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Targeted nanostructured lipid carriers for doxorubicin oral delivery
S Moraes1, A Marinho2, S Lima2
1IFIMUP, Faculty of Sciences of Porto University, Portugal; LAQV, REQUIMTE, Faculty of Pharmacy of Porto University, Portugal.
Abstract:
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.
Insights
This study developed folic acid-conjugated nanostructured lipid carriers (NLCs) for targeted doxorubicin delivery to breast cancer cells, enhancing cellular uptake and enabling potential oral administration.
Area of Science:
- Nanomedicine
- Drug Delivery Systems
- Oncology
Background:
- Anticancer drug treatment faces challenges due to off-target effects.
- Targeted drug delivery aims to improve efficacy and reduce side effects.
Purpose of the Study:
- To develop and evaluate folic acid-conjugated nanostructured lipid carriers (NLCs) for targeted doxorubicin delivery to breast cancer cells.
- To assess the in vitro efficacy, targeting potential, and stability of the developed NLCs.
Main Methods:
- Two NLC formulations were designed and optimized for doxorubicin encapsulation.
- In vitro cytotoxicity and cellular uptake studies were performed using the MDA-MB-231 breast cancer cell line.
- In vitro drug release and storage stability tests were conducted.
Main Results:
- NLCs achieved over 65% encapsulation efficiency for doxorubicin.
- Conjugated NLCs demonstrated enhanced cellular uptake in breast cancer cells.
- Formulations showed potential for oral administration, reaching the tumor microenvironment with 50% drug payload, and exhibited storage stability for at least 42 days.
Conclusions:
- Folic acid-conjugated NLCs are a promising platform for targeted doxorubicin delivery to breast cancer.
- The developed NLCs offer potential for improved oral administration and reduced systemic toxicity.
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