Morellic acid (MA), a typical compound found in Garcinia plants, is known for its anticancer properties. In present study, we isolated MA from resin of using preparative chromatography. We have successfully prepared MA-loaded nanostructured lipid carriers (MA-NLCs) and refined the production process via orthogonal testing. Optimization of the preparation process resulted in an average particle size of 165.50±1.70 nm with a PDI of 0.19±0.01. The EE% and DL% of MA-NLCs were 78.17±0.34% and 7.25±0.38%, respectively. The zeta potential of MA-NLCs was -21.85±0.67 mV. Comparatively, MA-NLCs showed a greater area under the curve (AUC) and an extended half-life (t1/2) than free MA. Pharmacokinetics analysis revealed that the AUC increased from 4.91±0.65 μg/mL∙min (free MA) to 18.91±3.40 μg/mL∙min (MA-NLCs) and the t value for MA-NLCs was 7.93-fold longer than that of free MA. cytotoxic assessments indicated that MA formulations curtailed the proliferation of cancer cells. , MA-NLCs significantly inhibited the tumor growth in tumor-bearing mouse model. Molecular mechanism studies revealed that up-regulation of apaf-1 and activation of caspase-3, caspase-9 and GSDME by MA-NLCs may trigger to apoptosis and pyroptosis in cancer cells. Consequently, our findings support the potential of NLCs as an effective MA delivery system for the clinical management of cancer.

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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC10998744PMC
http://dx.doi.org/10.62347/VBOX7111DOI Listing

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