Abstract
More than one out of every three new cancers is a skin cancer, and the large majority are basal cell carcinomas (BCC). Targeted therapy targets the cancer’s specific genes, proteins, or tissue environment that contributes to cancer growth and survival and blocks the growth as well as the spread of cancer cells while limiting damage to healthy cells. Therefore, in the present study AS1411 aptamer-functionalized liposomes for the treatment of BCC were obtained and characterized. Aptamer conjugation increased liposome size, suggesting that the presence of an additional hydrophilic molecule on the liposomal surface increased the hydrodynamic diameter. As expected, the negatively charged DNA aptamer reduced the surface potential of the liposomes. Vertical Franz diffusion cells with artificial membranes were used to evaluate the in vitro release of 5-fluorouracil (5-FU). The aptamer moieties increase the stability of the liposomes and act as a supplementary steric barrier leading to a lower cumulative amount of the released 5-FU. The in vitro cell viability, targeting capability and apoptotic effects of liposomes on the human dermal fibroblasts and on the basal cell carcinoma TE 354.T cell lines were also evaluated. The results indicate that the functionalized liposomes are more efficient as nanocarriers than the non-functionalized ones.
Highlights
Cancer remains one of the world’s most devastating diseases, and skin cancer is the most common form of malignancy in the United States and many other countries [1,2]
The main purpose of this study was to develop a new type of AS1411 aptamer-functionalized liposomes loaded with 5-FU, which could present an excellent alternative for the treatment of basal cell carcinomas (BCC)
Liposomes composed of PC, Chol, and DSPE-PEG-MAL were prepared, and aptamer AS1411, which targets tumor cells, was conjugated onto the external surface of liposomes
Summary
Cancer remains one of the world’s most devastating diseases, and skin cancer is the most common form of malignancy in the United States and many other countries [1,2]. BCC, among one of the most common forms of human cancer, constitutes approximately 74% of skin cancer cases worldwide, and its incidence is increasing [3]. Focused intervention, including cryotherapy, surgical excision, radiation therapy, photodynamic therapy, and chemotherapy (using antiproliferation drugs such as 5-aminolevulinic acid (5-ALA), 5-fluorouracil (5-FU), paclitaxel, resveratrol, imiquimod, temoporfin, and vismodegib) are usually used to combat the tumors [5,6,7,8,9]. Conventional chemotherapy applied to these conditions shows non-specific targeting, and high doses of anticancer drugs affect both normal and tumor cells, Polymers 2019, 11, 1515; doi:10.3390/polym11091515 www.mdpi.com/journal/polymers
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