Related Experiment Video
Updated: Jan 9, 2026
Author Spotlight: Innovative Cancer Therapies with Iron Oxide Nanoparticles for Glioblastoma Treatment
Published on: September 27, 2024
Intranasal Delivery of Ligand-Conjugated NLCs Co-Loaded With Docetaxel and Quercetin: HPLC Method Development,
Zufika Qamar1, Saif Ahmad Khan1, Farhan Haider1
1Department of Pharmaceutics, School of Pharmaceutical Education and Research, Jamia Hamdard, New Delhi, India.
Abstract:
Glioblastoma multiforme (GB) is the most aggressive type of brain cancer, with treatment hindered by ineffective drug delivery across the blood-brain barrier and systemic side effects. Nanostructured lipid carriers (NLCs) are innovative nanocarriers that can improve drug solubility, stability, and targeted delivery to the brain. (DX-QR) NLC was developed and optimized using a modified emulsification-sonication method and a central composite rotatable design. Surface conjugation of (DX-QR) NLC with transferrin (Tf) was achieved through carbodiimide chemistry resulting in the formulation of Tf-(DX-QR) NLC. A high-performance liquid chromatography (HPLC) method was established and validated according to ICH Q2(R1) standards for simultaneous measurement of docetaxel (DX) and quercetin (QR) in plasma, brain tissue, and other organs of Wistar rats. Using a Shim-pack Solar C18 column and an acetonitrile-water (60:40) mobile phase at a 242 nm wavelength, the method demonstrated linearity (R2 > 0.9900), along with accuracy, precision, and recovery rates > 98%. The developed method was used to evaluate the pharmacokinetics and biodistribution of DX and QR, indicating that intranasal (IN) administration of Tf-(DX-QR) NLC resulted in brain concentrations of DX (4.6-fold) and QR (8.8-fold) higher than those achieved through (DX-QR) suspension delivered via intravenous (IV) and IN, highlighting their potential as noninvasive, effective, and targeted treatments for GB.
Insights
Targeted nanocarriers improve brain cancer treatment. Transferrin-conjugated nanostructured lipid carriers (Tf-NLCs) enhanced docetaxel and quercetin delivery to the brain via intranasal administration, showing potential for glioblastoma therapy.
Area of Science:
- Nanomedicine
- Pharmacology
- Biotechnology
Background:
- Glioblastoma multiforme (GBM) is an aggressive brain cancer with poor treatment outcomes due to drug delivery challenges across the blood-brain barrier.
- Nanostructured lipid carriers (NLCs) offer potential for improved drug solubility, stability, and targeted delivery.
- Transferrin (Tf) conjugation can enhance brain-specific targeting of nanocarriers.
Purpose of the Study:
- To develop and characterize transferrin-conjugated nanostructured lipid carriers (Tf-NLCs) for enhanced brain delivery of docetaxel (DX) and quercetin (QR).
- To establish and validate a bioanalytical method for quantifying DX and QR in biological matrices.
- To evaluate the pharmacokinetic and biodistribution profile of Tf-NLCs following intranasal administration.
Main Methods:
- NLCs loaded with docetaxel and quercetin (DX-QR) were formulated using emulsification-sonication and optimized via a central composite design.
- Surface functionalization of (DX-QR) NLC with transferrin (Tf) was achieved using carbodiimide chemistry.
- A validated High-Performance Liquid Chromatography (HPLC) method was employed for simultaneous quantification of DX and QR in plasma and tissues.
Main Results:
- The validated HPLC method demonstrated high linearity (R² > 0.9900), accuracy, precision, and recovery (>98%).
- Intranasal administration of Tf-(DX-QR) NLC resulted in significantly higher brain concentrations of DX (4.6-fold) and QR (8.8-fold) compared to non-conjugated suspension.
- Biodistribution studies confirmed enhanced brain accumulation of drugs delivered via Tf-NLCs.
Conclusions:
- Tf-conjugated NLCs represent a promising nanocarrier system for improving brain drug delivery for glioblastoma treatment.
- Intranasal administration of Tf-(DX-QR) NLC offers a noninvasive and effective strategy to enhance drug exposure in the brain.
- This approach holds potential for overcoming the blood-brain barrier limitations in treating aggressive brain cancers like glioblastoma.
