scholarly journals Cisplatin-Loaded Polybutylcyanoacrylate Nanoparticles with Improved Properties as an Anticancer Agent

2019 ◽  
Vol 20 (7) ◽  
pp. 1531 ◽  
Author(s):  
Seyed Alavi ◽  
Sitah Muflih Al Harthi ◽  
Hasan Ebrahimi Shahmabadi ◽  
Azim Akbarzadeh
Keyword(s):  
Lung Cancer ◽  
Drug Release ◽  
Drug Loading ◽  
Release Profile ◽  
Therapeutic Effects ◽  
Drug Release Profile ◽  
Standard Drug ◽  
Loading Efficiency ◽  
Drug Loading Efficiency

This study aims to improve the cytotoxicity and potency of cisplatin-loaded polybutylcyanoacrylate (PBCA) nanoparticles (NPs) for the treatment of lung cancer through the modulation of temperature and polyethylene glycol (PEG) concentration as effective factors affecting the NPs’ properties. The NPs were synthesized using an anionic polymerization method and were characterized in terms of size, drug loading efficiency, drug release profile, cytotoxicity effects, drug efficacy, and drug side effects. In this regard, dynamic light scattering (DLS), scanning electron microscopy (SEM), 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) methods, and hematoxylin and eosin (H&E) staining were used. The results showed that the size and the drug loading efficiency of the synthesized spherical NPs were 355–386 nm and 14–19%, respectively. Also, the drug release profile showed a controlled and slow drug release pattern with approximately 10% drug release over 48 h. In addition, the NPs significantly increased the cytotoxicity of the cisplatin in vitro environment by approximately 2 times and enhanced the therapeutic effects of the drug in vivo environment by increasing the survival time of lung-cancer-bearing mice by 20% compared to the standard drug receiver group. Also, the nanoformulation decreased the drug toxicity in an in vivo environment. According to the results, increasing the temperature and PEG concentration improved the properties of the drug loading efficiency, drug release profile, and cytotoxicity effect of drug-loaded NPs. Consequently, the synthesized formulation increased the survival of tumor-bearing mice and simultaneously decreased the cisplatin toxicity effects. In conclusion, the prepared nanoformulation can be considered a promising candidate for further evaluation for possible therapeutic use in the treatment of lung cancer.

scholarly journals Preparation, Characterization, and Evaluation of Cisplatin-Loaded Polybutylcyanoacrylate Nanoparticles with Improved In Vitro and In Vivo Anticancer Activities

2020 ◽  
Vol 13 (3) ◽  
pp. 44 ◽  
Author(s):  
Mohsen Ghaferi ◽  
Samar Amari ◽  
Bhalchandra Vivek Mohrir ◽  
Aun Raza ◽  
Hasan Ebrahimi Shahmabadi ◽  
...  
Keyword(s):  
Drug Release ◽  
Kidney Cancer ◽  
Drug Loading ◽  
Drug Candidate ◽  
Therapeutic Effects ◽  
Anticancer Activities ◽  
Drug Release Profile ◽  
Cytotoxicity Effects

This study aimed to evaluate the therapeutic efficacy of the cisplatin encapsulated into polybutylcyanoacrylate (PBCA) nanoparticles for the treatment of kidney cancer. The nanoformulation was successfully developed using the miniemulsion polymerization method and characterized in terms of size, size distribution, drug loading and encapsulation efficiencies, drug release behavior, in vitro cytotoxicity effects, in vivo toxicity, and therapeutic effects. Cisplatin-loaded PBCA nanoparticles were confirmed to be in nanoscale with the drug entrapment efficiency of 23% and controlled drug release profile, in which only 9% of the loaded drug was released after 48 h. The nanoparticles caused an increase in the cytotoxicity effects of cisplatin against renal cell adenocarcinoma cells (ACHN) (2.3-fold) and considerably decreased blood urea nitrogen and creatinine concentrations when compared to the standard cisplatin (1.6-fold and 1.5-fold, respectively). The nanoformulation also caused an increase in the therapeutic effects of cisplatin by 1.8-fold, in which a reduction in the mean tumor size was seen (3.5 mm vs. 6.5 mm) when compared to the standard cisplatin receiver rats. Overall, cisplatin-loaded PBCA nanoparticles can be considered as a promising drug candidate for the treatment of kidney cancer due to its potency to reduce the side effects of cisplatin and its toxicity and therapeutic effects on cancer-bearing Wistar rats.

scholarly journals Targeted and modular architectural polymers employing bioorthogonal chemistry for quantitative therapeutic delivery

2020 ◽  
Vol 11 (12) ◽  
pp. 3268-3280 ◽  
Author(s):  
Gayathri R. Ediriweera ◽  
Joshua D. Simpson ◽  
Adrian V. Fuchs ◽  
Taracad K. Venkatachalam ◽  
Matthias Van De Walle ◽  
...  
Keyword(s):  
Side Effects ◽  
Cancer Therapy ◽  
Drug Release ◽  
Standard Of Care ◽  
Release Profile ◽  
Specific Drug ◽  
Bioorthogonal Chemistry ◽  
Drug Release Profile ◽  
Therapeutic Delivery

There remain several key challenges to existing therapeutic systems for cancer therapy, such as quantitatively determining the true, tissue-specific drug release profile in vivo, as well as reducing side-effects for an increased standard of care.

scholarly journals Drug Release from a Spherical Matrix: Theoretical Analysis for a Finite Dissolution Rate Affected by Geometric Shape of Dispersed Drugs

Pharmaceutics ◽  
2020 ◽  
Vol 12 (6) ◽  
pp. 582
Author(s):  
Yung-Sheng Lin ◽  
Ruey-Yug Tsay
Keyword(s):  
Drug Release ◽  
Release Rate ◽  
Shape Factor ◽  
Numerical Solutions ◽  
Drug Loading ◽  
Spherical Geometry ◽  
Detailed Comparison ◽  
Release Profile ◽  
Drug Release Profile ◽  
Drug Release Rate

Amending the neglect of finite dissolution in traditional release models, this study proposed a more generalized drug release model considering the simultaneous dissolution and diffusion procedure from a drug-loaded spherical matrix. How the shape factor (n = 0, 1/2, and 2/3 for the planar, cylindrical, and spherical geometry, respectively) of dispersed drug particles affected the release from the matrix was examined for the first time. Numerical solutions of this generalized model were validated by consensus with a short-time analytical solution for planar drugs and by the approach of the diffusion-controlled limits with Higuchi’s model. The drug release rate increases with the ratio of dissolution/diffusion rate (G) and the ratio of solubility/drug loading (K) but decreases with the shape factor of drug particles. A zero-order release profile is identified for planar drugs before starting the surface depletion layer, and also found for cylindrical and spherical dispersed drugs when K and G are small, i.e. the loaded drug is mainly un-dissolved and the drug release rate is dissolution-controlled. It is also shown that for the case of a small G value, the variation of drug release profile, due to the drug particle geometry, becomes prominent. Detailed comparison with the results of the traditional Higuchi’s model indicates that Higuchi’s model can be applied only when G is large because of the assumption of an instantaneous dissolution. For K = 1/101–1/2, the present analysis suggests an error of 33–85% for drug release predicted by Higuchi’s model for G = 100, 14–44% error for G = 101, while a less than 5% error for G ≧ 103.

Well-defined diblock brush polymer–drug conjugates for sustained delivery of paclitaxel

2015 ◽  
Vol 3 (7) ◽  
pp. 1078-1084 ◽  
Author(s):  
Jiong Zou ◽  
Yun Yu ◽  
Yukun Li ◽  
Wei Ji ◽  
Chih-Kuang Chen ◽  
...  
Keyword(s):  
Drug Release ◽  
Release Profile ◽  
Therapeutic Effects ◽  
Sustained Delivery ◽  
Drug Release Profile ◽  
Drug Conjugates ◽  
Brush Polymer ◽  
Polymer Drug Conjugates

The synthesis, characterization and property studies of paclitaxel (PTXL)-containing brush polymer–drug conjugates (BPDCs) are presented and the influence of grafting structures of BPDCs on their assembly behaviour, drug release profile and therapeutic effects is discussed in this article.

Preparation and Properties of PLA Microspheres Containing ENRO by an S/O/W Emulsion Technique

2011 ◽  
Vol 335-336 ◽  
pp. 1439-1442 ◽  
Author(s):  
Yu Yan Zhou ◽  
Gui Yu Li ◽  
Hong Xia Wang ◽  
Lei Tao ◽  
Jian Ping Liang
Keyword(s):  
High Performance ◽  
Drug Loading ◽  
Controlled Drug Release ◽  
Poly Lactic Acid ◽  
Modified Technique ◽  
Loading Efficiency ◽  
Oil In Water ◽  
Drug Loading Efficiency

In the present paper, monodisperse poly(lactic acid) (PLA) microspheres (MS) containing the enrofloxacin (ENRO), were manufactured by using a modified solid in oil in water (S/O/W) emulsion solvent evaporation method. In order to prepare PLA microspheres with a higher drug loading efficiency by this modified technique, the test of stability and productivity of the primary emulsion was preliminary examined by change species or concentration of the oil-soluble surfactant and the ratio of water and organic solvent. Firstly, enrofloxacin polylactic acid microspheres (ENRO-PLA-MS) were producted, then the morphology and particle size distribution were estimated by scanning electron microscopy (SEM), its encapsulation efficiency and drug loading efficiency were assessed by High performance liquid chromatography (HPLC). In vivo conditions were simulated by an stable release buffer to obtain a detailed release and polymer degradation profile. Consequently, the ENRO-PLA-MS had a denser structure with a smooth, pore-free surface, the preparation of microspheres was simple, the prepared microspheres had excellent controlled drug release characteristics in vitro.

scholarly journals Release profile and characteristics of electrosprayed particles for oral delivery of a practically insoluble drug

2012 ◽  
Vol 9 (75) ◽  
pp. 2437-2449 ◽  
Author(s):  
Adam Bohr ◽  
Jakob Kristensen ◽  
Mark Dyas ◽  
Mohan Edirisinghe ◽  
Eleanor Stride
Keyword(s):  
Drug Release ◽  
Oral Delivery ◽  
Drug Loading ◽  
Chemical Properties ◽  
Processing Parameters ◽  
Solute Concentration ◽  
Release Profile ◽  
Drug Release Profile ◽  
Physico Chemical ◽  
Dissolution Apparatus

Poly(lactic-co-glycolic acid) (PLGA) microspheres containing celecoxib were prepared via electrospraying, and the influence of three processing parameters namely flow rate, solute concentration and drug loading, on the physico-chemical properties of the particles and the drug-release profile was studied. Microspheres with diameters between 2 and 8 μm were produced and a near-monodisperse size distribution was achieved (polydispersivity indices of 6–12%). Further, the inner structure of the particles showed that the internal porosity of the particles increased with increasing solvent concentration. X-ray powder diffraction (XRPD) analysis indicated that the drug was amorphous and remained stable after eight months of storage. Drug release was studied in USP 2 (United States Pharmacopeia Dissolution Apparatus 2) dissolution chambers, and differences in release profiles were observed depending on the parametric values. Changes in release rate were found to be directly related to the influence of the studied parameters on particle size and porosity. The results indicate that electrospraying is an attractive technique for producing drug-loaded microspheres that can be tailored towards an intended drug-delivery application. Compared with the more conventional spray-drying process, it provides better control of particle characteristics and less aggregation during particle formation. In particular, this study demonstrated its suitability for preparing capsules in which the drug is molecularly dispersed and released in a sustained manner to facilitate improved bioavailability.

scholarly journals Studies on the Drug Loading and Release Profiles of Degradable Chitosan-Based Multilayer Films for Anticancer Treatment

Cancers ◽  
2020 ◽  
Vol 12 (3) ◽  
pp. 593 ◽  
Author(s):  
Hyeongdeok Sun ◽  
Daheui Choi ◽  
Jiwoong Heo ◽  
Se Yong Jung ◽  
Jinkee Hong
Keyword(s):  
Drug Release ◽  
Multilayer Film ◽  
Drug Loading ◽  
Building Blocks ◽  
Multilayer Films ◽  
Release Profile ◽  
Layer By Layer ◽  
Drug Release Profile ◽  
Sustained Drug Release ◽  
Release Profiles

This study demonstrates the possibility of developing a rapidly degradable chitosan-based multilayer film for controlled drug release. The chitosan (CHI)-based multilayer nanofilms were prepared with three different types of anions, hyaluronic acid (HA), alginic acid (ALG) and tannic acid (TA). Taking advantage of the Layer-by-Layer (LBL) assembly, each multilayer film has different morphology, porosity and thickness depending on their ionic density, molecular structure and the polymer functionality of the building blocks. We loaded drug models such as doxorubicin hydrochloride (DOX), fluorescein isothiocyanate (FITC) and ovalbumin (Ova) into multilayer films and analyzed the drug loading and release profiles in phosphate-buffered saline (PBS) buffer with the same osmolarity and temperature as the human body. Despite the rapid degradation of the multilayer film in a high pH and salt solution, the drug release profile can be controlled by increasing the functional group density, which results in interaction with the drug. In particular, the abundant carboxylate groups in the CHI/HA film increased the loading amount of DOX and decreased rapid drug release. The TA interaction with DOX via electrostatic interaction, hydrogen bonding and hydrophobic interaction showed a sustained drug release profile. These results serve as principles for fabricating a tailored multilayer film for drug delivery application.

scholarly journals Influence of Terpene Type on the Release from an O/W Nanoemulsion: Experimental and Theoretical Studies

Molecules ◽  
2020 ◽  
Vol 25 (12) ◽  
pp. 2747 ◽  
Author(s):  
Małgorzata Miastkowska ◽  
Paweł Śliwa
Keyword(s):  
Molecular Dynamics ◽  
Drug Release ◽  
Ursolic Acid ◽  
Drug Loading ◽  
In Vitro Release ◽  
Perillyl Alcohol ◽  
Release Profile ◽  
Theoretical Studies ◽  
Drug Release Profile ◽  
Experimental And Theoretical Studies

The interaction between a drug molecule and its carrier’s components is an important factor which influences the drug release profile. For this purpose, molecular dynamics (MD) may be the in silico tool which can help to understand the mechanism of drug loading/release. The aim of this work is to explain the effect of interactions between different types of terpenes, namely perillyl alcohol, forskolin, ursolic acid, and the nanoemulsion droplet core, on the release by means of experimental and theoretical studies. The basic nanoemulsion was composed of caprylic/capric triglyceride as the oil phase, polysorbate 80 as the emulsifier, and water. The in vitro release tests from a terpene-loaded nanoemulsion were carried out to determine the release profiles. The behavior of terpenoids in the nanoemulsion was also theoretically investigated using the molecular dynamics method. The forskolin-loaded nanoemulsion showed the highest percentage of drug release (almost 80% w/w) in contrast to ursolic acid and perillyl alcohol-loaded nanoemulsions (about 53% w/w and 19% w/w, respectively). The results confirmed that the kinetic model of release was terpene-type dependent. The zero-order model was the best to describe the ursolic acid release profile, while the forskolin and the perillyl alcohol followed a first-order and Higuchi model, respectively. Molecular dynamics simulations, especially energetical analysis, confirmed that the driving force of terpenes diffusion from nanoemulsion interior was their interaction energy with a surfactant.

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