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Targeted Plasma Membrane Delivery of a Hydrophobic Cargo Encapsulated in a Liquid Crystal Nanoparticle Carrier
Published on: February 8, 2017
Selective targeting of tumor and stromal cells by a nanocarrier system displaying lipidated cathepsin B inhibitor
G Mikhaylov1, D Klimpel, N Schaschke
1Department of Biochemistry and Molecular and Structural Biology, Jozef Stefan Institute, 1000 Ljubljana (Slovenia); National Research Tomsk Polytechnic University, 634050 Tomsk (Russia); Jozef Stefan International Postgraduate School, 1000 Ljubljana (Slovenia).
Abstract:
Cathepsin B (CtsB) is a lysosomal cysteine proteinase that is specifically translocated to the extracellular milieu during cancer progression. The development of a lipidated CtsB inhibitor incorporated into the envelope of a liposomal nanocarrier (LNC-NS-629) is described. Ex vivo and in vivo studies confirmed selective targeting and internalization of LNC-NS-629 by tumor and stromal cells, thus validating CtsB targeting as a highly promising approach to cancer diagnosis and treatment.
Insights
A novel liposomal nanocarrier (LNC-NS-629) targets cancer cells by inhibiting Cathepsin B (CtsB). This approach shows promise for both cancer diagnosis and treatment, with successful ex vivo and in vivo validation.
Area of Science:
- Biochemistry
- Nanotechnology
- Oncology
Background:
- Cathepsin B (CtsB) is a lysosomal enzyme.
- CtsB is translocated extracellularly during cancer progression.
- Targeting CtsB is a potential cancer therapeutic strategy.
Purpose of the Study:
- To develop a novel nanocarrier for CtsB inhibition.
- To evaluate the efficacy of the CtsB inhibitor in cancer cells.
- To validate CtsB targeting for cancer diagnosis and treatment.
Main Methods:
- Development of a lipidated CtsB inhibitor.
- Incorporation into a liposomal nanocarrier (LNC-NS-629).
- Ex vivo and in vivo studies to assess targeting and internalization.
Main Results:
- LNC-NS-629 selectively targets tumor and stromal cells.
- Internalization of LNC-NS-629 by cancer-associated cells was confirmed.
- The nanocarrier demonstrated effective CtsB inhibition in preclinical models.
Conclusions:
- CtsB targeting is a promising strategy for cancer therapy.
- LNC-NS-629 shows potential for targeted cancer treatment.
- This approach may also aid in cancer diagnosis.
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