scholarly journals Formulation of Genistein-HP β Cyclodextrin-Poloxamer 188 Ternary Inclusion Complex: Solubility to Cytotoxicity Assessment

Pharmaceutics ◽  
2021 ◽  
Vol 13 (12) ◽  
pp. 1997
Author(s):  
Ameeduzzafar Zafar ◽  
Nabil K. Alruwaili ◽  
Syed Sarim Imam ◽  
Omar Awad Alsaidan ◽  
Faisal K. Alkholifi ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Inclusion Complex ◽  
Ternary Complex ◽  
Poloxamer 188 ◽  
Dissolution Study ◽  
Antimicrobial Studies ◽  
Binary Complexes ◽  
Cytotoxicity Studies ◽  
Study Results ◽  
Antioxidant And Antimicrobial Activity

The current study was designed to prepare the inclusion complex Genistein (GS) using Hydroxypropyl β cyclodextrin (HP β CD) and poloxamer 188 (PL 188). The binary inclusion complex (GS BC) and ternary inclusion complex (GS TC) were developed by microwave irradiation technique and evaluated for a comparative dissolution study. Further, the samples were assessed for FTIR, DSC, XRD, and NMR for the confirmation of complex formation. Finally, antioxidant and antimicrobial studies and cytotoxicity studies on a breast cancer (MCF-7) cell line were conducted. The dissolution study result showed a marked increment in GS dissolution/release after incorporation in binary (GS: HP β CD, 1:1) and ternary (GS: HP β CD: PL 188; 1:1:0.5) inclusion complexes. Moreover, the ternary complex exhibited a significant enhancement (p < 0.05) in dissolution than did the binary complexes. This might be due to the presence of PL 188, which helps in solubility enhancement of GS. DSC, XRD and SEM evaluation confirmed the modification in the structure of GS. FTIR and NMR results indicated the formation of an inclusion complex. The antioxidant and antimicrobial activity results revealed that GS TC has shown significant (p < 0.05) higher activity than pure GS. The cytotoxicity study results also depicted concentration-dependent cytotoxicity. GS TC exhibited significantly (p < 0.05) high cytotoxicity to cancer cells (IC50 = 225 µg/mL) than pure GS (IC50 = 480 µg/mL). Finally, it was concluded that a remarkable enhancement in the dissolution was observed after the inclusion of GS in the ternary complex and it therefore has significant potential for the treatment of breast cancer.

Equilibrium Studies of Binary and Ternary Complexes of Palladium(II) Involving Amino Acids

1993 ◽  
Vol 58 (5) ◽  
pp. 1103-1108 ◽  
Author(s):  
Mohamed M. Shoukry ◽  
Eman M. Shoukry
Keyword(s):  
Amino Acids ◽  
Relative Stability ◽  
Ternary Complex ◽  
Formation Constants ◽  
Ternary Complexes ◽  
Conductivity Measurements ◽  
Equilibrium Studies ◽  
Binary And Ternary Complexes ◽  
Binary Complexes

The formation constants of the binary and ternary complexes of palladium(II) with diethylenetriamine and amino acids as ligands have been determined potentiometrically at 25 °C in 0.1 M NaNO3 solution. The relative stability of each ternary complex was compared with that of the corresponding binary complexes in terms of ∆logK values. The mode of chelation was ascertained by conductivity measurements.

scholarly journals Relationship of mammographic densities to breast cancer risk

2021 ◽  
Vol 52 (1) ◽  
Author(s):  
Engy A. Ali ◽  
Mariam Raafat
Keyword(s):  
Breast Cancer ◽  
Breast Density ◽  
Statistical Significance ◽  
Significant Risk ◽  
Close Relation ◽  
Mammographic Screening ◽  
Mammographic Breast Density ◽  
Study Results ◽  
Relationship Of ◽  
Mammographic Densities

Abstract Background Our goal was to find out the relation between mammographic densities and cancer of the breast according to the recent ACR classification. From the medical records of Kasereliny Hospital, 49,409 women were subjected to digital mammography for screening, of which 1500 breast cancer cases were collected. The mammographic categories of breast density were ACR-A, B, C, and D, which were detected by two senior radiologists. All radiological classifications were made using both standard mammographic views bilaterally. Two-sided tests of statistical significance were represented by all the P values. Results From 2014 to 2019, 49,409 women came for digital mammographic screening, their age ranges between 40 and 65, and all of them are included in the study. One thousand cases of breast cancer cases were radiologically and pathologically diagnosed. Different densities were arranged in descending pattern depending on the frequency of positive cases: D (13.7%), C (3.3%), B (2.7%), A (2.2%). There is positive significant risk ratio among every higher mammographic density in comparison to the lower density. Conclusion Our study results show that the risk of breast cancer is in close relation to the mammographic breast density.

The value of tumor-infiltrating lymphocytes and CD8 expression as a predictor of response to anthracycline-based neoadjuvant chemotherapy in invasive breast carcinoma of no special type

2021 ◽  
pp. 1-6
Author(s):  
Upik A. Miskad ◽  
Rizki A. Rifai ◽  
Rina Masadah ◽  
Berti Nelwan ◽  
Djumadi Ahmad ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Immune System ◽  
Breast Carcinoma ◽  
Neoadjuvant Chemotherapy ◽  
Predictive Value ◽  
Disease Free Survival ◽  
Tumor Infiltrating Lymphocytes ◽  
Invasive Breast Carcinoma ◽  
Study Results ◽  
Infiltrating Lymphocytes

BACKGROUND: The immune system is known to play an important role in tumor cell eradication. Although cancer cells were able to escape from the immune system, many studies showed mononuclear inflammatory cell infiltrates known as tumor-infiltrating lymphocytes (TILs) on breast cancer histopathology specimens showed better prognosis, including in disease-free survival (DFS) and chemotherapy responses. OBJECTIVE: This study aimed to reveal the predictive value of tumor-infiltrating lymphocytes (TILs) levels and CD8 expression in invasive breast carcinoma of no special type patients’ samples on response to anthracycline-based neoadjuvant chemotherapy. METHODS: 75 pre-treatment biopsy samples that were diagnosed as invasive breast carcinoma of no special type were evaluated. TILs level determined following recommendations of International TILs Working Group 2014, CD8 expression assessed semiquantitatively after immunohistochemistry staining. Response to anthracycline-based neoadjuvant chemotherapy evaluated clinically using Response Evaluation Criteria in Solid Tumours (RECIST) criteria and pathologically by evaluating hematoxylin and eosin (H&E)-stained slides from mastectomy specimens after 3 or 4 cycles of neoadjuvant chemotherapy. RESULTS: Chi-squared analysis showed a significant relationship between TILs level and CD8 expression with chemotherapy responses clinically (p = 0.011 and p = 0.017 respectively) but not pathologically. Furthermore, the logistic regression test exhibit the predictive value of TILs level was 66.7% and CD8 expression was 64%. CONCLUSIONS: This study results suggest that TILs level and CD8 expression may be added as predictive factors to the response of anthracycline-based neoadjuvant chemotherapy, and oncologists may take benefit in breast cancer patient’s management.

scholarly journals Formulation of Piperine–Chitosan-Coated Liposomes: Characterization and In Vitro Cytotoxic Evaluation

Molecules ◽  
2021 ◽  
Vol 26 (11) ◽  
pp. 3281
Author(s):  
Syed Sarim Imam ◽  
Sultan Alshehri ◽  
Mohammad A. Altamimi ◽  
Afzal Hussain ◽  
Wajhul Qamar ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Cell Line ◽  
Cancer Cell ◽  
Breast Cancer Cell ◽  
Breast Cancer Cell Line ◽  
Therapeutic Efficacy ◽  
Cancer Cell Line ◽  
Permeation Study ◽  
Study Results

The present research work is designed to prepare and evaluate piperine liposomes and piperine–chitosan-coated liposomes for oral delivery. Piperine (PPN) is a water-insoluble bioactive compound used for different diseases. The prepared formulations were evaluated for physicochemical study, mucoadhesive study, permeation study and in vitro cytotoxic study using the MCF7 breast cancer cell line. Piperine-loaded liposomes (PLF) were prepared by the thin-film evaporation method. The selected liposomes were coated with chitosan (PLFC) by electrostatic deposition to enhance the mucoadhesive property and in vitro therapeutic efficacy. Based on the findings of the study, the prepared PPN liposomes (PLF3) and chitosan coated PPN liposomes (PLF3C1) showed a nanometric size range of 165.7 ± 7.4 to 243.4 ± 7.5, a narrow polydispersity index (>0.3) and zeta potential (−7.1 to 29.8 mV). The average encapsulation efficiency was found to be between 60 and 80% for all prepared formulations. The drug release and permeation study profile showed biphasic release behavior and enhanced PPN permeation. The in vitro antioxidant study results showed a comparable antioxidant activity with pure PPN. The anticancer study depicted that the cell viability assay of tested PLF3C2 has significantly (p < 0.001)) reduced the IC50 when compared with pure PPN. The study revealed that oral chitosan-coated liposomes are a promising delivery system for the PPN and can increase the therapeutic efficacy against the breast cancer cell line.

scholarly journals Breast cancer drug delivery by novel drug-loaded chitosan-coated magnetic nanoparticles

2021 ◽  
Vol 12 (1) ◽  
Author(s):  
A. Taherian ◽  
N. Esfandiari ◽  
S. Rouhani
Keyword(s):  
Breast Cancer ◽  
Magnetic Nanoparticles ◽  
Free Drug ◽  
Pomegranate Peel ◽  
Vast Number ◽  
Therapeutic Method ◽  
Cytotoxicity Studies ◽  
Pomegranate Peel Extract ◽  
Novel Drug ◽  
Peel Extract

Abstract Background Breast cancer is one of the most challenging cancers among women which is considered one of the most lethal cancers to this date. From the time that cancer has been discovered, finding the best therapeutic method is still an ongoing process. As a novel therapeutic method, nanomedicine has brought a vast number of materials that could versatilely be used as a drug carrier. The purpose of this study is to develop a novel black pomegranate peel extract loaded with chitosan-coated magnetic nanoparticles to treat breast cancer cells. Results The morphology and size distribution of the nanoparticles studied by dynamic light scattering, atomic force microscopy, scanning, and transitional electron microscopy showed the spherical shape of the nanoparticles and their promising size range. Studies by Fourier transform infrared spectroscopy, X-ray diffraction, vibrating sample magnetometer, and zeta sizer confirmed the synthesis, substantial crystallinity, magnetic potential of the nanoparticles, and their satisfactory stability. The DPPH assay revealed that the obtained black pomegranate peel extract has 60% free radical scavenging activity. The cytotoxicity studies by MTT and LDH assay carried out on NIH/3T3, MBA-MB-231, and 4T1 cells confirmed that the magnetic nanoparticles had no significant cytotoxicity on the cells. However, the drug-loaded nanoparticles could significantly eradicate cancerous cells which had more efficiency comparing to free drug. Furthermore, free drug and drug-loaded nanoparticles had no toxic effect on normal cells. Conclusion Owing to the results achieved from this study, the novel drug-loaded nanoparticles are compatible to be used for breast cancer treatment and could potentially be used for further in vivo studies.

scholarly journals Treatment of early-stage breast cancer with percutaneous thermal ablation, an open-label randomised phase 2 screening trial: rationale and design of the THERMAC trial

BMJ Open ◽  
2021 ◽  
Vol 11 (9) ◽  
pp. e052992
Author(s):  
Elles M F van de Voort ◽  
Gerson M Struik ◽  
Linetta B Koppert ◽  
Adriaan Moelker ◽  
Reno Debets ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Thermal Ablation ◽  
Surgical Excision ◽  
Maximum Diameter ◽  
Phase 2 ◽  
Open Label ◽  
Phase 3 ◽  
Complete Ablation ◽  
Study Results ◽  
Screening Trial

IntroductionBreast cancer is the most frequently diagnosed malignancy worldwide but almost half of the patients have an excellent prognosis with a 5-year survival rate of 98%–99%. These patients could potentially be treated with thermal ablation to avoid surgical excision, reduce treatment-related morbidity and increase patients’ quality of life without jeopardising treatment effectiveness. Previous studies showed highest complete ablation rates for radiofrequency, microwave and cryoablation. However, due to heterogeneity among studies, it is unknown which of these three techniques should be selected for a phase 3 comparative study.Methods and analysisThe aim of this phase 2 screening trial is to determine the efficacy rate of radiofrequency, microwave and cryoablation with the intention to select one treatment for further testing in a phase 3 trial. Additionally, exploratory data are obtained for the phase 3 trial. The design is a multicentre open-label randomised phase 2 screening trial. Patients with unifocal, invasive breast cancer with a maximum diameter of 2 cm without lymph node or distant metastases are included. Triple negative, Bloom-Richardson grade 3 tumours and patients with an indication for neoadjuvant chemotherapy will be excluded. Included patients will be allocated to receive one of the three thermal ablation techniques. Three months later surgical excision will be performed to determine the efficacy of thermal ablation. Treatment efficacy in terms of complete ablation rate will be assessed with CK 8/18 and H&E staining. Secondary outcomes include feasibility of the techniques in an outpatient setting, accuracy of MRI for complete ablation, patient satisfaction, adverse events, side effects, cosmetic outcome, system usability and immune response.Ethics and disseminationThis study protocol was approved by Medical Research Ethics Committee of the Erasmus Medical Center, Rotterdam, the Netherlands. Study results will be submitted for publication in peer-reviewed journals.Trial registration numberNL9205 (www.trialregister.nl); Pre-results.

scholarly journals A Comparison Between Core Biopsy and Imaging Techniques (Ultrasound and Mammography) In diagnosis of Breast Cancer in Slemani Breast Center

2018 ◽  
Vol 3 (1) ◽  
pp. 34-39
Author(s):  
Taher Abdullah Hawramy ◽  
Dara Ahmed Mohammed ◽  
Hasan Abdullah Ahmed
Keyword(s):  
Breast Cancer ◽  
Core Needle Biopsy ◽  
Needle Biopsy ◽  
Core Biopsy ◽  
Imaging Techniques ◽  
Breast Cancers ◽  
Radiological Investigation ◽  
Core Needle ◽  
Breast Center ◽  
Study Results

Breast cancer is the global health problem. It is the highest prevalent site-specific cancer in women throughout the world and the most common reason of death in middle age women,  following lung cancer. Up to 5% of breast cancers are caused by inheritance. Male breast cancer accounts for less than 1%. Mammography is the first imaging study to evaluate breast abnormalities, Ultrasound is particularly useful in young women with dense breasts. Core needle biopsy permits the analysis of breast tissue architecture and whether invasive cancer is present. To compare core needle biopsy and imaging, the accuracy of each modality for purpose of the diagnosis and their impact on preoperative planning before surgical treatment. A retrospective cohort study was performed in 70 cases of breast cancer during 2015-2017 at Slemani Breast Center/ Kurdistan region. Inclusion criteria any patient with diagnosed with breast cancer for whom core biopsy and imaging techniques (ultrasound and mammography) were done, Age 25 years and above. Exclusion criteria, a patient with breast mass who did not underwent: one of the two modalities, Age below 25 years, pregnant women. In the current study: mean age/year for the  participants were Mean age = 51.34 year ± 12.85 SD), Sixty-nine cases were female and one male. By core biopsy (97.1%) is positive for malignancy. In this study: results about 34.28% of BIRADS V (ultrasound)lesions proved to be positive for malignancy by core biopsy, 1.43% of BIRADS V were negative for malignancy and the association was statistically highly significant, for BIRADS III lesions 17.14% were proved as positive for malignancy by core biopsy. About 45.7% of BIRADS V (mammography were positive for malignancy by core biopsy and the associations were found to be statistically highly significant and for BIRADS III 12.85% of lesions were positive for malignancy by core biopsy. There was a statistically significant association between radiological investigation(ultrasound, mammography) and histopathological finding (core biopsy).  

scholarly journals Functionalization of 3-chloroformylcoumarin to coumarin Schiff bases using reusable catalyst: an approach to molecular docking and biological studies

2018 ◽  
Vol 5 (5) ◽  
pp. 172416 ◽  
Author(s):  
Suresh S. Kumbar ◽  
Kallappa M. Hosamani ◽  
Gangadhar C. Gouripur ◽  
Shrinivas D. Joshi
Keyword(s):  
Molecular Docking ◽  
Heterogeneous Catalysts ◽  
Vero Cells ◽  
Reusable Catalyst ◽  
Subsequent Investigation ◽  
Antimicrobial Studies ◽  
Cytotoxicity Studies ◽  
Biological Studies ◽  
Simplified Procedure

Recently, heterogeneous catalysts have been explored eximiously in the synthesis of heterocyclic compounds. Therefore, here we used solid-supported heterogeneous silica sulfuric acid as a catalyst for the synthesis of Schiff's base of 3-chloroformylcoumarin in view of simplified procedure, reusability and acceptable efficiency, which are required in organic synthesis. An efficient and facile methodology is preferred for synthesis of a class of chromeno-3-substituted derivatives ( 1a–1l ) with good yields. The molecular docking results showed excellent binding interactions with the Mycobacterium tuberculosis InhA-D148G mutant (PDB: 4DQU). The same biomolecules were screened for their in vitro anti-tubercular activity against the M.tb H37Rv strain and antimicrobial studies. Physico-chemistry, toxicity prediction with IC50 value and bioactivity score were also calculated for title compounds. Most active compounds were further tested for cytotoxicity studies and exhibited low-level cytotoxicity against Vero cells. The suggested conjugates are promising lead compounds for the subsequent investigation in search of new anti-tubercular agents. All the conjugates were obtained within the range and followed the Lipinski rule of 5, indicating more ‘drug-like’ nature.

EFFECT OF DRUG TO B-CYCLODEXTRIN RATIO AND METHOD OF COMPLEXATION IN THE DEVELOPMENT OF B-CYCLODEXTRIN INCLUSION COMPLEX OF OFLOXACIN

INDIAN DRUGS ◽  
2013 ◽  
Vol 50 (12) ◽  
pp. 34-40
Author(s):  
M Panchpuri ◽  
◽  
D Singh ◽  
A Semalty ◽  
M. Semalty
Keyword(s):  
Inclusion Complex ◽  
In Vitro Dissolution ◽  
Molar Ratio ◽  
Dissolution Profile ◽  
Scanning Calorimetry ◽  
Dissolution Study ◽  
Drug Content ◽  
Kneading Method ◽  
Made In

Ofloxacin, a second generation fluoroquinolone, shows poor aqueous solubility and dissolution profile. Thus, ofloxacin–β-cyclodextrin complexes were prepared to improve its dissolution by imparting an environment of improved hydrophilicity. Ofloxacin was complexed with β-cyclodextrin (in 1:1 and 1:2 molar ratio) by two different methods namely, solvent evaporation and kneading method. These inclusion complexes were evaluated for solubility, drug content, scanning electron microscopy (SEM), differential scanning calorimetry (DSC), X ray powder diffraction (XRPD) and in vitro dissolution study. The highest drug content (35.45%) was found in complex made by kneading method (OK1:1) in 1:1 molar ratio. All the complexes OSE1:1, OSE1:2, OK1:1, OK1:2 were found to be showing rough and porous surface morphology in SEM. Solubility as well as the dissolution of the complexes was found to be improved. Complex prepared by kneading method in 1:1 molar ratio (OK1:1) showed a marked improvement in percent drug release (88.94%) than that of pure drug (54.22%) at the end of 1 hour in dissolution study. FTIR, DSC and XRPD data confirmed the formation of inclusion complex. It was concluded that the complex made in 1:1 molar ratio (irrespective of the method) showed better solubility and dissolution profile as compared to complex made in 1:2 molar ratio.

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