Fluorescent tamoxifen-encapsulated nanocapsules functionalized with folic acid for enhanced drug delivery toward breast cancer cell line MCF-7 and cancer cell imaging

• Published in: Naunyn-Schmiedeberg's archives of pharmacology 2020-07, Vol.393 (7), p.1211-1219
• Main Authors: Nankali, Ehsan, Shaabanzadeh, Masoud, Torbati, Maryam Bikhof
• Format: Article
• Language: English
• Subjects: Antineoplastic Agents, Hormonal - administration & dosage; Antineoplastic Agents, Hormonal - chemistry; Antineoplastic Agents, Hormonal - pharmacology; Biocompatibility; Biodegradability; Biomedical and Life Sciences; Biomedicine; Breast cancer; Breast Neoplasms - drug therapy; Controlled release; Cytotoxicity; Delayed-Action Preparations; Drug delivery; Drug Delivery Systems; Drug Liberation; Drug Stability; Encapsulation; Female; Fluorescein isothiocyanate; Fluorescein-5-isothiocyanate - chemistry; Folic acid; Folic Acid - chemistry; Humans; Inhibitory Concentration 50; MCF-7 Cells; Nanocapsules; Neurosciences; Original Article; Pharmacology/Toxicology; Solubility; Tamoxifen; Tamoxifen - administration & dosage; Tamoxifen - chemistry; Tamoxifen - pharmacology
• ISSN: 0028-1298; 1432-1912
• DOI: 10.1007/s00210-020-01825-1

Nanoscale drug delivery systems such as nanocapsules at the convergence of nanotechnology and biomedical sciences have been widely used. In the present study, with the aim of simultaneous imaging and therapy of cancer cells based on biodegradable/biocompatible polymers, we designed and synthesized tamoxifen-encapsulated nanocapsules to target the folate receptor positive breast cancer cells. Noteworthy, to monitor and link to the cancer cells, these nanocapsules were functionalized with fluorescein isothiocyanate and folic acid. The synthesized nanocapsules were characterized by FTIR, XRD, and PL spectroscopy, as well as FESEM and TEM techniques. Although the free tamoxifen has low solubility in physiological solutions, the synthesized tamoxifen-encapsulated nanocapsules have enough solubility, good stability, and more biocompatibility in these solutions. The encapsulation of tamoxifen into the nanocapsules, tamoxifen loading, and its subsequent release behavior were studied. In order to investigate the biological role of these nanocapsules, MTT assay and cell imaging analysis have also been examined. The cytotoxicity test exhibit that the mean IC 50 values on the MCF-7 cell line were found to be 15.52 and 8.46 μg/ml in 24 h and 48 h respectively and the cytotoxicity increased by approximately 2.72-fold compared with free TAM against the MCF-7 cancer cell line. Also, cell imaging experiments showed that the synthesized nanocapsules have appropriate cellular uptake efficiency, good potential for monitoring of these particles in vitro. The experimental results suggest that the synthesized tamoxifen nanocapsules facilitate the proper targeting, drug encapsulation efficiency, and controlled release of tamoxifen in vitro.