scholarly journals Cholesterol Levels Affect the Performance of AuNPs-Decorated Thermo-Sensitive Liposomes as Nanocarriers for Controlled Doxorubicin Delivery

Pharmaceutics ◽  
2021 ◽  
Vol 13 (7) ◽  
pp. 973
Author(s):  
Mónica C. García ◽  
Nabila Naitlho ◽  
José Manuel Calderón-Montaño ◽  
Estrella Drago ◽  
Manuela Rueda ◽  
...  
Keyword(s):  
Drug Release ◽  
Cancer Cells ◽  
Electrostatic Interactions ◽  
Drug Loading ◽  
Gradient Methods ◽  
Spherical Shape ◽  
Morphological Properties ◽  
Ovarian Cancer Cells ◽  
Cholesterol Levels ◽  
L1 And L2

Stimulus-responsive liposomes (L) for triggering drug release to the target site are particularly useful in cancer therapy. This research was focused on the evaluation of the effects of cholesterol levels in the performance of gold nanoparticles (AuNPs)-functionalized L for controlled doxorubicin (D) delivery. Their interfacial and morphological properties, drug release behavior against temperature changes and cytotoxic activity against breast and ovarian cancer cells were studied. Langmuir isotherms were performed to identify the most stable combination of lipid components. Two mole fractions of cholesterol (3.35 mol% and 40 mol%, L1 and L2 series, respectively) were evaluated. Thin-film hydration and transmembrane pH-gradient methods were used for preparing the L and for D loading, respectively. The cationic surface of L allowed the anchoring of negatively charged AuNPs by electrostatic interactions, even inducing a shift in the zeta potential of the L2 series. L exhibited nanometric sizes and spherical shape. The higher the proportion of cholesterol, the higher the drug loading. D was released in a controlled manner by diffusion-controlled mechanisms, and the proportions of cholesterol and temperature of release media influenced its release profiles. D-encapsulated L preserved its antiproliferative activity against cancer cells. The developed liposomal formulations exhibit promising properties for cancer treatment and potential for hyperthermia therapy.

scholarly journals One-Pot Method for Preparation of Magnetic Multi-Core Nanocarriers for Drug Delivery

Materials ◽  
2019 ◽  
Vol 12 (3) ◽  
pp. 540 ◽  
Author(s):  
Črt Dragar ◽  
Tanja Potrč ◽  
Sebastjan Nemec ◽  
Robert Roškar ◽  
Stane Pajk ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Aqueous Phase ◽  
Colloidal Stability ◽  
Drug Loading ◽  
Spherical Shape ◽  
Surfactant Solution ◽  
Time Frame ◽  
One Pot ◽  
Magnetic Nanocarriers

The development of various magnetically-responsive nanostructures is of great importance in biomedicine. The controlled assembly of many small superparamagnetic nanocrystals into large multi-core clusters is needed for effective magnetic drug delivery. Here, we present a novel one-pot method for the preparation of multi-core clusters for drug delivery (i.e., magnetic nanocarriers). The method is based on hot homogenization of a hydrophobic phase containing a nonpolar surfactant into an aqueous phase, using ultrasonication. The solvent-free hydrophobic phase that contained tetradecan-1-ol, γ-Fe2O3 nanocrystals, orlistat, and surfactant was dispersed into a warm aqueous surfactant solution, with the formation of small droplets. Then, a pre-cooled aqueous phase was added for rapid cooling and the formation of solid magnetic nanocarriers. Two different nonpolar surfactants, polyethylene glycol dodecyl ether (B4) and our own N1,N1-dimethyl-N2-(tricosan-12-yl)ethane-1,2-diamine (SP11), were investigated for the preparation of MC-B4 and MC-SP11 magnetic nanocarriers, respectively. The nanocarriers formed were of spherical shape, with mean hydrodynamic sizes <160 nm, good colloidal stability, and high drug loading (7.65 wt.%). The MC-B4 nanocarriers showed prolonged drug release, while no drug release was seen for the MC-SP11 nanocarriers over the same time frame. Thus, the selection of a nonpolar surfactant for preparation of magnetic nanocarriers is crucial to enable drug release from nanocarrier.

scholarly journals Oleic Acid Copolymer as A Novel Upconversion Nanomaterial to Make Doxorubicin-Loaded Nanomicelles with Dual Responsiveness to pH and NIR

Pharmaceutics ◽  
2020 ◽  
Vol 12 (7) ◽  
pp. 680
Author(s):  
Jin Zhang ◽  
Xiaoyue Tang ◽  
Chuanqing Huang ◽  
Zeyu Liu ◽  
Yong Ye
Keyword(s):  
Oleic Acid ◽  
Drug Release ◽  
Cancer Cells ◽  
Anticancer Drugs ◽  
Cellular Uptake ◽  
Drug Loading ◽  
A549 Cells ◽  
Infrared Light ◽  
Plant Oil ◽  
Dual Response

Oleic acid (OA) as main component of plant oil is an important solvent but seldom used in the nanocarrier of anticancer drugs because of strong hydrophobicity and little drug release. In order to develop a new type of OA nanomaterial with dual responses to pH and near infrared light (NIR) to achieve the intelligent delivery of anticancer drugs. The novel OA copolymer (mPEG-PEI-(NBS, OA)) was synthesized by grafting OA and o-nitrobenzyl succinate (NBS) onto mPEGylated polyethyleneimine (mPEG-PEI) by amidation reaction. It was further conjugated with NaYF4:Yb3+/Er3+ nanoparticles, and encapsulated doxorubicin (DOX) through self-assembly to make upconversion nanomicelles with dual response to pH and NIR. Drug release behavior of DOX, physicochemical characteristics of the nanomicelles were evaluated, along with its cytotoxic profile, as well as the degree of cellular uptake in A549 cells. The encapsulation efficiency and drug loading capacity of DOX in the nanomicelles were 73.84% ± 0.58% and 4.62% ± 0.28%, respectively, and the encapsulated DOX was quickly released in an acidic environment exposed to irradiation at 980 nm. The blank nanomicelles exhibited low cytotoxicity and excellent biocompatibility by MTT assay against A549 cells. The DOX-loaded nanomicelles showed remarkable cytotoxicity to A549 cells under NIR, and promoted the cellular uptake of DOX into the cytoplasm and nucleus of cancer cells. OA copolymer can effectively deliver DOX to cancer cells and achieve tumor targeting through a dual response to pH and NIR.

Functionalized Bacterial Cellulose Microparticles for Drug Delivery in Biomedical Applications

2019 ◽  
Vol 25 (34) ◽  
pp. 3692-3701 ◽  
Author(s):  
Hanif Ullah ◽  
Munair Badshah ◽  
Alexandra Correia ◽  
Fazli Wahid ◽  
Hélder A. Santos ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Antibacterial Activity ◽  
Drug Release ◽  
Bacterial Cellulose ◽  
Biomedical Applications ◽  
Drug Carrier ◽  
Drug Loading ◽  
Antibacterial Properties ◽  
Amorphous State ◽  
Spherical Shape

Background: Bacterial cellulose (BC) has recently attained greater interest in various research fields, including drug delivery for biomedical applications. BC has been studied in the field of drug delivery, such as tablet coating, controlled release systems and prodrug design. Objective: In the current work, we tested the feasibility of BC as a drug carrier in microparticulate form for potential pharmaceutical and biomedical applications. Method : For this purpose, drug-loaded BC microparticles were prepared by simple grinding and injection moulding method through regeneration. Model drugs, i.e., cloxacillin (CLX) and cefuroxime (CEF) sodium salts were loaded in these microparticles to assess their drug loading and release properties. The prepared microparticles were evaluated in terms of particle shapes, drug loading efficiency, physical state of the loaded drug, drug release behaviour and antibacterial properties. Results: The BC microparticles were converted to partially amorphous state after regeneration. Moreover, the loaded drug was transformed into the amorphous state. The results of scanning electron microscopy (SEM) showed that microparticles had almost spherical shape with a size of ca. 350-400 μm. The microparticles treated with higher drug concentration (3%) exhibited higher drug loading. Keeping drug concertation constant, i.e., 1%, the regenerated BC (RBC) microparticles showed higher drug loading (i.e., 37.57±0.22% for CEF and 33.36±3.03% for CLX) as compared to as-synthesized BC (ABC) microparticles (i.e., 9.46±1.30% for CEF and 9.84±1.26% for CLX). All formulations showed immediate drug release, wherein more than 85% drug was released in the initial 30 min. Moreover, such microparticles exhibited good antibacterial activity with larger zones of inhibition for drug loaded RBC microparticles as compared to corresponding ABC microparticles. Conclusion : Drug loaded BC microparticles with immediate release behaviour and antibacterial activity were fabricated. Such functionalized microparticles may find potential biomedical and pharmaceutical applications.

Preparation of ciprofloxacin-encapsulated poly-ε- caprolactone microcapsules by the solvent evaporation technique

e-Polymers ◽  
2013 ◽  
Vol 13 (1) ◽  
Author(s):  
Marta Przybyslawska ◽  
Aleksandra Amelian ◽  
Katarzyna Winnicka
Keyword(s):  
Drug Release ◽  
Drug Loading ◽  
Spherical Shape ◽  
Entrapment Efficiency ◽  
Solvent Evaporation ◽  
Scanning Calorimetry ◽  
In Vitro Drug Release ◽  
Encapsulation Process ◽  
Evaporation Technique

Abstract The objective of this study was to prepare ciprofloxacin (CIP) encapsulated poly-ε-caprolactone (PCL) microcapsules by the single emulsion oilin- water (o/w) solvent evaporation method. The obtained microcapsules were characterized for size, morphology, drug loading and entrapment efficiency. The physical state of microcapsules was determined by differential scanning calorimetry (DSC) and thermogravimetric analysis (TG). Storage stability, the in vitro drug release and mathematical modeling of drug release were also tested. It was found that obtained microcapsules had spherical shape and their size range was from 57.5 μm to 234.7 μm. The drug loading of microcapsules was from 1.72% to 11.02%. The optimal conditions of the encapsulation process include the drug/polymer ratio 2/1, using homogenizer for 5 min at 15000 rpm to disperse CIP in PCL solution and aqueous phase at pH 5.5. The results of CIP release study indicate that obtained microcapsules might be successfully used for designing sustained release dosage forms.

scholarly journals Taste Masking of Nizatidine Using Ion-Exchange Resins

Processes ◽  
2019 ◽  
Vol 7 (11) ◽  
pp. 779 ◽  
Author(s):  
Pattaraporn Panraksa ◽  
Kasidech Boonsermsukcharoen ◽  
Kyu-Mok Hwang ◽  
Eun-Seok Park ◽  
Pensak Jantrawut
Keyword(s):  
Drug Release ◽  
Bitter Taste ◽  
Drug Loading ◽  
Electronic Tongue ◽  
Spherical Shape ◽  
Batch Process ◽  
Taste Masking ◽  
Simulated Gastric Fluid ◽  
Exchange Resins

The purpose of this study was to mask the bitter taste of nizatidine (NZD) using cation-exchange resins. Amberlite IRP-69 and Dowex-50 containing cross-linked polystyrene backbones were used. The drug resin complexes were prepared by batch process using drug: resin ratios of 1:1, 1:3, and 1:5. The optimum drug: resin ratio and the time required for maximum percentage drug loading into the complexes were determined. The selected drug-resin complexes were evaluated for morphology, drug release, and taste. The NZD-Dowex complex was obtained at a drug: resin ratio of 1:5 using a stirring time of 1 h in order to get 100% loading of NZD. The NZD-Dowex complex had a spherical shape and smooth texture similar to Dowex resin. The NZD-Dowex complex with a ratio of 1:5 showed that in vitro drug release of 4.27% at 5 min in simulated salivary fluid of pH 6.8 and 99.67% at 1 h in simulated gastric fluid of pH 1.2. NZD’s bitter taste was effectively masked when it formed a complex with Dowex at a ratio of 1:5. This was proved by an electronic tongue and human test panel.

scholarly journals ID:2024 Synthesis and Characterization of PLGA-PEG Thymoquinone Nanoparticle and its Cytotoxicity Effects in Tamoxifen-resistant Breast Cancer Cells

2017 ◽  
Vol 4 (S) ◽  
pp. 55 ◽  
Author(s):  
Rozaina Ahmad ◽  
Noor Haida Mohd Kaus ◽  
Shahrul Hamid
Keyword(s):  
Breast Cancer ◽  
Drug Release ◽  
Cancer Cells ◽  
Breast Cancer Cells ◽  
Spherical Shape ◽  
Entrapment Efficiency ◽  
Volatile Oil ◽  
Pluronic F68

Background: Drug resistance has been a continuous challenge in cancer treatment. The use of nanotechnology in the development of new cancer drugs has potential. One of the extensively studied compound is thymoquinone (TQ) and this work aims to compare two types of TQ-nanoformulation and its cytotoxicity towards resistant cancer cells. Methods: TQ-nanoparticles were prepared and optimized by using 2 different formulation with different drug to PLGA-PEG ratio (1:20 and 1:7) and different PLGA-PEG to pluronic F68 ratio (10:1 and 2:1). The morphology and size were determined using TEM and DLS. Characterization of particles were done using UV-VIS, ATR-IR, entrapment efficiency and drug release. The effects of drug, polymer and surfactants were compared between the two formulations. Cytotoxicity assay was performed using MTS assay. Results: TEM finding showed 96% of particles produced with 1:7 drug to PLGA-PEG were less than 90 nm in size and spherical in shape. This was confirmed with DLS which showed smaller particle size than those formed with 1:20 drug to PLGA-PEG ration. Further analysis showed zeta potential was negatively charge which could facilitate cellular uptake as reported previously. In addition, PDI value was less than 0.1 in both formulations indicating monodispersed and less broad in size distribution. The absorption peak of PLGA-PEG-TQ-Nps were at 255 nm. The 1:7 drug to polymer formulation was selected for further analysis where the entrapment efficiency was 79.9% and in vitro drug release showed a maximum release of TQ at 64% respectively. Cytotoxicity result showed IC50 of TQ-nanoparticle at 20.05 µM and free TQ was 8.25 µM. Conclusion: This study showed that nanoparticle synthesized with 1:7 drug to PLGA-PEG ratio and 2:1 PLGA-PEG to pluronic F68 were less than 100 nm and had spherical shape as confirmed with DLS. This could facilitate its transportation and absorption to reach its target. There was conserved TQ stability as exhibited by slow release of this volatile oil. Cytotoxicity effect was noted when resistant breast cancer cells were treated with these particles.

scholarly journals PLGA Nanoparticles for the Intraperitoneal Administration of CBD in the Treatment of Ovarian Cancer: In Vitro and In Ovo Assessment

Pharmaceutics ◽  
2020 ◽  
Vol 12 (5) ◽  
pp. 439 ◽  
Author(s):  
Ana I. Fraguas-Sánchez ◽  
Ana I. Torres-Suárez ◽  
Marie Cohen ◽  
Florence Delie ◽  
Daniel Bastida-Ruiz ◽  
...  
Keyword(s):  
Ovarian Cancer ◽  
Cancer Treatment ◽  
Cancer Cells ◽  
Intraperitoneal Administration ◽  
Spherical Shape ◽  
Plga Nanoparticles ◽  
Ovarian Cancer Cells ◽  
In Ovo ◽  
Anticancer Efficacy

The intraperitoneal administration of chemotherapeutics has emerged as a potential route in ovarian cancer treatment. Nanoparticles as carriers for these agents could be interesting by increasing the retention of chemotherapeutics within the peritoneal cavity. Moreover, nanoparticles could be internalised by cancer cells and let the drug release near the biological target, which could increase the anticancer efficacy. Cannabidiol (CBD), the main nonpsychotropic cannabinoid, appears as a potential anticancer drug. The aim of this work was to develop polymer nanoparticles as CBD carriers capable of being internalised by ovarian cancer cells. The drug-loaded nanoparticles (CBD-NPs) exhibited a spherical shape, a particle size around 240 nm and a negative zeta potential (−16.6 ± 1.2 mV). The encapsulation efficiency was high, with values above 95%. A controlled CBD release for 96 h was achieved. Nanoparticle internalisation in SKOV-3 epithelial ovarian cancer cells mainly occurred between 2 and 4 h of incubation. CBD antiproliferative activity in ovarian cancer cells was preserved after encapsulation. In fact, CBD-NPs showed a lower IC50 values than CBD in solution. Both CBD in solution and CBD-NPs induced the expression of PARP, indicating the onset of apoptosis. In SKOV-3-derived tumours formed in the chick embryo model, a slightly higher—although not statistically significant—tumour growth inhibition was observed with CBD-NPs compared to CBD in solution. To sum up, poly-lactic-co-glycolic acid (PLGA) nanoparticles could be a good strategy to deliver CBD intraperitoneally for ovarian cancer treatment.

scholarly journals Optimized Icariin Phytosomes Exhibit Enhanced Cytotoxicity and Apoptosis-Inducing Activities in Ovarian Cancer Cells

Pharmaceutics ◽  
2020 ◽  
Vol 12 (4) ◽  
pp. 346 ◽  
Author(s):  
Nabil A. Alhakamy ◽  
Usama A. Fahmy ◽  
Shaimaa M. Badr-Eldin ◽  
Osama A. A. Ahmed ◽  
Hani Z. Asfour ◽  
...  
Keyword(s):  
Ovarian Cancer ◽  
Drug Release ◽  
Cancer Cells ◽  
Annexin V ◽  
Cytotoxic Agents ◽  
Ovarian Cancer Cells ◽  
Cytotoxic Activities ◽  
In Vitro Drug Release ◽  
Cytotoxicity Activity

Icariin (ICA) is a flavonol glycoside that has pleiotropic pharmacological actions. It has cytotoxic effects against ovarian cancer cells and increases their chemosensitivity to chemotherapeutic drugs. Phytosomes are identified for their potential in drug delivery of cytotoxic agents. Thus, the purpose of this study was to determine the potential enhancement of ICA cytotoxicity activity in OVCAR-3 ovarian cancer cells via its formulation in phytosomes. ICA-phytosomal formulation was optimized using a Box–Behnken design. Particle size, shape, and in vitro drug release were used to characterize the optimized formula. The optimized formulation exhibited enhanced in vitro drug release. ICA-phytosomes exhibited enhanced cytotoxicity against ovarian cancer cells. Cell cycle analysis indicated accumulation of cells challenged with ICA-phytosomes in G2/M and pre-G1 phases. Staining of cells with annexin V indicated significant elevation of percentage cells with early and late apoptosis as well as total cell death. In addition, the formulation significantly disturbed mitochondrial membrane potential and cellular content of caspase 3. In addition, intracellular release of reactive oxygen species (ROS) was enhanced by ICA-phytosomes. In conclusion, phytosome formulation of ICA significantly potentiates its cytotoxic activities against OVCAR-3 cells. This is mediated, at least partly, by enhanced ICA cellular permeation, apoptosis, and ROS.

Cytotoxic effects of disulfiram and synergism with cisplatin on ovarian cancer cells in vitro

2018 ◽  
Author(s):  
F Guo ◽  
Z Yang ◽  
J Xu ◽  
J Sehouli ◽  
AE Albers ◽  
...  
Keyword(s):  
Ovarian Cancer ◽  
Cancer Cells ◽  
Ovarian Cancer Cells ◽  
Cytotoxic Effects
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