Characterization and toxicity of citral incorporated with nanostructured lipid carrier

The nanoparticle as a cancer drug delivery vehicle is rapidly under investigation due to its promising applicability as a novel drug delivery system for anticancer agents. This study describes the development, characterization and toxicity studies of a nanostructured lipid carrier (NLC) system for citral. Citral was loaded into the NLC using high pressure homogenization methods. The characterizations of NLC-citral were then determined through various methods. Based on Transmission Electron Microscope (TEM) analysis, NLC-Citral showed a spherical shape with an average diameter size of 54.12 ± 0.30 nm and a polydipersity index of 0.224 ± 0.005. The zeta potential of NLC-Citral was −12.73 ± 0.34 mV with an entrapment efficiency of 98.9 ± 0.124%, and drug loading of 9.84 ± 0.041%. Safety profile of the formulation was examined viain vitroandin vivoroutes to study its effects toward normal cells. NLC-Citral exhibited no toxic effects towards the proliferation of mice splenocytes. Moreover, no mortality and toxic signs were observed in the treated groups after 28 days of treatment. There were also no significant alterations in serum biochemical analysis for all treatments. Increase in immunomodulatory effects of treated NLC-Citral and Citral groups was verified from the increase in CD4/CD3 and CD8/CD3 T cell population in both NLC-citral and citral treated splenocytes. This study suggests that NLC is a promising drug delivery system for citral as it has the potential in sustaining drug release without inducing any toxicity.

Download Full-text

Enhancing Oral Bioavailability of Apigenin Using a Bioactive Self-Nanoemulsifying Drug Delivery System (Bio-SNEDDS): In Vitro, In Vivo and Stability Evaluations

Pharmaceutics ◽

10.3390/pharmaceutics12080749 ◽

2020 ◽

Vol 12 (8) ◽

pp. 749 ◽

Cited By ~ 3

Author(s):

Mohsin Kazi ◽

Abdullah Alhajri ◽

Sultan M. Alshehri ◽

Ehab M. Elzayat ◽

Osaid T. Al Meanazel ◽

...

Keyword(s):

Drug Delivery ◽

Drug Delivery System ◽

Delivery System ◽

Drug Loading ◽

Stability Study ◽

Bacterial Growth Rate ◽

Tem Analysis ◽

Pure Drug

Apigenin (APG) is a very well-known flavonoid for its anti-inflammatory and anticancer properties. The purpose of this study is to improve the solubility and bioavailability of APG using a stable bioactive self-nanoemulsifying drug delivery system (Bio-SNEDDS). APG was incorporated in an oil phase comprising coconut oil fatty acid, Imwitor 988, Transcutol P, and HCO30 to form a Bio-SNEDDS. This preparation was characterized for morphology, particle size, and transmission electron microscopy (TEM). The APG performance was investigated in terms of loading, precipitation, release and stability tests from the optimal Bio-SNEDDS. An antimicrobial test was performed to investigate the activity of the Bio-SNEDDS against the selected strains. Bioavailability of the Bio-SNEDDS was evaluated using Wister rats against the commercial oral product and the pure drug. The results demonstrated the formation of an efficient nanosized (57 nm) Bio-SNEDDS with a drug loading of 12.50 mg/gm which is around 500-fold higher than free APG. TEM analysis revealed the formation of spherical and homogeneous nanodroplets of less than 60 nm. The dissolution rate was faster than the commercial product and was able to maintain 90% APG in gastro intestinal solution for more than 4 h. A stability study demonstrated that the Bio-SNEDDS is stable at a harsh condition. The in vivo pharmacokinetics parameters of the Bio-SNEDDS formulation in comparison to the pure drug showed a significant increase in maximum concentration (Cmax) and area under the curve (AUC (0–t)) of 105.05% and 91.32%, respectively. Moreover, the antimicrobial study revealed moderate inhibition in the bacterial growth rate. The APG-Bio-SNEDDS could serve as potential carrier aimed at improving the clinical application of APG.

Download Full-text

A Smart Drug Delivery System Based on Thermo-Responsive Polymer Gated Au NRs@SiO2 Nano-Platform

Journal of Nanoelectronics and Optoelectronics ◽

10.1166/jno.2021.3071 ◽

2021 ◽

Vol 16 (7) ◽

pp. 1029-1036

Author(s):

Hongzhu Wang ◽

Mengxun Chen ◽

Liping Song ◽

Youju Huang

Keyword(s):

Drug Delivery ◽

Block Copolymer ◽

Drug Release ◽

Drug Delivery System ◽

Delivery System ◽

Photothermal Therapy ◽

Drug Loading ◽

Temperature Sensitive

A key challenge for nanoparticles-based drug delivery system is to achieve manageable drug release in tumour cell. In this study, a versatile system combining photothermal therapy and controllable drug release for tumour cells using temperature-sensitive block copolymer coupled Au NRs@SiO2 is reported. While the Au NRs serve as hyperthermal agent and the mesoporous silica was used to improve the drug loading and decrease biotoxicity. The block copolymer acted as “gatekeeper” to regulate the release of model drug (Doxorubicin hydrochloride, DOX). Through in vivo and in vitro experiments, we achieved the truly controllable drug release and photothermal therapy with the collaborative effect of the three constituents of the nanocomposites. The reported nanocomposites pave the way to high-performance controllable drug release and photothermal therapy system.

Download Full-text

Preparation and Characterization of Paclitaxel Palmitate Albumin Nanoparticles With High Loading Efficacy: an in Vitro and in Vivo Anti-tumor Study in Mouse Models

10.21203/rs.3.rs-131961/v1 ◽

2020 ◽

Author(s):

Hang Chen ◽

Sifan Huang ◽

Heyi Wang ◽

Xinmei Chen ◽

Haiyan Zhang ◽

...

Keyword(s):

Breast Cancer ◽

Drug Delivery ◽

Drug Delivery System ◽

Delivery System ◽

Drug Loading ◽

The Body ◽

Albumin Nanoparticles ◽

Loading System

Abstract Background: Combination of the prodrug technique with an albumin nanodrug-loaded system is a novel promising approach for cancer treatment. However, the long-lasting and far-reaching challenge for the treatment of cancers lies in how to construct the albumin nanometer drug delivery system with lead compounds and their derivatives. Results: In this study, we reported the preparation of injectable albumin nanoparticles (NPs) with a high and quantitative drug loading system based on the NabTM technology of paclitaxel palmitate (PTX-PA). Our experimental study on drug tissue distribution in vivo demonstrated that the paclitaxel palmitate albumin NPs (Nab-PTX-PA) remained in the tumor for a longer time post injection. Compared with saline and Abraxane® (nanoparticle albumin-bound (nab)-paclitaxel), intravenous injection of Nab-PTX-PA not only reduced the toxicity of the drug in normal organs and increased the body weight of the animals but maintained sustained release of paclitaxel (PTX) in the tumor, thereby displaying an excellent antitumor activity. Blood routine analysis showed that Nab-PTX-PA had fewer adverse effects or less toxicity to the normal organsand more importantly it inhibited tumor cell proliferation more effectively as compared with commercial Abraxane®.Conclusions: This carrier strategy for small molecule drugs is based on naturally evolved interactions between LCFAs(Long Chain Fatty Acids) and HSA(human serum albumin), demonstrated here for PTX. Nab-PTX-PA shows higher maximum tolerated doses and increased efficacy in vivo in breast cancer models, as compared to Abraxane for FDA-approved clinical formulations. This novel injectable Nab-PTX-PA platform has great potential as an effective drug delivery system in the treatment of breast cancer.

Download Full-text

Mesoporous bioglass/silk fibroin scaffolds as a drug delivery system: Fabrication, drug loading and release in vitro and repair calvarial defects in vivo

Journal of Wuhan University of Technology-Mater Sci Ed ◽

10.1007/s11595-014-0929-0 ◽

2014 ◽

Vol 29 (2) ◽

pp. 401-406 ◽

Cited By ~ 9

Author(s):

Xiaoxin Zhang ◽

Jiayin Zhang ◽

Bin Shi

Keyword(s):

Drug Delivery ◽

Drug Delivery System ◽

Silk Fibroin ◽

Delivery System ◽

Drug Loading ◽

Calvarial Defects ◽

Release In Vitro

Download Full-text

Exosome-based biomimetic nanoparticles targeted to inflamed joints for enhanced treatment of rheumatoid arthritis

10.21203/rs.3.rs-33553/v1 ◽

2020 ◽

Author(s):

Feili Yan ◽

Zhirong Zhong ◽

Yao Wang ◽

Hui Li ◽

Zhiqiang Mei ◽

...

Keyword(s):

Rheumatoid Arthritis ◽

Drug Delivery ◽

Drug Delivery System ◽

Delivery System ◽

Drug Loading ◽

Safety Evaluation ◽

Biomimetic Nanoparticles ◽

Term Administration

Abstract Backgroud: Glucocorticoids (GCs) show powerful treatment effect on rheumatoid arthritis (RA). However, the clinical application is limited by their nonspecific distribution after systemic administration and serious adverse reactions during long-term administration. To achieve better treatment and reduce side effect, we here established a biomimetic exosome (Exo) encapsulating dexamethasone sodium phosphate (Dex) nanoparticle (Exo/Dex), whose surface was modified with folic acid (FA)-polyethylene glycol (PEG)-cholesterol (Chol) compound to attain FPC-Exo/Dex active targeting drug delivery system. Results The size of FPC-Exo/Dex was 128.43 ± 16.27 nm, with a polydispersity index (PDI) of 0.36 ± 0.05, and the Zeta potential was − 22.73 ± 0.91 mV. The encapsulation efficiency (EE) of the preparation was 10.26 ± 0.73%, with drug loading efficiency (DLE) of 18.81 ± 2.05%. In vitro study showed this system displayed enhanced endocytosis and excellent anti-inflammation effect against RAW264.7 cells by suppressing pro-inflammatory cytokines and increasing anti-inflammatory cytokine. Further biodistribution study showed the fluorescence intensity of FPC-Exo/Dex was stronger than other Dex formulations in joints, suggesting its enhanced accumulation to inflammation sites. In vivo pharmacodynamic experiment displayed FPC-Exo/Dex could preserve the bone and cartilage of CIA mice better and significantly reduce inflamed joints. Next in vivo safety evaluation demonstrated this biomimetic drug delivery system had no obvious hepatotoxicity and exhibited desirable biocompatibility. Conclusion The present study provides a promising strategy for using exosome as nanocarrier to enhance the therapeutic effect of GCs against RA.

Download Full-text

RESEALED ERYTHROCYTES: A PROMISING APPROACH TO ENHANCE EFFICACY OF ANTICANCER DRUGS

INDIAN DRUGS ◽

10.53879/id.57.03.11645 ◽

2020 ◽

Vol 57 (03) ◽

pp. 9-20

Author(s):

◽

Prathibha Salve ◽

Rajendra Doijad ◽

Niranjan Chivate

Keyword(s):

Drug Delivery ◽

Drug Delivery System ◽

Anticancer Drugs ◽

Delivery System ◽

Release Kinetics ◽

Drug Loading ◽

The Body ◽

Zero Order Release

Targeted drug delivery system is a potential drug delivery system which delivers the drug to particular organ of interest only. This improves the therapeutic efficacy of the treatment by reducing the side effects of drug which are required in case of anticancer drugs. Erythrocytes have been the most interesting carrier and have found to possess great potential in drug targeting. Resealed erythrocytes are gaining more popularity because of their ability to circulate throughout the body, biocompatibility, zero order release kinetics, reproducibility and ease of preparation. In this review, we have made an attempt to understand the process in detail to prepare resealed erythrocytes, including its mechanism, source and isolation of erythrocytes, methods of drug loading, in vivo and in vitro characterization of resealed erythrocytes, with special emphasis on applications of resealed erythrocytes for cancer treatment. With this review we can conclude that resealed erythrocyte is a promising approach to enhance efficacy of anticancer drugs.

Download Full-text

Exosome-based biomimetic nanoparticles targeted to inflamed joints for enhanced treatment of rheumatoid arthritis

10.21203/rs.3.rs-33553/v2 ◽

2020 ◽

Author(s):

Feili Yan ◽

Zhirong Zhong ◽

Yao Wang ◽

Yue Feng ◽

Zhiqiang Mei ◽

...

Keyword(s):

Rheumatoid Arthritis ◽

Drug Delivery ◽

Drug Delivery System ◽

Delivery System ◽

Drug Loading ◽

Safety Evaluation ◽

Biomimetic Nanoparticles ◽

Term Administration

Abstract Background: Glucocorticoids (GCs) show powerful treatment effect on rheumatoid arthritis (RA). However, the clinical application is limited by their nonspecific distribution after systemic administration and serious adverse reactions during long-term administration. To achieve better treatment and reduce side effect, we here established a biomimetic exosome (Exo) encapsulating dexamethasone sodium phosphate (Dex) nanoparticle (Exo/Dex), whose surface was modified with folic acid (FA)-polyethylene glycol (PEG)-cholesterol (Chol) compound to attain FPC-Exo/Dex active targeting drug delivery system. Results: The size of FPC-Exo/Dex was 128.43 ± 16.27 nm, with a polydispersity index (PDI) of 0.36 ± 0.05, and the Zeta potential was -22.73 ± 0.91 mV. The encapsulation efficiency (EE) of the preparation was 10.26 ± 0.73%, with drug loading efficiency (DLE) of 18.81 ± 2.05%. In vitro study showed this system displayed enhanced endocytosis and excellent anti-inflammation effect against RAW264.7 cells by suppressing pro-inflammatory cytokines and increasing anti-inflammatory cytokine. Further biodistribution study showed the fluorescence intensity of FPC-Exo/Dex was stronger than other Dex formulations in joints, suggesting its enhanced accumulation to inflammation sites. In vivo biodistribution experiment displayed FPC-Exo/Dex could preserve the bone and cartilage of CIA mice better and significantly reduce inflamed joints. Next in vivo safety evaluation demonstrated this biomimetic drug delivery system had no obvious hepatotoxicity and exhibited desirable biocompatibility.Conclusion: The present study provides a promising strategy for using exosome as nanocarrier to enhance the therapeutic effect of GCs against RA.

Download Full-text