Potential of transpapillary route for artesunate-loaded microneedles against breast cancer cell line

Abstract

Breast cancer is the most common cancer in women with highest mortality rate wherein, mastectomy, lumpectomy, radiation therapy, hormone therapy, chemotherapy, and biological therapy are some of the current therapeutic alternatives for breast cancer. The treatments, however, are linked to short and long-term side effects like cardiac problems, anemia, physiological distress, myelosuppression, peripheral neuropathy and thrombosis. Hence, the transpapillary route is a promising route for delivering drugs directly to the underlying breast tissues for the treatment of breast cancer by achieving higher drug levels at the tumor site. The aim of the present study was to check the potential of transpapillary route for artesunate-loaded microneedles, solid lipid nanoparticles (SLN)-loaded microneedles and layer-by-layer (LBL)-coated SLN-loaded microneedles against breast cancer. SLNs were prepared by hot-melt emulsification method and LBL-coating on SLNs was achieved by 1 mg/1 mL of chitosan and 2 mg/mL of hyaluronic acid. The particle sizes of selected formulations of SLNs and LBL-coated SLNs were found to be 213.72 ± 2.53 nm and 319.39 ± 1.25 nm, respectively. Zeta potentials of selected formulations SLNs and LBL-coated SLNs were found to be −27.32 ± 4.45 mV and −28.41 ± 3.67 mV, respectively. Three formulations of microneedles were prepared for comparative evaluation using artesunate, SLNs, LBL-coated SLNs. Microneedles were evaluated for FTIR, DSC, mechanical insertion property, surface morphology, in-vitro release, ex-vivo release and cell line studies. The cell line study and ex-vivo release profile of LBL-coated SLN microneedles showed a reduction in growth of cell line MCF 7 by 7.92 ± 1.54% and higher ex-vivo release (84.75 ± 2.02%) in comparison to plain drug. Thus, the LBL-coated SLNs microneedles of artesunate proved as an effective alternative against breast cancer cell line.