ABSTRACTDespite being a well‐known anti‐obesity chemical, piperine has only found limited therapeutic use because of its poor bioavailability at the site of action. In order to test this hypothesis, we placed piperine sodium caseinate nanoglobules (PSN) in microneedle patches (MNPs), which may enhance piperine transdermal delivery and absorption. Clove oil, sodium caseinate to make nanoglobules, and PEG 400 as a stabilizer were used in a nanoglobules process to create the PSN. The polydispersity index (0.256) and particle size (134.4 nm) of the developed PSN were both smaller, while their zeta potential (−44.4 mV) and encapsulation efficiency (90%–95%) were both greater. Compared to native piperine, the PSN increased solubility, bioaccessibility (6.5 times), and bioavailability (2.8 fold). Moreover, the PSN‐loaded MNPs were created using the micro‐molding (poly‐dimethylsiloxane (PDMS) mold) approach. In both PBS buffer and porcine skin, the PSN‐loaded MNPs were rapidly hydrolyzed, with 50% piperine release in less than 5 min. Also, the produced MNPs demonstrated improved bioavailability of piperine in the plasma (180 ng/mL) and adipose (425 ng/mL) tissue of C57BL6 mice. In conclusion, the work offered a theoretical foundation for utilizing new PSN‐loaded MNPs as a viable piperine delivery method for treating obesity.
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