Targeted Drug Delivery of Teniposide by Magnetic Nanocarrier

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.

Download Full-text

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

Journal of Drug Delivery and Therapeutics ◽

10.22270/jddt.v9i4-s.3400 ◽

2019 ◽

Vol 9 (4-s) ◽

pp. 589-594

Author(s):

Sweta Garg ◽

Ashish Garg ◽

Nitendra K. Sahu ◽

Awesh K Yadav

Keyword(s):

Drug Delivery ◽

Drug Release ◽

Anticancer Drug ◽

Amide Bond ◽

Cancer Drug ◽

Drug Candidate ◽

Cytotoxicity Studies ◽

In Vitro Investigation ◽

Mcf 7

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

Download Full-text

Functional Magnetic Core-Shell System-Based Iron Oxide Nanoparticle Coated with Biocompatible Copolymer for Anticancer Drug Delivery

Pharmaceutics ◽

10.3390/pharmaceutics11030120 ◽

2019 ◽

Vol 11 (3) ◽

pp. 120 ◽

Cited By ~ 15

Author(s):

Thai Hoang Thi ◽

Diem-Huong Nguyen Tran ◽

Long Bach ◽

Hieu Vu-Quang ◽

Duy Nguyen ◽

...

Keyword(s):

Drug Delivery ◽

Iron Oxide ◽

Anticancer Drug ◽

Targeted Delivery ◽

Superparamagnetic Iron Oxide ◽

Proton Nuclear Magnetic Resonance ◽

Iron Oxide Nanoparticle ◽

Core Shell ◽

Anticancer Drug Delivery ◽

Shell System

Polymer coating has drawn increasing attention as a leading strategy to overcome the drawbacks of superparamagnetic iron oxide nanoparticles (SPIONs) in targeted delivery of anticancer drugs. In this study, SPIONs were modified with heparin-Poloxamer (HP) shell to form a SPION@HP core-shell system for anticancer drug delivery. The obtained formulation was characterized by techniques including transmission electron microscopy (TEM), Fourier transform infrared spectra (FT-IR), vibration sample magnetometer (VSM), proton nuclear magnetic resonance (1H-NMR), and powder X-ray diffraction (XRD). Results showed the successful attachment of HP shell on the surface of SPION core and the inability to cause considerable effects to the crystal structure and unique magnetic nature of SPION. The core-shell system maintains the morphological features of SPIONs and the desired size range. Notably, Doxorubicin (DOX), an anticancer drug, was effectively entrapped into the polymeric shell of SPION@HP, showing a loading efficiency of 66.9 ± 2.7% and controlled release up to 120 h without any initial burst effect. Additionally, MTT assay revealed that DOX-loaded SPION@HP exerted great anticancer effect against HeLa cells and could be safely used. These results pave the way for the application of SPION@HP as an effective targeted delivery system for cancer treatment.

Download Full-text

Functional responsive superparamagnetic core/shell nanoparticles and their drug release properties

RSC Advances ◽

10.1039/c7ra02437a ◽

2017 ◽

Vol 7 (42) ◽

pp. 26243-26249 ◽

Cited By ~ 9

Author(s):

Zied Ferjaoui ◽

Raphaël Schneider ◽

Abdelaziz Meftah ◽

Eric Gaffet ◽

Halima Alem

Keyword(s):

Folic Acid ◽

Iron Oxide ◽

Drug Release ◽

Drug Loading ◽

Superparamagnetic Iron Oxide ◽

Cancer Drug ◽

Oxide Nanoparticles ◽

Core Shell ◽

Shell Nanoparticles ◽

Core Shell Nanoparticles

Folic acid functionalized responsive core/shell superparamagnetic iron oxide nanoparticles were successfully synthesized for further application in cancer therapy. Their cancer drug loading and release performances were demonstrated.

Download Full-text

Gemcitabine-incorporated polyurethane films for controlled release of an anticancer drug

Biomaterials Research ◽

10.1186/s40824-019-0169-7 ◽

2019 ◽

Vol 23 (1) ◽

Author(s):

Seong Hoon Choi ◽

Il-Hoon Cho ◽

Sangsoo Park

Keyword(s):

Drug Delivery ◽

Drug Release ◽

Plasma Treatment ◽

Anticancer Drug ◽

Film Surface ◽

Cancer Drug ◽

Anti Cancer ◽

Polyurethane Film ◽

Silicone Film ◽

Scanning Electron

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.

Download Full-text

Polymer Coated Iron Nanoparticles: Radiolabeling & In Vitro Studies

Current Radiopharmaceuticals ◽

10.2174/1874471013666200430094113 ◽

2020 ◽

Vol 13 ◽

Author(s):

Selin Yılmaz ◽

Çiğdem İçhedef ◽

Kadriye Buşra Karatay ◽

Serap Teksöz

Keyword(s):

Breast Cancer ◽

Drug Delivery ◽

Iron Oxide ◽

Cancer Cells ◽

Iron Oxide Nanoparticles ◽

Breast Cancer Cells ◽

Cancer Drug ◽

Oxide Nanoparticles ◽

Sem Images

Backgorund: Superparamagnetic iron oxide nanoparticles (SPIONs) have been extensively used for targeted drug delivery systems due to their unique magnetic properties. Objective: In this study, it’s aimed to develop a novel targeted 99mTc radiolabeled polymeric drug delivery system for Gemcitabine (GEM). Methods: Gemcitabine, an anticancer agent, was encapsulated into polymer nanoparticles (PLGA) together with iron oxide nanoparticles via double emulsion technique and then labeled with 99mTc. SPIONs were synthesized by reduction–coprecipitation method and encapsulated with oleic acid for surface modification. Size distribution and the morphology of the synthesized nanoparticles were caharacterized by dynamic light scattering(DLS)and scanning electron microscopy(SEM), respectively. Radiolabeling yield of SPION-PLGAGEM nanoparticles were determined via Thin Layer Radio Chromatography (TLRC). Cytotoxicity of GEM loaded SPION-PLGA were investigated on MDA-MB-231 and MCF7 breast cancer cells in vitro. Results: SEM images displayed that the average size of the drug-free nanoparticles was 40 nm and the size of the drug-loaded nanoparticles was 50 nm. The diameter of nanoparticles were determined as 366.6 nm by DLS, while zeta potential was found as-29 mV. SPION was successfully coated with PLGA, which was confirmed by FTIR. GEM encapsulation efficiency of SPION-PLGA was calculated as 4±0.16 % by means of HPLC. Radiolabeling yield of SPION-PLGA-GEM nanoparticles were determined as 97.8±1.75 % via TLRC. Cytotoxicity of GEM loaded SPION-PLGA were investigated on MDA-MB-231 and MCF7 breast cancer cells. SPION-PLGA-GEM showed high uptake on MCF-7, whilst incorporation rate was increased for both cell lines which external magnetic field application. Conclusion: 99mTc labeled SPION-PLGA nanoparticles loaded with GEM may overcome some of the obstacles in anti-cancer drug delivery because of their appropriate size, non-toxic, and supermagnetic characteristics.

Download Full-text

Folate-conjugated dually responsive micelles for targeted anticancer drug delivery

RSC Advances ◽

10.1039/c6ra01885h ◽

2016 ◽

Vol 6 (42) ◽

pp. 35658-35667 ◽

Cited By ~ 9

Author(s):

Lingling Zhao ◽

Yajuan Zhang ◽

Jia Shao ◽

Hongze Liang ◽

Haining Na ◽

...

Keyword(s):

Drug Delivery ◽

Drug Release ◽

Anticancer Activity ◽

Anticancer Drug ◽

Anticancer Drug Delivery ◽

Dual Responsive

Folate-conjugated dual-responsive micelles were developed, sustained and sensitive drug release from the drug loaded micelles was observed. Folate-targeted micelles showed higher anticancer activity and enhanced cellar uptake than non-targeted ones.

Download Full-text