Abstract:
Colorectal cancer (CRC) despite notable progress in treatment still ranks third in terms of
occurrences and second in terms of mortality. Numerous synthetic chemotherapies have
been used in CRC; nevertheless, they do not specifically target cancerous cells resulting
in serious side effects and significant harm to healthy cells. Accordingly, many alternative
safer therapies have been extensively investigated against CRC. Azithromycin (AZI), a
member of macrolides antibiotics, has been reported to inhibit the proliferation of cancer
cells by targeting mitochondria and eradicating cancer cells. Despite its promising
therapeutic activity, it is restricted by its poor aqueous solubility leading to efforts
focusing on the development of safe and efficient anticancer Nano carriers. Liposomes
are the most widely studied Nano-drug carriers in drug delivery. Compared with other
Nano carriers, liposomes exhibit prominent properties that include targeted delivery, high
biocompatibility, biodegradability, low toxicity, and improved therapeutic indices. Thus,
the current work aims is to design a liposome to augment azithromycin anticancer effects.
Liposome was prepared from soybean phospholipid using an ethanol injection technique
and coated chitosan. The designed coated and uncoated systems were characterized both
physicochemically and on colorectal cancer cell line in vitro. The results displayed Nano
metric size range for azithromycin-loaded uncoated and coated liposomes of values 65.5± 2.83 nm and 73.53 ± 2.01 nm, respectively with uni-modal particle size distribution with
PDI less than 0.3. The shifting of the negative charge (-17.22± 5.99 mV) of the uncoated
liposomes to the positive charge (13.17± 3.34 mV) of the coated one approved the
success of the coating. The formulation showed ideal characteristics of 70% AZI
entrapment and in vitro controlled release. It displayed a safe profile on HT29 cell line,
with the coated formulation having the lowest IC50= 24.17 μM at 24 hours that even
decreases at longer time intervals, which confirms its potential for colorectal cancer management.
