A Biocompatible GdIII–Organic Framework Incorporating Polar Pores for pH-Sensitive Anti-Cancer Drug Delivery and Inhibiting Human Bone Tumour Cells

2019 ◽  
Vol 72 (3) ◽  
pp. 233
Author(s):  
Mingliang Ren ◽  
Hui Li ◽  
Hu Liu ◽  
Lei Wang ◽  
Haibo Xiang ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Bone Tumour ◽  
Ph Sensitive ◽  
Tumour Cells ◽  
Human Bone ◽  
X Ray ◽  
Gcmc Simulation ◽  
Bet Analysis ◽  
Organic Framework

With the aim of developing new and effective drug delivery systems for cancer treatments, great effort has been devoted to the field of porous metal–organic framework (MOF) platforms because of their controlled drug release performance, high drug loading, and acceptable biocompatibility. In this contribution, we report a MOF [Gd2(H2O)3(SDBA)3](DMA)3] (1, DMA=N,N-dimethylacetamide) with open O donor sites functionalised 1D pores, which has been fabricated using a bent polycarboxylic acid organic linker 4,4′-sulfonyldibenzoic acid (H2SDBA) under solvothermal conditions. Single crystal X-ray diffraction (SCRD), thermogravimetric analysis (TGA), elemental analysis, X-ray powder diffraction (XPRD), and Brunauer–Emmett–Teller (BET) analysis were used to characterise the as-prepared complex 1. 5-Fluorouracil (5-Fu) loaded 1 was soaked in phosphate buffer saline (PBS) and the invitro drug release performance was monitored by HPLC analysis under different pH conditions. At the pH values of 7.4 and 6.5, different profiles of pH-responsive release were achieved, indicating that the drug release performance of 5-Fu loaded 1 is pH sensitive. Grand Canonical Monte Carlo (GCMC) simulation results demonstrate that the open O donor sites in the framework of 1 account for the slower drug release rate. The prepared carrier is found to be bio-compatible with MG63 cells (cancerous tissue) and oral epidermal cells (normal tissue), when tested by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. The 5-Fu loaded carrier also shows a promising growth inhibition effect towards the human bone tumour cells MG63.

scholarly journals Design, Development, and Optimization of Polymeric Based-Colonic Drug Delivery System of Naproxen

2013 ◽  
Vol 2013 ◽  
pp. 1-12 ◽  
Author(s):  
Pooja Sharma ◽  
Anuj Chawla ◽  
Pravin Pawar
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Ph Sensitive ◽  
Time Dependent ◽  
Wet Granulation ◽  
Design Development ◽  
Caecal Content ◽  
S 100 ◽  
Eudragit S 100

The aim of present investigation deals with the development of time-dependent and pH sensitive press-coated tablets for colon specific drug delivery of naproxen. The core tablets were prepared by wet granulation method then press coated with hydroxypropyl cellulose (HPC) or Eudragit RSPO : RLPO mixture and further coated with Eudragit S-100 by dip immerse method. Thein vitrodrug release study was conducted in different dissolution media such as pH 1.2, 6.8, and 7.4 with or without rat caecal content to simulate GIT conditions. Surface morphology and cross-sectional view of the tablets were visualized by scanning electron microscopy (SEM). All prepared batches were in compliance with the pharmacopoeial standards. The tablets which are compression coated with HPC followed by Eudragit S-100 coated showed highestin vitrodrug release of 98.10% in presence of rat caecal content. The SEM of tablets suggested that the number of pores got increased in pH 7.4 medium followed by dissolution of coating layer. The tablets coat erosion study suggested that the lag time depends upon the coating concentrations of polymers. A time-dependent hydrophilic polymer and pH sensitive polymer based press-coated tablets of naproxen were promising delivery for colon targeting.

Schiff base-containing dextran nanogel as pH-sensitive drug delivery system of doxorubicin: Synthesis and characterization

2018 ◽  
Vol 33 (2) ◽  
pp. 170-181 ◽  
Author(s):  
Hongying Su ◽  
Wen Zhang ◽  
Yayun Wu ◽  
Xiaodong Han ◽  
Gang Liu ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Schiff Base ◽  
Drug Release ◽  
Drug Delivery System ◽  
Delivery System ◽  
Ph Sensitive ◽  
Cell Uptake ◽  
Stimuli Responsive ◽  
Drug Release Profile

Stimuli-responsive hydrogels have been widely researched as carrier systems, due to their excellent biocompatibility and responsiveness to external physiologic environment factors. In this study, dextran-based nanogel with covalently conjugated doxorubicin (DOX) was developed via Schiff base formation using the inverse microemulsion technique. Since the Schiff base linkages are acid-sensitive, drug release profile of the DOX-loaded nanogel would be pH-dependent. In vitro drug release studies confirmed that DOX was released much faster under acidic condition (pH 2.0, 5.0) than that at pH 7.4. Approximately 66, 28, and 9% of drug was released in 72 h at pH 2.0, 5.0, and 7.4, respectively. Cell uptake by the human breast cancer cell (MCF-7) demonstrated that the DOX-loaded dextran nanogel could be internalized through endocytosis and distributed in endocytic compartments inside tumor cells. These results indicated that the Schiff base-containing nanogel can serve as a pH-sensitive drug delivery system. And the presence of multiple aldehyde groups on the nanogel are available for further conjugations of targeting ligands or imaging probes.

SCANNING ION MICROBEAM ANALYSIS OF DIFFUSION IN IN-MOUTH DRUG RELEASE POLYMERS

2005 ◽  
Vol 15 (03n04) ◽  
pp. 161-167 ◽  
Author(s):  
G. MASSINGHAM ◽  
R. ARSLANOGLU ◽  
F. E. GAUNTLETT ◽  
M. S. RIHAWY ◽  
R. W. SMITH ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Nuclear Reaction ◽  
Drug Delivery Systems ◽  
Saline Solution ◽  
Pure Water ◽  
X Ray ◽  
Preliminary Results ◽  
Water Infusion ◽  
Phosphate Buffered Saline

With the aim of characterizing polymer-based drug delivery systems a combination of Scanning MeV 3 He microbeam Nuclear Reaction, Backscattering and Particle Induced X-ray Emission (PIXE) techniques has been developed. This, together with gravimetric and UV techniques has been applied to characterize both water infusion and drug effusion for three in-mouth polymer–drug systems. Preliminary results are presented from the exposure of polymers, containing drug at a level of 9% by weight of the dry polymer, to both pure water and a phosphate buffered saline solution at 37°C.

Composite microparticle drug delivery systems based on chitosan, alginate and pectin with improved pH-sensitive drug release property

2009 ◽  
Vol 68 (2) ◽  
pp. 245-249 ◽  
Author(s):  
Cui-Yun Yu ◽  
Bo-Cheng Yin ◽  
Wei Zhang ◽  
Si-Xue Cheng ◽  
Xian-Zheng Zhang ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Drug Delivery Systems ◽  
Delivery Systems ◽  
Ph Sensitive ◽  
Release Property

scholarly journals Synthesis and characterization of oral drug delivery, a pH – sensitive silver nanocomposite based on sodium alginate extracted from Sargassum asperifolium collected from Jazan coasts, KSA

2019 ◽  
Author(s):  
Fatimah. A. Agili ◽  
Sahera. F. Mohamed
Keyword(s):  
Electron Microscope ◽  
Drug Release ◽  
Sodium Alginate ◽  
Oral Drug Delivery ◽  
Drug Carrier ◽  
Gastric Fluid ◽  
Ph Sensitive ◽  
Oral Drug ◽  
Release Mechanism ◽  
X Ray

AbstractThe pH-sensitive nanocomposite composed of sodium alginate/ Pectin/ Tannic acid – silver SA/Pec/TA-Ag was prepared using microwave irradiation and employed as a carrier for Propranolol drug. Physico-chemical characteristics of the prepared systems using Fourier Transform Infrared Spectroscopy (FTIR), X-ray Diffraction (XRD), Field Emission Scanning Electron Microscope (FESEM), High-Resolution Transmission Electron Microscope (HRTEM), Dynamic light Scattering instrument (DLS), and Energy Dispersive X-Ray Analysis (EDX). The percentage drug release was 96% at pH 7.4 within 420 min. The drug release data was fitted into different kinetic models included zero order, First order, Higuchi and Ritger-Peppas model. The release mechanism is non-Fickian character where it controlled by diffusion and relaxation of polymer chains. It can be concluded that SA/Pec/TA-Ag nanocomposite is candidate for the oral drug carrier specific for intestinal system and has stability against gastric fluid.

Physicochemical characterization and release properties of oral drug delivery: A pH-sensitive nanocomposite based on sodium alginate–pectin–tannic acid–silver

2019 ◽  
Vol 28 (8-9) ◽  
pp. 598-608
Author(s):  
Fatimah A Agili ◽  
Sahera FM Aly
Keyword(s):  
Electron Microscope ◽  
Drug Release ◽  
Sodium Alginate ◽  
Tannic Acid ◽  
Drug Carrier ◽  
Ph Sensitive ◽  
Diffraction Field ◽  
Oral Drug ◽  
Release Mechanism ◽  
X Ray

A pH-sensitive nanocomposite formed from sodium alginate (SA)/pectin (Pec)/tannic acid (TA)–silver (Ag) was developed using microwave irradiation and it was applied as a carrier for propranolol drug. TA acts as a cross-linker and a reducing agent for Ag ions. Physicochemical characteristics of the fabricated system using Fourier transform infrared spectroscopy, X-ray diffraction, field-emission scanning electron microscope, high-resolution transmission electron microscope, dynamic light scattering instrument, and energy dispersive X-ray analysis. The swelling percent and the drug release were observed to be pH-sensitive. The occurrence of Ag nanoparticles in the network enhances the drug release that is 96% at pH 7.4 within 420 min. The drug release data were adjusted into different kinetic models involved zero order, first order, Higuchi, and Ritger–Peppas models. The release mechanism is a non-Fickian character where it controls by diffusion and relaxation of polymer chains. It can be concluded that SA/Pec/TA-Ag nanocomposite is a candidate for the oral drug carrier specific for the intestinal system and has ability against the gastric fluid.

Combine Drug Delivery of Thymoquinone-Doxorubicin by Cockle Shellderived pH-sensitive Aragonite CaCO3 Nanoparticles

2020 ◽  
Vol 10 (4) ◽  
pp. 518-533 ◽  
Author(s):  
Kehinde M. Ibiyeye ◽  
Abu B.Z. Zuki ◽  
Norshariza Nurdin ◽  
Mokrish Ajat
Keyword(s):  
Electron Microscopy ◽  
Drug Delivery ◽  
Calcium Carbonate ◽  
Drug Release ◽  
Release Kinetics ◽  
Drug Loading ◽  
Ph Sensitive ◽  
Multiple Drug ◽  
Burst Release ◽  
Cockle Shell

Background: Cockleshell-derived aragonite calcium carbonate nanoparticles were prepared by the top-down approach for combine delivery of two types of drugs. Objective: The aim of this study was to synthesize and characterize thymoquinone-doxorubicin loaded cockle shell-derived aragonite calcium carbonate nanoparticle. Aragonite calcium carbonate nanoparticles encapsulating thymoquinone and doxorubicin alone were also prepared. Methods: The blank and drug-loaded nanoparticles were characterized by field emission scanning electron microscopy, transmission electron microscopy, Zeta potential, Fourier transformed infrared and X-ray diffraction. Drug delivery properties, in vitro drug release study at pH 7.4, 6 and 4.8, and effect of blank nanoparticles on MCF10A, 3T3, MDA MB231 cells were also analyzed. Results: The blank and drug-loaded nanoparticles were pleomorphic and their sizes varying from 53.65 ± 10.29 nm to 60.49 ± 11.36 nm with an overall negative charge. The entrapment efficiency of thymoquinone and doxorubicin were 41.6 and 95.8, respectively. The FTIR showed little alteration after loading thymoquinone and doxorubicin while XRD patterns revealed no changes in the crystallizations of nanoparticles after drug loading. The drug release kinetics of doxorubicin and thymoquinone from the nanoparticles showed a continuous and gradual release after an initial burst release was observed. At pH 4.8, about 100% of drug release was noticed, 70% at pH 6 while only 50% at pH 7.4. The cell viability was 80% at a concentration of 1000 ug/ml of blank nanoparticle. Conclusion: The cockle shell-derived pH sensitive aragonite calcium carbonate nanoparticle provides an effective and simple means of multiple drug delivery and function as a platform for pH controlled release of loaded therapeutic agents.

Dual-pH-sensitive mesoporous silica nanoparticle-based drug delivery system for tumor-triggered intracellular drug release

2018 ◽  
Vol 53 (15) ◽  
pp. 10653-10665 ◽  
Author(s):  
Hui Chen ◽  
Ying Kuang ◽  
Rong Liu ◽  
Zhongyin Chen ◽  
Bingbing Jiang ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Mesoporous Silica ◽  
Drug Delivery System ◽  
Delivery System ◽  
Silica Nanoparticle ◽  
Ph Sensitive ◽  
Mesoporous Silica Nanoparticle

scholarly journals Drug Delivery System Based on pH-Sensitive Biocompatible Poly(2-vinyl pyridine)-b-poly(ethylene oxide) Nanomicelles Loaded with Curcumin and 5-Fluorouracil

Polymers ◽  
2020 ◽  
Vol 12 (7) ◽  
pp. 1450 ◽  
Author(s):  
Camelia-Elena Iurciuc-Tincu ◽  
Monica Stamate Cretan ◽  
Violeta Purcar ◽  
Marcel Popa ◽  
Oana Maria Daraba ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Ethylene Oxide ◽  
Ph Sensitive ◽  
Hydrophobic Drugs ◽  
Practical Utilization ◽  
Vinyl Pyridine ◽  
Poly Ethylene Oxide ◽  
Poly Ethylene

Smart polymeric micelles (PMs) are of practical interest as nanocarriers for the encapsulation and controlled release of hydrophobic drugs. Two hydrophobic drugs, naturally-based curcumin (Cur) and synthetic 5-fluorouracil (5-FU), were loaded into the PMs formed by a well-defined pH-sensitive poly(2-vinyl pyridine)-b-poly(ethylene oxide) (P2VP90-b-PEO398) block copolymer. The influence of the drug loading on the micellar sizes was investigated by dynamic light scattering (DLS) and it appears that the size of the PMs increases from around 60 to 100 nm when Cur is loaded. On the contrary, the loading of the 5-FU has a smaller effect on the micellar sizes. This difference can be attributed to higher molar mass of Cur with respect to 5-FU but also to higher loading efficiency of Cur, 6.4%, compared to that of 5-FU, 5.8%. In vitro drug release was studied at pH 2, 6.8, and 7.4, and it was observed that the pH controls the release of both drugs. At pH 2, where the P2VP sequences from the “frozen-in” micellar core are protonated, the drug release efficiencies exceed 90%. Moreover, it was demonstrated, by in vitro assays, that these PMs are hemocompatible and biocompatible. Furthermore, the PMs protect the Cur against the photo-degradation, whereas the non-ionic PEO corona limits the adsorption of bovine serum albumin (BSA) protein on the surface. This study demonstrates that these pH-sensitive PMs are suitable for practical utilization as human-safe and smart, injectable drug delivery systems.

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