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

Abstract

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.

Emerging Trends in Bilosomes as Therapeutic Drug Delivery Systems

“…This has led to the development of several mixed micelle systems to enhance the solubility of extremely lipophilic pharmaceuticals [31]. Bile salts have the additional effect of improving the flexibility of bilosomes in simulated fluids and the same is reported by Mondal et al through the use of microscopy and fluorescence techniques [32]. This is achieved through the induction of repulsion between the bile salts contained inside the bilosomes and the external bile salts found in the gut lumen.…”

Recent Advances of Ocular Drug Delivery Systems: Prominence of Ocular Implants for Chronic Eye Diseases

“…The negatively charged bile salts serve to maintain the bilosomal structure [ 372 ]. In comparison to niosomes and liposomes, these drug carriers are more stable and can effectively increase drug absorption through biological membranes [ 373 ]. Moreover, bilosomes can enhance the permeability of polysaccharides, proteins, and polypeptides, which are poorly transported through mucosal epithelial cells [ 374 ].…”

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

“…Earlier, this group had shown that bilosomes show superior temporal stability and sustained delivery (of the antioxidant curcumin) compared to niosomes. 28 The bilosomes used in the previous work comprised the bile salts NaDC and NaC. In this work, the bile salt sodium taurocholate (NaTC) was used to prepare the bilosomes.…”