PEG-PLGA Nanoparticles Entrapping Doxorubicin Reduced Doxorubicin-Induced Cardiotoxicity in Rats

2014 ◽  
Vol 912-914 ◽  
pp. 263-268 ◽  
Author(s):  
Jin Ning Mao ◽  
Ai Jun Li ◽  
Liang Ping Zhao ◽  
Lan Gao ◽  
Wei Ting Xu ◽  
...  
Keyword(s):  
Drug Loading ◽  
Entrapment Efficiency ◽  
Average Diameter ◽  
Plga Nanoparticles ◽  
Heart Weight ◽  
Loading Capacity ◽  
Group Level ◽  
Clinical Utilization ◽  
Sd Rats ◽  
Plga Nanoparticle

Aim:Doxorubicin-induced cardiotoxicity limited its clinical utilization in oncology. In this study, Dox was entrapped into PEG-PLGA Nanoparticles, cardiotoxicity of Dox or PEG-PLGA-Dox was investigated in rats. Materials and methods :PEG-PLGA-Dox was prepared via modified single emulsion method. Its characterization including size, Drug loading capacity (DLC), entrapment efficiency (EE) were estimated. The cardiotoxicity of PEG-PLGA-Dox was assessed on SD rats via echocardiography and biochemical indicators compare to free Dox and physical sodium. Results:The average diameter of PEG-PLGA-Dox is around 200 nm, with DLC about 10%.After administered PEG-PLGA-Dox, the ratio of heart weight to body weight decreased not as significant as Dox group, level of serum parameters and echocardiography parameter also decreased little compared to the Dox group. Conclusions:After entrapped into PEG-PLGA nanoparticle, Dox-induced cardiotoxicity was reduced significantly.

PEG-PLGA Nanoparticle Modified by Transferrin Loading Doxorubicin: In Vitro and In Vivo Studies for Glioma

2013 ◽  
Vol 750-752 ◽  
pp. 1643-1650 ◽  
Author(s):  
Guo Dong Liu ◽  
Jin Ning Mao ◽  
Tao Sun ◽  
Zhen Jiang ◽  
Jun Dong ◽  
...  
Keyword(s):  
Mtt Assay ◽  
Drug Loading ◽  
Entrapment Efficiency ◽  
Average Diameter ◽  
C6 Glioma ◽  
C6 Glioma Cells ◽  
Hplc Assay ◽  
Plga Nanoparticle

Purpose A biodegradable PEG-PLGA nanoparticle (NP) modified by transferrin (Tf) was conceived. Doxorubicin (Dox), a widely used antitumor agent, without passing through the BBB, which limited its utility on glioma, was encapsulated inside (Tf-NP-Dox). Furthermore, its therapeutic efficacy to glioma was evaluated both in vitro and in vivo. Methods Tf-NP-Dox was prepared via modified single emulsion method. Its characterization including size, Drug loading capacity (DLC), entrapment efficiency (EE), Tf number on Tf-NP-Dox surface were estimated. The antitumor efficiency in vitro was evaluated via MTT assay. The transmembrane transportation was evaluated via HPLC assay. The antitumor efficiency in vivo was assessed on C6 glioma intracranial implant rats model. Results The average diameter of Tf-NP-Dox is around 200 nm with surface Tf molecule number per Tf-NP-Dox approximately 25. MTT assay demonstrated stronger cytotoxicity of Tf-NP-Dox to C6 glioma cells (P<0.01). HPLC assay showed Tf-NP-Dox transport Dox into C6 with higher efficiency compare to NP-Dox or Dox (P<0.01). On C6 glioma bearing rat, Tf-NP-Dox could transport more Dox into tumors tested by HPLC assay (P<0.05), and extended life span markedly compared to NP-Dox or Dox (P<0.05). Conclusions Tf-NP-Dox had a potential of glioma targeting and had a better therapeutic effect to glioma both in vitro and in vivo.

Photodynamic Treatment of Colorectal Cancer Using Chlorin e6-Loaded Poly(lactide-co-glycolide)- Based Nanoparticles

2021 ◽  
Vol 17 (10) ◽  
pp. 1939-1950
Author(s):  
Beibei Lin ◽  
Xuegu Xu ◽  
Xiaobi Zhang ◽  
Yinfei Yu ◽  
Xiaoling Wang
Keyword(s):  
Colorectal Cancer ◽  
Drug Loading ◽  
Average Diameter ◽  
Plga Nanoparticles ◽  
Chlorin E6 ◽  
Photodynamic Treatment ◽  
Hct 116 ◽  
Hct 116 Cells ◽  
The Stability

We prepared poly(lactide-co-glycolide) (PLGA) encapsulated with chlorin e6 (Ce6) in an effort to increase the stability and efficiency of photosensitizers for photodynamic therapy (PDT). We determined that Ce6-loaded PLGA nanoparticles (PLGA-Ce6 NPs) had drug-loading efficiency of 5%. The efficiency of encapsulation was 82%, the zeta potential was- 25 mV, and the average diameter was 130 nm. The encapsulation of Ce6 in PLGA nanoparticles showed excellent stability. The nanoparticles exhibited sustained Ce6 release profiles with 50% released at the end of 3 days, whereas free Ce6 showed rapid release within 1 day. Ce6 release patterns were controlled by encapsulation into PLGA. The uptake of PLGA-Ce6 NPs was significantly enhanced by endocytosis in the first 8 hours in the HCT-116 cell line. An intracellular reactive oxygen species assay revealed the enhanced uptake of the nanoparticles. An in vitro anti-tumor activity assay showed that the PLGA-Ce6 NPs exhibited enhanced phototoxicity toward HCT-116 cells and a slightly lower IC50 value in HCT-116 cells than Ce6 solution alone. Exposure of HCT-116 cell spheroids to PLGA-Ce6 NPs penetrated more profoundly and had better phototoxicity than pure drugs. These findings suggest that PLGA-Ce6 NPs might serve as PDT for colorectal cancer.

INFLUENCE OF SELECTED VARIABLES ON FABRICATION OF MUPIROCIN LOADED PLGA NANOCARRIERS

INDIAN DRUGS ◽  
2017 ◽  
Vol 54 (05) ◽  
pp. 67-71
Author(s):  
R. K Panik ◽  
◽  
M. R Singh ◽  
D. Singh
Keyword(s):  
Particle Size ◽  
Surfactant Concentration ◽  
Drug Loading ◽  
Entrapment Efficiency ◽  
Plga Nanoparticles ◽  
Independent Variables ◽  
Nanoprecipitation Method ◽  
Dependent Variables ◽  
Effective Delivery ◽  
Polymer Ratio

Aim of the study was to develop PLGA nanoparticles (PLGA-NP) of mupirocin (MP) and to study the effect of independent variables in order to optimize the formulation for effective delivery. Drug loaded PLGA-NPs were successfully prepared by nanoprecipitation method and characterized by mean particle size, zeta potential, entrapment efficiency, drug loading, drug release, TEM, and DSC study. Independent variables like drug-polymer ratio, surfactant concentration, and stirring speed showed significant effect on the dependent variables like particle size, entrapment efficiency and drug loading. The ANOVA results showed that selected independent variables had a significant effect on the preparation of mupirocin loaded PLGA-NP.

Utilization of Microfluidics for the Preparation of Polymeric Nanoparticles for the Antioxidant Rutin: A Comparison with Bulk Production

2019 ◽  
Vol 7 (6) ◽  
pp. 469-483 ◽  
Author(s):  
Hanh T.H. Vu ◽  
Sarah Streck ◽  
Sarah M. Hook ◽  
Arlene McDowell
Keyword(s):  
Solid State ◽  
Polymeric Nanoparticles ◽  
Drug Loading ◽  
Entrapment Efficiency ◽  
Production Method ◽  
Plga Nanoparticles ◽  
Burst Release ◽  
Biorelevant Media ◽  
Nanoprecipitation Method ◽  
Bulk Production

Objective: To compare the characteristics of rutin-loaded PLGA (poly(lactic-coglycolic acid)) nanoparticles prepared using a single emulsion evaporation method (bulk method) and a nanoprecipitation method using microfluidics. Method: Rutin-loaded PLGA nanoparticles were produced using different methods and characterized for size, zeta potential, entrapment efficiency (EE) and drug loading (DL). A design of experiments approach was used to identify the effect of method parameters to optimize the formulation. DSC was used to investigate the solid-state characteristics of rutin and PLGA and identify any interactions in the rutin-loaded PLGA nanoparticles. The release of rutin from PLGA nanoparticles was examined in biorelevant media and phosphate buffer (PBS). Results : The optimal formulation of rutin-loaded PLGA nanoparticles produced using a microfluidics method resulted in a higher entrapment efficiency of 34 ± 2% and a smaller size of 123 ± 4 nm compared to a bulk method (EE 27 ± 1%, size 179 ± 13 nm). The solidstate of rutin and PLGA changed from crystalline to amorphous with the preparation of rutin- loaded PLGA nanoparticles. More importantly, using microfluidics, rutin released faster from rutin-loaded PLGA nanoparticles in biorelevant media and PBS with higher burst release compared to the rutin release from the nanoparticles prepared by using the bulk method. Conclusion: Rutin can be encapsulated in nanoparticles formulated with different methods with mean sizes of less than 200 nm. Microfluidics produced more uniform rutin-loaded PLGA nanoparticles with a higher EE, DL and faster release compared to a bulk production method.

Preparation and Characterization of PEGylated Iron Oxide-Gold Nanoparticles for Delivery of Sulforaphane and Curcumin

Drug Research ◽  
2017 ◽  
Vol 67 (12) ◽  
pp. 698-704 ◽  
Author(s):  
Hossein Danafar ◽  
Ali Sharafi ◽  
Sonia Askarlou ◽  
Hamidreza Manjili
Keyword(s):  
Cell Line ◽  
Water Solubility ◽  
Drug Loading ◽  
In Vitro Study ◽  
Entrapment Efficiency ◽  
Breast Adenocarcinoma ◽  
Therapeutic Effects ◽  
Loading Capacity ◽  
Au Nps

AbstractNatural products have been used for the treatment of various diseases such as cancer. Curcumin (CUR) and sulforaphane (SF) have anti-cancer effects, but their application is restricted because of their low water solubility and poor oral bioavailability. To improve the bioavailability and solubility of SF and CUR, we performed an advanced delivery of SF and CUR with PEGylated gold coated Fe3O4 magnetic nanoparticles (PEGylated Fe3O4@Au NPs) to endorse SF and CUR maintenance as an effective and promising antitumor drugs. The structure of the synthesized nanocarrieris evaluated by, transmission electron microscopy (TEM) and Fourier transform infrared spectroscopy (FT-IR). The results revealed that the size of NPs was 20 nm. They were mono-dispersed in water, with high drug-loading capacity and stability. CUR and SF were encapsulated into NPs with loading capacity of 16.32±0.023% and 15.74±0.015% and entrapment efficiency of 74.57±0.14% and 72.20±0.18% respectively. The in-vitro study of SF and CUR loaded PEGylated Fe3O4@Au NPs on human breast adenocarcinoma cell line (SK-BR-3) confirmed that cytotoxicity of SF and CUR can enhance when they are loaded on PEGylated Fe3O4@Au NPs in comparison to Free SF and void CUR. The results of flow cytometry and real-time PCR shown that nano-carriers can increase therapeutic effects of SF and CUR by apoptosis and necrosis induction as well as inhibiting of migration in SK-BR-3 cell line.

Optimization of Curcuminoid-Loaded PLGA Nanoparticles Using Box-Behnken Statistical Design

2015 ◽  
Vol 33 ◽  
pp. 60-71 ◽  
Author(s):  
Praewpun Boonyasirisri ◽  
Ubonthip Nimmannit ◽  
Pranee Rojsitthisak ◽  
Settapon Bhunchu ◽  
Pornchai Rojsitthisak
Keyword(s):  
Particle Size ◽  
Curcuma Longa ◽  
Statistical Design ◽  
Entrapment Efficiency ◽  
Plga Nanoparticles ◽  
Molar Ratio ◽  
Diffusion Method ◽  
Alkaline Solutions ◽  
Loading Capacity ◽  
Spontaneous Emulsification

Curcuminoids are a mixture of phenolic compounds isolated from Curcuma longa L. (turmeric) rhizomes that possess antioxidant, anti-inflammatory, anti-Alzheimer and anticancer activities. However, curcuminoids have poor solubility in acid and neutral solutions, rapid decomposition in neutral and alkaline solutions, and low bioavailability that limits their use as therapeutic agents. To overcome these problems, statistical design for preparation and characterization of poly(D,L-lactide-co-glycolide) (PLGA) nanoparticles as a carrier for curcuminoids was evaluated in this study. The curcuminoid-loaded PLGA nanoparticles were prepared by a modified spontaneous emulsification solvent diffusion method using polyvinyl alcohol (PVA) as a stabilizer. The formulations were optimized using three-factor, three-level Box-Behnken experimental design. The independent variables in the formulations were the lactide/glycolide (LA/GA) molar ratio of PLGA (50:50 to 85:15), the curcuminoid concentration (2%-10%, w/v), and the PVA concentration (3%-7%, w/v). The dependent variables were particle size, loading capacity and entrapment efficiency. Statistical evaluation showed that the LA/GA molar ratio of PLGA and the curcuminoid and PVA concentrations all affected the characteristics of the PLGA nanoparticles. To achieve a minimum particle size and maximum loading capacity and entrapment efficiency, the optimal formulation of the curcuminoid-loaded PLGA nanoparticles had a LA/GA molar ratio of PLGA of 50:50, 10% (w/v) curcuminoids, and 3% (w/v) PVA. A sustainable in vitro release profile of curcuminoids was obtained from this optimal formulation.

Preparation and Properties of 5-Fluorouracil-Loaded Chitosan Microspheres for the Intranasal Administration

Drug Research ◽  
2018 ◽  
Vol 68 (12) ◽  
pp. 673-679 ◽  
Author(s):  
Wanqing Li ◽  
Hongyuan Ba ◽  
Peng Huang ◽  
Aiping Zheng ◽  
Xi Yang
Keyword(s):  
Intranasal Administration ◽  
Drug Loading ◽  
Entrapment Efficiency ◽  
Average Diameter ◽  
Orthogonal Experimental Design ◽  
Preparation Technique ◽  
Drug Release Profile ◽  
Chitosan Microspheres ◽  
Release Characteristic

Abstract Objective To study the preparation technique of 5-fluorouracil and the release characteristic of 5-fluorouracil-loaded chitosan microspheres for the intranasal administration. Methods 5-fluorouracil-loaded chitosan microspheres were prepared by emulsion chemical cross-link technique. The orthogonal experimental design was used to optimize the preparation procedure. Dynamic dialysis method was applied to determine the release characteristic of microspheres in vitro and its influencing factors. Swelling behavior was expressed by swelling ratio. The degree of mucoadhesion was investigated by determining the mucociliary transport rate(MTR) of the microparticle across a frog palate. Results Microspheres with a good shape and narrow size distribution were prepared. The average diameter was 43±4 μm. The drug loading was (38.5±1.0) %. The entrapment efficiency was (79.0±1.8) %. The drug release profile in vitro could be described by Higuichi eqution as Q=0.1035t1/2+0.0284 (r=0.9965). Chitosan had good mucoadhesive property and caused a significant reduction in MTR(P<0.01). Conclusion The optimized technique has a good reproducibility and a high entrapment efficiency, so it could be used to prepare 5-fluorouracil-loaded chitosan microspheres for the intranasal administration.Chitosan is a good material for nasal preparation and has prospective development in the pharmaceutical field.

scholarly journals Preparation and In vitro Evaluation of Isoniazid-Containing Dex-HEMA-Co-PNIPAAm Nanogels

2015 ◽  
Vol 37 ◽  
pp. 55 ◽  
Author(s):  
Maryam Jafari ◽  
Babak Kaffashi
Keyword(s):  
Drug Loading ◽  
Antimicrobial Properties ◽  
Entrapment Efficiency ◽  
Loading Capacity ◽  
In Vitro Drug Release ◽  
E Coli ◽  
Toxic Product ◽  
Good Biocompatibility ◽  
Characteristic Features

In this work, Dex-HEMA-Co-PNIPAAm nanogels containing Isoniazid antibiotic were made. Characteristic features of nanogels were studied by Fourier transform infrared spectroscopy (FTIR), dynamic light scattering (DLS) and scanning electron microscopy (SEM). Drug loading capacity and entrapment efficiency were determined. In vitro drug release amount was estimated at room and body temperature. Biocompatibility of gels was investigated through cytotoxicity assay. Finally antimicrobial properties of synthesized gels were studied. It was shown from the experimental data that the nanogels size after drug loading increased about 1-2%. %Isoniazid loading and %entrapment efficiency were in the range of 15-22% and 37-48% respectively. After 10 days of degradation ca. 80% at 25ºC and ca. 90% at 37ºC of the nanogel structures were destructed. No significant toxic product produced while degradation and all nanogels depicted good biocompatibility. No antimicrobial features observed through the test condition against gram negative E Coli.

scholarly journals GENERATION DEPENDENT TARGETING POTENTIAL OF DONEPEZIL LOADED POLY (PROPYLENEIMINE) DENDRIMER THROUGH GOAT NASAL MUCOSA

2018 ◽  
Vol 10 (12) ◽  
pp. 80
Author(s):  
Nitin Dwivedi ◽  
Balak Das Kurmi ◽  
Prashant Kesharwani ◽  
Jigna Shah
Keyword(s):  
Drug Delivery ◽  
Sustained Release ◽  
Nasal Mucosa ◽  
Ex Vivo ◽  
Drug Loading ◽  
Entrapment Efficiency ◽  
Loading Capacity ◽  
Franz Diffusion Cell ◽  
Nano Drug Delivery ◽  
Ex Vivo Study

Objective: In the domain of nano drug delivery, dendrimers are the most explored bioactive polymeric carrier system. The present work was aimed to study the diffusion potential of different generations of Poly (propyleneimine) (PPI) dendrimers on goat nasal mucosa in an ex vivo study and synthesize a stable dendrimer for olfactory drug delivery.Methods: The generations (3.0G, 4.0G, and 5.0G) of PPI dendrimer were synthesized, and PEGylated by MPEG 5000 and then loaded with donepezil. A comparative study was carried out among all generations in term of their drug loading capacity, stability, sustained release behaviour as well as for targeting efficacy. An ex-vivo study was carried out on Franz Diffusion Cell with goat nasal mucosa.Results: The developed G3, G4, and G5 dendrimerformulations had entrapment efficiency of 24.33±0.56%, 40.12±0.62%, and 60.4±0.6%, respectively. The nasal diffusion study revealed that 5.0G PPI dendrimer increased diffusion of donepezil up to 47% as compared to the pure solution of donepezil while 10% improvement in diffusion was seen as compared to 4.0 G PPI dendrimer. Thus obtained results claimed that the drug loading as well as targeting potential of PPI dendrimers increased with the increase in the number of generation. The investigation outcome indicated promising results of 5.0G PPI dendrimer over the 3.0G and 4.0G PPI dendrimer generations for their drug loading capacity, stability, and sustained release action.Conclusion: The 5.0G PPI dendrimer proved its superior candidature over the other lower generations of PPI dendrimers for drug delivery and drug targeting.

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