article · Drug Delivery
Curcumin possesses anticancer, anti-inflammatory, and antioxidant properties, but its clinical utility is restricted by poor solubility, stability, and bioavailability. To address these limitations, a curcumin analog known as PIP was developed, offering superior stability and antiproliferative activity against hepatocellular carcinoma. In this work, PIP was encapsulated into nano-bilosomes using a full factorial design to further boost its solubility and delivery. The optimised nano-formulation displayed a particle size of approximately 112 nanometres, high entrapment efficiency, and a biphasic release profile sustained over 24 hours. When evaluated in cell cultures, the nano-formulation exhibited antiproliferative activity comparable to the standard chemotherapy drug doxorubicin. Furthermore, it demonstrated a selectivity index of 420.55 against Huh-7 liver cancer cells, vastly outperforming both free curcumin and doxorubicin while maintaining lower toxicity toward non-cancerous cells.
Liver cancer treatments often rely on chemotherapy drugs like doxorubicin, which can cause severe toxic side effects in healthy tissues. Formulating a modified natural compound within lipid-based nano-carriers provides strong anticancer potency while significantly reducing harm to non-cancerous cells. This approach offers a potential route to safer and more targeted cancer therapies by overcoming the poor solubility and bioavailability of natural therapeutic agents.
This early-stage research could inform the development of targeted nanomedicines for hepatocellular carcinoma, of interest to pharmaceutical developers and drug delivery formulation specialists. While the formulation demonstrates strong in vitro efficacy and high selectivity compared to conventional chemotherapy, testing remains limited to laboratory cell lines and early safety assays. Additional animal pharmacokinetics, comprehensive in vivo toxicity studies, and clinical trials are necessary before any therapeutic application can be realised.
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Curcumin (CU) is a natural polyphenolic phytoingredient. CU has anti-inflammatory, anti-oxidant, and anticancer activities. The poor solubility, bioavailability, and stability of CU diminish its clinical application. Hence, structural modification of CU is highly recommended. The CU analog; 3,5-bis(4-bromobenzylidene)-1-propanoylpiperidin-4-one (PIP) exhibited high stability, safety, and more potent antiproliferative activity against hepatocellular carcinoma. In the present study, nano-bilosomes (BLs) were formulated to augment PIP delivery and enhance its solubility. A 2<sup>1</sup>.3<sup>1</sup> full factorial design was adopted to prepare the synthesized PIP-loaded BLs. Optimized F4 showed a biphasic release pattern extended over 24 h, with EE%, ZP, and PS of 90.21 ± 1.0%, -27.05 ± 1.08 mV, and 111.68 ± 1.4 nm. PIP-loaded BLs were tested for safety against a non-cancerous cell line (Wi-38) and for anticancer activity against the Huh-7 human hepatocellular carcinoma cells and compared to the standard anticancer drug doxorubicin (Dox). The anticancer selectivity index of PIP-loaded BLs recorded 420.55 against Huh-7 liver cancer cells, markedly higher than a CU suspension (18.959) or the Dox (20.82). The antiproliferative activity of nano-encapsulated PIP was roughly equivalent to Dox. PIP-loaded BLs, showed enhanced drug solubility, and enhanced anticancer effect, with lower toxicity and higher selectivity against Huh-7 liver cancer cells, compared to the parent CU.
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DOI: 10.1080/10717544.2022.2044938
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