Novel self-assembled lithocholic acid nanoparticles for drug delivery in cancer

Abstract

Novel versatile self-assembled nanoparticles were developed from biocompatible, biodegradable lithocholic acid derivatives. These nanoparticles can incorporate different cytotoxic drugs (paclitaxel and doxorubicin) and PI3K signalling inhibitor (PI103). Drugs were released from the nanoparticles in a slow, sustained manner at acidic pH. The drug loaded nanoparticles were internalized through lysosomal compartments and induced cell death in HeLa cervical cancer cells.

Facially amphiphilic polyionene biocidal polymers derived from lithocholic acid

“…They typically stay conjugated with taurine or glycine in the liver forming bile salts that serve as surfactants to solubilize dietary lipids and fats by the formation of micelles allowing digestion of food. Bile acids have been utilized in many areas including gene delivery [ 19 , 20 ], drug delivery [ 21 ], sensing [ 22 ], polymeric gels [ 23 ], antimicrobial agents [ [24] , [25] , [26] ] and other biological applications [ 27 ].…”

Galactosylated Poly(Ethyleneglycol)‐Lithocholic Acid Selectively Kills Hepatoma Cells, While Sparing Normal Liver Cells

“…LCA is a naturally occurring secondary bile acid that is formed in the gut during bacterial degradation of the primary bile acids and metabolized in liver . Bile acids are steroidal amphipathic molecules that facilitate excretion, absorption, and transport of fats and sterols in the intestine and liver . Although some bile acid derivatives have been identified to exhibit potent cytotoxic properties, recent researches suggest that LCA not only kills neuroblastoma cells selectively, but also displays anti‐tumor effect in several types of cultured cancer cells at physiologically relevant concentrations .…”

Pharmacological and Biological Study of Microencapsulated Probucol-Secondary Bile Acid in a Diseased Mouse Model

“…All three groups were given the same PB dose, so they showed equal concentration in the stomach. However, G-4 mice gavaged with PB-LCA microcapsules had higher PB levels in the small intestine and large intestine, indicating gastro-protection until the drug reaches the absorption site in the gut, which demonstrates that bile acids enhance absorption and improve stability of the drug [ 67 ]. Likewise, we found a higher level of PB in blood and other tissues, which proves that PB-LCA microcapsule enhanced drug absorption and increased bioavailability and tissue accumulation, probably through the inhibition of the efflux system leading to increased PB net absorption and cellular permeation [ 68 , 69 ].…”