Polycaprolactone nanofibers as an adjuvant strategy for Tamoxifen release and their cytotoxicity on breast cancer cells

Breast cancer is the second leading cause of death in women, and tamoxifen citrate (TMX) is accepted widely for the treatment of hormone receptor–positive breast cancers. Several local drug-delivery systems, including nanofibers, have been developed for antitumor treatment. Nanofibers are biomaterials that mimic the natural extracellular matrix, and they have been used as controlled release devices because they enable highly efficient drug loading. The purpose of the present study was to develop polycaprolactone (PCL) nanofibers incorporating TMX for use in the treatment of breast tumors. Pristine PCL and PCL-TMX nanofibers were produced by electrospinning and characterized physiochemically using different techniques. In addition, an in vitro study of TMX release from the nanofibers was performed. The PCL-TMX nanofibers showed sustained TMX release up to 14 h, releasing 100% of the TMX. The Resazurin reduction assay was used to evaluate the TMX cytotoxicity on MCF-7 breast cancer cell line and PBMCs human. The PCL-TMX nanofiber was cytotoxic toPBMCs and MCF-7. Based on these results, the PCL-TMX nanofibers developed have potential as an alternative for local chronic TMX use for breast cancer treatment, however tissue tests must be done.

Characterization and anticancer efficacy of tamoxifen citrate nanosuspension against MCF-7 breast cancer cells

Nanotechnology is one of the important fields that developed strategies to solve the issue of Tamoxifen (TAM) toxicity, owing to the capacity of nano-enabled-formulations to deliver smaller concentrations of TAM to cancer cells, over a longer period of time. Many different TAM-containing-nano systems have been successfully fabricated to selectively deliver TAM to particular molecular targets on tumour membranes, decreasing unwanted toxic effects. The present study was carried out to synthesis the tamoxifen citrate nanosuspension and also to find its effectiveness against breast cancer cells. Nanoparticles were made using multiple emulsion solvent evaporation method and its characterizations were studied. The structure and morphological examination of tamoxifen citrate Liquid self-nanoemulsifying drug delivery systems were observed with transmission electron microscopy. The cytotoxic effect of tamoxifen citrate L-SNEDDS against breast cancer MCF-7 cells was measured by cell viability assay. The cytotoxic effect of tamoxifen citrate L-SNEDDS enhanced significantly as the concentration of drug enhanced from 25 μM to 250 μM. The toxic action of tamoxifen citrate L-SNEDDS on cancer cells remarkably reduced cell viability from 100% to 20.3%, while nanosuspension devoid of the drug presented cell viability of 99.5%. A significant decrease in cell viability was found in tamoxifen citrate free drug from 100% to 30.9%. In conclusion, tamoxifen citrate Liquid self-nanoemulsifying drug delivery systems showed cytotoxic activity on MCF-7 breast cancer cell lines.

Long-Term Outcomes of Tamoxifen Citrate Therapy and Histo- and Immunopathological Properties in Riedel Thyroiditis

<b><i>Background:</i></b> Riedel thyroiditis (RT) is a rare form of thyroiditis; thus, data about the disease course and treatment options are limited. Therefore, we aimed to assess the clinical, serological, radiological, and histopathological features, as well as short- and long-term follow-up of RT patients under glucocorticoid (GC) and tamoxifen citrate (TMX). Parameters related to IgG4-related diseases (IgG4-RD) were also investigated. <b><i>Methods:</i></b> Eight patients with RT diagnosed between 2000 and 2019 were enrolled. Data were collected in a retrospective and prospective manner. The diagnosis was confirmed with histopathological features in all patients. Results of the treatment with GCs on short- to mid-term, followed by TMX in the long term, were evaluated. <b><i>Results:</i></b> The mean age at diagnosis was 40.5 ± 6.8 years; female predominance was observed (F/M:7/1). Parameters related to IgG4-RD, like increase in IgG4 serum levels, total plasmablast counts, and IgG4+ plasmablasts, were negative in most of our patients in both active and inactive states of the disease. Likewise, an increased ratio of IgG4/IgG-positive plasma cells &#x3e;40% could only be observed in 2 cases. GCs followed by TMX were given to the patients with an over-all median follow-up time of 67 (8–216) months. All the patients considerably improved clinically and had a reduction in the size of the mass lesion on GCs, followed by TMX therapy. None of the patients had a recurrence under TMX therapy for a median period of 18.5 (7–96) months. <b><i>Conclusion:</i></b> Even though RT is suggested to be a member of IgG4-RD, serologic or histological evidence of IgG4 elevation or positivity is only useful for diagnosis and follow-up of RT. The diagnosis should be based on clinical and radiological evidence and confirmed by histopathology. GCs are effective for initial treatment, and TMX is a successful and safe therapeutic option for long-term maintenance therapy.

Formulation and Development of Transferrin Targeted Solid Lipid Nanoparticles for Breast Cancer Therapy

Breast cancer is conventionally treated by surgery, chemotherapy and radiation therapy followed by post operational hormonal therapy. Tamoxifen citrate is a best option to treat breast cancer because its selective estrogen receptor modulation activity. Owing to its antiestrogenic action on breast as well as uterine cells, Tamoxifen citrate shows uterine toxicity. The dose 20 mg per day of Tamoxifen citrate required to show therapeutic effect causes side effects and toxicity to vital organs such as liver, kidney and uterus. In the present study, transferrin-conjugated solid lipid nanoparticles (SLNs) were successfully prepared to enhance the active targeting of tamoxifen citrate in breast cancer. Developed formulations were evaluated for particle size, surface charge, surface morphology and in vitro dissolution studies. Developed formulations exhibited more cytotoxicity as compared to pure Tamoxifen citrate solution in time as well as concentration dependent manner on human breast cancer MCF-7 cells. Further, cell uptake and flow cytometry studies confirmed the qualitative uptake of developed D-SLN and SMD-SLN by human breast cancer MCF-7 cells. Overall, proposed study highlights that transferrin engineered nanocarriers could enhance the therapeutic response of nanomedicines for breast cancer treatment.