Related Experiment Video
Updated: Jul 20, 2025
Encapsulation of Cancer Therapeutic Agent Dacarbazine Using Nanostructured Lipid Carrier
Published on: April 26, 2016
Sorafenib-Loaded PLGA Carriers for Enhanced Drug Delivery and Cellular Uptake in Liver Cancer Cells
Tania Mariastella Caputo1, Angela Maria Cusano2, Sofia Principe1
1Optoelectronics Group, Department of Engineering, University of Sannio, Palazzo Dell' Aquila Bosco Lucarelli, Benevento, Italy.
Introduction:
Currently, conventional treatments of hepatocellular carcinoma (HCC) are not selective enough for tumor tissue and lead to multidrug resistance and drug toxicity. Although sorafenib (SOR) is the standard first-line systemic therapy approved for the clinical treatment of HCC, its poor aqueous solubility and rapid clearance result in low absorption efficiency and severely limit its use for local treatment.
Methods:
Herein, we present the synthesis of biodegradable polymeric Poly (D, L-Lactide-co-glycolide) (PLGA) particles loaded with SOR (PS) by emulsion-solvent evaporation process. The particles are carefully characterized focusing on particle size, surface charge, morphology, drug loading content, encapsulation efficiency, in vitro stability, drug release behaviour and tested on HepG2 cells. Additionally, PLGA particles have been coupled on side emitting optical fibers (seOF) integrated in a microfluidic device for light-triggered local release.
Results:
PS have a size of 248 nm, tunable surface charge and a uniform and spherical shape without aggregation. PS shows encapsulation efficiency of 89.7% and the highest drug loading (8.9%) between the SOR-loaded PLGA formulations. Treating HepG2 cells with PS containing SOR at 7.5 µM their viability is dampened to 40%, 30% and 17% after 48, 129 and 168 hours of incubation, respectively.
Conclusion:
The high PS stability, their sustained release profile and the rapid cellular uptake corroborate the enhanced cytotoxicity effect on HepG2. With the prospect of developing biomedical tools to control the spatial and temporal release of drugs, we successfully demonstrated the potentiality of seOF for light-triggered local release of the carriers. Our prototypical system paves the way to new devices integrating microfluidics, optical fibers, and advanced carriers capable to deliver minimally invasive locoregional cancer treatments.
Insights
Biodegradable polymeric particles loaded with sorafenib (SOR) offer improved hepatocellular carcinoma (HCC) treatment. This system enables light-triggered local drug release, enhancing efficacy and minimizing toxicity for minimally invasive cancer therapy.
Area of Science:
- Biomaterials Engineering
- Nanotechnology
- Cancer Therapeutics
Background:
- Conventional hepatocellular carcinoma (HCC) treatments lack tumor selectivity, leading to multidrug resistance and toxicity.
- Sorafenib (SOR), a standard HCC therapy, exhibits poor aqueous solubility and rapid clearance, limiting its local treatment efficacy.
Purpose of the Study:
- To synthesize biodegradable Poly (D, L-Lactide-co-glycolide) (PLGA) particles loaded with SOR (PS).
- To characterize PS for particle size, surface charge, morphology, drug loading, encapsulation efficiency, stability, and release kinetics.
- To evaluate the potential of integrating PS with side-emitting optical fibers (seOF) in a microfluidic device for light-triggered local drug release.
Main Methods:
- Emulsion-solvent evaporation process for synthesizing SOR-loaded PLGA particles (PS).
- Comprehensive characterization of PS including size (248 nm), surface charge, morphology, drug loading (8.9%), encapsulation efficiency (89.7%), in vitro stability, and drug release.
- Integration of PS-loaded seOF within a microfluidic device for controlled, light-triggered drug delivery.
Main Results:
- Synthesized PS exhibited uniform spherical morphology, tunable surface charge, and high drug loading and encapsulation efficiency.
- PS demonstrated sustained drug release and enhanced cytotoxicity against HepG2 cells, reducing viability to 17% after 168 hours at 7.5 µM SOR.
- The seOF-integrated microfluidic system successfully demonstrated light-triggered local release of PS.
Conclusions:
- Biodegradable PLGA particles offer a promising carrier for SOR, enhancing its anti-cancer activity and stability.
- The developed system integrating microfluidics and optical fibers enables controlled, light-triggered local drug delivery for HCC.
- This prototypical system paves the way for advanced, minimally invasive locoregional cancer treatment strategies.
