In Vitro Cytotoxicity and Cellular Uptake of Tamoxifen Citrate-Loaded Polymeric Micelles
- PDF / 1,015,051 Bytes
- 11 Pages / 595.276 x 790.866 pts Page_size
- 60 Downloads / 183 Views
Research Article In Vitro Cytotoxicity and Cellular Uptake of Tamoxifen Citrate-Loaded Polymeric Micelles Mohamed Nasr,1,2 Fahima Hashem,1 Raghda Abdelmoniem,1 Norhan Tantawy,1 and Mohamed Teiama1
Received 20 July 2020; accepted 12 October 2020 Abstract.
The main intent of this treatise was to encapsulate tamoxifen citrate (TMXC) into polymeric micellar delivery system and evaluate the influence of TMXC-loaded micelles as a promising carrier on the in vitro cytotoxicity and cellular uptake of TMXC in treatment of breast cancer. Different formulae of polymeric micelles loaded with TMXC using mixtures of different Pluronic polymers were fabricated by thin-film hydration method and evaluated for morphology, drug entrapment efficiency, particle size, surface charge, in vitro liberation of TMXC, uptake by cancer cell lines, and cytotoxic effect against breast cancer cell lines such as MCF-7. The optimal TMXC-loaded micelles exhibited nano-sized particles and entrapped about 89.09 ± 4.2% of TMXC. In vitro liberation study revealed an extended TMXC escape of about 70.23 ± 5.9% over a period of 36 h. The optimized TMXC-loaded micelles formula showed enhanced cellular uptake of TMXC by 2.28 folds and showed a significant cytotoxic effect with MCF-7 breast cancer cells compared to TMXC solution. The obtained yield proposed that Pluronic micelles could be a promising potential delivery system for anticancer moieties.
KEY WORDS: Pluronic polymers; polymeric micelles; tamoxifen citrate; cellular uptake; cytotoxicity; breast cancer.
INTRODUCTION Breast cancer is a prevalent tumor amongst women (1) and represents the foremost reason of cancer’s mortality in females (2). Treatment of breast cancer includes local treatment such as surgery which depends on the type and stage of tumor. Also, systemic drugs can be used to reach cancer cells at any part of the body. These systemic drugs comprise chemotherapy, hormonal therapy, and immunotherapy. Hormonal therapy is used to prevent attachment of progesterone and estrogen to their receptors in some types of breast cancer that affected by hormonal level. Some of these hormonal drugs are named as estrogen blocker which works by stopping estrogen from helping breast cancer cells to grow such as tamoxifen, toremifene, and fulvestrant (3). Tamoxifen citrate (TMXC) is the most commonly used chemotherapy for siege of breast cancer (4). Although TMXC exhibits favorable outcomes, not all treated patients get the hopeful result. High doses of TMXC presented numerous hormonal effects even dependent and independent (5). However, most anticancer drugs that can successfully
1
Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Helwan University, Cairo, 11790, Egypt. 2 To whom correspondence should be addressed. (e–mail: [email protected])
diminish the neoplastic cells exhibit remarkable side effects mainly because of absence of precise targeting ability (6). Nanocarriers have got extensive concern as a promising carrier for chemotherapy in respect to their capability to carry d
Data Loading...
