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Development, optimization, and evaluation of PEGylated brucine-loaded PLGA nanoparticles
Heba S Elsewedy1,2, Bandar E Al Dhubiab2, Mahmoud A Mahdy1
1Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Zagazig University, Zagazig, Egypt.
Drug Delivery
|July 31, 2020
Summary
Polyethylene glycol (PEG)-modified poly(lactic-co-glycolic acid) (PLGA) nanoparticles effectively deliver brucine (BRU) for cancer therapy. These long-circulating nanoparticles demonstrated significant in vivo anti-tumor activity, reducing tumor growth and mortality rates.
Area of Science:
- Biomedical Engineering
- Nanotechnology
- Materials Science
Background:
- Nanotechnology offers advanced drug delivery systems for cancer therapy.
- Poly(lactic-co-glycolic acid) (PLGA) nanoparticles are widely researched for drug encapsulation.
- Surface modification with polyethylene glycol (PEG) enhances nanoparticle circulation time and passive targeting.
Purpose of the Study:
- To develop and characterize passively targeted, long-circulating PLGA nanoparticles loaded with brucine (BRU).
- To evaluate the in vitro drug release and in vivo anti-tumor efficacy of BRU-loaded nanoparticles.
Main Methods:
- PLGA nanoparticles loaded with brucine were formulated using a factorial design.
- Characterization included drug-excipient compatibility (FTIR, DSC), physicochemical properties (particle size, zeta potential, morphology, entrapment efficiency, yield), protein adsorption, and in vitro drug release.
- In vivo anti-tumor activity was assessed in tumor-bearing mice.
Main Results:
- Optimized nanoparticles exhibited smooth surfaces, particle sizes ranging from 94-253 nm, and a slightly positive zeta potential (1.09-3.71 mV).
- Brucine entrapment efficiency ranged from 37.5% to 77%, with high yield (>70.8%).
- Low protein adsorption (<25.5 µg/mg NP) and sustained in vitro release (<99.1% at 168 h) were observed.
- PEGylated PLGA nanoparticles significantly reduced tumor growth rate and mortality compared to brucine solution and non-PEGylated nanoparticles.
Conclusions:
- PEGylated PLGA nanoparticles represent a promising platform for passive targeting in cancer therapy.
- The developed nanoparticles effectively encapsulate and deliver brucine, enhancing its anti-tumor efficacy.
- This nanotechnology-based approach shows potential for improved cancer treatment outcomes.
