Folic acid engineered sulforaphane loaded microbeads for targeting breast cancer

Abstract

Non-targeted cancer therapy poses a huge risk to the cancer patients’ life due to high toxicity offered by chemotherapy. Breast carcinoma is one of such deleterious disease, demanding a highly effectual treatment option which could reduce the toxicity and extend survival rate. Since, folate receptors extensively display themselves on the cancer cell surface, targeting them would help to ameliorate the progression and metastasis. Considering this, we envisaged and developed sulforaphane loaded folate engineered microbeads to target breast cancer cells over-expressing folate receptors. The surface engineered microbeads were optimized and developed using emulsion gelation technique, among which the best developed preparation demonstrated the particle size of 1302 ± 3.98 µm, % EE of 84.1 ± 3.32% and in vitro drug release of 98.1 ± 4.42%@24h. The spherical sized microbead showed controlled release with improved haem-compatibility in comparison to the bare drug. Free radical scavenging activity by ABTS assay showed strong anti-oxidant activity (IC₅₀ 20.62 µg/ml) of the targeted microbeads with profound cancer cell sup pressing effect (IC₅₀ 17.48 ± 3.5 µM) as observed in MCF-7 cells by MTT assay. Finally, in comparison to lone SFN, the targeted therapy showed enhanced uptake by the intestinal villi indicating a suitable oral targeted therapy against breast carcinoma.

Keywords:

• Breast cancer
• folate-targeted
• microbeads
• sulforaphane
• targeted drug delivery

Disclosure statement

No potential conflict of interest was reported by the author(s).

Additional information

Funding

The author (Mohammed A. S. Abourehab) would like to thank the Deanship of Scientific Research at Umm Al-Qura University for supporting this work with Grant Code (23UQU4290565DSR108). The author (Zafar Khan) would like to thank DST-FIST for providing departmental and instrumental facilities, as well as DST-Purse for giving a fellowship from December 2017 to May 2019. The authors would like to thank ICMR (ICMR-SRF-45/40/2019-NAN/BMS) for their support. For bestowing a Senior Research Fellowship to the author in June 2019.