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Updated: Jul 17, 2025
Solid Lipid Nanoparticles SLNs for Intracellular Targeting Applications
Published on: November 17, 2015
Surface-decorated nanoliposomal leonurine targets activated fibroblast-like synoviocytes for efficient rheumatoid
Shiyu Meng1, Zhiling Song1, Zhuang Tang1
1School of Pharmacy and State Key Laboratory of Quality Research in Chinese Medicine, Macau University of Science and Technology, Macao 999078, China. yzzhu@must.edu.mo.
Abstract:
Rheumatoid arthritis (RA) is a chronic autoimmune disease that causes progressive joint destruction, leading to impaired life quality, disability, and even premature mortality. However, current medications suffer from limited clinical outcomes and severe side effects due to low bioavailability and non-specific distribution after administration. Herein, a targeting nanosystem (HAP-Lipo@Leo) was constructed for efficient RA treatment, which can precisely deliver a natural anti-arthritic drug leonurine (Leo) to the inflamed joint by HAP-1 peptide-mediated recognition of activated fibroblast-like synoviocytes (FLS). More specifically, HAP-Lipo@Leo was prepared by a combination of thin film hydration and high-pressure microfluidization and surface-decorated with HAP-1 peptide and PEG before encapsulating Leo by the ammonium sulfate gradient method. The as-obtained HAP-Lipo@Leo can be selectively internalized by activated FLS and impairs the lamellipodia formation and overexpression of inflammatory cytokines, both of which play detrimental roles in joint damage. Furthermore, HAP-Lipo@Leo demonstrated arthritic joint-specific distribution, significant inhibition of synovial inflammation, and reversal of cartilage and bone destruction in adjuvant-induced arthritis rats as evidenced by comprehensive investigations including ELISA tests, histopathology examinations, and micro-CT analysis. In addition, HAP-Lipo@Leo exhibited good biocompatibility and safety both in vitro and in vivo. Taken together, HAP-Lipo@Leo holds great potential for clinical RA management by integrating activated FLS targeting, long circulation, multifaceted therapeutic effects, and excellent biocompatibility.
Insights
A novel targeted nanosystem, HAP-Lipo@Leo, effectively delivers the drug leonurine to inflamed joints for rheumatoid arthritis (RA) treatment. This approach improves drug delivery and reduces joint damage with good safety.
Area of Science:
- Biomedical Engineering
- Nanotechnology
- Rheumatology
Background:
- Rheumatoid arthritis (RA) is a chronic autoimmune disease causing joint destruction and reduced quality of life.
- Current RA treatments have limited efficacy and significant side effects due to poor drug bioavailability and distribution.
- Targeted drug delivery systems are needed to improve RA treatment outcomes.
Purpose of the Study:
- To construct a targeted nanosystem (HAP-Lipo@Leo) for efficient rheumatoid arthritis treatment.
- To achieve precise delivery of leonurine (Leo) to inflamed joints via HAP-1 peptide targeting of activated fibroblast-like synoviocytes (FLS).
- To evaluate the therapeutic efficacy and safety of HAP-Lipo@Leo in an animal model of RA.
Main Methods:
- HAP-Lipo@Leo was prepared using thin film hydration, high-pressure microfluidization, and surface modification with HAP-1 peptide and PEG.
- Leonurine (Leo) was encapsulated using the ammonium sulfate gradient method.
- In vitro and in vivo studies were conducted, including FLS internalization assays, assessment of inflammatory markers, and evaluation in adjuvant-induced arthritis rats using ELISA, histopathology, and micro-CT.
Main Results:
- HAP-Lipo@Leo was selectively internalized by activated FLS, inhibiting lamellipodia formation and inflammatory cytokine overexpression.
- The nanosystem demonstrated specific distribution to arthritic joints, significantly inhibiting synovial inflammation.
- HAP-Lipo@Leo effectively reversed cartilage and bone destruction in arthritis rats and showed good biocompatibility and safety.
Conclusions:
- The HAP-Lipo@Leo nanosystem enables targeted delivery of leonurine to activated FLS in rheumatoid arthritis.
- This targeted approach offers multifaceted therapeutic effects, including reduced inflammation and protection against joint destruction.
- HAP-Lipo@Leo demonstrates significant potential for clinical application in rheumatoid arthritis management due to its efficacy, targeting ability, and safety profile.
