Related Experiment Video
Updated: May 21, 2025
Solid Lipid Nanoparticles SLNs for Intracellular Targeting Applications
Published on: November 17, 2015
Surface-modified nintedanib-loaded solid lipid nanoparticles for effective targeting of non-small cell lung cancer
Shubhangi Nalawade1, Mahavir Narwade1, Vishambhar Deshmukh1
1Department of Pharmaceutics, Poona College of Pharmacy, Bharati Vidyapeeth, Pune, Maharashtra, India.
Abstract:
Lung cancer remains a significant global health burden as the second most common and fatal malignancy, with treatment complexities heightened by limited knowledge of inhaler techniques and respiratory challenges, particularly in elderly and pediatric patients. Despite the availability of oral chemotherapeutics like Nintedanib, its clinical efficacy is undermined by suboptimal pharmacokinetics, high systemic toxicity, and low bioavailability. To overcome these limitations, we developed folic acid-conjugated Nintedanib-loaded solid lipid nanoparticles (FA-NIN-SLNPs), which offer targeted therapy with enhanced delivery and reduced adverse effects, potentially improving patient adherence. Prepared through a refined nanoprecipitation and self-assembly method, FA-NIN-SLNPs exhibited a particle size of 220.5 ± 6.08 nm, a zeta potential of 32.1 ± 3.05 mV, and an entrapment efficiency of 98.3 ± 0.80 %. In vitro release studies indicated accelerated drug release at acidic tumor pH, with FA-NIN-SLNPs showing significantly enhanced apoptosis (86.65 %) in A549 lung cancer cells versus NIN-SLNPs (67.65 %) and free drug (23.53 %). Cellular uptake assays highlighted its targeted capabilities, while histopathological and hemolysis assessments confirmed its safety profile. In vivo pharmacokinetic and biodistribution studies further demonstrated superior lung-specific accumulation, positioning this nanoformulation as a promising, safer, and more efficacious approach for targeted lung cancer therapy.
Insights
New folic acid-conjugated Nintedanib nanoparticles target lung cancer effectively. This targeted therapy enhances drug delivery, reduces toxicity, and shows improved efficacy in preclinical models for lung cancer treatment.
Area of Science:
- Nanomedicine
- Pharmacology
- Oncology
Background:
- Lung cancer is a leading cause of mortality globally, with current treatments facing challenges like poor drug delivery and systemic toxicity.
- Oral Nintedanib shows limited efficacy due to suboptimal pharmacokinetics, high toxicity, and low bioavailability.
- Targeted drug delivery systems are needed to improve lung cancer treatment outcomes.
Purpose of the Study:
- To develop and characterize folic acid-conjugated Nintedanib-loaded solid lipid nanoparticles (FA-NIN-SLNPs) for targeted lung cancer therapy.
- To evaluate the in vitro and in vivo performance of FA-NIN-SLNPs compared to free Nintedanib and non-conjugated nanoparticles.
- To assess the safety and efficacy of the novel nanoformulation for enhanced lung cancer treatment.
Main Methods:
- FA-NIN-SLNPs were prepared using nanoprecipitation and self-assembly.
- Physicochemical properties (particle size, zeta potential, entrapment efficiency) were determined.
- In vitro drug release, cellular uptake, apoptosis assays (A549 cells), histopathology, hemolysis, and in vivo pharmacokinetic/biodistribution studies were conducted.
Main Results:
- FA-NIN-SLNPs demonstrated optimal particle size, high entrapment efficiency, and stability.
- Accelerated drug release was observed at acidic tumor pH.
- FA-NIN-SLNPs significantly enhanced apoptosis in A549 cells (86.65%) compared to controls.
- Cellular uptake assays confirmed targeted delivery, and safety assessments showed a favorable profile.
- In vivo studies revealed superior lung-specific accumulation of the nanoformulation.
Conclusions:
- FA-NIN-SLNPs represent a promising nanoformulation for targeted lung cancer therapy.
- The targeted approach enhances drug delivery to the lungs, improving efficacy and reducing systemic toxicity.
- This novel nano-drug delivery system offers a safer and more effective strategy for lung cancer treatment.
