Therapeutic Effects of Paclitaxel Loaded Polyethylene Glycol-Polylactic Acid-Glycolic Acid Copolymer Nanoparticles on Pancreatic Cancer in Rats

2020 ◽  
Vol 20 (12) ◽  
pp. 7271-7275
Author(s):  
Yu Fu ◽  
Ludong Tan ◽  
Lingyu Meng ◽  
Xuexue Lei
Keyword(s):  
Pancreatic Cancer ◽  
Flow Cytometry ◽  
Particle Size ◽  
Drug Loading ◽  
Average Particle Size ◽  
Pancreatic Cancer Cell Line ◽  
Human Pancreatic Cancer ◽  
Average Particle ◽  
Therapeutic Effects ◽  
Significant Difference

To establish a simple and safe method for the preparation of paclitaxel PEG-PLGA nanoparticles emulsified in tpgs (PTX-pegpllga-np), for high drug loading; and to study its effect on proliferation and apoptosis of human pancreatic cancer cell line MIAPACA-2. PTX-PEG-PLGA-NP was prepared by one-step precipitation, using tpgs as emulsifier. The drug loading and particle size were used as an index to optimize the formulation, and the physical and chemical properties such as in vitro release and stability were characterized. The uptake of fluorescein coumarin 6 (C6) loaded PEG-PLGA-NP by MIAPACA-2 cells was observed by fluorescence microscope, and the growth and apoptosis of MIAPACA-2 cells after PTX-PEG-PLGA-NP were detected by MTT and flow cytometry respectively. The entrapment efficiency of the nanoparticles was 90.26%, the drug loading was 10.13%, the average particle size was 92.3±3.1 nm, and the zeta potential was 10.48±1.54 mV. The cumulative releases of nano preparation and general preparation (Taxol injection) in four hours were 25.9% and 98.5%, respectively; and the former had a strong sustained-release effect. The results of cell uptake experiments showed that the uptake of c6-PEG-PLGA-NP by MIAPACA-2 cells increased gradually with time. MTT results showed that PTX-PEG-PLGA-NP had no significant difference in the inhibition rate of MIAPACA-2 cells compared with PTX group. Flow cytometry showed that PTX-PEG-PLGAnp was superior better than PTX in inducing apoptosis in MIAPACA-2 cells. The tpgs emulsification method is simple and environment-friendly. The paclitaxel loaded nanoparticles prepared through the optimization of the formulation have large drug loading capacity and uniform particle size, which can target the pancreatic cancer MIAPACA-2 cells, and do not weaken its ability to inhibit the growth of MIAPACA-2 cells. The nanoparticles also induce apoptosis in cancer MIAPACA-2 cells, and could be used for further clinical treatment of pancreatic cancer.

Preparation of Epidermal Growth Factor-Modified Targeted Doxorubicin Nanoliposomes and Therapy of Liver Cancer

2021 ◽  
Vol 21 (9) ◽  
pp. 4565-4572
Author(s):  
Yongan Chen ◽  
Lei Cheng ◽  
Dan Yu ◽  
Jie Shen ◽  
Zhengrong Zhou ◽  
...  
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Release Rate ◽  
Encapsulation Efficiency ◽  
Drug Loading ◽  
Average Particle Size ◽  
Hepatoma Cells ◽  
Average Particle ◽  
Therapeutic Effects ◽  
Drug Release Rate

The objective of this study was to prepare doxorubicin-loaded EGF modified PEG-nanoparticles and evaluate its targeting capability and therapeutic effects with EGFR-expressing hepatocellular carcinoma cells. The morphology, particle size distribution, and doxorubicin content of the nanoparticles were measured, and the drug loading and encapsulation efficiency were calculated. The doxorubicin nanoparticles prepared were regular circular, with good dispersibility, no adhesion, and the average particle size was (136.7±9.3) nm. The average encapsulation efficiency was (76.67±8.63)%, the average drug loading was (3.86±0.55)%; the drug release rate of doxorubicin was 100% for 12 h, and the doxorubicin nanometer was loaded. The drug release rate of the granules was 52.9% at 24 h and 81.2% at 144 h. The inhibition rate of the proliferation of hepatocarcinoma cells by the doxorubicin-containing nanoparticles was slower than that of doxorubicin, and the IC50 of the two cells was 1.844 and 0.345 μg/mL, respectively. At the same time, apoptosis and cycle analysis showed that the doxorubicin nanoparticles could significantly inhibit the cell cycle of hepatoma cells and promote the apoptosis of hepatoma cells. This study successfully produced nanoparticles loaded with doxorubicin targeting EGFR, which has a good sustained release effect, and its antitumor effect is stronger than free doxorubicin.

Formulating SLN and NLC as Innovative Drug Delivery Systems for Non-Invasive Routes of Drug Administration

2020 ◽  
Vol 27 (22) ◽  
pp. 3623-3656 ◽  
Author(s):  
Bruno Fonseca-Santos ◽  
Patrícia Bento Silva ◽  
Roberta Balansin Rigon ◽  
Mariana Rillo Sato ◽  
Marlus Chorilli
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Drug Release ◽  
Drug Loading ◽  
Average Particle Size ◽  
Delivery Systems ◽  
Average Particle ◽  
Minor Importance ◽  
Routes Of Administration ◽  
Non Invasive

Colloidal carriers diverge depending on their composition, ability to incorporate drugs and applicability, but the common feature is the small average particle size. Among the carriers with the potential nanostructured drug delivery application there are SLN and NLC. These nanostructured systems consist of complex lipids and highly purified mixtures of glycerides having varying particle size. Also, these systems have shown physical stability, protection capacity of unstable drugs, release control ability, excellent tolerability, possibility of vectorization, and no reported production problems related to large-scale. Several production procedures can be applied to achieve high association efficiency between the bioactive and the carrier, depending on the physicochemical properties of both, as well as on the production procedure applied. The whole set of unique advantages such as enhanced drug loading capacity, prevention of drug expulsion, leads to more flexibility for modulation of drug release and makes Lipid-based nanocarriers (LNCs) versatile delivery system for various routes of administration. The route of administration has a significant impact on the therapeutic outcome of a drug. Thus, the non-invasive routes, which were of minor importance as parts of drug delivery in the past, have assumed added importance drugs, proteins, peptides and biopharmaceuticals drug delivery and these include nasal, buccal, vaginal and transdermal routes. The objective of this paper is to present the state of the art concerning the application of the lipid nanocarriers designated for non-invasive routes of administration. In this manner, this review presents an innovative technological platform to develop nanostructured delivery systems with great versatility of application in non-invasive routes of administration and targeting drug release.

scholarly journals Sodium Alginate Nanoparticles of Isoniazid: Preparation and Evaluation

2019 ◽  
Vol 11 (06) ◽  
Author(s):  
Sumit Kumar ◽  
Dinesh Chandra Bhatt
Keyword(s):  
Particle Size ◽  
Sodium Alginate ◽  
Encapsulation Efficiency ◽  
Drug Loading ◽  
Average Particle Size ◽  
Average Particle ◽  
In Vitro Drug Release ◽  
Ionotropic Gelation ◽  
Preparation And Evaluation

Fabrication and evaluation of the Isoniazid loaded sodium alginate nanoparticles (NPs) was main objective of current investigation. These NPs were engineered using ionotropic gelation technique. The NPs fabricated, were evaluated for average particle size, encapsulation efficiency, drug loading, and FTIR spectroscopy along with in vitro drug release. The particle size, drug loading and encapsulation efficiency of fabricated nanoparticles were ranging from 230.7 to 532.1 nm, 5.88% to 11.37% and 30.29% to 59.70% respectively. Amongst all batches studied formulation F-8 showed the best sustained release of drug at the end of 24 hours.

Mechanism of Hydrogen Sulfide Drug-Loaded Nanoparticles Promoting the Repair of Spinal Cord Injury in Rats Through Mammalian Target of Rapamycin/Signal Transducer and Activator of Transcription 3 Signaling Pathway

2021 ◽  
Vol 13 (9) ◽  
pp. 1691-1698
Author(s):  
Hongzhe Liu ◽  
Kai Tong ◽  
Ziyi Zhong ◽  
Gang Wang
Keyword(s):  
Spinal Cord ◽  
Spinal Cord Injury ◽  
Particle Size ◽  
Dispersion Coefficient ◽  
Drug Loading ◽  
Average Particle Size ◽  
Mammalian Target Of Rapamycin ◽  
Average Particle ◽  
Recovery Effect ◽  
Cord Injury

To explore the effect of hydrogen sulfide (H2S) drug-loaded nanoparticles (H2S-NPs) on the mTOR/STAT3 signaling pathway in rats and its mechanism on repair of spinal cord injury (SCI), a new H2S-NP (G16MPG-ADT) was prepared and synthesized. The rats were selected as the research objects to explore the mechanism of SCI repair. The G16MPG-ADT NPs were evaluated by average particle size (APS), dispersion coefficient (DC), drug loading content (DLC), drug loading efficacy (DLE), in vitro release (IV-R), and acute toxicity (AT). It was found that G16MPG-ADT nanoparticles had a uniform particle size distribution with a unimodal distribution, with an average particle size of 186.5 nm and a dispersion coefficient of 0.129; within the concentration range of 8~56 μg/L, there was a good linear relationship with the peak area; and the release rate of the nanoparticles within 16 h~32 h was higher than 50%. G16MPG-ADT NP injection treatment was performed on rats with SCI. Western blotting (WB) and immunofluorescence staining were adopted to analyze the expression levels of mammalian target of rapamycin (mTOR) and signal transducers and activators of transcription (STAT3) protein and the growth of neurites. It was found that G16MPG-ADT can increase mTOR and STAT3 protein levels and promote nerve growth after SCI. Finally, the Basso, Beattie and Bresnahan locomotor rating (BBB) score was to evaluate the recovery effect of rats after treatment. It was found that the recovery effect was excellent after G16MPG-ADT treatment. In summary, G16MPG-ADT has a good effect on SCI repair in rats and can be promoted in the clinic.

scholarly journals Bio Pharmaceutics Classification System (BCS) Class IV Drug Nanoparticles: Quantum Leap to Improve Their Therapeutic Index

2018 ◽  
Vol 8 (4) ◽  
pp. 617-625 ◽  
Author(s):  
Sachin Kumar ◽  
Ramneek Kaur ◽  
Rashi Rajput ◽  
Manisha Singh
Keyword(s):  
Particle Size ◽  
Classification System ◽  
Drug Loading ◽  
Average Particle Size ◽  
Therapeutic Index ◽  
Diffusion Profile ◽  
Average Particle ◽  
Linear Diffusion ◽  
Quantum Leap ◽  
Class Iv

Purpose: Biopharmaceutics classification system (BCS) class IV compounds, exhibits least oral bioavailability, low solubility and intestinal permeability among all pharmaceutical classes of drugs. Thus, these drugs need more compatible and efficient delivery system. Since, their solubility in various medium, remains a limitation so, polymeric nano coacervates based drug loading with modified approach for them may prove to be a solution ahead. Therefore, in present study Chitosan is opted for encapsulating the BCS class IV drug (Hydrochlorothiazide) to attain better stability, enhanced permeability and lower toxicity. Methods: For this study, Hydrochlorothiazide (HCTZ) was opted for formulating chitosan based nano-coacervate system. Results: Optimized HCTZ nanocoacervates exhibited the average particle size of 91.39 ± 0.75 nm with Poly-dispersity index score of 0.159 ± 0.01, indicating homogeneity of colloidal solution. Zeta potential and encapsulation efficiency of HCTZ nanocoacervates were recorded as -18.9 ± 0.8 mV and 76.69 ± 0.82 % respectively. Further, from TEM and SEM evaluation the average particle size for the same were found in conformity (35-50 nm), with almost spherical morphology. Also, the EDX (Electron Dispersive X-ray) spectrometry and FT – IR analysis of optimized formulation indicated the balanced chemical composition and interaction between the polymeric molecules. The HCTZ nano coacervates showed the linear diffusion profile through the dialysis membrane. Conclusion: We can conclude from the present study that the optimized HCTZ nano coacervates may prove to be a suitable potential option for effective delivery of BCS class IV drugs.

Synthesis of n-Hexadecylphosphonic Acid-Coated Monodisperse Fe3O4 Superparamagnetic Nanoparticles

2012 ◽  
Vol 512-515 ◽  
pp. 170-173
Author(s):  
Xue Song Tang ◽  
Ming Li
Keyword(s):  
Crystal Structure ◽  
Particle Size ◽  
Drug Loading ◽  
Average Particle Size ◽  
Superparamagnetic Nanoparticles ◽  
Average Particle ◽  
X Ray Diffraction ◽  
Cubic Crystal ◽  
Transmission Electron ◽  
Potential Applications

Monodisperse Fe3O4 Superparamagnetic Nanoparticles Were Synthesized in N-Hexadecylphosphonic Acid/ Cyclohexane/ Water/ Ethanol Microemulsion under Solvothermal Conditions at 100°C. the Crystal Structure and Particle Size of Synthesized Fe3O4 Were Observed by X-Ray Diffraction (XRD) as Well as Transmission Electron Microscopy (TEM). the Results Show that the Nanoparticles Have a Cubic Crystal System and a Average Particle Size of about 10nm. each Nanoparticle Has a Single Crystal Structure. the Surface Chemistry of Synthesized Fe3O4 Nanoparticles Was Characterized by Fourier Transform Infrared Spectroscopy (FTIR), Indicating that the Nanoparticles Were Covered by a Layer of N-Hexadecylphosphonic Acid, which Made the Nanoparticles Totally Lipophilic. Magnetic Properties of the Nanoparticles Were Investigated by Using Vibrating Sample Magnetometer (VSM). the Result Reveals that the Saturation Magnetization (Ms) of the Nanoparticles Is Higher than 40 Emu/G and the Coercive Force Is near to 0. the Monodisperse Fe3O4 Nanoparticles Have Superparamagnetic Property and May Find Potential Applications in many Fields, such as Ferrofluids, Drug Loading and Release, Selective Biomolecular Separation and MRI.

Preparation of Poly[lactic-co-glycolic] Acid Nanospheres and Its Role in Hepatoma Cells

2021 ◽  
Vol 21 (2) ◽  
pp. 977-986
Author(s):  
Zhongxing Shi ◽  
Jinping Li ◽  
Hongwei Liang ◽  
Hongbo Hu ◽  
Huijie Jiang
Keyword(s):  
Particle Size ◽  
Release Rate ◽  
Hepg2 Cells ◽  
Glycolic Acid ◽  
Drug Loading ◽  
Average Particle Size ◽  
Plga Nanoparticles ◽  
Toxin Gene ◽  
Average Particle

Poly[lactic-co-glycolic] acid (PLGA) targeting nanoparticles AFP/PLGA/Dt386, loaded with Dt386 plasmid of diphtheria toxin gene, modified by Alpha fetoprotein (AFP) monoclonal antibody, is prepared. Its physical and chemical properties and its effect on HepG2 cells are studied. Firstly, Dt386 expression plasmid pET11a/Dt386 is constructed and PLGA nanoparticles are prepared by emulsion solvent evaporation (ESE). Scanning electron microscope (SEM) is used to observe its morphology. Laser Particle Sizer is used to measure the particle size. In addition, the encapsulation efficiency, drug loading and in vitro release rate of PLGA nanoparticles are measured. Carboxy fluorescein and rhodamine fluorescein are used to double label IgG/PLGA/Dt386 and AFP/PLGA/Dt386 nanospheres, respectively, the entry of nanospheres into HepG2 cells are observed at 3 h and 12 h. The effect of AFP/PLGA/Dt386 nanospheres on the migration of HepG2 cells is examined by wounding healing assay. Transwell chamber experiment is used to detect the effect of AFP/PLGA/Dt386 nanospheres on the invasion of HepG2 cells. MTT method is utilized to determine the inhibitory activity of nanoparticles on HepG2 cell proliferation. After treated with IgG/PLGA/Dt386 and AFP/PLGA/Dt386 nanoparticles for 48 hours, flow cytometry is used to detect the apoptosis rate and cell cycle of HepG2 cells in each group. The results show that the prepared nanospheres have regular morphology, flat surface, average particle size of 265.72±12.46 nm, zeta potential of −18.15 mV. The average entrapment efficiency and drug loading are 78.48±1.71% and 3.16±0.35%, respectively. The nanoparticles release slowly and stably in vitro. At the 10th day, the release rate reaches 75.13%. PLGA nanospheres can effectively protect DNA from nuclease degradation. The results show that AFP/PLGA/Dt386 nanospheres have biological targeting effect and can be enriched in cells. AFP/PLGA/Dt386 nanoparticles can significantly inhibit the migration, invasion and proliferation of HepG2 cells, and promote apoptosis.

scholarly journals Biphenyl Wrinkled Mesoporous Silica Nanoparticles for pH-Responsive Doxorubicin Drug Delivery

Materials ◽  
2020 ◽  
Vol 13 (8) ◽  
pp. 1998 ◽  
Author(s):  
Jason Lin ◽  
Chuanqi Peng ◽  
Sanjana Ravi ◽  
A. K. M. Nur Alam Siddiki ◽  
Jie Zheng ◽  
...  
Keyword(s):  
Particle Size ◽  
Mesoporous Silica ◽  
Silica Nanoparticles ◽  
Surface Area ◽  
Mesoporous Silica Nanoparticles ◽  
Drug Loading ◽  
High Surface ◽  
Average Particle Size ◽  
Average Particle ◽  
Mcf 7

Biphenyl wrinkled mesoporous silica nanoparticles with controlled particle size and high surface area were evaluated for the storage and delivery of doxorubicin. The average particle size and surface area were ~70 nm and ~1100 m2/g. The doxorubicin loading efficiency was 38.2 ± 1.5 (w/w)% and the release was pH dependent. The breast cancer cell line, MCF-7 (Michigan Cancer Foundation-7) was used for the in vitro drug release study. The cytotoxicity of doxorubicin-loaded nanoparticles was significantly higher than free doxorubicin. Fluorescence images showed biphenyl wrinkled mesoporous silica (BPWS) uptake by the MCF-7 cells. The biphenyl bridged wrinkled silica nanoparticles appear promising for hydrophobic drug loading and delivery.

scholarly journals Casein Micelles as Nanocarriers for Benzydamine Delivery

Polymers ◽  
2021 ◽  
Vol 13 (24) ◽  
pp. 4357
Author(s):  
Nikolay Zahariev ◽  
Maria Marudova ◽  
Sophia Milenkova ◽  
Yordanka Uzunova ◽  
Bissera Pilicheva
Keyword(s):  
Particle Size ◽  
Encapsulation Efficiency ◽  
Drug Loading ◽  
Average Particle Size ◽  
Crosslinking Agent ◽  
Morphological Characteristics ◽  
Average Particle ◽  
Scanning Calorimetry ◽  
Casein Micelles ◽  
Fourier Transformed Infrared Spectroscopy

The aim of the present work was to optimize the process parameters of the nano spray drying technique for the formulation of benzydamine-loaded casein nanoparticles and to investigate the effect of some process variables on the structural and morphological characteristics and release behavior. The obtained particles were characterized in terms of particle size and size distribution, surface morphology, production yield and encapsulation efficiency, drug-polymer compatibility, etc., using dynamic light scattering, scanning electron microscopy, differential scanning calorimetry, and Fourier transformed infrared spectroscopy. Production yields of the blank nanoparticles were significantly influenced by the concentration of both casein and the crosslinking agent. The formulated drug-loaded nanoparticles had an average particle size of 135.9 nm to 994.2 nm. Drug loading varied from 16.02% to 57.41% and the encapsulation efficiency was in the range 34.61% to 78.82%. Our study has demonstrated that all the investigated parameters depended greatly on the polymer/drug ratio and the drug release study confirmed the feasibility of the developed nanocarriers for prolonged delivery of benzydamine.

scholarly journals Effect of the stirring speed on the struvite formation using the centrate from a WWTP

2019 ◽  
pp. 42-50 ◽  
Author(s):  
Carolina Gonzalez Morales ◽  
Miller Alonso Camargo-Valero ◽  
Francisco José Molina Pérez ◽  
Belén Fernández
Keyword(s):  
Particle Size ◽  
Wastewater Treatment Plants ◽  
Average Particle Size ◽  
Average Particle ◽  
X Ray Diffraction ◽  
Mean Values ◽  
X Ray ◽  
Operational Conditions ◽  
Significant Difference ◽  
Speed Range

The formation of struvite (MgNH4PO4·6H2O) for nutrient recovery in wastewater treatment plants has been widely investigated; however, little attention has been paid to the effect of stirring speeds on the resulting particle size, which could affect its agronomic value as a slow-release fertilizer. In this study, struvite formation from the centrate of sewage digestate was performed under six stirring speeds (0, 100, 200, 300, 400, 500 rpm). The resulting struvite crystals were characterised using X-ray diffraction and scanning electron microscopy with energy dispersive X-ray spectroscopy. The average particle size of struvite crystals increased from 55 µm at 0 rpm to 127 µm at 100 rpm and 128 μm at 200 rpm.  Further increments in stirring speeds resulted in smaller crystal sizes. These results indicated that the largest particle size can be obtained at stirring speeds ranging from 100 to 200 rpm, equivalent to a velocity gradient between 79 and 188 s-1, as there was no statistically significant difference between mean values (t-test, p<0.05). The optimum stirring speed range reported herein can be used to set operational conditions for struvite crystallisation with the benefit of producing large crystals and reducing energy consumption in stirring tanks.

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