scholarly journals Preparation and pharmacokinetics of genistein MePEG-PLGA copolymer micelles

2019 ◽  
Author(s):  
Mina Swartz ◽  
John Smith
Keyword(s):  
Particle Size ◽  
Encapsulation Efficiency ◽  
Drug Loading ◽  
Weibull Model ◽  
Pharmacokinetic Parameters ◽  
Release Behavior ◽  
Concentration Data ◽  
Tail Vein ◽  
Initial Stability ◽  
Copolymer Micelles

AbstractIn this report, we demonstrated a novel technique to prepare genistein (GEN) MePEG-PLGA copolymer micelles. Initial stability and pharmacokinetic behavior in rats after intravenous administration were investigated. The micelles were prepared by modified self-emulsifying solvent evaporation method. The morphology, encapsulation efficiency, drug loading, particle size and Zeta potential were investigated. The release behavior was investigated by dynamic membrane dialysis technique. The micelles were stored in a refrigerator at 4 °C, and samples were taken after 1 d, 10 d, 1 month, 3 months, and 6 months, and the encapsulation efficiency and drug loading were examined. The GEN micelles were injected into the tail vein of healthy rats. The blood concentration of GEN in rats was determined by HPLC. The plasma concentration data was processed by DAS 2.0 software. The main pharmacokinetic parameters were statistically analyzed by SPSS 17.0 software. Results The encapsulation efficiency of the prepared micelles was (84.43+/-2.93) %, the drug loading was (2.63+/-0.91) %, and the particle size was (63.75+/-4.12) nm. The release behavior of GEN micelles was in line with the Weibull model. The 6-month leakage rate of GEN micelles was 2.45%, and the drug loading decreased by 0.18%. The main pharmacokinetic parameters AUC0-t after GEN micelles and GEN emulsion 40 mg·kg-1 were injected into the tail vein of rats. They were (99.46+/- 4.77) mg · L-1 ·h and (57.51+/-1.37) mg·L-1 ·h, and t1/2 were (7.48+/-1.15)h and (4.95+/- 1.15)h, respectively, and Cmax was (16.03+/-1.20) mg·L-1 and (16.73+/-1.10) mg·L-1, CL are (0.36+/-0.02) L·h-1 ·kg-1 and (0.67+/-0.02)L·h-1 ·kg-1.

Simultaneous Incorporation of 5-Fluorouracil and Leucovorin into Chitosan Nanoparticle as Drug Carrier and Its Characterization

2010 ◽  
Vol 654-656 ◽  
pp. 2265-2268
Author(s):  
Pu Wang Li ◽  
Yi Chao Wang ◽  
Zheng Peng ◽  
Ling Xue Kong
Keyword(s):  
Particle Size ◽  
Strong Interaction ◽  
Encapsulation Efficiency ◽  
Drug Carrier ◽  
Drug Loading ◽  
Anti Cancer ◽  
Chitosan Nanoparticle ◽  
Combined Drugs ◽  
Drug Encapsulation Efficiency ◽  
Interaction Between Drugs

A combined drug loaded system containing two most common anti-cancer drugs 5-fluorouracil (5-FU) and leucovorin (LV) was designed and prepared by ion crosslinking technology. The resulted nanoparticles are spherical in shape, and the particle size becomes larger when drug combination are loaded. Efficient drug encapsulation efficiency (EE) and drug loading (LC) are obtained due to the strong interaction between drugs and polymer. The combined drugs are distributed in the particles in amorpholous state which are demonstrated by the XRD results.

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.

scholarly journals Formulation of Solid Lipid Nanoparticles of Cilnidipine for the Treatment of Hypertension

2019 ◽  
Vol 9 (3) ◽  
pp. 212-221 ◽  
Author(s):  
Aparna Bhalerao ◽  
Pankaj Prakash Chaudhari
Keyword(s):  
Particle Size ◽  
Solid Lipid Nanoparticles ◽  
Encapsulation Efficiency ◽  
Drug Loading ◽  
Lipid Nanoparticles ◽  
Water Soluble ◽  
Solid Lipid Nanoparticle ◽  
Solid Lipid ◽  
Lipid Nanoparticle

Cilinidipine is a fourth generation N and L-type calcium channel antagonists used alone or in combination with another drug to treat hypertension. Cilnidipine is poorly water -soluble, BCS class II drug with 6 to 30 percent oral bioavailability due to first pass metabolism. So to protect the drug from degradation and improve its dissolution, solid lipid nanoparticles were prepared. Glyceryl monostearate was selected as lipid while span 20: tween 20 were selected as surfactant blends. The formulations were evaluated for various parameters, as percent transmittance, drug content, percent encapsulation efficiency; percent drug loading, In vitro drug release and particle size. Optimized formulation was lyophilized using lactose as a cryo-protectant. The lyophilized formulation was evaluated for micromeritic properties, particle size and in vitro dissolution. It was further evaluated for DSC, XRD, and SEM. Percent encapsulation efficiency and percent drug loading of optimized formulation (F3) were 78.66percent and 9.44percent respectively. The particle size of F3 formulation without drug was 204 nm and with the drug was 214 nm. The particle size of the reconstituted SLN was 219 nm. In DSC study, no obvious peaks for cilnidipine were found in the SLN of cilnidipine indicated that the cilnidipine must be present in a molecularly dissolved state in SLN. In X-ray diffractometry absence of peaks representing crystals of cilnidipine in SLN indicated that the drug was in an amorphous or disordered crystalline phase in the lipid matrix. Thus, solid lipid nanoparticle formulation is a promising way to enhance the dissolution rate of cilnidipine. Keywords: Cilnidipine, Solid Lipid Nanoparticle, Hypertension

Liposomal Mediated Carriers of α Lipoic Acid for the Treatment of Acute Lung Injury: Preclinical Study in Rat Model

2020 ◽  
Vol 10 (1) ◽  
pp. 53-57
Author(s):  
Yu Cao ◽  
Yanling Chai ◽  
Xiaoqun Niu ◽  
Bing Hai ◽  
Xiaojie He ◽  
...  
Keyword(s):  
Thin Film ◽  
Particle Size ◽  
Pulmonary Fibrosis ◽  
Lung Injury ◽  
Lipoic Acid ◽  
Encapsulation Efficiency ◽  
Drug Loading ◽  
Preclinical Study ◽  
Liposomal Formulation ◽  
Experimental Animals

The present investigation deals with formulation of lipoic acid as liposomal formulation and to evaluate its efficacy in Lung injury (Pulmonary Fibrosis). The liposomal formulation of Lipoic acid (LA-liposomes) was successfully prepared by thin film hydration method. Such prepared liposomes were characterized for particle size, encapsulation efficiency, drug loading etc. characteristic. An Pulmonary fibrosis was induced using Bleomycin experimental animals rats. The effect of LA liposomal formulation on pulmonary fibrosis was observed. The histopathological finding confirms the efficiency of formulation in attenuation of pulmonary fibrosis.

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.

Preparation of Simvastatin Loaded Nanostructured Lipid Carriers and Its Therapeutic Effect on Patients with Severe Acute Lung Injury

2021 ◽  
Vol 21 (2) ◽  
pp. 1184-1189
Author(s):  
Xijiao Yan ◽  
Wenkai Zhang ◽  
Xiangli Cheng ◽  
Linyi Hou
Keyword(s):  
Particle Size ◽  
Acute Lung Injury ◽  
Lung Injury ◽  
Encapsulation Efficiency ◽  
Drug Loading ◽  
Treated Group ◽  
Nanostructured Lipid Carriers ◽  
Average Particle ◽  
Inflammatory Factor ◽  
Group Model

Acute lung injury (ALI) is a critical illness but have not effective therapeutic modalities currently where recent studies have revealed anti-inflammatory pleiotropic effects and plaque stabilizing effects of statins so the purpose of this work is preparation of simvastatin loaded nanostructured lipid carriers (simvastatin-NLCs) and investigation of its efficacy in lung injury mice. The simvastatin-NLCs was prepared by thermal melting-low temperature curing method and the quality evaluation was performed with particle size distribution, encapsulation efficiency, and drug loading. Sixty C57BL/6 mice were divided into three experimental groups: blank group model group and simvastatin treated group. Simvastatin was administered intraperitoneally immediately after the LPS injection in animals of the treated group at a dose of 20 mg/kg/day. Lung injury degree and the protective effects of simvastatin against LPS-induced lung injury were assessed at the time-points of 24, 48, and 72 h post injection, and the in vivo efficacy of simvastatin-NLCs on mice was investigated. The average particle size of simvastatin-NLCs was (102.1±42.2) nm, the encapsulation efficiency was (94.6±2.5)%, and the drug loading was (5.78±0.57)%. After 24 hours of administration, the data shows that simvastatin-NLCs inhibit the levels of IL-6 and TNF-α inflammatory factor in the lungs of mice.

scholarly journals Encapsulation of L-ascorbic acid via polycaprolactone-polyethylene glycol-casein bioblends

2015 ◽  
Vol 17 (4) ◽  
pp. 32-36
Author(s):  
Erhan Ozsagiroglu ◽  
Yuksel Avcibasi Guvenilir
Keyword(s):  
Particle Size ◽  
Ascorbic Acid ◽  
Polyethylene Glycol ◽  
Drug Release ◽  
Encapsulation Efficiency ◽  
Drug Loading ◽  
Fickian Diffusion ◽  
Polymer Mixture ◽  
Release Ratio

Abstract The aim of this study was to encapsulate, L-ascorbic acid, in biopolymers in order to obtain (i) enhancing its encapsulation efficiency (ii) increasing drug release ratio using different pH mediums. Microparticles based on polycaprolactone, polyethylene glycol and casein are prepared by spray drying technique. Microparticles are in vitro characterized in terms of yield of production, particle size, morphology, encapsulation efficiency, and drug release. In this manner, the importance of the study is producing of a stable and effective drug encapsulation system by PCL-PEG-CS polymer mixture by spray dryer. We achieved minimum 27.540±0.656 μm particle size with 0.512 m2/g surface area, 84.05% maximum drug loading, and 68.92% drug release ratio at pH 9.6. Release profiles are fitted to previously developed kinetic models to differentiate possible release mechanisms. The Korsmeyer–Peppas model is the best described each release scenario, and the drug release is governed by non-Fickian diffusion at pH 9.6. Our study proposed as an alternative or adjuvants for controlling release of L-ascorbic acid.

scholarly journals Development of a novel intraarticular injection of diclofenac for the treatment of arthritis: a preclinical study in the rabbit model

2021 ◽  
Author(s):  
Xinyuan Wen ◽  
Xiaoqing Huang ◽  
Huosheng Wu
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Zeta Potential ◽  
Encapsulation Efficiency ◽  
Drug Loading ◽  
Average Particle Size ◽  
Rabbit Model ◽  
Intraarticular Injection ◽  
Average Particle ◽  
Prepared Nanoparticles

Purpose: To develop a novel intraarticular injection of diclofenac for the treatment of arthritis. Method: Diclofenac loaded nanoparticles were prepared by a nanoprecipitation technique using Eudragit L 100 as the polymer and polyvinyl alcohol as the surfactant. The nanoparticles were evaluated for particle size, zeta potential, scanning electron microscopy, drug release, encapsulation efficiency, and loading efficiency studies. The optimized nanoparticulate formulation was developed for intra articular injection. Intraarticulate injection was evaluated for pH, appearance, viscosity, osmolarity and syringability studies. The optimized injection formulation was tested in an arthritic model consisting of 25 rabbits. Result: Nanoprecipitation method was found to be suitable for diclofenac nanoparticles. The shape of the prepared nanoparticles was found to be spherical and devoid of any cracks and crevices. The average particle size of a diclofenac nanoparticle was found to range from 87±0.47 to 103±0.26 nm. The zeta potential of the prepared nanoparticles was found to be in the range of 0.598±0.34 to 0.826±0.25 mV. The encapsulation efficiency was found to be between 73.45% to 99.03%, while the drug loading was observed between 10.34 to 35.32%. The percentage drug release at 12 hours was found to range from 73.45% to 99.03%. Conclusion: The developed intraarticular injection was found to be within the physically and chemically accepted limits. Animals treated with the intra articular injection of diclofenac showed a significant reduction in swelling as compares to the other groups.

scholarly journals Preparation, Characterization, and Pharmacokinetic Evaluation of Imperatorin Lipid Microspheres and Their Effect on the Proliferation of MDA-MB-231 Cells

Pharmaceutics ◽  
2018 ◽  
Vol 10 (4) ◽  
pp. 236 ◽  
Author(s):  
Xinli Liang ◽  
Xulong Chen ◽  
Guowei Zhao ◽  
Tao Tang ◽  
Wei Dong ◽  
...  
Keyword(s):  
Particle Size ◽  
Response Surface ◽  
Encapsulation Efficiency ◽  
Drug Loading ◽  
Experimental Conditions ◽  
Zeta Potentials ◽  
Preparation Conditions ◽  
Egg Lecithin ◽  
Central Composite ◽  
Lipid Microsphere

Imperatorin is a chemical compound belonging to the linear furanocoumarins. Imperatorin is attracting considerable attention because of its antitumor, antibacterial, anti-inflammatory, and anticoagulant activities, inhibition of myocardial hypertrophy, and other pharmacological efficacies. However, imperatorin has limited water solubility and has better lipid solubility; thus, we decided to design and synthesize imperatorin lipid microspheres to optimize the preparation conditions. The aim was to develop and formulate imperatorin lipid microspheres through nanoemulsion technology and apply the response surface–central composite design to optimize the imperatorin lipid microsphere formulation. The influence of the amounts of egg lecithin, poloxamer 188, and soybean oil for injection on the total percentage of the oil phase was investigated. The integrated effect of dependent variables, including particle size, polydispersity index, zeta potentials, drug loading, and encapsulation efficiency, was investigated. Data of overall desirabilities were fitted to a second-order polynomial equation, through which three-dimensional response surface graphs were described. Optimum experimental conditions were calculated by Design-Expert 8.06. Results indicated that the optimum preparation conditions were as follows: 1.39 g of egg lecithin, 0.21 g of poloxamer 188, and 10.57% soybean oil for injection. Preparation of imperatorin lipid microspheres according to the optimum experimental conditions resulted in an overall desirability of 0.7286, with the particle size of 168 ± 0.54 nm, polydispersity index (PDI) of 0.138 ± 0.02, zeta potentials of −43.5 ± 0.5 mV, drug loading of 0.833 ± 0.27 mg·mL−1, and encapsulation efficiency of 90 ± 1.27%. The difference between the observed and predicted values of the overall desirability of the optimum formulation was in the range from 2.4% to 4.3%. Subsequently, scanning electron microscopy was used to observe the micromorphology of the imperatorin lipid microspheres, showing round globules of relatively uniform shape and sizes within 200 nm. The effect of imperatorin lipid microspheres on MDA-MB-231 proliferation was investigated by the MTT method. Furthermore, pharmacokinetics in Sprague-Dawley rats was evaluated using orbital bleeding. A sensitive and reliable liquid chromatography with the high-performance liquid chromatography (HPLC) method was established and validated for the quantification of imperatorin in rat plasma samples. The data were calculated by DAS (drug and statistics) Pharmacokinetic Software version 3.3.0 (Version 3.3.0, Shanghai, China). Results demonstrated that imperatorin lipid microspheres can significantly enhance the bioavailability of imperatorin and can significantly inhibit MDA-MB-231 cell proliferation. In conclusion, our results suggested that the response surface–central composite design is suitable for achieving an optimized lipid microsphere formulation. Imperatorin lipid microspheres can improve the bioavailability of imperatorin and better inhibit the proliferation of MDA-MB-231 cells as compared to imperatorin alone.

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.

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