One Pot Doxorubicin Partitioning and Encapsulation on Silica Nanoparticle, Applying Aqueous Two Phase System for Preparation of pH-Responsive Nanocarriers

Author(s):  
Mojhdeh Baghbanbashi ◽  
Gholamreza Pazuki ◽  
Sepideh Khoee

Abstract Providing an efficient system for drug delivery and chemotherapy has always been an important issue. Modification of the surface of silica nanoparticles (SiO2) provides an opportunity for achieving stimulus-sensitive drug delivery system. Here, we have modified the surface of SiO2 using hydrogen bonding interactions by employing an aqueous two-phase system (ATPS) based on polyethylene glycol and lysine. This novel biocompatible ATPS provides an environment for simultaneous drug encapsulation, SiO2 modification, and drug partitioning in one pot. Addition of SiO2 to ATPS increased the partitioning of doxorubicin (DOX) as an anti-cancer drug from 47.92 in the absence of nanoparticles to 92.33 due to the interactions between drug and nanoparticles. The formation of nanoformulation and its characteristics were investigated applying microscopy, spectroscopy and thermal analysis. Drug release study demonstrated that DOX is loaded on nanoformulations efficiently with an encapsulation efficiency of 63.84% and shows lower release in physiological environment compared to the unmodified nanoparticles. While in acidic conditions of pH 5.5, significant increase was observed in the release profile. MTT assay on MCF-7 cancer cells confirmed that the nanoformulations were non-toxic and DOX-loaded nanocarrier showed anti-cancer behavior. These results indicate that the prepared nanoformulations are promising nanocarriers for controlled drug release purposes.

2020 ◽  
Author(s):  
Barbara Souza ◽  
Jin-Chong Tan

We report two solvent-free mechanochemical methods to achieve one‑pot encapsulation of anti-cancer drug 5‑Fluorouracil (5‑FU) in the iron-based MIL‑100 metal-organic framework (MOF). We compare the structural and physicochemical properties of drug@MIL‑100 systems derived from <i>in situ </i>manual and vortex grinding, where the former exhibits a slower drug release due to stronger guest-host interactions.


2014 ◽  
Vol 2 (10) ◽  
pp. 1327-1334 ◽  
Author(s):  
Guofang Chen ◽  
Ruoyao Chen ◽  
Chunxiao Zou ◽  
Danwen Yang ◽  
Zhe-Sheng Chen

Fragmented polymer nanotubes with a thermo-responsive gating system were prepared by a 2-fold “grafting-from” strategy and sonication-induced scission for efficient drug delivery. In vitro thermo-responsive DOX drug release and chemotoxicity were testified with such nanocarriers.


2018 ◽  
Vol 127 ◽  
pp. 177-182 ◽  
Author(s):  
Xunan Zhang ◽  
Wei Zong ◽  
Hongmei Bi ◽  
Kunming Zhao ◽  
Thomas Fuhs ◽  
...  

2012 ◽  
Vol 600 ◽  
pp. 137-143
Author(s):  
Jing Hui ◽  
Xiao Jie Yu ◽  
Yue Zhang ◽  
Feng Qing Hu

Poly (3-hydroxybutyrate-co-3-hydroxyhexanoate) (PHBHHx) is one of the components of polyhydroxyalkanoates (PHAs) and some of its mechanical properties have been shown to improve over poly (3-hydroxybutyrate) (PHB) and poly (3-hydroxybutyrate-co-3-hydroxyvalerate) (PHBV). The investigation of PHBHHx microspheres as a drug delivery system was prepared by emulsion-solvent evaporation method for the sustained release of anti-cancer drug 5-fluorouracil (5-FU) and cyclosporin A (CsA). The mean diameter of the PHBHHx microspheres ranged from 5.24 to 22.10 μm dependent on the different processing parameters. The PHBHHx concentration, emulsifier concentration, anti-cancer drug dosage, and agitation speed, were optimized according to the encapsulation efficiency of 4% PHBHHx, 0.5% SDS, 10 mg anti-cancer drug, and 500 rpm. Under optimized conditions, the encapsulation efficiency of 5-FU and CsA microspheres were 7.19% and 96.44%, respectively. The morphologies of scanning electron microscope (SEM) suggested that PHBHHx microspheres were relatively smooth that provided better dispersion compared to PHB microspheres. The in vitro release profiles indicated 32.42% of 5-FU and 30.61% of CsA were released from PHBHHx microspheres during the initial burst phase, and the drug release from PHBHHx microsphere could be detected even after one month. The characteristics of PHBHHx microspheres demonstrated the feasibility of PHBHHx microsphere as a novel matrix for drug release system. With positive maintenance of the therapeutic concentrations of the drug, side effects can be reduced and patient compliance can be improved.


2019 ◽  
Vol 23 (1) ◽  
Author(s):  
Seong Hoon Choi ◽  
Il-Hoon Cho ◽  
Sangsoo Park

Abstract Background Local delivery of anti-cancer drugs through a stent is a very promising and anticipated treatment modality for patients who have obstructions in their gastrointestinal tract with malignant tumors. Anticancer drug release via stents, however, needs to be optimized with respect to drug delivery behavior for the stents to be effective for prolonged containment of tumor proliferation and stent re-obstruction. Local stent-based drug delivery has been tested using an effective anti-cancer drug, gemcitabine, but the release from the stent-coated polyurethane films is often too fast and the drug is depleted from the coated film virtually in a day. Methods To moderate the drug release from a polyurethane film, a gemcitabine-incorporated polyurethane film was enveloped with a pure polyurethane film, with no drug loading, and with a silicone film by solution casting after activation of the silicone film surface with plasma treatment. Results The pure polyurethane barrier film was effective; the interface of the two were indistinguishable on scanning electron microscopy, and the initial burst, i.e., the cumulative release in a day, decreased from 90 to 26%. The silicone film barrier, on the other hand, was defective as voids were seen using a scanning electron microscope, and micro-separation of the two layers was observed after the film was immersed in phosphate-buffered saline for 1 day during the in vitro drug release study. Conclusions Enveloping a gemcitabine-releasing polyurethane film with a homo-polymer barrier film was quite effective for moderating the initial burst of gemcitabine, thus, prolonging the release time of the drug. Enveloping the polyurethane film with a silicone film was also possible after plasma treatment of the silicone film surface, but the two films eventually separated in the aqueous environment. More studies are needed to tune the drug release behavior of gemcitabine from the stent covering film before attempting a clinical application of an anti-cancer drug releasing stent.


Polymers ◽  
2020 ◽  
Vol 12 (1) ◽  
pp. 82 ◽  
Author(s):  
Yunwei Huang ◽  
Jingye Yan ◽  
Shiyuan Peng ◽  
Zilun Tang ◽  
Cuiying Tan ◽  
...  

Novel approach has been constructed for preparing the amphiphilic star copolymer pH/reduction stimuli-responsive cross-linked micelles (SCMs) as a smart drug delivery system for the well-controlled anti-tumor drug doxorubicin (DOX) release. The SCMs had a low CMC value of 5.3 mg/L. The blank and DOX-loaded SCMs both had a spherical shape with sizes around 100–180 nm. In addition, the good stability and well pH/reduction-sensitivity of the SCMs were determined by dynamic light scattering (DLS) as well. The SCMs owned a low release of DOX in bloodstream and normal tissues while it had a fast release in tumor higher glutathione (GSH) concentration and/or lower pH value conditions, which demonstrates their pH/reduction dual-responsiveness. Furthermore, we conducted the thermodynamic analysis to study the interactions between the DOX and polymer micelles in the DOX release process. The values of the thermodynamic parameters at pH 7.4 and at pH 5.0 conditions indicated that the DOX release was endothermic and controlled mainly by the forces of an electrostatic interaction. At pH 5.0 with 10 mM GSH condition, electrostatic interaction, chemical bond, and hydrophobic interactions contributed together on DOX release. With the low cytotoxicity of blank SCMs and well cytotoxicity of DOX-loaded SCMs, the results indicated that the SCMs could form a smart cancer microenvironment-responsive drug delivery system. The release kinetic and thermodynamic analysis offer a theoretical foundation for the interaction between drug molecules and polymer matrices, which helps provide a roadmap for the oriented design and control of anti-cancer drug release for cancer therapy.


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