Targeted nanostructured lipid carriers for doxorubicin oral delivery

• Published in: International journal of pharmaceutics 2021-01, Vol.592, p.120029-120029, Article 120029
• Main Authors: Moraes, S., Marinho, A., Lima, S., Granja, A., Araújo, J.P., Reis, S., Sousa, C.T., Nunes, C.
• Format: Article
• Language: English
• Subjects: Folic acid; Lipid nanoparticles; Oral administration of anticancer-drugs; Targeted delivery
• ISSN: 0378-5173; 1873-3476
• DOI: 10.1016/j.ijpharm.2020.120029

[Display omitted] •The produced lipid carriers show potential to be administered by the oral route.•The stability of the formulations is, at room temperature, at least 42 days.•80% of the functionalized particles are uptaken in less then 40 min. The treatment with anticancer drugs remains a challenge, as available drugs still entail the risk of deleterious off-target effects. The present study describes folic acid conjugated nanostructured lipid carriers (NLCs) as an effective doxorubicin delivery approach targeted to breast cancer cells. Two distinct NLCs formulations were designed and optimized leading to an encapsulation efficiency over than 65%. Cytotoxic and targeting potential of NLCs were studied in vitro, using MDA-MB-231 cell line. Results showed an enhanced cellular uptake of conjugated NLCs. In vitro release studies, mimicking the path in the body after oral administration, show that all formulations would reach the tumor microenvironment bearing 50% of the encapsulated doxorubicin. Moreover, NLCs demonstrated storage stability at 25 °C for at least 42 days. Overall, results revealed that the developed NLCs enable the possibility of oral administration and are a promising approach for the targeted delivery of doxorubicin to breast cancer cells.