cabazitaxel in the tumor tissue. These findings suggested that specific binding of aptamer (TLS1c) to the targeted cells (MEAR) facilitated the accumulation of liposomes in the target tissue.…”

On the Choice of the Extracellular Vesicles for Therapeutic Purposes

“…The liposomes are spherical lipid bilayers synthesized easily in the laboratory, whose features are dependent on the lipids of which are constituted [83,84,85]. However, there are a number of concerns on both their real efficacy in delivering the drugs to the disease site, and, more importantly, on the side effects due to the high catabolic index [86,87,88]. It is therefore mandatory to investigate the whole potential of exosomes as a natural delivery for both chemical and biological therapeutic molecules.…”