Breast cancer is one of the most prevalent causes of
cancer mortality in women. In order to increase patient prognosis and survival rates, new technologies are urgently required to deliver
therapeutics in a more effective and efficient manner.
Niosome nanoparticles have been recently employed as therapeutic platforms capable of loading and carrying drugs within their core for both mono and combination
therapy. Here,
niosome-based nanoscale carriers were investigated as a targeted delivery system for
breast cancer therapy. The platform developed consists of
niosomes loaded with
letrozole and
cyclophosphamide (NLC) and surface-functionalized with a
folic-acid-targeting moiety (NLCPFA). Drug release from the formulated particles exhibited pH-sensitive properties in which the
niosome showed low and high release in physiological and cancerous conditions, respectively. The results revealed a synergic effect in cytotoxicity by co-loading
letrozole and
cyclophosphamide with an efficacy increment in NLCPFA use in comparison with NLC. The NLCPFA resulted in the greatest drug internalization compared to the non-targeted formulation and the free drug. Additionally, downregulation of
cyclin-D,
cyclin-E, MMP-2, and MMP-9 and upregulating the expression of
caspase-3 and
caspase-9 genes were observed more prominently in the nanoformulation (particularly for NLCPFA) compared to the free drug. This exciting data indicated that
niosome-based nanocarriers containing
letrozole and
cyclophosphamide with controlled release could be a promising platform for drug delivery with potential in
breast cancer therapy.