scholarly journals Optimization of Hemoglobin Encapsulation within PLGA Nanoparticles and Their Investigation as Potential Oxygen Carriers

Pharmaceutics ◽  
2021 ◽  
Vol 13 (11) ◽  
pp. 1958
Author(s):  
Clara Coll-Satue ◽  
Michelle Maria Theresia Jansman ◽  
Peter Waaben Thulstrup ◽  
Leticia Hosta-Rigau
Keyword(s):  
Double Emulsion ◽  
Entrapment Efficiency ◽  
Cd Spectroscopy ◽  
Plga Nanoparticles ◽  
Loading Capacity ◽  
Oxygen Carriers ◽  
Solvent Evaporation Method ◽  
Donor Blood ◽  
Composition And Structure ◽  
Potential Oxygen

Hemoglobin (Hb)-based oxygen carriers (HBOCs) display the excellent oxygen-carrying properties of red blood cells, while overcoming some of the limitations of donor blood. Various encapsulation platforms have been explored to prepare HBOCs which aim to avoid or minimize the adverse effects caused by the administration of free Hb. Herein, we entrapped Hb within a poly(lactide-co-glycolide) (PLGA) core, prepared by the double emulsion solvent evaporation method. We study the effect of the concentrations of Hb, PLGA, and emulsifier on the size, polydispersity (PDI), loading capacity (LC), and entrapment efficiency (EE) of the resulting Hb-loaded PLGA nanoparticles (HbNPs). Next, the ability of the HbNPs to reversibly bind and release oxygen was thoroughly evaluated. When needed, trehalose, a well-known protein stabilizer that has never been explored for the fabrication of HBOCs, was incorporated to preserve Hb’s functionality. The optimized formulation had a size of 344 nm, a PDI of 0.172, a LC of 26.9%, and an EE of 40.7%. The HbNPs were imaged by microscopy and were further characterized by FTIR and CD spectroscopy to assess their chemical composition and structure. Finally, the ability of the encapsulated Hb to bind and release oxygen over several rounds was demonstrated, showing the preservation of its functionality.

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.

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.

scholarly journals Effect of Chitosan Coating on PLGA Nanoparticles for Oral Delivery of Thymoquinone: In Vitro, Ex Vivo, and Cancer Cell Line Assessments

Coatings ◽  
2020 ◽  
Vol 11 (1) ◽  
pp. 6
Author(s):  
Sultan Alshehri ◽  
Syed Sarim Imam ◽  
Md Rizwanullah ◽  
Khalid Umar Fakhri ◽  
Mohd Moshahid Alam Rizvi ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Particle Size ◽  
Oral Delivery ◽  
Ex Vivo ◽  
Cancer Cell Line ◽  
Entrapment Efficiency ◽  
Plga Nanoparticles ◽  
Cancer Management ◽  
Mcf 7

In the present study, thymoquinone (TQ)-encapsulated chitosan- (CS)-coated poly(d,l-lactide-co-glycolide) (PLGA) nanoparticles (NPs) were formulated using the emulsion evaporation method. NPs were optimized by using 33-QbD approach for improved efficacy against breast cancer. The optimized thymoquinone loaded chitosan coated Poly (d,l-lactide-co-glycolide) nanoparticles (TQ-CS-PLGA-NPs) were successfully characterized by different in vitro and ex vivo experiments as well as evaluated for cytotoxicity in MDA-MB-231 and MCF-7 cell lines. The surface coating of PLGA-NPs was completed by CS coating and there were no significant changes in particle size and entrapment efficiency (EE) observed. The developed TQ-CS-PLGA-NPs showed particle size, polydispersibility index (PDI), and %EE in the range between 126.03–196.71 nm, 0.118–0.205, and 62.75%–92.17%. The high and prolonged TQ release rate was achieved from TQ-PLGA-NPs and TQ-CS-PLGA-NPs. The optimized TQ-CS-PLGA-NPs showed significantly higher mucoadhesion and intestinal permeation compared to uncoated TQ-PLGA-NPs and TQ suspension. Furthermore, TQ-CS-PLGA-NPs showed statistically enhanced antioxidant potential and cytotoxicity against MDA-MB-231 and MCF-7 cells compared to uncoated TQ-PLGA-NPs and pure TQ. On the basis of the above findings, it may be stated that chitosan-coated TQ-PLGA-NPs represent a great potential for breast cancer management.

scholarly journals PREPARATION, CHARACTERIZATION AND EVALUATION OF POLY (LACTIDE –CO –GLYCOLIDE) MICROSPHERES FOR THE CONTROLLED RELEASE OF ZIDOVUDINE

2017 ◽  
Vol 9 (12) ◽  
pp. 70 ◽  
Author(s):  
Seema Kohli ◽  
Abhisek Pal ◽  
Suchit Jain
Keyword(s):  
Particle Size ◽  
Controlled Release ◽  
Double Emulsion ◽  
Entrapment Efficiency ◽  
Diffusion Method ◽  
Average Particle ◽  
Plga Microspheres ◽  
Good Reproducibility ◽  
Solvent Diffusion ◽  
Emulsion Solvent Diffusion Method

Objective: The purpose of this research work was to develop and evaluate microspheres appropriate for controlled release of zidovudine (AZT).Methods: The AZT loaded polylactide-co-glycolide (PLGA) microspheres were prepared by W/O/O double emulsion solvent diffusion method. Compatibility of drug and polymer was studied by Fourier-transform infrared spectroscopy (FTIR). The influence of formulation factors (drug: polymer ratio, stirring speed, the concentration of surfactant) on particle size encapsulation efficiency and in vitro release characteristics of the microspheres was investigated. Release kinetics was studied and stability study was performed as per ICH guidelines.Results: Scanning electron microscopy (SEM) images show good reproducibility of microspheres from different batches. The average particle size was in the range of 216-306 μm. The drug-loaded microspheres showed 74.42±5.08% entrapment efficiency. The cumulative percentage released in phosphate Buffer solution (PBS) buffer was found to be 55.32±5.89 to 74.42±5.08 %. The highest regressions (0.981) were obtained for zero order kinetics followed by Higuchi (0.968) and first order (0.803).Conclusion: Microsphere prepared by double emulsion solvent diffusion method was investigated and the results revealed that 216-306 μm microsphere was successfully encapsulated in a polymer. FT-IR analysis, entrapment efficiency and SEM Studies revealed the good reproducibility from batch to batch. The microspheres were of an appropriate size and suitable for oral administration. Thus the current investigation show promising results of PLGA microspheres as a matrix for drug delivery and merit for In vivo studies for scale up the technology.

scholarly journals Dual Drug Delivery of Sorafenib and Doxorubicin from PLGA and PEG-PLGA Polymeric Nanoparticles

Polymers ◽  
2018 ◽  
Vol 10 (8) ◽  
pp. 895 ◽  
Author(s):  
György Babos ◽  
Emese Biró ◽  
Mónika Meiczinger ◽  
Tivadar Feczkó
Keyword(s):  
Drug Delivery ◽  
Polymeric Nanoparticles ◽  
Single Agent ◽  
Double Emulsion ◽  
Controlled Drug Release ◽  
Chemical Characteristics ◽  
Solvent Evaporation Method ◽  
Polymeric Carrier ◽  
Sustained Drug Delivery ◽  
Dual Drug

Combinatorial drug delivery is a way of advanced cancer treatment that at present represents a challenge for researchers. Here, we report the efficient entrapment of two clinically used single-agent drugs, doxorubicin and sorafenib, against hepatocellular carcinoma. Biocompatible and biodegradable polymeric nanoparticles provide a promising approach for controlled drug release. In this study, doxorubicin and sorafenib with completely different chemical characteristics were simultaneously entrapped by the same polymeric carrier, namely poly(d,l-lactide-co-glycolide) (PLGA) and polyethylene glycol-poly(d,l-lactide-co-glycolide) (PEG-PLGA), respectively, using the double emulsion solvent evaporation method. The typical mean diameters of the nanopharmaceuticals were 142 and 177 nm, respectively. The PLGA and PEG-PLGA polymers encapsulated doxorubicin with efficiencies of 52% and 69%, respectively, while these values for sorafenib were 55% and 88%, respectively. Sustained drug delivery under biorelevant conditions was found for doxorubicin, while sorafenib was released quickly from the PLGA-doxorubicin-sorafenib and PEG-PLGA-doxorubicin-sorafenib nanotherapeutics.

scholarly journals Metformin Hydrochloride-Loaded PLGA Nanoparticle in Periodontal Disease Experimental Model Using Diabetic Rats

2018 ◽  
Vol 19 (11) ◽  
pp. 3488 ◽  
Author(s):  
Aline Pereira ◽  
Gerly Brito ◽  
Maria Lima ◽  
Arnóbio Silva Júnior ◽  
Emanuell Silva ◽  
...  
Keyword(s):  
Bone Loss ◽  
Cathepsin K ◽  
Immunohistochemical Analysis ◽  
Entrapment Efficiency ◽  
Inflammatory Cells ◽  
Plga Nanoparticles ◽  
Diabetic Rats ◽  
Metformin Hydrochloride ◽  
Tnf Α ◽  
Mean Diameter

Evidence shows that metformin is an antidiabetic drug, which can exert favorable anti-inflammatory effects and decreased bone loss. The development of nanoparticles for metformin might be useful for increased therapeutic efficacy. The aim of this study was to evaluate the effect of metformin hydrochloride-loaded Poly (d,l-Lactide-co-glycolide) (PLGA)/(MET-loaded PLGA) on a ligature-induced periodontitis model in diabetic rats. MET-loaded PLGA were characterized by mean diameter, particle size, polydispensity index, and entrapment efficiency. Maxillae were scanned using Microcomputed Tomography (µCT) and histopathological and immunohistochemical analysis. IL-1β and TNF-α levels were analyzed by ELISA immunoassay. Quantitative RT-PCR was used (AMPK, NF-κB p65, HMGB1, and TAK-1). The mean diameter of MET-loaded PLGA nanoparticles was in a range of 457.1 ± 48.9 nm (p < 0.05) with a polydispersity index of 0.285 (p < 0.05), Z potential of 8.16 ± 1.1 mV (p < 0.01), and entrapment efficiency (EE) of 66.7 ± 3.73. Treatment with MET-loaded PLGA 10 mg/kg showed low inflammatory cells, weak staining by RANKL, cathepsin K, OPG, and osteocalcin, and levels of IL-1β and TNF-α (p < 0.05), increased AMPK expression gene (p < 0.05) and decreased NF-κB p65, HMGB1, and TAK-1 (p < 0.05). It is concluded that MET-loaded PLGA decreased inflammation and bone loss in periodontitis in diabetic rats.

scholarly journals Ex-vivo Ex-Vivo Absorption Study of a Novel Dabigatran Etexilate Loaded Nanostructured Lipid Carrier Using Non-Everted Intestinal Sac Model

2019 ◽  
Vol 28 (2) ◽  
pp. 37-45
Author(s):  
Haithem N Abed ◽  
Ahmed A. Hussein
Keyword(s):  
Particle Size ◽  
Oleic Acid ◽  
Zeta Potential ◽  
Oral Absorption ◽  
Ex Vivo ◽  
Dabigatran Etexilate ◽  
Entrapment Efficiency ◽  
Nanostructured Lipid Carrier ◽  
Loading Capacity ◽  
Intestinal Permeation

Abstract The purpose of our study was to develop Dabigatran Etexilate loaded nanostructured lipid carriers (DE-NLCs) using Glyceryl monostearate and Oleic acid as lipid matrix, and to estimate the potential of the developed delivery system to improve oral absorption of low bioavailability drug, different Oleic acid ratios effect on particle size, zeta potential, entrapment efficiency and loading capacity were studied, the optimized DE-NLCs shows a particle size within the nanorange, the zeta potential (ZP) was 33.81±0.73mV with drug entrapment efficiency (EE%) of  92.42±2.31% and a loading capacity (DL%) of 7.69±0.17%. about 92% of drug was released in 24hr in a controlled manner, the ex-vivo intestinal permeation study using the non-everted sac model shows four folds increment in the permeation of DE-NLCs compared to dabigatran etexilate suspension (DE-S).

scholarly journals 1-Laurin-3-Palmitin as a Novel Matrix of Solid Lipid Particles: Higher Loading Capacity of Thymol and Better Stability of Dispersions Than Those of Glyceryl Monostearate and Glyceryl Tripalmitate

Nanomaterials ◽  
2019 ◽  
Vol 9 (4) ◽  
pp. 489 ◽  
Author(s):  
Hao Shi ◽  
Shuangshuang Huang ◽  
Junbo He ◽  
Lijuan Han ◽  
Weinong Zhang ◽  
...  
Keyword(s):  
Model Compound ◽  
Entrapment Efficiency ◽  
Bioactive Molecules ◽  
Prolonged Storage ◽  
Loading Capacity ◽  
X Ray Diffraction ◽  
Glyceryl Monostearate ◽  
X Ray ◽  
Solid Lipid ◽  
Solid Lipid Particles

To develop solid lipid nanoparticles (SLNs) with a new lipid matrix for delivery of hydrophobic bioactive molecules, high purity 1-laurin-3-palmitin (1,3-LP) was synthesized and the prepared 1,3-LP SLNs were compared with those of two common SLN matrices in glyceryl monostearate (GMS) and glyceryl tripalmitate (PPP). Conditions of preparing SLNs were first optimized by evaluating the particle size, polydispersity index (PDI), zeta-potential, and stability. Thereafter, the performance of SLN loading of a model compound in thymol was studied. The loading capacity of thymol in 1,3-LP SLNs was 16% of lipids and higher than 4% and 12% for GMS- and PPP-SLNs, respectively. The 1,3-LP SLNs also had the best efficiency to entrapment thymol during the prolonged storage. X-ray diffraction (XRD) analyses confirmed the excellent crystalline stability of 1,3-LP leading to the stable entrapment efficiency and better stability of thymol-loaded SLNs. Conversely, the polymorphic transformation of GMS and PPP resulted in the declined entrapment efficiency of thymol in the corresponding SLNs. This work indicated the 1,3-diacylglycerol (DAG) SLNs could be used as a promising delivery system for the encapsulation of hydrophobic bioactive molecules with high loading capacity and stability.

scholarly journals Enhanced Transdermal Delivery of Concentrated Capsaicin from Chili Extract-Loaded Lipid Nanoparticles with Reduced Skin Irritation

Pharmaceutics ◽  
2020 ◽  
Vol 12 (5) ◽  
pp. 463 ◽  
Author(s):  
Phunsuk Anantaworasakul ◽  
Wantida Chaiyana ◽  
Bozena B. Michniak-Kohn ◽  
Wandee Rungseevijitprapa ◽  
Chadarat Ampasavate
Keyword(s):  
Skin Irritation ◽  
Chorioallantoic Membrane ◽  
Crystallinity Index ◽  
Entrapment Efficiency ◽  
Lipid Nanoparticles ◽  
Loading Capacity ◽  
High Concentration ◽  
Fatty Esters ◽  
Solid Lipid

The aim of this study was to develop lipid-based nanoparticles that entrapped a high concentration of capsaicin (0.25%) from a capsicum oleoresin extract. The solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs) were strategically fabricated to entrap capsaicin without a hazardous solvent. Optimized nanosize lipid particles with high capsaicin entrapment and loading capacity were achieved from pair-wise comparison of the solid lipid mixtures consisting of fatty esters and fatty alcohols, representing small and large crystal-structure molecules combined with a compatible liquid lipid and surfactants (crystallinity index = 3%). This report was focused on selectively captured capsaicin from oleoresin in amorphous chili extract-loaded NLCs with 85.27% ± 0.12% entrapment efficiency (EE) and 8.53% ± 0.01% loading capacity (LC). The particle size, polydispersity index, and zeta potential of chili extract-loaded NLCs were 148.50 ± 2.94 nm, 0.12 ± 0.03, and −29.58 ± 1.37 mV, respectively. The favorable zero-order kinetics that prolonged capsaicin release and the significantly faster transdermal penetration of the NLC attributed to the reduction in skin irritation of the concentrated capsaicin NLCs, as illustrated by the in vitro EpiDermTM three-dimensional human skin irritation test and hen’s egg test chorioallantoic membrane assay (HET-CAM).

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