scholarly journals Size-Dependent Biodistribution of Fluorescent Furano-Allocolchicinoid-Chitosan Formulations in Mice

Polymers ◽  
2021 ◽  
Vol 13 (13) ◽  
pp. 2045
Author(s):  
Iuliia Gracheva ◽  
Maria Konovalova ◽  
Dmitrii Aronov ◽  
Ekaterina Moiseeva ◽  
Alexey Fedorov ◽  
...  

The aim of this study was to compare the biodistribution in mice of functionalized rhodamine B (Rh) labeled colchicine derivative furano-allocolchicinoid (AC, 6) either conjugated to 40 kDa chitosan (AC-Chi, 8) or encapsulated into chitosan nanoparticles (AC-NPs). AC-NPs were formed by ionotropic gelation and were 400–450 nm in diameter as estimated in mice by dynamic light scattering and confocal microscopy. AC-Chi and AC-NPs preserved the specific colchicine activity in vitro. AC preparations were once IV injected into C75BL/6 mice; muscles, spleen, kidney, liver, lungs, blood cells and serum were collected at 30 min, 2, 5, 10, and 20 h post injection. To analyze the distribution of the furano-allocolchicinoid preparations in body liquids and tissues, Rh was measured directly in sera or extracted by acidic ethanol from tissue homogenates. Preliminary Rh extraction rate was estimated in vitro in tissue homogenates and was around 25–30% from total quantity added. After in vivo injection, AC-NPs were accumulated more in liver and spleen, while less in kidney and lungs in comparison with free AC and AC-Chi. Therefore, incorporation of colchicine derivatives as well as other hydrophobic substances into nano/micro sized carriers may help redistribute the drug to different organs and, possibly, improve antitumor accumulation.

2021 ◽  
Vol 8 (2) ◽  
Author(s):  
Yue Li ◽  
QingQing Leng ◽  
XianLun Pang ◽  
Huan Shi ◽  
YanLin Liu ◽  
...  

Abstract Dermal injury, including trauma, surgical incisions, and burns, remain the most prevalent socio-economical health care issue in the clinic. Nanomedicine represents a reliable administration strategy that can promote the healing of skin lesions, but the lack of effective drug delivery methods can limit its effectiveness. In this study, we developed a novel nano-drug delivery system to treat skin defects through spraying. We prepared curcumin-loaded chitosan nanoparticles modified with epidermal growth factor (EGF) to develop an aqueous EGF-modified spray (EGF@CCN) for the treatment of dermal wounds. In vitro assays showed that the EGF@CCN displayed low cytotoxicity, and that curcumin was continuously and slowly released from the EGF@CCN. In vivo efficacy on wound healing was then evaluated using full-thickness dermal defect models in Wistar rats, showing that the EGF@CCN had significant advantages in promoting wound healing. On day 12 post-operation, skin defects in the rats of the EGF@CCN group were almost completely restored. These effects were related to the activity of curcumin and EGF on skin healing, and the high compatibility of the nano formulation. We therefore conclude that the prepared nano-scaled EGF@CCN spray represents a promising strategy for the treatment of dermal wounds.


1973 ◽  
Vol 51 (12) ◽  
pp. 933-941 ◽  
Author(s):  
Njanoor Narayanan ◽  
Jacob Eapen

The effect of cycloheximide in vitro and in vivo on the incorporation of labelled amino acids into protein by muscles, liver, kidneys, and brain of rats and pigeons was studied. In vitro incorporation of amino acids into protein by muscle microsomes, myofibrils, and myofibrillar ribosomes was not affected by cycloheximide. In contrast, administration of the antibiotic into intact animals at a concentration of 1 mg/kg body weight resulted in considerable inhibition of amino acid incorporation into protein by muscles, liver, kidneys, and brain. This inhibition was observed in all the subcellular fractions of these tissues during a period of 10–40 min after the administration of the precursor. Tissue homogenates derived from in vivo cycloheximide-treated animals did not show significant alteration in in vitro amino acid incorporation with the exception of brain, which showed a small but significant enhancement.


Nanoscale ◽  
2013 ◽  
Vol 5 (24) ◽  
pp. 12633 ◽  
Author(s):  
Yun Zeng ◽  
Shaojuan Zhang ◽  
Menghui Jia ◽  
Yang Liu ◽  
Jin Shang ◽  
...  

2009 ◽  
Vol 20 (11) ◽  
pp. 1587-1596 ◽  
Author(s):  
Dongqing Luo ◽  
Jianhua Guo ◽  
Fengjie Wang ◽  
Jing Sun ◽  
Guangwu Li ◽  
...  

Author(s):  
Ranjith Kumar Averineni ◽  
Gopal Venkatesh Shavi ◽  
Om Prakash Ranjan ◽  
Praful Balavant Deshpande ◽  
Gurram Aravind Kumar ◽  
...  

2015 ◽  
Vol 51 (2) ◽  
pp. 467-477 ◽  
Author(s):  
Abdul Baquee Ahmed ◽  
Ranjit Konwar ◽  
Rupa Sengupta

<p>In this study, we prepared atorvastatin calcium (AVST) loaded chitosan nanoparticles to improve the oral bioavailability of the drug. Nanoparticles were prepared by solvent evaporation technique and evaluated for its particle size, entrapment efficiency, zeta potential, <italic>in vitro</italic> release and surface morphology by scanning electron microscopy (SEM). In addition, the pharmacokinetics of AVST from the optimized formulation (FT5) was compared with marketed immediate release formulation (Atorva<sup>(r))</sup> in rabbits. Particle size of prepared nanoparticles was ranged between 179.3 ± 7.12 to 256.8 ± 8.24 nm with a low polydispersity index (PI) value. Zeta potential study showed that the particles are stable with positive values between 13.03 ± 0.32 to 46.90 ± 0.49 mV. FT-IR studies confirmed the absence of incompatibility of AVST with excipient used in the formulations. <italic>In vitro</italic> release study showed that the drug release was sustained for 48 h. Results of pharmacokinetics study showed significant changes in the pharmacokinetic parameter (2.2 fold increase in AUC) of the optimized formulation as compared to marketed formulation (Atorva<sup>(r))</sup>. Thus, the developed nanoparticles evidenced the improvement of oral bioavailability of AVST in rabbit model.</p>


2019 ◽  
Vol 2019 ◽  
pp. 1-9 ◽  
Author(s):  
Li Zhang ◽  
Yaoren Hu

Alphastatin is a 24-amino acid peptide and can suppress tumor angiogenesis by inhibiting both the migration and tubule formation of vascular endothelial cells. However, the anticancer effect of Alphastatin is limited due to the short half-life and degradation in the body. In this study, Alphastatin-loaded chitosan nanoparticles (AsCs NPs) were prepared with an initial concentration of 2 mg/ml for chitosan and 1 mg/ml for Alphastatin. AsCs NPs presented the encapsulation efficiency of 32.4%, the mean particle size of 387.4 nm, the polydispersity index of 0.223, and the zeta potential of +28.1 mV. AsCs NPs have a sustained release for 6 days and were stable in serum for at least 24 hours. And the NPs could preserve the integrity of encapsulated Alphastatin and released Alphastatin for 24 hours. In a subcutaneous LA975 lung carcinoma xenograft T739 mouse model, AsCs NPs significantly inhibited the tumor growth, tumor volume, and microvessel density (MVD), and the antitumor effect was even stronger than that of Alphastatin. In addition, the VEGF-induced tube formation of HUVEC could be inhibited by AsCs NPs in vitro and the serum containing AsCs NPs, and the protein level of SphK1 in HUVEC was also decreased by AsCs NPs, suggesting an inhibitory effect of AsCs NPs on the SphK1-S1P signaling pathway. Furthermore, hemolysis assay showed a safety on blood compatibility of AsCs NPs. Our study indicated that AsCs NPs inhibited the SphK1-S1P signaling pathway and enhanced the antiangiogenic effect of Alphastatin both in vitro and in vivo.


Sign in / Sign up

Export Citation Format

Share Document