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<p>To overcome the limitations of poor BBB permeability and short half-life associated with zidovudine (AZT), mesoporous silica nanoparticles (MSNPs) were developed and evaluated for enhanced bioavailability and brain targeting. MSNPs and non-porous silica nanoparticles (NSNPs) were synthesized via modified Stöber and sol-gel methods, respectively, and coated with human serum albumin (HSA). NSNPs residing in the range of 30-50&#xa0;nm showed lower surface area (~ 13.11 m<sup>2</sup>/g), while MSNPs in the range of 90-110&#xa0;nm exhibited a significantly higher surface area (&gt; 750.21 m<sup>2</sup>/g) and a pore radius of ~ 10&#xa0;nm. Higher zeta potential of MSNPs indicated greater stability, and superior drug loading as an outcome of its porous architecture. This HSA corona served a dual function as a capping agent and a biocompatibility enhancer, achieving a superior drug loading efficiency of 98.7% and facilitating a controlled, sustained release profile (23.44% over 8&#xa0;h) governed by a non-Fickian diffusion mechanism. Biocompatibility studies revealed LC₅₀ value of 500&#xa0;µg/ml in brine shrimp, and zebrafish embryos could tolerate MSNP concentrations up to 250&#xa0;µg/ml without substantial developmental toxicity. The biodistribution studies in mice revealed a substantial increase in AZT accumulation within the brain (peaking at 23.22&#xa0;µg/g at 48&#xa0;h) for HSA-coated MSNPs, while concurrently reducing off-target deposition in the liver and spleen. The key findings revealed that HSA-coated MSNPs significantly improved drug loading efficiency, sustained release, reduced toxicity, and enhanced brain uptake, demonstrating their potential as an effective nanocarrier for brain-targeted drug delivery.</p>

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Targeted brain delivery of zidovudine via protein-modified mesoporous silica nanoparticles: design and evaluation

  • 期刊论文

  • 发表日期：

    2026年3月12日

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  • Aparna Datta,
  • Leena Kumari,
  • Sourya Ghosh,
  • Srijan Bhattacharya

摘要

To overcome the limitations of poor BBB permeability and short half-life associated with zidovudine (AZT), mesoporous silica nanoparticles (MSNPs) were developed and evaluated for enhanced bioavailability and brain targeting. MSNPs and non-porous silica nanoparticles (NSNPs) were synthesized via modified Stöber and sol-gel methods, respectively, and coated with human serum albumin (HSA). NSNPs residing in the range of 30-50 nm showed lower surface area (~ 13.11 m2/g), while MSNPs in the range of 90-110 nm exhibited a significantly higher surface area (> 750.21 m2/g) and a pore radius of ~ 10 nm. Higher zeta potential of MSNPs indicated greater stability, and superior drug loading as an outcome of its porous architecture. This HSA corona served a dual function as a capping agent and a biocompatibility enhancer, achieving a superior drug loading efficiency of 98.7% and facilitating a controlled, sustained release profile (23.44% over 8 h) governed by a non-Fickian diffusion mechanism. Biocompatibility studies revealed LC₅₀ value of 500 µg/ml in brine shrimp, and zebrafish embryos could tolerate MSNP concentrations up to 250 µg/ml without substantial developmental toxicity. The biodistribution studies in mice revealed a substantial increase in AZT accumulation within the brain (peaking at 23.22 µg/g at 48 h) for HSA-coated MSNPs, while concurrently reducing off-target deposition in the liver and spleen. The key findings revealed that HSA-coated MSNPs significantly improved drug loading efficiency, sustained release, reduced toxicity, and enhanced brain uptake, demonstrating their potential as an effective nanocarrier for brain-targeted drug delivery.