Related Experiment Video
Updated: Oct 11, 2025
Synthesis and Characterization of Placental Chondroitin Sulfate A plCSA-Targeting Lipid-Polymer Nanoparticles
Published on: September 18, 2018
Sialic Acid Conjugated Chitosan Nanoparticles: Modulation to Target Tumour Cells and Therapeutic Opportunities
Rafquat Rana1, Sarita Rani1, Vipin Kumar1
1Department of Pharmacy, School of Chemical Sciences and Pharmacy, Central University of Rajasthan, Bandarsindri, Ajmer, Rajasthan, 305817, India.
Abstract:
Targeted delivery of therapeutics forestalls the dreadful delocalized effects, drug toxicities and needless immunosuppression. Cancer cells are bounteous with sialic acid and the differential expression of glycosyl transferase, glycosidase and monosaccharide transporter compared to healthy tissues. The current study entails the development and characterisation of sialic acid (SA)-labelled chitosan nanoparticles encapsulating gemcitabine (GEM). Chitosan (CS) was conjugated with SA using coupling reaction and characterised spectroscopically. Furthermore, different concentrations of chitosan and tripolyphosphate (TPP) were optimised to fabricate surface modified chitosan nanoparticles. SA conjugated chitosan nanoparticles encapsulating GEM (SA-CS_GEM NPs) of 232 ± 9.69 nm with narrow distribution (PDI < 0.5) and zeta potential of - 19 ± 0.97 mV was fabricated. GEM was successfully loaded in the SA-CS NPs, depicting prolonged and biphasic drug release pattern more elated at low pH. Pronounced cellular uptake (FITC tagged) and cytotoxicity (IC50 487.4 nM) was observed in SA-CS_GEM NPs against A549 cells. IC50 for SA-CS_GEM NPs plunged with an increase in the time points from 24 to 72 h. Concentration-dependent haemolytic study confirmed significant haemocompatibility of SA-CS_GEM NPs. Pharmacokinetic study was performed on Sprague-Dawley rats and the kinetic parameters were calculated using PKSolver 2.0. Results demonstrated a consequential refinement of 2.98 times in modified SA-CS_GEM NPs with a significant increase in retention time, bioavailability and elimination half-life, and decrease in elimination rate constant and volume of distribution in comparison to CS_GEM NPs. Therefore, SA-CS shell core nanoparticles could be a beneficial approach to target and treat NSCLC (non-small cell lung cancer) and direct for research possibilities to target the other tumour cells.
Insights
Sialic acid-labelled chitosan nanoparticles effectively deliver gemcitabine, enhancing cancer treatment. These nanoparticles show improved drug retention, bioavailability, and reduced toxicity for non-small cell lung cancer therapy.
Area of Science:
- Nanotechnology
- Materials Science
- Biomedical Engineering
Background:
- Cancer cells exhibit higher sialic acid expression than healthy tissues.
- Targeted drug delivery minimizes side effects and improves therapeutic efficacy.
- Gemcitabine (GEM) is a chemotherapy drug often used for non-small cell lung cancer (NSCLC).
Purpose of the Study:
- To develop and characterize sialic acid (SA)-labelled chitosan nanoparticles (NPs) encapsulating gemcitabine (GEM).
- To evaluate the targeted delivery, cellular uptake, cytotoxicity, and pharmacokinetic profile of SA-GEM NPs.
- To assess the potential of SA-CS NPs for non-small cell lung cancer (NSCLC) treatment.
Main Methods:
- Chitosan (CS) was conjugated with sialic acid (SA) and characterized.
- SA-conjugated chitosan nanoparticles encapsulating GEM (SA-CS_GEM NPs) were fabricated and optimized.
- Drug loading, release kinetics (especially at low pH), cellular uptake (using FITC tagging), cytotoxicity (IC50 determination), haemocompatibility, and pharmacokinetic studies in rats were performed.
Main Results:
- SA-CS_GEM NPs were successfully fabricated with a size of 232 nm and narrow PDI (<0.5).
- Enhanced gemcitabine loading and a prolonged, biphasic drug release pattern were observed, particularly at low pH.
- Significantly increased cellular uptake and cytotoxicity against A549 cells were noted for SA-CS_GEM NPs compared to controls.
- Pharmacokinetic studies revealed a 2.98-fold improvement in SA-CS_GEM NPs, with increased retention time, bioavailability, and half-life, alongside decreased elimination rate and distribution volume.
Conclusions:
- Sialic acid-labelled chitosan nanoparticles demonstrate enhanced drug delivery and therapeutic potential for NSCLC.
- The SA-CS shell-core nanoparticle system offers a promising approach for targeted cancer therapy.
- Further research into targeting other tumor cells using this nanoparticle system is warranted.
