Drug development and industrial pharmacy · 2025
Delivery of GRg3 via alginate/PLGA nanoparticles: physicochemical, cellular, and in vivo biocompatibility assessments.
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Sargazi Saman, Mirinejad Shekoufeh, Hajinezhad Mohammad Reza, Madani Fatemeh, Majidpour Mahdi, Barani Mahmood
Аннотация
OBJECTIVE: This study aimed to develop and evaluate ginsenoside Rg3 (GRg3)-loaded alginate/poly(lactic-co-glycolic acid) (PLGA) nanoparticles (NPs) as an oral drug delivery system with improved anticancer and antioxidant potential.
SIGNIFICANCE: Despite its pharmacological promise, GRg3 suffers from poor solubility, instability, and low oral bioavailability. Encapsulation in biopolymeric NPs may overcome these barriers by enhancing stability and providing controlled release.
METHODS: GRg3-loaded alginate/PLGA NPs were synthesized and characterized for size, stability, rheology, and release kinetics. Antiproliferative activity, cell cycle effects, and apoptosis markers were assessed in PC-3 prostate cancer cells. In vivo safety and antioxidant effects were evaluated in healthy rats using biochemical assays and histopathological analysis of liver and kidney tissues.
RESULTS: The NPs had a mean diameter of ∼200 nm with shear-thinning behavior. GRg3 release followed a sustained pattern, best fitting the Korsmeyer-Peppas model with anomalous transport. In vitro, the formulation inhibited PC-3 cell proliferation in a concentration- and time-dependent manner, induced G0-G1 arrest, and elevated caspase-3 activity within 6 h. In vivo, oral administration caused no significant hepatic or renal alterations, and histopathology showed no inflammation or necrosis. GRg3 also reduced malondialdehyde levels, confirming antioxidant activity.
CONCLUSIONS: Encapsulation of GRg3 in alginate/PLGA NPs enhanced its stability, anticancer activity, and antioxidant potential without systemic toxicity. These findings highlight the promise of GRg3-loaded nanocarriers for cancer therapy, warranting further evaluation in disease-specific models.
SIGNIFICANCE: Despite its pharmacological promise, GRg3 suffers from poor solubility, instability, and low oral bioavailability. Encapsulation in biopolymeric NPs may overcome these barriers by enhancing stability and providing controlled release.
METHODS: GRg3-loaded alginate/PLGA NPs were synthesized and characterized for size, stability, rheology, and release kinetics. Antiproliferative activity, cell cycle effects, and apoptosis markers were assessed in PC-3 prostate cancer cells. In vivo safety and antioxidant effects were evaluated in healthy rats using biochemical assays and histopathological analysis of liver and kidney tissues.
RESULTS: The NPs had a mean diameter of ∼200 nm with shear-thinning behavior. GRg3 release followed a sustained pattern, best fitting the Korsmeyer-Peppas model with anomalous transport. In vitro, the formulation inhibited PC-3 cell proliferation in a concentration- and time-dependent manner, induced G0-G1 arrest, and elevated caspase-3 activity within 6 h. In vivo, oral administration caused no significant hepatic or renal alterations, and histopathology showed no inflammation or necrosis. GRg3 also reduced malondialdehyde levels, confirming antioxidant activity.
CONCLUSIONS: Encapsulation of GRg3 in alginate/PLGA NPs enhanced its stability, anticancer activity, and antioxidant potential without systemic toxicity. These findings highlight the promise of GRg3-loaded nanocarriers for cancer therapy, warranting further evaluation in disease-specific models.