scholarly journals Incorporation of doxorubicin in different polymer nanoparticles and their anti-cancer activity

2018 ◽  
Author(s):  
S. Pieper ◽  
H. Onafuye ◽  
D. Mulac ◽  
Jindrich Cinatl ◽  
Mark N. Wass ◽  
...  
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
Neuroblastoma Cells ◽  
Controlled Drug Release ◽  
Plga Nanoparticles ◽  
Cellular Level ◽  
Drug Load ◽  
Anti Cancer ◽  
Solvent Displacement ◽  
Cancer Activity

AbstractNanoparticles are under investigation as carrier systems for anti-cancer drugs. They have been shown to accumulate in cancer tissues through the enhanced permeability and retention (EPR) effect, to reduce toxicity to non-target tissues, and to protect drugs from preliminary inactivation. However, nanoparticle preparations are not commonly compared for their anti-cancer effects at the cellular level. Here, we prepared doxorubicin-loaded nanoparticles based on poly(lactic-co-glycolic acid) (PLGA), polylactic acid (PLA), and PEGylated PLGA (PLGA-PEG) by solvent displacement and emulsion diffusion approaches. The resulting nanoparticles covered a size range between 73 and 246 nm. PLGA-PEG nanoparticle preparation by solvent displacement resulted in the smallest nanoparticles. In PLGA nanoparticles, the drug load could be optimised using solvent displacement at pH7 reaching 53 µg doxorubicin/mg nanoparticle. In addition, these PLGA nanoparticles displayed sustained doxorubicin release kinetics compared to the more burst-like kinetics of the other preparations. In neuroblastoma cells, doxorubicin-loaded PLGA-PEG nanoparticles (presumably due to their small size) and PLGA nanoparticles prepared by solvent displacement at pH7 (presumably due to their high drug load and superior drug release kinetics) exerted the strongest anti-cancer effects. In conclusion, doxorubicin-loaded nanoparticles made by different methods from different materials displayed substantial discrepancies in their anti-cancer activity at the cellular level. Optimised preparation methods resulted in PLGA nanoparticles characterised by increased drug load, controlled drug release, and high anti-cancer efficacy. The design of drug-loaded nanoparticles with optimised anti-cancer activity at the cellular level is an important step in the development of improved nanoparticle preparations for anti-cancer therapy.

scholarly journals Incorporation of doxorubicin in different polymer nanoparticles and their anticancer activity

2019 ◽  
Vol 10 ◽  
pp. 2062-2072 ◽  
Author(s):  
Sebastian Pieper ◽  
Hannah Onafuye ◽  
Dennis Mulac ◽  
Jindrich Cinatl ◽  
Mark N Wass ◽  
...  
Keyword(s):  
Drug Release ◽  
Anticancer Activity ◽  
Cancer Cells ◽  
Release Kinetics ◽  
Neuroblastoma Cells ◽  
Plga Nanoparticles ◽  
Cellular Level ◽  
Drug Load ◽  
Anticancer Efficacy ◽  
Solvent Displacement

Background: Nanoparticles are under investigation as carrier systems for anticancer drugs. The expression of efflux transporters such as the ATP-binding cassette (ABC) transporter ABCB1 is an important resistance mechanism in therapy-refractory cancer cells. Drug encapsulation into nanoparticles has been shown to bypass efflux-mediated drug resistance, but there are also conflicting results. To investigate whether easy-to-prepare nanoparticles made of well-tolerated polymers may circumvent transporter-mediated drug efflux, we prepared poly(lactic-co-glycolic acid) (PLGA), polylactic acid (PLA), and PEGylated PLGA (PLGA-PEG) nanoparticles loaded with the ABCB1 substrate doxorubicin by solvent displacement and emulsion diffusion approaches and assessed their anticancer efficiency in neuroblastoma cells, including ABCB1-expressing cell lines, in comparison to doxorubicin solution. Results: The resulting nanoparticles covered a size range between 73 and 246 nm. PLGA-PEG nanoparticle preparation by solvent displacement led to the smallest nanoparticles. In PLGA nanoparticles, the drug load could be optimised using solvent displacement at pH 7 reaching 53 µg doxorubicin/mg nanoparticle. These PLGA nanoparticles displayed sustained doxorubicin release kinetics compared to the more burst-like kinetics of the other preparations. In neuroblastoma cells, doxorubicin-loaded PLGA-PEG nanoparticles (presumably due to their small size) and PLGA nanoparticles prepared by solvent displacement at pH 7 (presumably due to their high drug load and superior drug release kinetics) exerted the strongest anticancer effects. However, nanoparticle-encapsulated doxorubicin did not display increased efficacy in ABCB1-expressing cells relative to doxorubicin solution. Conclusion: Doxorubicin-loaded nanoparticles made by different methods from different materials displayed substantial discrepancies in their anticancer activity at the cellular level. Optimised preparation methods resulted in PLGA nanoparticles characterised by increased drug load, controlled drug release, and high anticancer efficacy. The design of drug-loaded nanoparticles with optimised anticancer activity at the cellular level is an important step in the development of improved nanoparticle preparations for anticancer therapy. Further research is required to understand under which circumstances nanoparticles can be used to overcome efflux-mediated resistance in cancer cells.

Eremurus spectabilis, Rich Source of Isoorientin: Isolation, Quantification and Anti-Cancer Activity on SH-SY5Y Neuroblastoma Cells

2018 ◽  
Vol 14 (6) ◽  
pp. 578-585
Author(s):  
Esen Sezen Karaoglan ◽  
Gulsah Gundogdu ◽  
Mucahit Secme ◽  
Onur Senol ◽  
Fatma Demirkaya Miloglu ◽  
...  
Keyword(s):  
Neuroblastoma Cells ◽  
Rich Source ◽  
Anti Cancer ◽  
Cancer Activity

scholarly journals Modeling of Anti-Cancer Drug Release Kinetics From Liposomes and Micelles: A Review

2021 ◽  
Vol 20 (4) ◽  
pp. 565-576
Author(s):  
Nour Al Sawaftah ◽  
Vinod Paul ◽  
Nahid Awad ◽  
Ghaleb A. Husseini
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
Cancer Drug ◽  
Drug Release Kinetics ◽  
Anti Cancer

scholarly journals FORMULATION AND IN-VITRO EVALUATION OF THEOPHYLLINE HYDROCHLORIDE EFFERVESCENT FLOATING TABLETS: EFFECT OF POLYMER CONCENTRATION ON TABLET BUOYANCY

2019 ◽  
pp. 59-65
Author(s):  
AKPABIO E. I. ◽  
EFFIONG D. E. ◽  
UWAH T. O. ◽  
SUNDAY N. I.
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
Polymer Concentration ◽  
Hydroxypropyl Methylcellulose ◽  
Controlled Drug Release ◽  
Fickian Diffusion ◽  
Wet Granulation ◽  
Floating Tablets ◽  
Swelling Characteristics

Objective: This study was undertaken to formulate a floating drug delivery system of theophylline hydrochloride using different concentrations of a chosen polymer and then investigate how polymer concentration affects buoyancy and drug release properties of the tablets. Methods: Hydroxypropyl methylcellulose (HPMC) at different concentration levels of 15% (F1), 20% (F2) and 30% (F3) was used to form the three formulation batches of floating tablets. Wet granulation method was used for the granule preparation while Sodium bicarbonate and citric acid were used as the gas generating agent. The physical properties of the granules and the floating tablets were evaluated. Also determined were the physicomechanical properties, buoyancy and swelling characteristics of the tablets. The in vitro drug release study was carried out according to the USP I (basket method) for 8h in 900 ml 0.1N HCl at 50 rpm. Samples withdrawn at the regular predetermined time were analyzed spectrophotometrically at a wavelength of 271 nm and data obtained statistically analyzed by one-way analysis of variance (ANOVA). The differences between means were considered significant at P<0.05. Results: The result showed that polymer (HPMC) concentration significantly (p>0.05) increased swelling index and improved floating lag time, it had no significant effect on the total floating time. Percentage drug release at the end of 8 h was 100%, 98.2% and 96.13% for formulation F1, F2 and F3, respectively. All three formulations followed the Higuchi drug release kinetics model and the mechanism of drug release was the non Fickian diffusion with exponents of 0.46, 0.51 and 0.56 for the respective batch. Conclusion: Batch F3 gave a better-controlled drug release and floating properties in comparison to batch F1 and F2 thus Polymer concentration influenced the onset of floating and controlled the release of Theophylline.

scholarly journals Enhanced intracellular delivery and controlled drug release of magnetic PLGA nanoparticles modified with transferrin

2017 ◽  
Vol 38 (6) ◽  
pp. 943-953 ◽  
Author(s):  
Yan-na Cui ◽  
Qing-xing Xu ◽  
Pooya Davoodi ◽  
De-ping Wang ◽  
Chi-Hwa Wang
Keyword(s):  
Drug Release ◽  
Intracellular Delivery ◽  
Controlled Drug Release ◽  
Plga Nanoparticles

scholarly journals Preparation and Drug-Release Kinetics of Porous Poly(L-lactic acid)/Rifampicin Blend Particles

2014 ◽  
Vol 2014 ◽  
pp. 1-6 ◽  
Author(s):  
Takashi Sasaki ◽  
Hiroaki Matsuura ◽  
Kazuki Tanaka
Keyword(s):  
Lactic Acid ◽  
Drug Release ◽  
Release Kinetics ◽  
Drug Carrier ◽  
Controlled Drug Release ◽  
Solution Concentration ◽  
Porous Polymer ◽  
High Porosity ◽  
Original Solution ◽  
Kinetics Of

Porous polymer spheres are promising materials as carriers for controlled drug release. As a new drug-carrier material, blend particles composed of poly(L-lactic acid) (PLLA) and rifampicin were developed using the freeze-drying technique. The blend particles exhibit high porosity with a specific surface area of 10–40 m2 g−1. Both the size and porosity of the particles depend on the concentration of the original solution and on the method of freezing. With respect to the latter, we used the drop method (pouring the original solution dropwise into liquid nitrogen) and the spray method (freezing a mist of the original solution). The release kinetics of rifampicin from the blend particles into water depends significantly on the morphology of the blend particles. The results show that the release rate can be controlled to a great extent by tuning the size and porosity of the blend particles, both of which are varied by parameters such as the solution concentration and the method of freezing.

scholarly journals Mathematical Modeling for Pharmaco-Kinetic and -Dynamic Predictions from Controlled Drug Release NanoSystems: A Comparative Parametric Study

Scientifica ◽  
2019 ◽  
Vol 2019 ◽  
pp. 1-5 ◽  
Author(s):  
Grigorios P. Panotopoulos ◽  
Ziyad S. Haidar
Keyword(s):  
Mathematical Modeling ◽  
Drug Release ◽  
Dynamic Systems ◽  
Release Kinetics ◽  
Controlled Drug Release ◽  
Quantitative Prediction ◽  
Exact Mass ◽  
Minimization Method ◽  
Measured Concentration ◽  
Measured Variable

Predicting pharmacokinetics, based on the theory of dynamic systems, for an administered drug (whether intravenously, orally, intramuscularly, etc.), is an industrial and clinical challenge. Often, mathematical modeling of pharmacokinetics is preformed using only a measured concentration time profile of a drug administered in plasma and/or in blood. Yet, in dynamic systems, mathematical modeling (linear) uses both a mathematically described drug administration and a mathematically described body response to the administered drug. In the present work, we compare several mathematical models well known in the literature for simulating controlled drug release kinetics using available experimental data sets obtained in real systems with different drugs and nanosized carriers. We employed the χ2 minimization method and concluded that the Korsmeyer–Peppas model (or power-law model) provides the best fit, in all cases (the minimum value of χ2 per degree of freedom; χmin2/d.o.f. = 1.4183, with 2 free parameters or m = 2). Hence, (i) better understanding of the exact mass transport mechanisms involved in drugs release and (ii) quantitative prediction of drugs release can be computed and simulated. We anticipate that this work will help devise optimal pharmacokinetic and dynamic release systems, with measured variable properties, at nanoscale, characterized to target specific diseases and conditions.

scholarly journals Fabrication of Photothermo-Responsive Drug-Loaded Nanogel for Synergetic Cancer Therapy

Polymers ◽  
2018 ◽  
Vol 10 (10) ◽  
pp. 1098 ◽  
Author(s):  
Ray Chang ◽  
Wei-Bor Tsai
Keyword(s):  
Cancer Therapy ◽  
Drug Release ◽  
Controlled Drug Release ◽  
Green Laser ◽  
Cancer Drug ◽  
Cell Mortality ◽  
Anti Cancer ◽  
Temperature Stimulus ◽  
Sodium Copper Chlorophyllin ◽  
532 Nm

Temperature stimulus, easy modulation in comparison to other environmental stimuli, makes thermo-responsive nanocarriers popular in the applications of controlled drug release for cancer therapy. In this study, photosensitive sodium copper chlorophyllin (SCC) was incorporated into thermo-responsive polymeric nanogels consisted of N-isopropylacrylamide and N-(hydroxymethyl)acrylamide. Significant heat was generated from the SCC-containing nanogels under the exposure to 532-nm green laser, and resulted in cell mortality. The thermo-responsive nanogel loaded with 5-FU, an anti-cancer drug, released the drug explosively when exposed to green laser. The combination of hyperthermia and temperature-induced drug release via green laser irradiation greatly enhanced cell mortality to a maximal extent. Such photothermo-responsive nanogel possesses a great potential in anti-cancer treatment.

scholarly journals Reduction-Responsive Molecularly Imprinted Poly(2-isopropenyl-2-oxazoline) for Controlled Release of Anticancer Agents

Pharmaceutics ◽  
2020 ◽  
Vol 12 (6) ◽  
pp. 506 ◽  
Author(s):  
Michał Cegłowski ◽  
Valentin Victor Jerca ◽  
Florica Adriana Jerca ◽  
Richard Hoogenboom
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Anticancer Agents ◽  
Release Kinetics ◽  
Controlled Drug Release ◽  
Release Mechanism ◽  
Molecularly Imprinted ◽  
Responsive Materials ◽  
Future Work ◽  
Specific Trigger

Trigger-responsive materials are capable of controlled drug release in the presence of a specific trigger. Reduction induced drug release is especially interesting as the reductive stress is higher inside cells than in the bloodstream, providing a conceptual controlled release mechanism after cellular uptake. In this work, we report the synthesis of 5-fluorouracil (5-FU) molecularly imprinted polymers (MIPs) based on poly(2-isopropenyl-2-oxazoline) (PiPOx) using 3,3′-dithiodipropionic acid (DTDPA) as a reduction-responsive functional cross-linker. The disulfide bond of DTDPA can be cleaved by the addition of tris(2-carboxyethyl)phosphine (TCEP), leading to a reduction-induced 5-FU release. Adsorption isotherms and kinetics for 5-FU indicate that the adsorption kinetics process for imprinted and non-imprinted adsorbents follows two different kinetic models, thus suggesting that different mechanisms are responsible for adsorption. The release kinetics revealed that the addition of TCEP significantly influenced the release of 5-FU from PiPOx-MIP, whereas for non-imprinted PiPOx, no statistically relevant differences were observed. This work provides a conceptual basis for reduction-induced 5-FU release from molecularly imprinted PiPOx, which in future work may be further developed into MIP nanoparticles for the controlled release of therapeutic agents.

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