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Biotinylated HPMA centered polymeric nanoparticles for Bortezomib delivery
Sarita Rani1, Rakesh K Sahoo1, Kartik T Nakhate2
1Department of Pharmacy, School of Chemical Sciences and Pharmacy, Central University of Rajasthan, Bandarsindri, Ajmer, Rajasthan 305817, India.
International Journal of Pharmaceutics
|February 26, 2020
Summary
This study developed novel polymeric nanoparticles (PNPs) for Bortezomib (BTZ) delivery, improving its anti-cancer efficacy and bioavailability. The biotinylated PNPs demonstrated enhanced targeting and reduced toxicity, offering a promising formulation for cancer therapy.
Area of Science:
- Biomaterials Science
- Nanotechnology
- Pharmaceutical Sciences
Background:
- Bortezomib (BTZ), a proteasome inhibitor for multiple myeloma, faces formulation challenges due to poor aqueous solubility and stability.
- Developing effective drug delivery systems is crucial to enhance BTZ's anti-cancer properties against solid tumors.
Purpose of the Study:
- To synthesize and characterize N-(2-hydroxypropyl) methacrylamide (HPMA)-based copolymeric conjugates and biotinylated polymeric nanoparticles (PNPs) for improved Bortezomib (BTZ) delivery.
- To evaluate the anti-cancer activity, hemocompatibility, cellular uptake, and in vivo pharmacokinetics of the developed BTZ-loaded PNPs.
Main Methods:
- Synthesis of functional polymeric conjugates: HPMA-Biotin (HP-BT), HPMA-Polylactic acid (HPLA), and HPMA-PLA-Biotin (HPLA-BT).
- Characterization of nanoparticles using spectroscopic and microscopic techniques; assessment of drug release kinetics at different pH values.
- Evaluation of hemocompatibility (hemolysis assay), in vitro anti-cancer activity (IC50 determination against MCF-7 cells), cellular uptake, and in vivo pharmacokinetics.
Main Results:
- Successfully synthesized and characterized BTZ-loaded HPMA-based PNPs with a narrow size distribution (199.7 ± 1.32 nm).
- PNPs exhibited significantly reduced hemolytic activity compared to free BTZ (p < 0.0001).
- BTZ-loaded HPLA-BT PNPs showed enhanced anti-cancer efficacy (IC50: 56.06 ± 0.12 nM) and increased cellular uptake, attributed to biotin targeting.
- In vivo studies demonstrated improved bioavailability and half-life for the developed PNPs compared to free BTZ.
Conclusions:
- HPMA-based biotinylated PNPs represent an effective strategy for delivering Bortezomib (BTZ), overcoming its solubility and stability limitations.
- The developed nanocarrier system enhances BTZ's anti-cancer activity, selectivity, and pharmacokinetic profile, offering a promising platform for cancer therapy.
