Co-delivery of Lapatinib and 5-Fluorouracil Transfersomes using Transpapillary Iontophoresis for Breast Cancer Therapy

• Published in: International journal of pharmaceutics Vol. 650; p. 123686
• Main Authors: Fernandes, Neha B, Velagacherla, Varalakshmi, Spandana, K J, N, Bhagya, Mehta, Chetan H, Gadag, Shivaprasad, Sabhahit, Jayalakshmi N, Nayak, Usha Y
• Format: Journal Article
• Language: English
• Published: Netherlands 25.01.2024
• Subjects: Transpapillary route; transfersomes; Breast cancer; Lapatinib; 5-Fluorouracil; iontophoresis
• ISSN: 0378-5173; 1873-3476
• DOI: 10.1016/j.ijpharm.2023.123686

Combination chemotherapy, involving the intervention of two or more anti-neoplastic agents has been the cornerstone in breast cancer treatment, owing to the applications it holds in contrast to the mono-therapy approach. This research predominantly focussed on proving the synergy between Lapatinib (LPT) and 5-Fluorouracil (5-FU) and further enhancing its localized permeation via transfersome-loaded delivery and iontophoresis to treat breast tumors. The IC50 values for LPT and 5-FU were found to be 19.38 µg/ml and 5.7 µg/ml respectively and their synergistic effect was proven by the Chou-Talalay assay using CompuSyn software. Furthermore, LPT and 5-FU were encapsulated within transfersomes and administered via the transpapillary route. The drug-loaded carriers were characterized for their particle size, polydispersity index, zeta potential, and entrapment efficiency. The ex vivo rat skin permeation studies indicated that when compared to LPT dispersion and 5-FU solution, drug-loaded transfersomes exhibited better permeability and their transpapillary permeation was enhanced on using iontophoresis. Moreover, both LPT and 5-FU transfersomes were found to be stable for 3 months when stored at a temperature of 5 ± 3 °C. The results indicated that this treatment strategy could be an effective approach in contrast to some of the conventional treatments employed to date.