Drug development and industrial pharmacy · 2025
Targeted antibacterial and anticancer therapeutics: PEGylated liposomal delivery of turmeric and cinnamon extracts-in vitro and in vivo efficacy.
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Alharthi Sitah, Alrashidi Amal Abdullah, Almawash Saud, Ebrahimi Shahmabadi Hasan, Alavi Seyed Ebrahim
Аннотация
OBJECTIVE: This study presents the characterization and evaluation of polyethylene glycol (PEG)-coated liposomal formulations loaded with turmeric (TUR) and cinnamon (CINN) extracts for the treatment of bacterial infections.
SIGNIFICANCE: TUR/CINN-loaded PEGylated liposomes enhance the antibacterial effects of TUR and CINN both in vitro and in vivo.
METHODS: PEGylated liposomes loaded with TUR and CINN were synthesized using the reverse-phase evaporation method and characterized by dynamic light scattering and spectrophotometry. The formulations were also evaluated for biocompatibility, permeability, and antibacterial efficacy in both in vitro and in vivo environments.
RESULTS: The nanoparticles, with dimensions ranging from 155 to 164 nm, exhibited consistent size distribution (polydispersity index (PDI) of 0.219 to 0.23), stable zeta potentials (-20 to -13 mV), and effective drug encapsulation rates (86.8% to 93.6%), suggesting their potential for targeted drug delivery. In vitro experiments demonstrated their biocompatibility (cell viability exceeding 75% at 40 µg/mL), permeability (transfer rates of 20.2% to 21.5%), antibacterial activity (minimum inhibitory concentrations of 8 to 64 µg/mL), and their ability to generate reactive oxygen species (1.2- to 2-fold increase compared to the control). In an in vivo murine model of Pseudomonas aeruginosa skin infections, significant reductions in viable bacterial counts were observed, with PEG-Lip-TUR/CINN leaving only 102 colony-forming units/mL. Additionally, this formulation displayed anti-metastatic properties, inhibiting cancer cell migration by 99%.
CONCLUSIONS: This study highlights the potential of PEGylated liposomal formulations loaded with TUR and CINN as versatile therapeutic platforms for the treatment of antibiotic-resistant infections and cancer metastasis.
SIGNIFICANCE: TUR/CINN-loaded PEGylated liposomes enhance the antibacterial effects of TUR and CINN both in vitro and in vivo.
METHODS: PEGylated liposomes loaded with TUR and CINN were synthesized using the reverse-phase evaporation method and characterized by dynamic light scattering and spectrophotometry. The formulations were also evaluated for biocompatibility, permeability, and antibacterial efficacy in both in vitro and in vivo environments.
RESULTS: The nanoparticles, with dimensions ranging from 155 to 164 nm, exhibited consistent size distribution (polydispersity index (PDI) of 0.219 to 0.23), stable zeta potentials (-20 to -13 mV), and effective drug encapsulation rates (86.8% to 93.6%), suggesting their potential for targeted drug delivery. In vitro experiments demonstrated their biocompatibility (cell viability exceeding 75% at 40 µg/mL), permeability (transfer rates of 20.2% to 21.5%), antibacterial activity (minimum inhibitory concentrations of 8 to 64 µg/mL), and their ability to generate reactive oxygen species (1.2- to 2-fold increase compared to the control). In an in vivo murine model of Pseudomonas aeruginosa skin infections, significant reductions in viable bacterial counts were observed, with PEG-Lip-TUR/CINN leaving only 102 colony-forming units/mL. Additionally, this formulation displayed anti-metastatic properties, inhibiting cancer cell migration by 99%.
CONCLUSIONS: This study highlights the potential of PEGylated liposomal formulations loaded with TUR and CINN as versatile therapeutic platforms for the treatment of antibiotic-resistant infections and cancer metastasis.