Lipid‐Coated Mesoporous Silica Nanoparticles for pH‐Responsive Release and Enhanced Anti‐Proliferative Activity of Piperlongumine Natural Product

Abstract The incorporation of natural products into a suitable delivery system has the potential to augment their therapeutic effectiveness significantly. In this study, we demonstrate how silicasomes, a lipid‐coated mesoporous silica nanorods, influence the anticancer potency and release behaviour of the natural product. Piperlongumine ( Pip ), a natural product isolated from long pepper, is loaded into mesoporous silica nanorods ( MSNRs ) followed by a bilayer coating made of 1,2‐Dimyristoyl‐sn‐glycero‐3‐phosphocholine ( DMPC ). The size and morphology of Pip‐loaded MSNRs ( Pip@MSNRs ) and phospholipid‐coated Pip@MSNRs ( PL‐Pip@MSNRs ) are characterized well using suitable analytical techniques. The release of Pip from Pip@MSNRs attained saturation at 48 h while PL‐Pip@MSNRs exhibited the same only after 100 h in both simulated physiological and endolysosomal acidic environments. Moreover, PL‐Pip@MSNRs displayed a higher percentage of Pip release in an acidic medium than in a physiological medium after 24 h. These results confirm that the DMPC coating could assist the pH‐responsive and sustained release of loaded drug from silica nanorods. Most importantly, PL‐Pip@MSNRs demonstrate a higher potency of cytotoxicity and apoptosis against MCF‐7 (Human Breast Carcinoma) cells than the Pip@MSNRs, emphasizing the significance of DMPC‐coated MSNRs as a suitable nanocarrier for natural product delivery.