Nano-Encapsulation of Herbal Alkaloids for Targeted Anti-Cancer Delivery
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Abstract
Background: Herbal alkaloids have potential cytotoxic activity but may be limited by poor solubility, restricted bioavailability, and rapid release. Objective: To prepare and characterize PLGA–chitosan nanoparticles containing berberine and piperine and compare the release and MCF-7 cytotoxicity of free and nanoencapsulated berberine. Methods: In this in vitro experimental study, blank, berberine-loaded, piperine-loaded, and combined berberine–piperine nanoparticles were prepared by modified solvent evaporation. Particle size, polydispersity index, zeta potential, encapsulation efficiency, and drug loading were evaluated. Berberine release was assessed for up to 48 hours, and MCF-7 metabolic viability was measured by MTT assay after 48-hour exposure. Results: Berberine-loaded nanoparticles had a particle size of 156.8 ± 5.6 nm, zeta potential of +24.7 ± 2.1 mV, encapsulation efficiency of 82.6 ± 3.4%, and drug loading of 14.8 ± 1.2%. At 4 and 24 hours, cumulative release was 34.5% and 76.4% from nanoparticles compared with 66.8% and >94% from free berberine. At 100 µg/mL, MCF-7 viability was 21.5 ± 2.8% with nanoencapsulated berberine and 39.7 ± 3.6% with free berberine. The reported IC₅₀ values were 38.7 and 56.4 µg/mL, respectively. Conclusion: Nanoencapsulation modified berberine release and was associated with lower MCF-7 metabolic viability under the tested in vitro conditions. Verification of the source data and further selectivity, mechanistic, and preclinical studies are required
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