Studies on Preparation of Artesunate-Loaded mPEG-PLGA-Nanoparticles and Its Inhibition on K562 cells

Blood ◽  
2010 ◽  
Vol 116 (21) ◽  
pp. 4712-4712
Author(s):  
Liu Xiaoli ◽  
Shuang Wang ◽  
Qingfeng Du ◽  
Na Xu ◽  
Jun Yang ◽  
...  
Keyword(s):  
Drug Loading ◽  
In Vitro Release ◽  
K562 Cells ◽  
Plga Nanoparticles ◽  
Leukemia Cells ◽  
Human Leukemia ◽  
The Mean ◽  
Poly Ethylene ◽  
Vitro Release

Abstract Abstract 4712 The aim of the present work was to investigate the characterization of Artesunate-loaded methoxy poly (ethylene glyeol) -poly (lactic-co- glycolic acid) copolymer (mPEG-PLGA) nanoparticles and the anti-tumoral activity of the Art-Nps on human leukemia cells K562. The Artesunate (Art) poly (ethylene glyeol-lactic-co-glycolic acid) nanoparticles (Art-Nps) were prepared by modified-Spontaneous emulsion solvent diffusion method. The shape of the nanoparticles was observed by SEM. The mean diameter and the size distribution of nanoparticles were determined by laser light scattering. The drug loading efficiency, encapsulation rate and releasing behavior of Art -NPs in vitro were examined by HPLC. The effects of Art-Nps on the proliferation of K562 cells were studied by MTT assay and Hoechst staining. Artesunate loaded mPEG-PLGA nanoparticles were spheric with the mean size of (156.7±1.01)nm, zeta potential was -(26.23±1.86) mV, and the average drug loading and encapsulation efficiency were (14.5±0.2)% and (86.5±0.5)%, respectively. In vitro release behavior could be described by the Higuchi equation: Q=4.11t1/2+27.05, r=0.983. MTT assay showed different concentrations. different times of Art-Nps could inhibit the proliferation of K562 cells (P<0.01), and both have a synergistic effect (P=0.002), it showed that concentration was dependented with time, and the inhibition rate after 72h was exceeded to the the control group (P<0.05), it was showed the Art-Nps had sustained-release effect. Art-NPs of the cells (treated by 12.5μ g/m. 25μ g/ml. 50μ g/ml) resulted in significantly higher apoptosis than blank groups. The Art-NP obtained were characted with a small size and high drug loading and entrapment efficiency, in vitro release showed a good sustained-release nature, and it can inhibit the proliferation of human leukemia K562 cells in vitro, extending the time on leukemia cells. This study was provide an experimental basis for develop a new intravenous artesunate formulations. Disclosures: No relevant conflicts of interest to declare.

scholarly journals Preparation of Artesunate mPEG-PLGA Nanoparticles and Its Application to K562 Apoptosis of cells

2019 ◽  
Author(s):  
Sushil Reddy ◽  
David Gupta
Keyword(s):  
Particle Size ◽  
Drug Loading ◽  
In Vitro Release ◽  
K562 Cells ◽  
Plga Nanoparticles ◽  
Human Leukemia ◽  
Apoptotic Bodies ◽  
Vitro Release ◽  
Human Leukemia K562 Cells

AbstractThe preparation process of artesunate-loaded polyethylene glycol monomethyl ether-polylactic acid-glycolic acid affinity block copolymer (mPEG-PLGA) nanoparticles and its growth inhibition on human leukemia K562 cells were investigated. METHODS: Artesunate mPEG-PLGA nanoparticles (Art-Nps) were prepared by modified self-emulsification method. The morphology of nanoparticles was characterized by scanning electron microscopy. The particle size distribution and zeta potential were measured by laser scattering particle size analyzer. The drug loading, encapsulation efficiency and in vitro release of Art-Nps were determined by chromatography. The proliferation and apoptosis of human leukemia K562 cells were observed by MTT assay and Hoechst staining. RESULTS: Art-Nps is a spherical solid particle with smooth surface, average particle size (156.70+/-1.01) nm, zeta potential of -(26.23+/-1.86) mV, average drug loading (14.51+/-0.20)%, average package. The sealing rate was (86.51+/-0.50)%, and the in vitro release law accorded with the Higuchi equation: Q=4.11t 1/2+27.05, R2=0.98. MTT assay showed that Art-Nps inhibited the proliferation of K562 cells in a time-dose-dependent manner, and the inhibition rate exceeded the artesunate-treated group after 72h, and sustained release. The number of cells was observed after cultured with different concentrations of Art-Nps for 48h. Significantly reduced, cell size is different, irregular shape, high magnification can be seen in the nucleus pyknosis, agglutination, and apoptotic bodies, and increased apoptotic bodies with increasing concentration.

Cationic Nanoliposomes Efficiently Delivering Phenylethyl Resorcinol Produce Enhanced Skin Lightening Effect

Nano LIFE ◽  
2020 ◽  
Vol 10 (04) ◽  
pp. 2040009
Author(s):  
Tianbao Wei ◽  
Dan Chen ◽  
Hexiang Mei ◽  
Zheng Zhou ◽  
Jianyong Sheng ◽  
...  
Keyword(s):  
Drug Loading ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
B16f10 Cells ◽  
Noticeable Reduction ◽  
The Mean ◽  
Skin Lightening ◽  
Vitro Release ◽  
Transdermal Permeability

Phenylethyl resorcinol-loaded cationic nanoliposomes (PR-CLPs) were prepared and characterized. Moreover, their transdermal properties, cellular uptake, and inhibition of tyrosinase activity and melanin production in B16F10 cells were studied. The mean particle size, polydispersity index (PDI) and zeta potential of the PR-CLPs were [Formula: see text][Formula: see text]nm, [Formula: see text][Formula: see text]mV [Formula: see text][Formula: see text]mV, respectively. The drug loading efficiency (DLE) and entrapment efficiency (EE) of PR in the PR-CLPs were [Formula: see text]% and [Formula: see text]%, respectively. Sustained release of PR from the PR-CLPs was observed in vitro release experiments. The results of the in vitro transdermal experiments showed that PR-CLPs significantly improved both the retention of PR in the skin and its transdermal permeability ([Formula: see text]) in comparison with PR solution or traditional phenylethyl resorcinol nanoliposomes (PR-LPs). The uptake and accumulation of FITC-CLPs in B16F10 cells was significantly enhanced as compared with that of FITC-LPs. Furthermore, at a PR concentration of 20 or 30[Formula: see text][Formula: see text]g/mL, PR-CLPs displayed a high tyrosinase inhibitory activity and caused a noticeable reduction in the melanin content in B16F10 cells. Taken together, these results indicate that PR-CLPs can efficiently deliver phenylethyl resorcinol to produce an enhanced skin lightening effect.

Preparation and in vitro Evaluation of Bioadhesive Microparticulate System

1970 ◽  
Vol 1 (3) ◽  
pp. 257-266
Author(s):  
Nagda C. D. ◽  
Chotai N. P. ◽  
Patel S. B. ◽  
Soni T. J ◽  
Patel U. L
Keyword(s):  
Drug Loading ◽  
In Vitro Release ◽  
Phenyl Acetic Acid ◽  
Solvent Evaporation Method ◽  
Elimination Half ◽  
Release Studies ◽  
Differential Scanning Colorimetry ◽  
Polymer Interactions ◽  
Vitro Release

Aceclofenac (ACE) is NSAIDs of a phenyl acetic acid class. It is indicated in arthritis and osteoarthritis, rheumatoid arthritis, ankylosing spondylitis. It has short elimination half life of 4 hours. The objective of the study is to design, characterize and evaluate bioadhesive microspheres of ACE employing carbopol (CP) as bioadhesive polymer. Bioadhesive microspheres of ACE were prepared by solvent evaporation method. The prepared microspheres were free flowing and spherical in shape and characterized for drug loading, mucoadhesion test, infrared spectroscopy (IR), differential scanning colorimetry (DSC) and scanning electron microscopy (SEM). The in-vitro release studies were performed using pH 6.8 phosphate buffer. The drug loaded microspheres in a ratio of 1:5 showed 47% of drug entrapment; percentage mucoadhesion was 81% and 89% release in 10 h. The infrared spectra and DSC showed stable character of aceclofenac in the drug loaded microspheres and revealed the absence of drug-polymer interactions. SEM studies showed that the microspheres are spherical and porous in nature. The in vitro release profiles from microspheres of different polymer-drug ratios followed Higuchi model.

Preparation, evaluation, and in vitro release of chitosan-alginate tanshinone self-microemulsifying sustained-release microcapsules

2020 ◽  
pp. 1-9
Author(s):  
Yunhong Wang ◽  
Rong Hu ◽  
Yanlei Guo ◽  
Weihan Qin ◽  
Xiaomei Zhang ◽  
...  
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Release Rate ◽  
Orthogonal Design ◽  
Drug Loading ◽  
In Vitro Release ◽  
Core Material ◽  
Evaluation Indexes ◽  
Vitro Release

OBJECTIVE: In this study we explore the method to prepare tanshinone self-microemulsifying sustained-release microcapsules using tanshinone self-microemulsion as the core material, and chitosan and alginate as capsule materials. METHODS: The optimal preparation technology of chitosan-alginate tanshinone self-microemulsifying sustained-release microcapsules was determined by using the orthogonal design experiment and single-factor analysis. The drug loading and entrapment rate were used as evaluation indexes to assess the quality of the drug, and the in vitro release rate was used to evaluate the drug release performance. RESULTS: The best technology of chitosan-alginate tanshinone self-microemulsifying sustained-release microcapsules is as follows: the concentration of alginate is 1.5%, the ratio of tanshinone self-microemulsion volume to alginate volume to chitosan mass is 1:1:0.5 (ml: ml: g), and the best concentration of calcium chloride is 2.0%. To prepare the microcapsules using this technology, the drug loading will be 0.046%, the entrapment rate will be 80.23%, and the 24-hour in vitro cumulative release rate will be 97.4%. CONCLUSION: The release of the microcapsules conforms to the Higuchi equation and the first-order drug release model and has a good sustained-release performance.

scholarly journals Cellulose/guar gum hydrogel microspheres as a magnetic anticancer drug carrier

BioResources ◽  
2019 ◽  
Vol 14 (2) ◽  
pp. 3615-3629 ◽  
Author(s):  
Yanli Li ◽  
Yucheng Feng ◽  
Jun Jing ◽  
Fei Yang
Keyword(s):  
Anticancer Drug ◽  
Guar Gum ◽  
Drug Carrier ◽  
Drug Loading ◽  
In Vitro Release ◽  
Adsorption Effect ◽  
Magnetic Hydrogel ◽  
Vitro Release ◽  
Hydrogel Microspheres

A novel magnetic anticancer drug carrier based on cellulose, guar gum, and Fe3O4 hydrogel microspheres was synthesized by chemical crosslinking. These microspheres were crosslinked with epoxy chloropropane and loaded with 5-fluorouracil (5-fu). The effect of the ratio of cellulose to guar gum on bead size, drug loading, and in vitro release behaviors were investigated. The influence of the magnetic content on drug loading and in vitro release behaviors were also evaluated. The magnetic hydrogel microspheres were characterized via an optical microscope, Fourier transform infrared spectroscopy, swelling behavior analysis, vibrating sample magnetometer, and ultraviolet absorption spectroscopy. The results showed that as the ratio of cellulose to guar gum increased from 3:1 to 5:1, the particle size increased from 395 to 459 um. Moreover, the drug loading capacity, encapsulation efficiency, and in vitro release behavior were influenced by the ratio of cellulose/guar gum and Fe3O4 content. Finally, the Fe3O4 particle had an adsorption effect on the drug, thereby reducing the maximum cumulative release.

Calcium phosphate porous pellets as drug delivery systems: Effect of drug carrier composition on drug loading and in vitro release

2012 ◽  
Vol 32 (11) ◽  
pp. 2679-2690 ◽  
Author(s):  
Hiva Baradari ◽  
Chantal Damia ◽  
Maggy Dutreih-Colas ◽  
Etienne Laborde ◽  
Nathalie Pécout ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Calcium Phosphate ◽  
Drug Delivery Systems ◽  
Drug Carrier ◽  
Drug Loading ◽  
In Vitro Release ◽  
Delivery Systems ◽  
Vitro Release

scholarly journals Thymoquinone-Loaded Soluplus®-Solutol® HS15 Mixed Micelles: Preparation, In Vitro Characterization, and Effect on the SH-SY5Y Cell Migration

Molecules ◽  
2020 ◽  
Vol 25 (20) ◽  
pp. 4707
Author(s):  
Maria Camilla Bergonzi ◽  
Marzia Vasarri ◽  
Giulia Marroncini ◽  
Emanuela Barletta ◽  
Donatella Degl’Innocenti
Keyword(s):  
Cell Migration ◽  
Load Capacity ◽  
Drug Loading ◽  
Neuroblastoma Cell ◽  
In Vitro Release ◽  
Human Neuroblastoma Cell ◽  
Prolonged Release ◽  
Human Neuroblastoma ◽  
Vitro Release

Thymoquinone (TQ) is the main active ingredient of Nigella sativa essential oil, with remarkable anti-neoplastic activities with anti-invasive and anti-migratory abilities on a variety of cancer cell lines. However, its poor water solubility, high instability in aqueous solution and pharmacokinetic drawbacks limits its use in therapy. Soluplus® and Solutol® HS15 were employed as amphiphilic polymers for developing polymeric micelles (SSM). Chemical and physical characterization studies of micelles are reported, in terms of size, homogeneity, zeta potential, critical micelle concentration (CMC), cloud point, encapsulation efficiency (EE%), load capacity (DL), in vitro release, and stability. This study reports for the first time the anti-migratory activity of TQ and TQ loaded in SSM (TQ-SSM) in the SH-SY5Y human neuroblastoma cell line. The inhibitory effect was assessed by the wound-healing assay and compared with that of the unformulated TQ. The optimal TQ-SSM were provided with small size (56.71 ± 1.41 nm) and spherical shape at ratio of 1:4 (Soluplus:Solutol HS15), thus increasing the solubility of about 10-fold in water. The entrapment efficiency and drug loading were 92.4 ± 1.6% and 4.68 ± 0.12, respectively, and the colloidal dispersion are stable during storage for a period of 40 days. The TQ-SSM were also lyophilized to obtain a more workable product and with increased stability. In vitro release study indicated a prolonged release of TQ. In conclusion, the formulation of TQ into SSM allows a bio-enhancement of TQ anti-migration activity, suggesting that TQ-SSM is a better candidate than unformulated TQ to inhibit human SH-SY5Y neuroblastoma cell migration.

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