A near-infrared two-photon-sensitive peptide-mediated liposomal delivery system
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Published on: January 5, 2015
Yang Yang1, YanFang Yang1, XiangYang Xie2
1Beijing Institute of Pharmacology and Toxicology, 27 Taiping Road, Beijing 100850, China.
Abstract:
Tumour-oriented nanocarrier drug delivery approaches with photo-sensitivity have been drawing considerable attention over the years. However, due to its low penetrability and ability to induce tissue damage, the use of UV light for triggered nanocarrier release in in vivo applications has been limited. Compared with UV light, near-infrared (NIR) light deeply penetrates tissues and is less damaging to cells. Here, we report on the development of a novel method employing photo-sensitive cell-penetrating peptides (CPPs), which can be used to trigger the transport of liposomes into cells following stimulation, which was irradiation with NIR light in this case. The positive charges of the lysine residues on the CPP were temporarily caged by a NIR two-photon excitation-responsive protective group (PG), thereby forming photo-sensitive peptides (PSPs). The PSP was connected with DSPE via a polyethylene glycol (PEG) spacer to prepare the modified liposomes (PSP-L). Once illuminated by NIR light in tumour tissues, these PGs were cleaved, and the positively charged CPP regained its activity and facilitated rapid intracellular delivery of the liposomes into cancer cells. The PSP-L carrying vinorelbine bitartrate prepared in this work possessed suitable physiochemical properties. In addition, strong cellular uptake and cytotoxic activity of PSP-L in MCF-7 cells were correlated with NIR illumination. Furthermore, triggered NIR activation of PSP-L led to higher antitumour efficacy in the MCF-7 tumour model in nude mice compared with the unmodified liposomes (N-L). In conclusion, the application of PSP modifications to drug-carrying liposomes may provide an approach for the targeted delivery of antitumour agents.
Insights
Researchers developed photo-sensitive peptides that use near-infrared (NIR) light to deliver cancer drugs into cells. This novel nanocarrier system enhances drug delivery and antitumour efficacy, overcoming limitations of UV-triggered approaches.
Area of Science:
- Biomedical Engineering
- Nanotechnology
- Drug Delivery
Background:
- Photo-sensitive nanocarriers offer targeted drug delivery but UV light has limited tissue penetration and causes damage.
- Near-infrared (NIR) light offers deeper tissue penetration and reduced cellular toxicity compared to UV light.
Purpose of the Study:
- To develop a novel nanocarrier system utilizing NIR light-sensitive peptides for enhanced intracellular drug delivery.
- To improve the efficacy of antitumour agents by enabling targeted delivery to cancer cells.
Main Methods:
- Developed photo-sensitive peptides (PSPs) by protecting cell-penetrating peptide (CPP) lysine residues with a NIR two-photon excitation-responsive group.
- Conjugated PSPs to liposomes via a polyethylene glycol (PEG) spacer to create modified liposomes (PSP-L).
- Investigated the NIR-triggered intracellular delivery, cellular uptake, and cytotoxicity of PSP-L carrying vinorelbine bitartrate in MCF-7 cells and a tumour model.
Main Results:
- PSP-L demonstrated suitable physicochemical properties and NIR-triggered cellular uptake and cytotoxicity in MCF-7 cells.
- NIR activation of PSP-L resulted in enhanced antitumour efficacy in an MCF-7 tumour model compared to unmodified liposomes.
- The protective groups were successfully cleaved by NIR light, restoring CPP activity for intracellular delivery.
Conclusions:
- Photo-sensitive peptide modification of liposomes provides a promising strategy for targeted delivery of antitumour agents.
- NIR-triggered activation of nanocarriers offers an effective and less damaging alternative to UV-based systems for in vivo applications.
- This approach facilitates rapid intracellular delivery of liposomes into cancer cells, improving therapeutic outcomes.
