Vesicle-Encapsulated Rolipram (PDE4 Inhibitor) and Its Anticancer Activity.

Vesicular carriers of drugs are popular for specific targeting and delivery. The most popular vesicles among these are liposomes. However, they suffer from some inherent limitations. In this work, alternative vesicles with enhanced stability, i.e., niosomes and bilosomes have been prepared, characterized, and their delivery efficiency studied. Bilosomes have the additional advantage of being able to withstand the harsh environment of the gastrointestinal tract (GIT). The taurine-derived bile salt (NaTC) was incorporated into the bilosome bilayer. The inspiration behind NaTC insertion is the recent reports on antiaging action and immune function of taurine. Fluorescence probing was used to study the vesicle environment. The entrapment and subsequent release of the important cAMP-specific PDE4 inhibitor/drug Rolipram, which has antibreast cancer properties, was assessed on the breast cancer cell line MCF-7. Rolipram has important therapeutic applications, one of the most significant in recent times being the treatment of Covid-19-triggered pneumonia and cytokine storms. As for cancer chemotherapy, the localization of drug, targeted delivery, and sustained release are extremely important issues, and it seemed worthwhile to explore the potential of the bilosomes and niosomes to entrap and release Rolipram. The important finding is that niosomes perform much better than bilosomes in the hormone-responsive breast cancer mileau MCF-7. Moreover, there was a 4-fold decrease in the IC50 of Rolipram encapsulated in niosomes compared to Rolipram alone. On the other hand, bilosome-encapsulated Rolipram shows higher IC50 value. The results can be further understood by molecular docking studies.

Addressing the Superior Drug Delivery Performance of Bilosomes─A Microscopy and Fluorescence Study.

The global health scenario in present times has raised human awareness about drug delivery strategies. Among colloidal drug delivery vehicles, vesicular nanocarriers such as liposomes and niosomes are popular. However, liposomes and niosomes get disrupted in the harsh environment of the gastrointestinal tract. In this context, the drug delivery community has reported the superior performance of vesicles containing bile salts, that is, bilosomes. The present work attempts to examine the structural/morphological aspects underlying the superior performance of bilosomes. Optical microscopy, electron microscopy, and light scattering give a definite proof of the enhanced stability of bilosomes compared to niosomes, both prepared from the same amphiphilic molecule. Fluorescence probing of the vesicles provides detailed insight into the bilayer characteristics and the differences between bilosomes and niosomes. Fluorescence resonance energy transfer studies lend further support to the findings that bilosomes have a more flexible bilayer structure than niosomes. The entrapment efficiency of the vesicles for the well-known antioxidant curcumin (whose bioavailability is a matter of concern due to low water solubility) was also studied. Bilosomes show higher curcumin entrapment efficiency than niosomes. For use in drug delivery, one needs to establish a trade-off between cargo/drug entrapment and release. Thus, a flexible bilayer structure is an advantage.