scholarly journals Evaluation of β-Sitosterol Loaded PLGA and PEG-PLA Nanoparticles for Effective Treatment of Breast Cancer: Preparation, Physicochemical Characterization, and Antitumor Activity

Pharmaceutics ◽  
2018 ◽  
Vol 10 (4) ◽  
pp. 232 ◽  
Author(s):  
Moses Andima ◽  
Gabriella Costabile ◽  
Lorenz Isert ◽  
Albert Ndakala ◽  
Solomon Derese ◽  
...  

β-Sitosterol (β-Sit) is a dietary phytosterol with demonstrated anticancer activity against a panel of cancers, but its poor solubility in water limits its bioavailability and therapeutic efficacy. In this study, poly(lactide-co-glycolic acid) (PLGA) and block copolymers of poly(ethylene glycol)-block-poly(lactic acid) (PEG-PLA) were used to encapsulate β-Sit into nanoparticles with the aim of enhancing its in vitro anticancer activity. β-Sitosterol-loaded PLGA and PEG-PLA nanoparticles (β-Sit-PLGA and β-Sit-PEG-PLA) were prepared by using a simple emulsion-solvent evaporation technique. The nanoparticles were characterized for size, particle size distribution, surface charge, and encapsulation efficiency. Their cellular uptake and antiproliferative activity was evaluated against MCF-7 and MDA-MB-231 human breast cancer cells using flow cytometry and MTT assays, respectively. β-Sit-PLGA and β-Sit-PEG-PLA nanoparticles were spherical in shape with average particle sizes of 215.0 ± 29.7 and 240.6 ± 23.3 nm, a zeta potential of −13.8 ± 1.61 and −23.5 ± 0.27 mV, respectively, and with narrow size distribution. The encapsulation efficiency of β-Sit was 62.89 ± 4.66 and 51.83 ± 19.72 % in PLGA and PEG-PLA nanoparticles, respectively. In vitro release in phosphate-buffered saline (PBS) and PBS/with 0.2% Tween 20 showed an initial burst release, followed by a sustained release for 408 h. β-Sit-PLGA nanoparticles were generally stable in a protein-rich medium, whereas β-Sit-PEG-PLA nanoparticles showed a tendency to aggregate. Flow cytometry analysis (FACS) indicated that β-Sit-PLGA nanoparticles were efficiently taken up by the cells in contrast to β-Sit-PEG-PLA nanoparticles. β-Sit-PLGA nanoparticles were therefore selected to evaluate antiproliferative activity. Cell viability was inhibited by up to 80% in a concentration range of 6.64–53.08 μg/mL compared to the untreated cells. Taken together, encapsulation of β-Sitosterol in PLGA nanoparticles is a promising strategy to enhance its anticancer activity against breast cancer cells.

2020 ◽  
Vol 21 (2) ◽  
pp. 187-200
Author(s):  
Corina Danciu ◽  
Oana Cioanca ◽  
Claudia Watz Farcaș ◽  
Monica Hancianu ◽  
Roxana Racoviceanu ◽  
...  

Background: This study was designed as a continuation of a complex investigation about the phytochemical composition and biological activity of chamomile, parsley, and celery extracts against A375 human melanoma and dendritic cells. Objective: The main aim was the evaluation of the antimicrobial potential of selected extracts as well as the in vitro anticancer activity against MCF7 human breast cancer cells. Methods: In order to complete the picture regarding the phytochemical composition, molecular fingerprint was sketched out by the help of FTIR spectroscopy. The activity of two enzymes (acetylcholinesterase and butyrylcholinesterase) after incubation with the three extracts was spectrophotometrically assessed. The antimicrobial potential was evaluated by disk diffusion method. The in vitro anticancer potential against MCF7 human breast cancer cells was appraised by MTT, LDH, wound healing, cell cycle, DAPI, Annexin-V-PI assays. Results: The results showed variations between the investigated extracts in terms of inhibitory activity against enzymes, such as acetyl- and butyrilcholinesterase. Chamomile and parsley extracts were active only against tested Gram-positive cocci, while all tested extracts displayed antifungal effects. Among the screened samples at the highest tested concentration, namely 60μg/mL, parsley was the most active extract in terms of reducing the viability of MCF7 - human breast adenocarcinoma cell line and inducing the release of lactate dehydrogenase. On the other hand, chamomile and celery extracts manifested potent anti-migratory effects. Furthermore, celery extract was the most active in terms of total apoptotic events, while chamomile extract induced the highest necrosis rate. Conclusion: The screened samples containing phytochemicals belonging in majority to the class of flavonoids and polyphenols can represent candidates for antimicrobial and anticancer agents.


2012 ◽  
Vol 11 (10) ◽  
pp. 2193-2201 ◽  
Author(s):  
Aamir Ahmad ◽  
Sanila H. Sarkar ◽  
Bassam Bitar ◽  
Shadan Ali ◽  
Amro Aboukameel ◽  
...  

Elkawnie ◽  
2020 ◽  
Vol 6 (1) ◽  
pp. 48 ◽  
Author(s):  
Vivi Mardina ◽  
Tisna Harmawan ◽  
Halimatussakdiah Halimatussakdiah ◽  
Syafruddin Ilyas ◽  
Masitta Tanjung

Abstract : Sphagneticola trilobata (L.) J.F. Pruski is one of the perennial herbs that is widely used by the national and international community to treat various diseases including cancer. The objective of this study was to assessment the anticancer activity of n-hexane extract of S. trilobata leaves for inhibiting the growth of MCF-7 breast cancer cells in vitro by MTT (microculture tetrazolium salt) method. The n-hexane extract of sernai leaves was obtained from the maceration process of samples that were collected from the Langsa city, Aceh. The cytotoxicity test was carried out by incubating MCF-7 cells which had been exposed to several series of sample levels, viz. 1000; 500; 100; 50; 25; 10; 5 and 1 µg/mL. LC50 values are calculated using probit analysis. The results revealed that the n-hexane extract of S. trilobata leaves was cytotoxic against breast cancer cells (MCF-7) with an LC50 value of  0.037 μg /mL.Abstrak : Sphagneticola trilobata (L.) J.F. Pruski merupakan salah satu tanaman herbal yang digunakan secara luas oleh masyarakat nasional dan internasional untuk mengobati berbagai penyakit termasuk kanker. Penelitian ini bertujuan untuk mengetahui aktivitas antikanker ekstrak n-heksana daun S. trilobata dalam menghambat pertumbuhan sel kanker payudara MCF-7 secara in vitro dengan metode MTT (microculture tetrazolium salt). Ekstrak n-heksana daun sernai diperoleh dari proses maserasi sampel yang dikoleksi dari kota Langsa, Aceh. Uji sitotoksisitas dilakukan dengan menginkubasi sel MCF-7 yang telah dipaparkan beberapa seri  kadar sampel yaitu 1000, 500, 100, 50, 25, 10, 5 dan 1 µg/mL. Nilai LC50 dihitung dengan menggunakan analisa probit. Hasil penelitian menunjukkan bahwa ekstrak n-heksana daun S. trilobata bersifat sitotoksik terhadap sel kanker payudara (MCF-7) dengan harga LC50 sebesar 0,037 µg/mL. 


2021 ◽  
Author(s):  
Saeedeh Ahmadi ◽  
Iman Akbarzadeh ◽  
Mohsen Chiani ◽  
Mahmoud Seraj ◽  
Hassan Noorbazargan ◽  
...  

Abstract This study aimed to improve the anticancer activity of letrozole through a niosomal formulation. Optimized niosomal formulation of letrozole was achieved by response surface methodology (RSM). The niosomes were well-characterized by several methods. The anticancer activity and its mechanism were studied in MCF-7 and MDA-MB-231 breast cancer cells. The release of the drug from the niosomes was according to the Kors Meyer-Peppa kinetic model. The niosomes were stable with high encapsulation efficiency. Significant higher anticancer activity and more induction of apoptosis were obtained for niosomal letrozole. Results indicated that niosomes could be a promising drug carrier for delivery of letrozole to breast cancer cells.


Pharmaceutics ◽  
2020 ◽  
Vol 12 (8) ◽  
pp. 727
Author(s):  
Natalia Sanz del Olmo ◽  
Marcin Holota ◽  
Sylwia Michlewska ◽  
Rafael Gómez ◽  
Paula Ortega ◽  
...  

Cancer treatment with small interfering RNA (siRNA) is one of the most promising new strategies; however, transfection systems that increase its bioavailability and ensure its delivery to the target cell are necessary. Transfection systems may be just vehicular or could contain fragments with anticancer activity that achieves a synergistic effect with siRNA. Cationic carbosilane dendrimers have proved to be powerful tools as non-viral vectors for siRNA in cancer treatment, and their activity might be potentiated by the inclusion of metallic complexes in its dendritic structure. We have herein explored the interaction between Schiff-base carbosilane copper (II) metallodendrimers, and pro-apoptotic siRNAs. The nanocomplexes formed by metallodendrimers and different siRNA have been examined for their zeta potential and size, and by transmission electron microscopy, fluorescence polarisation, circular dichroism, and electrophoresis. The internalisation of dendriplexes has been estimated by flow cytometry and confocal microscopy in a human breast cancer cell line (MCF-7), following the ability of these metallodendrimers to deliver the siRNA into the cell. Finally, in vitro cell viability experiments have indicated effective interactions between Cu (II) dendrimers and pro-apoptotic siRNAs: Mcl-1 and Bcl-2 in breast cancer cells. Combination of the first-generation derivatives with chloride counterions and with siRNA increases the anticancer activity of the dendriplex constructs and makes them a promising non-viral vector.


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