Fabrication of a pH-Responsive 5-FU@MSN-SA Nanoplatform for Anti-Tumor Activity

NANO ◽  
2021 ◽  
Vol 16 (03) ◽  
pp. 2150035
Author(s):  
Wenlong Li ◽  
Weiwei Zhang ◽  
Weihao Jin ◽  
Longbao Zhu ◽  
Wanzhen Li ◽  
...  

Design of high-performance drug delivery system is necessary to improve the anticancer ability of 5-fluorouracil (5-FU). In this work, we developed a pH-responsive 5-FU loaded and sodium alginate (SA) modified mesoporous silica nanoparticles (MSNs) drug delivery system (5-FU@MSN-SA). After 5-FU was loaded into the pores, MSNs were successfully functionalized with amino groups and then capped by sodium alginate. Compared to acidic conditions, the drug release rate in the neutral environment was quite low. Moreover, detailed investigations confirmed that 5-FU@MSN-SA can easily be up-taken by cancer cells and proved the high cytotoxicity to 4T1 cells. The calculated IC[Formula: see text] values for 5-FU and 5-FU@MSN-SA were 34.67[Formula: see text][Formula: see text][Formula: see text]g/mL and 54.95[Formula: see text][Formula: see text][Formula: see text]g/mL, respectively. These results indicated that 5-FU@MSNs-SA can be a promising nanoplatform in cancer therapy.

RSC Advances ◽  
2016 ◽  
Vol 6 (48) ◽  
pp. 42589-42595 ◽  
Author(s):  
W. Li ◽  
X. N. Tan ◽  
T. Luo ◽  
X. Huang ◽  
Q. Wang ◽  
...  

A novel nanofibrous membrane, which contains chitosan/sodium alginate nanocapsules constructed by vesicle systems, has been fabricated via an electrospinning process as a drug-delivery system.


2021 ◽  
Vol 8 (4) ◽  
Author(s):  
Mingwei He ◽  
Zainen Qin ◽  
Xiaonan Liang ◽  
Xixi He ◽  
Bikang Zhu ◽  
...  

Abstract Andrographolide (AG) has favorable anti-inflammatory and antioxidative capacity. However, it has low bioavailability due to high lipophilicity and can be easily cleared by the synovial fluid after intra-articular injection, leading to low therapeutic efficiency in osteoarthritis (OA). Herein, we designed a nano-sized pH-responsive drug delivery system (DDS) for OA treatment by using modified mesoporous silica nanoparticles (MSNs) with pH-responsive polyacrylic acid (PAA) for loading of AG to form AG@MSNs-PAA nanoplatform. The nanoparticles have uniform size (∼120 nm), high drug loading efficiency (22.38 ± 0.71%) and pH-responsive properties, beneficial to sustained release in OA environment. Compared with AG, AG@MSNs-PAA showed enhanced antiarthritic efficacy and chondro-protective capacity based on IL-1β-stimulated chondrocytes and anterior cruciate ligament transection-induced rat OA model, as demonstrated by lower expression of inflammatory factors and better prevention of proteoglycan loss. Therefore, the AG@MSNs-PAA nanoplatform may be developed as a promising OA-specific and on-demand DDS.


Blood ◽  
2011 ◽  
Vol 118 (21) ◽  
pp. 3479-3479 ◽  
Author(s):  
Hai-jun Zhang ◽  
Bao-An Chen

Abstract Abstract 3479 Daunorubicin (DNR) with a broad spectrum of anti-tumor activity is limited due to the serious side-effects in the clinical application. The aim of this study was to explore the novel pH-responsive drug delivery system (DDS) based on titanium dioxide (TiO2) nanoparticles (Nps) for its potential roles to enable more intelligently controlled release, enhance chemotherapeutic efficiency, and reduce the side-effects of DNR. DNR was loaded onto the TiO2 Nps by forming (six-membered chelate) complexes with transition metal Ti to contract DNR-TiO2 nanocomposites as DDS. The encapsulation efficiency and loading efficiency of DNR loaded TiO2 Nps were assessed and calculated as 65.46±6.82% and 20.63±3.55%, respectively.The DNR was released from the DDS much more rapidly at pH 5.0 and 6.0 than at pH 7.4. The release behavior is a desirable characteristic for tumor-targeted drug delivery. Most DNR will remain in the carrier for a considerable time period at normal physiological conditions (pH 7.4), indicating the potential for the prolonged DNR retention time in the blood circulation and thereby greatly reducing the side effects to the normal tissues. On the other hand, once the DNR loaded TiO2 Nps are taken up by tumor cells via endocytotic process, a faster release may occur at lower local pH, i.e, inside the endosome and lysosome of cancer cells ((pH 4.5∼6.5), leading to the significant improvement in cancer treatment efficacy. The DNR- TiO2 nanocomposites as DDS induced the remarkable improvement in the anti-tumor activity, which were demonstrated by the flow cytometry, MTT assay and nuclear DAPI staining. Furthermore, the possible signaling pathway was explored by Western blot. For instance, in human leukemia cells (K562 cells), our observations demonstrated that the DDS could obviously increase the intracellular concentration of DNR and enhance its potential anti-tumor efficiency through inducing apoptosis in a caspase-dependent manner, indicating that DNR-TiO2 nanocomposites could act as an efficient DDS importing DNR into target cancer cells. These findings revealed that such ‘smart' DNR delivery strategy represent a promising approach in hematologic malignancy therapy. Disclosures: No relevant conflicts of interest to declare.


2015 ◽  
Vol 3 (23) ◽  
pp. 4707-4714 ◽  
Author(s):  
Xuemei Yao ◽  
Xiaofei Chen ◽  
Chaoliang He ◽  
Li Chen ◽  
Xuesi Chen

By metallo-supramolecular coordinated interaction between Zn-Por and histidine, a dual pH-responsive mesoporous silica nanoparticle (MSN)-based drug delivery system has been fabricated for synergistic chemo-photodynamic therapy.


RSC Advances ◽  
2021 ◽  
Vol 11 (5) ◽  
pp. 2656-2663
Author(s):  
Boye Zhang ◽  
Qianqian Duan ◽  
Yi Li ◽  
Jianming Wang ◽  
Wendong Zhang ◽  
...  

The system is pH-responsive and redox-controlled release. And the charge reversal and size transitions of the system can enhance the targeted ability. Moreover, the system can recognize the cancer cells by the fluorescence imaging.


Pharmaceutics ◽  
2021 ◽  
Vol 13 (5) ◽  
pp. 619
Author(s):  
Krisztián Pamlényi ◽  
Katalin Kristó ◽  
Orsolya Jójárt-Laczkovich ◽  
Géza Regdon

Currently, pharmaceutical companies are working on innovative methods, processes and products. Oral mucoadhesive systems, such as tablets, gels, and polymer films, are among these possible products. Oral mucoadhesive systems possess many advantages, including the possibility to be applied in swallowing problems. The present study focused on formulating buccal mucoadhesive polymer films and investigating the physical and physical–chemical properties of films. Sodium alginate (SA) and hydroxypropyl methylcellulose (HPMC) were used as film-forming agents, glycerol (GLY) was added as a plasticizer, and cetirizine dihydrochloride (CTZ) was used as an active pharmaceutical ingredient (API). The polymer films were prepared at room temperature with the solvent casting method by mixed two-level and three-level factorial designs. The thickness, tensile strength (hardness), mucoadhesivity, surface free energy (SFE), FTIR, and Raman spectra, as well as the dissolution of the prepared films, were investigated. The investigations showed that GLY can reduce the mucoadhesivity of films, and CTZ can increase the tensile strength of films. The distribution of CTZ proved to be homogeneous in the films. The API could dissolve completely from all the films. We can conclude that polymer films with 1% and 3% GLY concentrations are appropriate to be formulated for application on the buccal mucosa as a drug delivery system.


2021 ◽  
pp. 150011
Author(s):  
Eva Benova ◽  
Virginie Hornebecq ◽  
Vladimír Zelenak ◽  
Veronika Huntosova ◽  
Miroslav Almasi ◽  
...  

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