Abstract
The study investigated in situ biosynthesis of albumin capped 5-fluorouracil (5-FU) loaded gold nanoparticles (NPs) using bacterial extract for enhanced efficacy against MCF-7 and in silico prediction using a GastroPlus® software. The optimized formulations were characterized for morphology, size, zeta potential, drug loading (%DL) and entrapment (%EE), compatibility, in vitro drug release, in vitro hemolysis, cellular toxicity and apoptosis studies. The results exhibited highly dispersed albumin capped mono-metallic stable NPs. Spherical size, negative zeta potential and polydispersity index were in range of 38.25–249.62 nm, 18.18–29.87 mV and 0.11–0.283, respectively. F11, F7 and F3 showed a progressive increase in %DL and %EE with increased concentration of the cellular lysate (100% > 50% > 10%). The drug release was relatively extended over 48 h as compared to drug solution (96.64% release within 5 h). The hemolysis result ensured hemocompatibility (<14%) at the explored concentration. The biogenic F11 was more cytotoxic (81.99% inhibition by F11 and 72.04% by pure 5-FU) to the MCF-7 cell lines as compared to others which may be attributed to the preferential accumulation by the tumor cell and capped albumin as the source of energy to the cancer cells. Finally, GastroPlus® predicted the key factors responsible for improved pharmacokinetics parameters and regional absorption from various segments of human intestine. Thus, the approach can be more efficacious and suitable to control breast cancer when administered transdermally or orally.
Highlights
Breast cancer is the second most common leading cause of death amongst women
gold NPs (GNs) have been reported to provide eminence in clinical benefits due to their distinctive properties such as (a) controlled size and shape owing to unique optical properties, (b) non-toxic and biocompatible mono metallic nanoparticles, (c) tunable surface dependent properties, (d) ease of synthesis, (e) desired surface functionalization, (f) protection drug from degradation, (g) increased blood circulation time, (h) enhanced efficacy through active or passive targeting and (i) preferential accumulation into the tumor tissue [13,14,15,16,17,18]
5-FU loaded gold NPs followed by albumin capping could be a promising approach with high drug payload, desired targeted drug release, increased accumulation to tumor tissue, reduced dose related side effect and minimized hemolysis in the treatment of breast cancer
Summary
Breast cancer is the second most common leading cause of death amongst women. GLOBOCAN estimated 2,088,849 new cases of breast cancer (including both sexes of all ages) which is 11.6% of total new cases in 2018 [1]. 5-fluorouracil (5-FU) is a pyrimidine analogue (antimetabolite) commonly used to treat solid tumors (breast, skin, liver, ovarian, rectal, colon and gastrointestinal cancers) despite of having several side effects (severe bone marrow deficiency, skin reactions, hair thinning, severe gastrointestinal disturbances, hematological disturbances, hand foot syndrome) in conventional dosage forms [2]. 5-FU loaded gold NPs followed by albumin (bovine serum albumin) capping could be a promising approach with high drug payload, desired targeted drug release, increased accumulation to tumor tissue, reduced dose related side effect and minimized hemolysis in the treatment of breast cancer. The optimized formulation needs to be investigated (in future communication) using suitable animal model to find the effect of capping on permeation parameters (permeation rate, targeted flux, enhancement ratio and permeation coefficient) as compared to free drug solution (DS) and uncapped gold NPs. The biogenic BSA capped gold NPs increased anticancer efficacy of 5-FU against MCF-7 cancer cell lines which could be a promising approach for transdermal or oral delivery to control breast cancer with minimum side effects and high patient compliance
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