scholarly journals Synthesis, Characterization, and Evaluation of a Novel Amphiphilic Polymer RGD-PEG-Chol for Target Drug Delivery System

2014 ◽  
Vol 2014 ◽  
pp. 1-10 ◽  
Author(s):  
Shi Zeng ◽  
Fengbo Wu ◽  
Bo Li ◽  
Xiangrong Song ◽  
Yu Zheng ◽  
...  

An amphiphilic polymer RGD-PEG-Chol which can be produced in large scale at a very low cost has been synthesized successfully. The synthesized intermediates and final products were characterized and confirmed by1H nuclear magnetic resonance spectrum (1H NMR) and Fourier transform infrared spectrum (FT-IR). The paclitaxel- (PTX-) loaded liposomes based on RGD-PEG-Chol were then prepared by film formation method. The liposomes had a size within 100 nm and significantly enhanced the cytotoxicity of paclitaxel to B16F10 cell as demonstrated by MTT test (IC50= 0.079 μg/mL of RGD-modified PTX-loaded liposomes compared to 9.57 μg/mL of free PTX). Flow cytometry analysis revealed that the cellular uptake of coumarin encapsulated in the RGD-PEG-Chol modified liposome was increased for HUVEC cells. This work provides a reasonable, facile, and economic approach to prepare peptide-modified liposome materials with controllable performances and the obtained linear RGD-modified PTX-loaded liposomes might be attractive as a drug delivery system.

2020 ◽  
Vol 35 (1) ◽  
pp. 15-27 ◽  
Author(s):  
Taicheng Lu ◽  
Zhenzhen Nong ◽  
Liying Wei ◽  
Mei Wei ◽  
Guo Li ◽  
...  

In this study, a transferrin/folic acid double-targeting graphene oxide drug delivery system loaded with doxorubicin was designed. Graphene oxide was prepared by ultrasound improved Hummers method and was modified with Pluronic F68, folic acid, and transferrin to decrease its toxicity and to allow dual-targeting. The results show that the double target drug delivery system (TFGP*DOX) has good and controllable drug delivery performance with no toxicity. Moreover, TFGP*DOX has a better inhibitory effect on SMMC-7721 cells than does a single target drug delivery system (FGP*DOX). The results of drug release analysis and cell inhibition studies showed that TFGP*DOX has a good sustained release function that can reduce the drug release rate in blood circulation over time and improve the local drug concentration in or near a targeted tumor. Therefore, the drug loading system (TFGP*DOX) has potential application value in the treatment of hepatocellular carcinoma.


2021 ◽  
Vol 19 (1) ◽  
Author(s):  
Yan Lin ◽  
Yujie Wan ◽  
Xingjie Du ◽  
Jian Li ◽  
Jun Wei ◽  
...  

Abstract Background Spinal Cord injury (SCI) is a kind of severe traumatic disease. The inflammatory response is a significant feature after SCI. Tetramethylpyrazine (TMP), a perennial herb of umbelliferae, is an alkaloid extracted from ligustici. TMP can inhibit the production of nitric oxide and reduce the inflammatory response in peripheral tissues. It can be seen that the therapeutic effect of TMP on SCI is worthy of affirmation. TMP has defects such as short half-life and poor water-solubility. In addition, the commonly used dosage forms of TMP include tablets, dropping pills, injections, etc., and its tissue and organ targeting is still a difficult problem to solve. To improve the solubility and targeting of TMP, here, we developed a nanotechnology-based drug delivery system, TMP-loaded nanoparticles modified with HIV trans-activator of transcription (TAT-TMP-NPs). Results The nanoparticles prepared in this study has integrated structure. The hemolysis rate of each group is less than 5%, indicating that the target drug delivery system has good safety. The results of in vivo pharmacokinetic studies show that TAT-TMP-NPs improves the bioavailability of TMP. The quantitative results of drug distribution in vivo show that TAT-TMP-NPs is more distributed in spinal cord tissue and had higher tissue targeting ability compared with other treatment groups. Conclusions The target drug delivery system can overcome the defect of low solubility of TMP, achieve the targeting ability, and show the further clinical application prospect.


2018 ◽  
Vol 8 (5) ◽  
pp. 28-34 ◽  
Author(s):  
Jyoti Jyoti ◽  
Sandeep Kumar

Microsponge type of drug delivery is the latest technology which has been introduced in topical skin care, drug products to facilitate the controlled release of the active medicament into the skin in order to reduce systemic exposure and control local cutaneous reactions to active drugs. Microsponge can be loaded into a topical route of drug delivery system for the residue of dosage form of skin and thus controlled release drug delivery system is achieved and in return improving the patient compliance by providing target drug delivery system and prolonging dosage intervals. Microsponge is polymeric delivery systems composed of porous microspheres. They are tiny sponge-like spherical particles and posses large porous surface area. Furthermore, they may enhance stability, reduce side effects, improve patient compliance and modify drug release. Microsponges are the polymer-based microspheres system that has the capacity to entrap a wide variety of substances, and can then be incorporated into a different formulation. Keywords: Microsponge Delivery System, Quasi- emulsion solvent diffusion.


2020 ◽  
Author(s):  
Damiri Fouad ◽  
Yahya Bachra ◽  
Grouli Ayoub ◽  
Amine Ouaket ◽  
Ahmed Bennamara ◽  
...  

Recently, chitosan (CS) was given much attention as a functional biopolymer for designing various hydrogels for industrial, environmental and biomedical applications, but their biomedical use is limited due to the toxicity of the crosslinker agents. To overcome this inconvenience, we developed an auto cross-linked material based on a chitosan backbone that carries an amino and aldehyde moieties. This new drug delivery system (DDS) was designed by using oxidized chitosan (OCS) that crosslinks chitosan (CS). In the first part, a simple, rapid, low-cost and eco-friendly green method was introduced to synthesize magnetite nanoparticles (Fe3O4-NPs) successfully. These nanoparticles Fe3O4 have received a great deal of attention in the biomedical field. Especially in a targeted drug delivery system, drug-loaded Fe3O4-NPs can accumulate at the tumor site by the aid of an external magnetic field and increase the effectiveness of drug release to the tumor site. In the second part, we have incorporated the Fe3O4-NPs into chitosan/oxidized chitosan solution because of their unique magnetic properties, outstanding magnetism, biocompatibility, lower toxicity, biodegradability, and other features. Three drugs (5-Fluorouracil (5-FU), Caffeine and Ascorbic acid)) were embedded into the magnetite solution that became quickly a hydrogel. The successful fabrication of the hydrogels and ferrogels was confirmed by (FT-IR), (TGA), (SEM), (VSM) analysis at room temperature. Finally, results showed that our hydrogels and ferrogels may be technologically used as devices for drug delivery in a controllable manner.


Biology Open ◽  
2020 ◽  
Vol 9 (6) ◽  
pp. bio052241
Author(s):  
Qiying Liang ◽  
Peng Ma ◽  
Qi Zhang ◽  
Youjie Yin ◽  
Ping Wang ◽  
...  

ABSTRACTLarge-scale compound screening in adult flies is hampered by the lack of continuous drug delivery systems and poor solubility of numerous compounds. Here we found that gum Arabic (Acacia/Senegal gum), a widely used stabilizer, can also emulsify lipophilic compounds and profoundly increase their accessibility to target tissues in Drosophila and mice. We further developed a gum Arabic-based drug delivery system, wherein the drug was ground into gum Arabic and emulsified in liquid food fed to flies by siphoning through a U-shape glass capillary. This system did not affect food intake nor cell viability. Since drugs were continuously delivered by siphoning, minimal compound waste and less frequent food changes make this system ideal for large-scale long-term screenings. In our pilot screening for antitumor drugs in the NCI DTP library, we used a Drosophila model of colorectal cancer and identified two drugs that are especially hydrophobic and were not identified in previous screenings. Our data demonstrated that gum Arabic facilitates drug delivery in animal models and the system is suitable for long-term high-throughput drug screening in Drosophila. This system would accelerate drug discovery for chronic and cognitive conditions.


2014 ◽  
Vol 256 ◽  
pp. 352-360 ◽  
Author(s):  
Faiyaz Shakeel ◽  
Nazrul Haq ◽  
Fars K. Alanazi ◽  
Ibrahim A. Alsarra

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