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Updated: Sep 9, 2025
Facile Preparation of Internally Self-assembled Lipid Particles Stabilized by Carbon Nanotubes
Published on: February 19, 2016
Phospholipid-Drug Conjugates Self-Organized into Well-Defined Supramolecular Nanotubes for Efficient Drug Delivery
Zhiguo Gao1,2, Wei He1, Ke Qin2
1State Key Laboratory of Natural Medicines, Jiangsu Key Laboratory of Drug Discovery for Metabolic Diseases and Jiangsu Key Laboratory of Drug Design and Optimization, Center of Advanced Pharmaceuticals and Biomaterials, School of Life Science and Technology, China Pharmaceutical University, Nanjing, 211198, China.
None:
Controlled self-organization of amphiphilic phospholipid camptothecin (CPT) conjugates (named PCCs) selectively forms supramolecular nanotubes with varying lengths and polydispersity. Our study elucidates the underlying mechanisms governing PCC assembly, demonstrating that π-π stacking interactions derived from the planar, conjugated structure of CPT play a pivotal role in nanotube formation. Precise modulation of the hydrophobic characteristics of PCC linkers enables fine-tuning of π-stacking strength, thereby controlling the length of the nanotubes, ranging from the nano- to micro-scale. With exceptionally high drug-loading efficiencies (43.9% to 52.3%) and stimulus-responsive release properties, the optimized PCC nanotubes exhibit tumor-selective cytotoxicity of 20- to 50-fold greater potency against tumor cells compared to normal cells. Furthermore, PCC nanotubes of intermediate length (0.3-0.5 µm) display prolonged circulation times than conventional liposomes, resulting in enhanced tumor-targeting and therapeutic efficacy.
