Cancer poses a significant threat to human health worldwide, and many
therapies have been used for its palliative and curative treatments.
Vincristine has been extensively used in
chemotherapy. However, there are two major challenges concerning its applications in various
tumors: (1)
Vincristine's antitumor mechanism is cell-cycle-specific, and the duration of its exposure to
tumor cells can significantly affect its antitumor activity and (2)
Vincristine is widely bio-distributed and can be rapidly eliminated. One
solution to these challenges is the encapsulation of
vincristine into
liposomes.
Vincristine can be loaded into conventional
liposomes, but it quickly leak out owing to its high membrane permeability. Numerous approaches have been attempted to overcome this problem.
Vincristine has been loaded into PEGylated
liposomes to prolong circulation time and improve
tumor accumulation. These
liposomes indeed prolong circulation time, but the payout characteristic of
vincristine is severer, resulting in a compromised outcome rather than a better efficacy compared to conventional
sphingomyelin (SM)/
cholesterol (Chol)
liposomes. In 2012, the USA Food and Drug Administration (FDA) approved SM/Chol liposomal
vincristine (Marqibo®) for commercial use. In this review, we mainly focus on the
drug's rapid leakage problem and the potentially relevant solutions that can be applied during the development of liposomal
vincristine and the reason for conventional liposomal
vincristine rather than PEGylated
liposomes has access to the market.