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Updated: Dec 11, 2025
Solid Lipid Nanoparticles SLNs for Intracellular Targeting Applications
Published on: November 17, 2015
Properties of rapamycin solid lipid nanoparticles for lymphatic access through the lungs & part II: the effect of
Emelie Landh1,2, Lyn M Moir1,2, Daniela Traini1,2
1Respiratory Technology, Woolcock Institute of Medical Research, Glebe, NSW, 2037, Australia.
Abstract:
Aim: Lymphangioleiomyomatosis is characterized by smooth muscle-like cells in the lungs that spread to other organs via lymphatic vessels. Oral rapamycin is restricted by low bioavailability approximately 15%. The aim of the present study is to systematically investigate the effect of inhaled rapamycin solid lipid nanoparticles (Rapa-SLN) surface charge on efficacy and penetration into the lymphatics. Materials & methods: Rapa-SLN formulations with different charge: neutral, positive and negative, were produced and assessed for their physicochemical particle characteristics and efficacy in vitro. Results: Negative Rapa-SLNs were significantly faster at entering the lymphatic endothelium and more potent at inhibiting lymphanigiogenesis compared with neutral and positive Rapa-SLNs. Conclusion: Negative Rapa-SLNs showed efficient lymphatic access and should therefore be investigated further as a treatment for targeting extrapulmonary lymphangioleiomyomatosis.
Insights
Negative surface charge on inhaled rapamycin solid lipid nanoparticles (Rapa-SLN) enhances lymphatic penetration and anti-angiogenesis efficacy for treating lymphangioleiomyomatosis.
Area of Science:
- Nanomedicine
- Pulmonary Medicine
- Pharmacology
Background:
- Lymphangioleiomyomatosis (LAM) involves lung smooth muscle cell proliferation and metastasis via lymphatics.
- Oral rapamycin for LAM has low bioavailability (~15%), limiting therapeutic effectiveness.
- Targeting lymphatic spread requires effective drug delivery to lymphatic vessels.
Purpose of the Study:
- To investigate the impact of surface charge on inhaled rapamycin solid lipid nanoparticles (Rapa-SLN) for LAM treatment.
- To evaluate Rapa-SLN efficacy and lymphatic penetration based on nanoparticle charge (neutral, positive, negative).
Main Methods:
- Synthesis and characterization of Rapa-SLN with varying surface charges (neutral, positive, negative).
- In vitro assessment of physicochemical properties and biological efficacy.
- Evaluation of lymphatic endothelial cell entry and anti-angiogenesis activity.
Main Results:
- Negative Rapa-SLNs demonstrated significantly enhanced entry into lymphatic endothelium compared to neutral and positive formulations.
- Negative Rapa-SLNs exhibited superior inhibition of lymphangiogenesis in vitro.
- Surface charge critically influences Rapa-SLN lymphatic targeting and therapeutic potency.
Conclusions:
- Negatively charged Rapa-SLNs offer efficient access to lymphatic vessels, suggesting improved therapeutic potential.
- Inhaled negative Rapa-SLNs represent a promising strategy for targeting extrapulmonary lymphangioleiomyomatosis.
- Further investigation of negative Rapa-SLNs is warranted for LAM treatment optimization.
