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RNA Interference and Gene Delivery / DNA and Nucleic Acid Chemistry · Journal article
Molecules · September 7, 2026
Early or partial results. Treat as a signal, not a conclusion.
This is a proof-of-concept study of aptamer-functionalized liposomes as a targeted drug delivery platform for NSCLC. The formulation achieved expected physicochemical properties and showed preferential activity in lung cancer cells in vitro, but the work is preclinical and requires in vivo validation before clinical relevance can be assessed.
In vitro cell culture study with formulation characterization. Human lung cancer cell line A549 (NSCLC) and human normal lung fibroblast cell line MRC-5. Intervention: AT11-L2-functionalized liposomes loaded with doxorubicin or BRACO-19. Compared with: Non-functionalized liposomes or untreated control cells (not explicitly stated).
AT11-L2-functionalized liposomes had average size of approximately 110 nm with reduced surface charge after functionalization Encapsulation efficiency was approximately 90% Aptamer retained G4 folding in 100 mM KCl after liposome conjugation
No in vivo efficacy or toxicity data reported Specific cytotoxicity or IC50 values not quantified numerically
This work is not yet actionable for clinicians. It represents early-stage drug delivery research requiring in vivo efficacy, safety, and pharmacokinetic studies before consideration for clinical development.
Early-phase in vitro characterization of a novel drug delivery system in cell lines; demonstrates proof-of-concept but lacks in vivo validation, clinical endpoints, or comparison to standard therapies.
As stated by the source record.
Quoted from the source exactly as published.
This work is not yet actionable for clinicians. It represents early-stage drug delivery research requiring in vivo efficacy, safety, and pharmacokinetic studies before consideration for clinical development.
Graded across the dimensions that decide whether you should act, each from what the source actually supports. There is no single score, and where a dimension was not assessed it says so.
Aptamer-functionalized liposomes are a promising strategy to improve the selectivity of anticancer therapies. AT11-L2 is a G-quadruplex (G4)-forming aptamer with high affinity for nucleolin (NCL), which is overexpressed at the surface of non-small cell lung cancer (NSCLC) cells. Here, we developed AT11-L2-functionalized liposomes loaded with doxorubicin (DOX) or BRACO-19 for targeted delivery to NSCLC cells. The effects of both compounds on AT11-L2 stability and the ability of the aptamer to retain G4 folding after liposome conjugation were evaluated. Liposomes were characterized for size, polydispersity, surface charge, stability, encapsulation efficiency, and release profile. Biological activity was assessed in A549 and MRC-5 cells. Liposomes had an average size of approximately 110 nm, with a slight size increase and reduced surface charge after AT11-L2 functionalization. The aptamer retained G4 folding in 100 mM KCl after conjugation. Encapsulation efficiency was approximately 90%. DOX showed substantial release within 72 h, whereas BRACO-19 exhibited a more sustained profile. AT11-L2-DOX liposomes showed preferential effects in A549 cells, while BRACO-19 formulations displayed lower selectivity and cytotoxicity. Additionally, the NCL-dependent internalization of AT11-L2-functionalized liposomes was supported by a protein-blocking assay using an anti-NCL antibody. These results support AT11-L2-functionalized liposomes as a versatile NCL-targeted delivery system for NSCLC.
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