scholarly journals Synthesis and Characterization of Nanodiamond-Doxorubicin (Dox) Conjugate for Effective Delivery against MCF-7 Cell Lines

2019 ◽  
Vol 9 (4-s) ◽  
pp. 589-594
Author(s):  
Sweta Garg ◽  
Ashish Garg ◽  
Nitendra K. Sahu ◽  
Awesh K Yadav

In this work, we have introduced a carbon nanomaterial (nanodiamond), to bind with anticancer drug doxorubicin (DOX) with via amide bond conjugation for cancer drug delivery and therapy. Nanodiamond (ND) was initially carboxylated by the surface modification along the treatment with strong alkaline solution (H2SO4:HNO3) and then activated the carboxyl moiety of ND with the addition of EDC. Anticancer drugs were bound to the ND through a succession of chemical modifications by adipic acid dihydrazide (ADH). The ND-Drug conjugate was analyzed by Nuclear Magnetic Resonance (1H-NMR) Spectroscopy, Fourier Transform Infrared (FTIR) Spectroscopy and Mass Spectroscopy (MS), Atomic Force Microscopy (AFM), Particle size, Zeta potential, Drug release, SRB assay against MCF-7 cells, and DNA fragmentation. Spectroscopic analysis confirms the conjugation of nanodiamond with different anticancer drug. AFM photomicrograph represents the surface morphological features of ND-DOX conjugates. In- vitro investigation showed that ND-DOX conjugates have slow and sustained drug release characteristics. In-vitro cytotoxicity studies, an enormous cytotoxic potential of ND-Drug conjugates were showed against cancer cell line. Above all findings were suggested that the ND-DOX conjugates may be a potential inhibitor of MCF-7 cancer cells to act as a drug candidate. According to all these data it can be confirm that the ND-DOX conjugates could be an effective agent for drug delivery and could be promising in future for tumor targeting strategy. Keywords: Nanodiamond, Sustained Release, Drug Delivery, Cytotoxicity, Conjugates

2020 ◽  
Vol 16 (4) ◽  
pp. 608-616
Author(s):  
Saeed Kakaei ◽  
Elham Sattarzadeh Khameneh ◽  
Effat Ghasemi ◽  
Mustafa Aghazadeh

Background:: Drug delivery technologies adjust drug release profile, absorption, distribution, and elimination for benefiting to the improvement of product efficacy, effectiveness, and safety. The IONPs release drugs via enzymatic activity, changes in physiological conditions such as pH, osmolality radiation, or temperature. In the case of nanoparticles that respond to the magnetic stimulus, the drug directs its action towards the site of a detected magnetic field. Objective:: In this study, the synthesis of a specific drug-delivery system based on magnetic nanocarrier for teniposide as an anticancer drug is reported. The iron oxide@SiO2 core-shell nanoparticles were functionalized with APTS as a spacer then coupling to the DOTA molecules. Anticancer drug of teniposide conjugated to the acidic group of DOTA via an amide bond. Multi-purpose magnetic nanoparticles were synthesized for targeted delivery of teniposide. Methods: Iron oxide nanoparticles were firstly coated with silica and their surface was then modified with aminopropyltriethoxysilane (APTES) through an in situ method. DOTA-NHS was also coupled to Fe3O4@SiO2-APTES via an amide bond formation. In the final step, teniposide as an anti-cancer drug was conjugated with DOTA through ester bonds, and the final compound of Fe3O4@SiO2- APTES-DOTA-Teniposide was obtained. The obtained nanocarrier was evaluated by various analyses. Results:: The multifunctional Fe3O4@SiO2-APTES-DOTA nanocarriers were successfully synthesized and characterized by XRD, FTIR, TGA, and UV-vis techniques. The silica-coated magnetic nanoparticle functionalized with aminopropyl triethoxysilane (APTES) was reacted with an acid group of DOTA, and teniposide was then coupled to DOTA through ester formation bonds. Drug release experiments showed that most of the conjugated teniposide were released within the first 12h. Conclusion:: The fabricated nano-carriers exhibited pH-sensitive drug release behavior, which can minimize the non-specific systemic spread of toxic drugs during circulation whilst maximizing the efficiency of tumor-targeted anticancer drug delivery for this purpose. The prepared teniposidegrafted Fe3O4@SiO2-APTES-DOTA core–shell structure nanoparticles showed a magnetic property with exposure to magnetic fields, indicating a great potential application in the treatment of cancer using magnetic targeting drug-delivery technology and multimodal imaging techniques.


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.


Polymers ◽  
2020 ◽  
Vol 12 (8) ◽  
pp. 1747
Author(s):  
Chiung-Hua Huang ◽  
Ting-Ju Chuang ◽  
Cherng-Jyh Ke ◽  
Chun-Hsu Yao

In this study, magnetic nanoparticles composed of a core (doxorubicin–gelatin) and a shell layer (Fe3O4–alginate) were developed to function as targeted anticancer drug delivery vehicles. The anticancer drug doxorubicin (DOX) was selected as a model drug and embedded in the inner gelatin core to obtain high encapsulation efficiency. The advantage of the outer magnetic layer is that it targets the drug to the tumor tissue and provides controlled drug release. The physicochemical properties of doxorubicin–gelatin/Fe3O4–alginate nanoparticles (DG/FA NPs) were characterized using scanning electron microscopy, Fourier transform infrared spectroscopy (FTIR), and X-ray diffraction. The mean diameter of DG/FA NPs, which was determined using a zeta potential analyzer, was 401.8 ± 3.6 nm. The encapsulation rate was 64.6 ± 11.8%. In vitro drug release and accumulation were also studied. It was found that the release of DOX accelerated in an acidic condition. With the manipulation of an external magnetic field, DG/FA NPs efficiently targeted Michigan Cancer Foundation-7 (MCF-7) breast cancer cells and showed in the nucleus after 6 h of incubation. After 12 h of incubation, the relative fluorescence intensity reached 98.4%, and the cell viability of MCF-7 cells decreased to 52.3 ± 4.64%. Dual-layer DG/FA NPs could efficiently encapsulate and deliver DOX into MCF-7 cells to cause the death of cancer cells. The results show that DG/FA NPs have the potential for use in targeted drug delivery and cancer therapy.


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.


2021 ◽  
Vol In Press (In Press) ◽  
Author(s):  
Masoomeh Nobahari ◽  
Kahin Shahanipour ◽  
Soheil Fatahian ◽  
Ramesh Monajemi

Background: Curcumin, a bioactive component of Curcuma langa, has been investigated for its anti-proliferative effects against various cancer cell lines. Although results are very promising, the poor water solubility and low bioavailability of curcumin are its main limitations for clinical application. Objectives: The purpose of this study was to develop a drug delivery system, consisting of hydroxyapatite (HAp) polymer and sodium alginate (NaAlg), covering the magnetic core of iron oxide nanoparticles (IONPs), and loaded with curcumin in order to enhance its bioavailability and therapeutic efficacy. Methods: In this study, IONPs were prepared by the co-precipitation method and coated with HAp and NaAlg. The nanoparticles (NPs) were characterized by X-ray diffraction, Fourier Transform Infrared Spectroscopy (FTIR), and electron microscopy (TEM and SEM). Encapsulation efficiency and curcumin loading rate were examined. Drug release rate was also measured in vitro at pH = 7.5 and 5.5. The toxicity of curcumin-loaded NPs and free curcumin was evaluated against HT-29 and MCF-7 cancer cells. Results: The assessment of physicochemical characteristics showed the synthesis of spherical particles with nanometer sizes (5 - 7 nm) and a high encapsulation efficiency (84.16 ± 3.51 %) and drug loading capacity (21.03 ± 0.87%). Maximum drug release was obtained at pH = 5.5. Iron oxide nanoparticles showed no significant cytotoxic effects. Curcumin-loaded coated IONPs showed a higher toxicity against HT-29 and MCF-7 cancer cells compared to free curcumin. Conclusions: This in vitro study showed that the encapsulation of curcumin, as a potent herbal drug, into IONPs enhanced its bioavailability, suggesting the NPs as an efficient vehicle for targeted drug delivery in cancer treatment.


2019 ◽  
Vol 43 (17) ◽  
pp. 6622-6635 ◽  
Author(s):  
Sevinc Ilkar Erdagi ◽  
Ufuk Yildiz

In this study, a polymeric nanoparticle-mediated dual anti-cancer drug delivery system was designed and developed.


2016 ◽  
Vol 2016 ◽  
pp. 1-8 ◽  
Author(s):  
Yuanfeng Ye ◽  
Xiaohong Hu

According to previous reports, low pH-triggered nanoparticles were considered to be excellent carriers for anticancer drug delivery, for the reason that they could trigger encapsulated drug release at mild acid environment of tumor. Herein, an acid-sensitiveβ-cyclodextrin derivative, namely, acetalated-β-cyclodextrin (Ac-β-CD), was synthesized by acetonation and fabricated to nanoparticles through single oil-in-water (o/w) emulsion technique. At the same time, camptothecin (CPT), a hydrophobic anticancer drug, was encapsulated into Ac-β-CD nanoparticles in the process of nanoparticle fabrication. Formed nanoparticles exhibited nearly spherical structure with diameter of209±40 nm. The drug release behavior of nanoparticles displayed pH dependent changes due to hydrolysis of Ac-β-CD. In order to overcome the disadvantages of nanoparticle and broaden its application, injectable hydrogels with Ac-β-CD nanoparticles were designed and prepared by simple mixture of nanoparticles solution and graphene oxide (GO) solution in this work. The injectable property was confirmed by short gelation time and good mobility of two precursors. Hydrogels were characterized by dynamic mechanical test and SEM, which also reflected some structural features. Moreover, all hydrogels underwent a reversible sol-gel transition in alkaline environment. Finally, the results ofin vitrodrug release profile indicated that hydrogel could control drug release or bind drug inside depending on the pH value of released medium.


Author(s):  
Pravin Patil ◽  
Anil Sharma ◽  
Subhash Dadarwal ◽  
Vijay Sharma

The objective of present investigation was to enhance brain penetration of Lamivudine, one of the most widely used drugs for the treatment of AIDS. This was achieved through incorporating the drug into solid lipid nanoparticles (SLN) prepared by using emulsion solvent diffusion technique. The formulations were characterized for surface morphology, size and size distribution, percent drug entrapment and drug release. The optimum rotation speed, resulting into better drug entrapment and percent yield, was in the range of 1000-1250 r/min. In vitro cumulative % drug release from optimized SLN formulation was found 40-50 % in PBS (pH-7.4) and SGF (pH-1.2) respectively for 10 h. After 24 h more than 65 % of the drug was released from all formulations in both mediums meeting the requirement for drug delivery for prolong period of time.


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