scholarly journals Copolymer Involving 2-Hydroxyethyl Methacrylate and 2-Chloroquinyl Methacrylate: Synthesis, Characterization and In Vitro 2-Hydroxychloroquine Delivery Application

Polymers ◽  
2021 ◽  
Vol 13 (23) ◽  
pp. 4072
Author(s):  
Abeer Aljubailah ◽  
Wafa Nazzal Odis Alharbi ◽  
Ahmed S. Haidyrah ◽  
Tahani Saad Al-Garni ◽  
Waseem Sharaf Saeed ◽  
...  

The Poly(2-chloroquinyl methacrylate-co-2-hydroxyethyl methacrylate) (CQMA-co-HEMA) drug carrier system was prepared with different compositions through a free-radical copolymerization route involving 2-chloroquinyl methacrylate (CQMA) and 2-hydroxyethyl methacrylate) (HEMA) using azobisisobutyronitrile as the initiator. 2-Chloroquinyl methacrylate monomer (CQMA) was synthesized from 2-hydroxychloroquine (HCQ) and methacryloyl chloride by an esterification reaction using triethylenetetramine as the catalyst. The structure of the CQMA and CQMA-co-HEMA copolymers was confirmed by a CHN elementary analysis, Fourier transform infra-red (FTIR) and nuclear magnetic resonance (NMR) analysis. The absence of residual aggregates of HCQ or HCQMA particles in the copolymers prepared was confirmed by a differential scanning calorimeter (DSC) and XR-diffraction (XRD) analyses. The gingival epithelial cancer cell line (Ca9-22) toxicity examined by a lactate dehydrogenase (LDH) assay revealed that the grafting of HCQ onto PHEMA slightly affected (4.2–9.5%) the viability of the polymer carrier. The cell adhesion and growth on the CQMA-co-HEMA drug carrier specimens carried out by the (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) (MTT) assay revealed the best performance with the specimen containing 3.96 wt% HCQ. The diffusion of HCQ through the polymer matrix obeyed the Fickian model. The solubility of HCQ in different media was improved, in which more than 5.22 times of the solubility of HCQ powder in water was obtained. According to Belzer, the in vitro HCQ dynamic release revealed the best performance with the drug carrier system containing 4.70 wt% CQMA.

Polymers ◽  
2019 ◽  
Vol 11 (3) ◽  
pp. 439 ◽  
Author(s):  
Abdulaziz Ali Alghamdi ◽  
Waseem Sharaf Saeed ◽  
Abdel-Basit Al-Odayni ◽  
Fahad A. Alharthi ◽  
Abdelhabib Semlali ◽  
...  

The release dynamics of aspirin(ASP), used as a drug model, from the poly(ethylene-co-vinyl alcohol)/poly(δ-valerolactone) (PE-co-VAL/Pδ-VL) hydrogel blend was controlled by varying the blend’s degree of swelling through a gradual loading of Pδ-VL (hydrophobic polymer) in this copolymer matrix. To achieve this goal, a series of PE-co-VAL/Pδ-VL blends with different ratios was prepared through the solvent casting method, and the miscibility of this polymer blend was evaluated by using Fourier transform infrared spectroscopy, differential scanning calorimetry, X-ray diffraction, and scanning electronic microscopy methods. The tests of cell adhesion and growth on the PE-co-VAL/Pδ-VL specimens were performed using the 3-(4,5-demethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) method and the results obtained were the best performance in terms of cell viability, cell adhesion, and growth of the PE-co-VAL/Pδ-VL50 material. The dynamic mechanical properties of the prepared material were also examined by dynamic mechanical analysis; the results obtained showed a material having intermediary mechanical properties between those of the two components. On the basis of these characterizations, the blend showing the best performance, such as the PE-co-VAL/Pδ-VL50 system, was chosen as a carrier to study the in vitro control of the release dynamics of ASP from the ASP/PE-co-VAL/Pδ-VL drug-carrier system when administered orally, in which the influences of the ASP content and the degree of swelling of the PE-co-VAL/Pδ-VL blend were investigated. Based on the data obtained and the gastrointestinal transit time reported by Beltzer et al., it was possible to estimate the distribution of the in vitro cumulative ASP released in different digestive system organs regardless of the actions of any enzymes and microorganisms and select the best-performing drug-carrier system.


2018 ◽  
Vol 21 (1) ◽  
pp. 145-162 ◽  
Author(s):  
Abdulaziz Ali Alghamdi ◽  
Abdulellah Alsolami ◽  
Waseem Sharaf Saeed ◽  
Abdel-Basit Mohammed Al-Odayni ◽  
Abdelhabib Semlali ◽  
...  

2021 ◽  
Vol 9 (9) ◽  
pp. 2233-2239
Author(s):  
Adrià Botet-Carreras ◽  
Cristina Tamames-Tabar ◽  
Fabrice Salles ◽  
Sara Rojas ◽  
Edurne Imbuluzqueta ◽  
...  

Despite the interesting chemopreventive, antioxidant and antiangiogenic effects of the natural bioflavonoid genistein (GEN), its low aqueous solubility and bioavailability make it necessary to administer it using a suitable drug carrier system.


Molecules ◽  
2020 ◽  
Vol 25 (5) ◽  
pp. 1110
Author(s):  
Nanyak Galam ◽  
Pinar Tulay ◽  
Terin Adali

Breast cancer ranks as the fifth leading cause of death worldwide. Chemotherapy is commonly used directly or as neo-adjuvant therapy for the management of breast cancer with its attendant adverse effects, underscoring the need to develop biocompatible bioactive compounds for pharmacological applications. The aim of this study is to encapsulate carboplatin (CP) with silk fibroin protein (SF) by using an ionic gelation method as a drug carrier system and assess the apoptotic effect on MCF-7 breast cancer cells during in vitro studies. The characterization of silk fibroin encapsulated carboplatin (SFCP) microparticles was analyzed by FTIR spectrophotometer, SEM, Mastersizer, and biodegradation methods. The encapsulation efficiency and release profile of SFCP microparticles were analyzed by an indirect UV–Vis spectrophotometric method. An apoptotic screening of MCF-7 cells was carried out with 10–200 µg/mL CP loaded SFCP, which were cultured for 24, 48, and 72 h. Data were analyzed using the Student’s t test and analysis of variance. FTIR and drug release studies confirmed an interaction of silk fibroin with the carboplatin moiety. SFCP showed successful encapsulation of the carboplatin moiety. Apoptotic screening showed a dose dependent increase in absorbance, indicating significant cell death (p < 0.05). Thus, the direct apoptotic effect of SFCP microparticles on MCF-7 was confirmed.


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