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.

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.

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.

Development of Oral Chewable Tablets Containing Montelukast Nanoparticles for the Treatment of Childhood Asthma: Preclinical Study in Animal Model

2021 ◽  
Vol 11 (4) ◽  
pp. 786-791
Author(s):  
Ye Liu ◽  
Guihua Xia ◽  
Shaosheng Liu ◽  
Zhenyu Song
Keyword(s):  
Zeta Potential ◽  
Encapsulation Efficiency ◽  
Drug Loading ◽  
Crosslinking Agent ◽  
Preclinical Study ◽  
Control Group ◽  
Physical Parameters ◽  
Disintegration Time ◽  
Saturation Solubility ◽  
Chewable Tablets

The aim of the present study was to formulate oral chewable tablets of Montelukast (MTL) in the form of nanoparticles (NP’s). The MTL loaded NP’s were formulated by ionotropic external gelation method using tripolyphosphate (TPP) as crosslinking agent and Tween 60 as surfactant. NP’s were characterized for drug loading, encapsulation efficiency, surface morphology, saturation solubility, particle size, zeta potential and polydispersity index. The optimized NP formulation was used for development of chewable tablets using direct compression method. The prepared tablets were characterized for disintegration test, dissolution, thickness, hardness, friability and assay. The optimized formulation was evaluated in asthamatic animals to demonstrate the efficiency in asthama. The encapsulation efficiency of NP’s was found between 91.24 to 98.21% while drug loading was in the range of 10.09–14.25%. All formulations were found of nanosized in nature (110 to 200 nm) with excellent zeta potential (20.12 to 22.27 mV). PDI of all NP formulations were found within acceptable limit (less than 0.3). The nanoparticles were found spherical in shape with smooth surface. The saturation solubility of MTL was enhanced nearly 10 times (92 mg/ml) as compared to pure MTL saturation solubility. All physical parameters of the tablets were found within range. The optimized tablets showed disintegration time of 20 sec while other formulations showed DT in the rage of 35–57 sec. Tab1 (Optimized formulation) showed almost 100% MTL release from chewable tablets within the period of 30 min. Reduction in lung resistance (RI) was found in animals treated with Tab1. This reduction in RI was found nearly two fold and three fold as compare to MTL treated and control group animals. These observations clearly support the efficacy of chewable tablets containing nanoparticulate MTL in asthmatic animals.

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.

NANOEMULSIONS BASED ON LIPOIC ACID DERIVATIVES WITH VARIOUS ALCOHOLS: PRODUCTION AND INFLUENCE ON FUNCTIONAL ACTIVITY OF PLATELETS

2020 ◽  
pp. 461-464
Author(s):  
A. Sinebryukhova ◽  
A. Shipelova ◽  
E. Darnotuk ◽  
A. Chekanov ◽  
O. Baranova ◽  
...  
Keyword(s):  
Particle Size ◽  
Arachidonic Acid ◽  
Lipoic Acid ◽  
Encapsulation Efficiency ◽  
Room Temperature ◽  
Optimal Conditions ◽  
Pluronic F68 ◽  
Long Term Storage ◽  
Term Storage

The optimal conditions were selected for obtaining homogeneous nanoemulsions (NE) of lipoic acid conjugates (LA-conjugates) based on Pluronic F68 (1,8%) with a particle size not exceeding 400 nm, characterized by 97±2% encapsulation efficiency of substances in nanoparticles (NP). A heterogeneous NE (polydispersity index, PDI>0,3) with the derivative of LA and myo-inositol based on phosphatidylcholine (PC, C = 3 mg/ml) was also obtained consisting of 2 particle fractions: 20–70 nm (27%) and 122–212 nm (73%). The obtained NEs with LA-conjugates based on Pluronic F68 and PC were stable during long-term storage (more than 12 months) at room temperature. The effect of the obtained NEs of LA-conjugates on platelet aggregation (Pt) caused by arachidonic acid (AA) was determined, and a mechanism of their action was proposed.

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

scholarly journals FORMULATION AND EVALUATION OF CURCUMIN LOADED LIPOSOME AND ITS BIO-ENHANCEMENT

2019 ◽  
Vol 9 (4-A) ◽  
pp. 425-437
Author(s):  
Khushboo Verma ◽  
Jhakeshwar Prasad ◽  
Suman Saha ◽  
Surabhi Sahu
Keyword(s):  
Thin Film ◽  
Particle Size ◽  
Drug Release ◽  
Zeta Potential ◽  
High Performance ◽  
Encapsulation Efficiency ◽  
Mean Particle Size ◽  
Liposome Formulation

The aim of this work was to develop and evaluate curcumin loaded liposome and its bio- enhancement. Curcumin was selected as a natural drug for liposome formulation. Curcumin show variety of biological activity but it also shows poor bioavailability due to low aqueous solubility (1 µg/ml), poor absorption and rapid metabolism so that piperine was selected as bio enhancer to improve curcumin bioavailability. Soy lecithin and cholesterol were used to prepared curcumin and curcumin-piperine loaded liposome at different ratio by thin film hydration method because of easy to perform, and high encapsulation rates of lipid. The all liposome formulations (F1-F5) were evaluated by mean particle size, polydispersity index, zeta potential, encapsulation efficiency and drug release. Bioavailability was also determined on rat. Blood samples were collected at specific intervals, and plasma was separated by ultracentrifugation. Plasma was analyzed by high-performance liquid chromatography at 425 nm taking acetonitrile: water (75:25 v/v) acidified with 2% acetic acid as a mobile phase at a flow rate of 0.5 ml/min using C18 column. The mean particle size was found in the range between 800-1100 that indicate liposome are large unilamellar vesical types. By zeta potential study its conform that the all formulation was stable. The encapsulation efficiency of all liposome formulation are varied between 59-67%. In vitro drug release was analyse in 7.4 pH phosphate buffer, the maximum %CDR observed at the 12 hrs., and formulation are follow sustained release thus they reduce metabolism, good absorption rate which improve bioavailability of drug. From in-vivo study, it is clear that curcumin-piperine liposomal formulation, increases Cmax, area under the curve, and mean residence time significantly as compared to pure curcumin and pure curcumin liposome. Keywords: liposome; Curcumin; Piperine, Thin film hydration method; Bioavailability

scholarly journals Characterization, purity assessment, and preparation of liposomal formulation of 2,4,6-trihydroxygeranylacetophenone

2020 ◽  
Vol 19 (10) ◽  
pp. 2025-2032
Author(s):  
Yamen Alkhateeb ◽  
Qais B. Jarrar ◽  
Faridah Abas ◽  
Yaya Rukayadi ◽  
Khozirah Shaari
Keyword(s):  
Particle Size ◽  
High Performance ◽  
Encapsulation Efficiency ◽  
Water Solubility ◽  
Analytical Techniques ◽  
Spectroscopic Characterization ◽  
Hplc Method ◽  
Liposomal Formulation ◽  
Poor Solubility ◽  
Quantitative Nuclear Magnetic Resonance

Purpose: To prepare, characterize, and determine the purity of 2,4,6-trihydroxygeranylacetophenone (tHGA), and also to develop and characterize a liposomal formulation of tHGA to overcome its poor water solubility. Methods: The tHGA was synthesized and then purified in two steps using two types of column chromatography separation techniques. The compound was characterized using different analytical techniques, while the purity of tHGA was determined by quantitative-nuclear magnetic resonance (qNMR). Proliposomes method was developed to produce liposome-encapsulated tHGA which was characterized based on particle size, polydispersity, stability, and encapsulation efficiency. A selective and rapid high-performance liquid chromatography (HPLC) method was developed and validated to quantify tHGA in a liposomal formulation in order to evaluate the encapsulation efficiency. Results: The tHGA was successfully prepared and characterized with 98.4 % purity. A simple and reproducible proliposomes method was successfully developed to produce liposome-encapsulated tHGA. The liposomal formulation exhibited excellent encapsulation efficiency (90.4 %). This formulation also yielded a homogenous liposome population (polydispersity index = 0.39) with a small particle size (250.8 nm). The prepared liposome-encapsulated tHGA was stable at refrigerated temperature (4 ºC) for at least four weeks. The developed HPLC method showed good linearity over the range of 10 to 500 μg/mL with high precision and accuracy. Conclusion: The compound produced has a high purity which can be used as an analytical reference standard. The developed formulation is  effective for dissolving and entrapping a high amount of tHGA which helps to overcome its poor solubility. Keywords: Liposomes, Proliposomes, Trihydroxygeranylacetophenone, tHGA, Spectroscopic characterization, Poor solubility

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.

scholarly journals Simple weak-acid derivatives of paclitaxel for remote loading into liposomes and improved therapeutic effects

RSC Advances ◽  
2020 ◽  
Vol 10 (46) ◽  
pp. 27676-27687
Author(s):  
Jiang Yu ◽  
Shuang Zhou ◽  
Jinbo Li ◽  
Yingli Wang ◽  
Yujiao Su ◽  
...  
Keyword(s):  
Encapsulation Efficiency ◽  
Drug Loading ◽  
Weak Acid ◽  
Liposomal Formulation ◽  
Therapeutic Effects ◽  
High Drug ◽  
Therapeutic Efficiency ◽  
Remote Loading ◽  
Derivatives Of ◽  
High Drug Loading

A remote loading liposomal formulation of weak-acid paclitaxel derivative with high encapsulation efficiency and high drug loading, improved therapeutic efficiency and negligible toxicity.

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