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

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.

Download Full-text

Sodium Alginate Nanoparticles of Isoniazid: Preparation and Evaluation

International Journal of Pharmaceutical Sciences and Drug Research ◽

10.25004/ijpsdr.2019.110616 ◽

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.

Download Full-text

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

Journal of Biomaterials and Tissue Engineering ◽

10.1166/jbt.2020.2204 ◽

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.

Download Full-text

Casein Micelles as Nanocarriers for Benzydamine Delivery

Polymers ◽

10.3390/polym13244357 ◽

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.

Download Full-text

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

Acta Biochimica Polonica ◽

10.18388/abp.2020_5401 ◽

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.

Download Full-text

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

Journal of Nanoscience and Nanotechnology ◽

10.1166/jnn.2021.19347 ◽

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.

Download Full-text

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

Current Medicinal Chemistry ◽

10.2174/0929867326666190624155938 ◽

2020 ◽

Vol 27 (22) ◽

pp. 3623-3656 ◽

Cited By ~ 1

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.

Download Full-text

EGCG promotes PRKCA expression to alleviate LPS-induced acute lung injury and inflammatory response

Scientific Reports ◽

10.1038/s41598-021-90398-x ◽

2021 ◽

Vol 11 (1) ◽

Author(s):

Mian Wang ◽

Hua Zhong ◽

Xian Zhang ◽

Xin Huang ◽

Jing Wang ◽

...

Keyword(s):

Acute Lung Injury ◽

Lung Injury ◽

Signaling Pathway ◽

Weight Ratio ◽

Mapk Signaling ◽

Mapk Signaling Pathway ◽

Protective Mechanism ◽

High Morbidity ◽

Inflammatory Factor ◽

Egcg Treatment

AbstractAcute lung injury (ALI), which could be induced by multiple factors such as lipopolysaccharide (LPS), refer to clinical symptoms of acute respiratory failure, commonly with high morbidity and mortality. Reportedly, active ingredients from green tea have anti-inflammatory and anticancer properties, including epigallocatechin-3-gallate (EGCG). In the present study, protein kinase C alpha (PRKCA) is involved in EGCG protection against LPS-induced inflammation and ALI. EGCG treatment attenuated LPS-stimulated ALI in mice as manifested as improved lung injury scores, decreased total cell amounts, neutrophil amounts and macrophage amounts, inhibited the activity of MPO, decreased wet-to-dry weight ratio of lung tissues, and inhibited release of inflammatory cytokines TNF-α, IL-1β, and IL-6. PRKCA mRNA and protein expression showed to be dramatically decreased by LPS treatment while reversed by EGCG treatment. Within LPS-stimulated ALI mice, PRKCA silencing further aggravated, while PRKCA overexpression attenuated LPS-stimulated inflammation and ALI through MAPK signaling pathway. PRKCA silencing attenuated EGCG protection. Within LPS-induced RAW 264.7 macrophages, EGCG could induce PRKCA expression. Single EGCG treatment or Lv-PRKCA infection attenuated LPS-induced increases in inflammatory factors; PRKCA silencing could reverse the suppressive effects of EGCG upon LPS-stimulated inflammatory factor release. In conclusion, EGCG pretreatment inhibits LPS-induced ALI in mice. The protective mechanism might be associated with the inhibitory effects of PRKCA on proinflammatory cytokine release via macrophages and MAPK signaling pathway.

Download Full-text

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

Materials Science Forum ◽

10.4028/www.scientific.net/msf.654-656.2265 ◽

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.

Download Full-text

Development of Solid Lipid Nanoparticles and Nanostructured Lipid Carriers of Loteprednol Etabonate: Physicochemical Characterization and Ex Vivo Permeation Studies

10.21203/rs.3.rs-1145116/v1 ◽

2021 ◽

Author(s):

Burcu Üner ◽

Samet Özdemir ◽

Çetin Taş ◽

Yıldız Özsoy ◽

Melike Üner

Keyword(s):

Particle Size ◽

Solid Lipid Nanoparticles ◽

Drug Loading ◽

Physicochemical Characterization ◽

Lipid Nanoparticles ◽

Nanostructured Lipid Carriers ◽

Fickian Diffusion ◽

Control Group ◽

Loteprednol Etabonate ◽

Solid Lipid

Abstract Purpose Loteprednol etabonate (LE) is a new generation corticosteroid that is used for the treatment of inflammatory and allergic conditions of the eye, and management of seasonal allergic rhinitis nasally. LE which is a poorly soluble drug with insufficient bioavailability, has a high binding affinity to steroid receptors. Sophisticated colloidal drug delivery systems of LE could present an alternative for treatment of inflammatory and allergic conditions of the skin. For this purpose, solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC) were attempted to improve for transdermal LE delivery for the first time. Methods SLN and NLC were produced by hot homogenization and ultrasonication technique. Formulations were characterized by dynamic light scattering, scanning electron microscopy, fourier transform infrared spectroscopy and differential scanning calorimetry. Their physical stability was monitored for 3 months of storage. Drug release profiles and permeation properties of SLN and NLC through the porcine skin were investigated. Results It was determined that SLN and NLC below 150 nm particle size had a homogeneous particle size distribution as well as high drug loading capacities. They were found to be stable both physically and chemically at room temperature for 90 days. In terms of release kinetics, it was determined that they released from SLN and NLC in accordance with Fickian diffusion release. Formulations prepared in this study were seen to significantly increase drug penetration through pig skin compared to the control group (p ≤ 0.05). Conclusion SLN and NLC formulations of LE can be stated among the systems that can be an alternative to conventional systems with less side-effect profile in the treatment of inflammatory problems on the skin.

Download Full-text

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

Science of Advanced Materials ◽

10.1166/sam.2021.4109 ◽

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.

Download Full-text