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1.
Eur J Pharm Biopharm ; : 114350, 2024 Jun 05.
Article in English | MEDLINE | ID: mdl-38848783

ABSTRACT

Ginsenoside (GS), one of the main active components in ginseng, can enhance insulin sensitivity, improve the function of islet ß cells, and reduce cell apoptosis in the treatment of diabetes. However, the drawbacks of high lipid solubility, poor water solubility, and low oral availability in Ginsenoside Rg3 (G-Rg3) seriously limit further application of GS. In this work, a G-Rg3 PEGylated long-circulating liposome (PEG-L-Rg3) is designed and developed to improve symptoms in type 2 diabetic mice. The as-prepared PEG-L-Rg3 with a spherical structure shows a particle size of ∼ 140.5 ±â€¯1.4 nm, the zeta potential of -0.10 ±â€¯0.05 mV, and a high encapsulation rate of 99.8 %. Notably, in vivo experimental results demonstrate that PEG-L-Rg3 exhibits efficient ability to improve body weight and food intake in streptozotocin-induced type 2 diabetic mice. Moreover, PEG-L-Rg3 also enhances fasting insulin (FINS) and insulin sensitivity index (ISI). In addition, the glucose tolerance of mice is significantly improved after the treatment of PEG-L-Rg3, indicating that PEG-L-Rg3 can be a potential drug for the treatment of type 2 diabetes, which provides a new way for the treatment of type 2 diabetes using ginsenosides.

2.
Acta Pharm Sin B ; 13(8): 3277-3299, 2023 Aug.
Article in English | MEDLINE | ID: mdl-37655333

ABSTRACT

In recent years, owing to the miniaturization of the fluidic environment, microfluidic technology offers unique opportunities for the implementation of nano drug delivery systems (NDDSs) production processes. Compared with traditional methods, microfluidics improves the controllability and uniformity of NDDSs. The fast mixing and laminar flow properties achieved in the microchannels can tune the physicochemical properties of NDDSs, including particle size, distribution and morphology, resulting in narrow particle size distribution and high drug-loading capacity. The success of lipid nanoparticles encapsulated mRNA vaccines against coronavirus disease 2019 by microfluidics also confirmed its feasibility for scaling up the preparation of NDDSs via parallelization or numbering-up. In this review, we provide a comprehensive summary of microfluidics-based NDDSs, including the fundamentals of microfluidics, microfluidic synthesis of NDDSs, and their industrialization. The challenges of microfluidics-based NDDSs in the current status and the prospects for future development are also discussed. We believe that this review will provide good guidance for microfluidics-based NDDSs.

3.
Int J Pharm ; 643: 123247, 2023 Aug 25.
Article in English | MEDLINE | ID: mdl-37467813

ABSTRACT

Ginsenoside compound K (GCK) can efficiently treat rheumatoid arthritis (RA) due to its immune and anti-inflammatory functions. However, GCK exists some shortcomings such as poor aqueous solubility, low permeability to the intestinal cell membrane, and serious P-gp efflux, thus limiting its application. In order to solve these problems, a folic acid-targeted drug delivery system based on liposomes (FA-LP-GCK) was developed. The prepared FA-LP-GCK had a uniform size distribution and spherical structure, the particle size was 249.13 ± 1.40 nm. Meanwhile, they had high encapsulation efficiency (93.33 ± 0.05 %). FA-LP-GCK also presented good stability in artificial gastric juice, so they can be absorbed into the intestine and enter the blood circulation. The activated RAW 264.7 cells were chosen to evaluate the cytotoxicity and cellular uptake capacity of FA-LP-GCK. FA-LP-GCK showed stronger growth inhibition and cellular uptake ability against activated macrophages. Finally, the efficacy of FA-LP-GCK in vivo was evaluated in the adjuvant arthritis rat model. The results showed that FA-LP-GCK can significantly reduce joint swelling. Furthermore, it can significantly inhibit the expression of pro-inflammatory cytokines and improve synovial hyperplasia of joints and pathological changes in the spleen. Therefore, FA-LP-GCK may be a potential therapeutic approach for RA.


Subject(s)
Arthritis, Rheumatoid , Ginsenosides , Rats , Animals , Liposomes/therapeutic use , Drug Delivery Systems , Ginsenosides/pharmacology , Arthritis, Rheumatoid/drug therapy , Arthritis, Rheumatoid/metabolism , Folic Acid/metabolism
4.
Asian J Pharm Sci ; 17(2): 193-205, 2022 Mar.
Article in English | MEDLINE | ID: mdl-35582642

ABSTRACT

As an important means of communication among cells, exosomes are being studied more and more widely, especially in the context of cancer immunotherapy. In the phase of tumor immunoediting, exosomes derived from tumor cells and different immune cells have complex and changeable physiological functions, because they carry different proteins and nucleic acid from the source cells. Based on the role of exosomes in the communication between different cells, cancer treatment methods are also under continuous research. This review briefly introduces the molecular composition of exosomes, which is closely related to their secretion mechanism. Subsequently, the role of exosomes encapsulating different information molecules is summarized. The role of exosomes in the three phases of tumor immunoediting is introduced in detail, and the relevant literature of exosomes in the tumor immune microenvironment is summarized by using a novel framework for extracting relevant documents. Finally, it summarizes the various exosome-based immunotherapies currently proposed, as well as the challenges and future prospects of exosomes in tumor immunotherapy.

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