Glutathione-responsive PLGA nanocomplex for dual delivery of doxorubicin and curcumin to overcome tumor multidrug resistance

Nanomedicine ◽  
2021 ◽  
Author(s):  
Xuandi Lai ◽  
Xinran Geng ◽  
Mengqing Li ◽  
Mengxiong Tang ◽  
Qiong Liu ◽  
...  

Aim: This work aims to develop an injectable nano-drug delivery system to overcome tumor multidrug resistance (MDR). Methods: A drug delivery nanoplatform based on PEGylated PLGA with glutathione (GSH) responsivity was constructed for dual delivery of doxorubicin and curcumin (termed DCNP), and its MDR reversal efficiency was studied in vitro and in vivo. Results: The DCNPs exhibited a rapid drug release profile under high GSH concentration and could enhance the cellular uptake and cytotoxicity of doxorubicin to MDR cancer cells. Moreover, the DCNPs showed better biocompatibility, longer blood circulation and enhanced antitumor efficiency compared with free drugs. Conclusion: The GSH-responsive nanocarrier is believed to be a promising candidate for overcoming tumor MDR.

2021 ◽  
Vol 21 (2) ◽  
pp. 909-913
Author(s):  
Bin Pan ◽  
Peipei Li ◽  
Jing Chen ◽  
Jian Sun ◽  
Na Huang

In recent years, nanotechnology has made great progress in the development and application of tumor detection, diagnosis, and treatment, and eventually formed a “tumor nanomedicine.” The emerging field of “materials.” Nanoparticles have attracted much attention because they can overcome physiological barriers, effectively deliver hydrophobic drugs, and specifically target tumor tissues. At present, nanomedicines mainly include lipid nanoparticles, polymer nanoparticles granules, gold nanoparticles, magnetic nanoparticles, mesoporous silica, and other dosage forms. The use of nanomaterials as carriers in the treatment of lung cancer has unique advantages in achieving targeted drug delivery, slow-release drugs, and improvement of poorly soluble drugs and peptide drugs show obvious advantages in terms of bioavailability and reduction of adverse reactions, and have broad research and development prospects. This paper reports a new type of self-assembled Ptx-SA drug-loaded nanometers based on the carrier-free concept fiber, and it was found that the drug-loaded fiber has better cellophilicity, anti-tumor effect in vitro and in vivo than naked drug, and may be mediated by regulating the expression of related proteins. Therefore, the paclitaxel-loaded nano drug delivery system serves as a new type of nano preparation for treating lung cancer is worth further research.


2012 ◽  
Vol 584 ◽  
pp. 258-262 ◽  
Author(s):  
Sundarrajan Parani ◽  
Baddireddi Subhadra Lakshmi ◽  
Kanniyan Pandian

Alginate biopolymer stabilized CdTe quantum dot (QD) was prepared and it was encapsulated with folic acid conjugated chitosan for controlled drug delivery of anticancer drug 6-mercaptopurine (6-MP). In addition to alginate, chitosan enhances the stability of QD. Also, in addition to chitosan, alginate binds to the drug leading to enhance the loading efficiency of the resulting drug carrier. The drug release profile of the carrier was investigated by in-vitro. The present study has shown that this drug carrier is feasible for drug delivery and will be important beneficiary for cancer therapy.


2019 ◽  
Vol 9 (2) ◽  
pp. 97-101
Author(s):  
Rinku Gonekar ◽  
Mohan Lal Kori

The objective of the present study is to develop colon targeted drug delivery system using dextrin (polysaccharide) as a carrier for Azathioprine.  Microspheres containing azathioprine, dextrin and various excipients were prepared by solvent evaporation technique. The prepared microsphere were evaluated by different methods parameters like particle size,  drug entrapment efficiency, percentage yield, shape and surface morphology  and in vitro drug release study. Drug release profile was evaluated in simulated gastric, intestinal fluid and simulated colonic fluid. Best formulation was decided on the basis drug release profile in simulated gastric, intestinal fluid and simulated colonic fluid. In dextrin based microspheres, dextrin as a carrier was found to be suitable for targeting of Azathioprine for local action in the site of colon. Dextrin microspheres released 95-99% of azathioprine in simulated colonic fluid with 4% human fecal matter solution. The results of in-vitro studies of the azathioprine microspheres indicate that for colon targeting dextrin are suitable carriers to deliver the drug specifically in the colonic region. Dextrin based azathoprine microspheres showed no significance change in particle size and % residual upon storage at 5 ± 3ºC, 25 ± 2ºC/60 ± 5% RH (room temperature) and 40 ± 2ºC/75 ±5%RH humidity for three months. Keywords: azathioprine, microsphere, dextrin, colon specific drug delivery.


2020 ◽  
Vol 60 ◽  
pp. 102039
Author(s):  
Majid Hassanzadeganroudsari ◽  
Majid Soltani ◽  
Amir Heydarinasab ◽  
Vasso Apostolopoulos ◽  
Azim Akbarzadehkhiyavi ◽  
...  

RSC Advances ◽  
2020 ◽  
Vol 10 (29) ◽  
pp. 17270-17279 ◽  
Author(s):  
Guolian Ren ◽  
Pei Chen ◽  
Jiaqi Tang ◽  
Wenju Guo ◽  
Rongrong Wang ◽  
...  

To develop new, more effective and lower toxicity antitumor dihydroartemisinin (DHA) nanocomplexes, a DHA prodrug synthesized in this study was used to prepare DHA prodrug self-assembled nanocomplexes (DHANPs) by molecular self-assembly technology.


Author(s):  
Ririyen Dessy N Siahaan ◽  
Hakim Bangun ◽  
Sumaiyah Sumaiyah

Objective: The objective of this study was to evaluate in vitro and in vivo of gastroretentive drug delivery system of cimetidine using hard alginate capsules.Methods: Drug release study was tested to various hard alginate capsules containing 200 mg cimetidine with paddle method dissolution apparatus in artificial gastric fluid pH 1.2. Concentrations of cimetidine were measured using ultraviolet spectrophotometer at 218.4 nm wavelength. The product that fulfilled the sustained release profile was evaluated for bioavailability using male rabbits at dose 9.3 mg/kg orally, and the antiulcer studies were evaluated by HCl-induced ulcer method at cimetidine dose 18 mg/kg once a day orally. Gastric lesions were evaluated by macroscopic and microscopic observations.Results: The results of drug release test showed that hard alginate capsule made from sodium alginate 500–600 cP gave sustained release profile of cimetidine for 12 h. In vivo bioavailability studies showed that cimetidine given with hard alginate capsules gave higher of Cmax, Tmax, and area under the curve of cimetidine compared to cimetidine that given with conventional hard gelatin capsules. The antiulcer studies showed that the healing effect of cimetidine that given with hard alginate capsules was faster than cimetidine given in suspension form. Cimetidine that given with hard alginate capsules macroscopically showed no gastric lesion and histopathologically also showed normal gastric mucosa of rats after 4 days treatment. However, cimetidine given in suspension form showed of 0.036±0.024 ulcer index and microscopically there was still erosion of gastric mucosa of rats after 4 days treatment.Conclusion: Floating gastroretentive of cimetidine using hard alginate capsules give a sustained release of cimetidine with better bioavailability and antiulcer effect of cimetidine.


2017 ◽  
Vol 9 (5) ◽  
pp. 109
Author(s):  
Raditya Iswandana ◽  
Kurnia Sari Setio Putri ◽  
Randika Dwiputra ◽  
Tryas Yanuari ◽  
Santi Purna Sari ◽  
...  

Objective: Drug delivery to the colon via oral route can be directly treated a variety of diseases in the colon, such as fibrosis. Tetrandrine is a drug that has anti-fibrosis effects. In this study, chitosan-tripolyphosphate (TPP) beads containing tetrandrine was made and evaluated for in vitro release profile and in vivo targeted test.Methods: Chitosan-TPP tetrandrine beads were prepared by ionic gelation method with variation in sodium tripolyphosphate concentration: 3% (Formula 1), 4% (Formula 2), and 5% (Formula 3). All formulae were characterized for its morphology, particle size, moisture content, process efficiency, entrapment efficiency, thermal character, crystallinity, and swelling. Then, the best formula was coated with HPMCP HP-55, CAP, Eudragit L100-55, or Eudragit L100 prior to drug release profile in vitro and in vivo test.Results: Beads from all formulae had an average size: 920.50±0.04 µm, 942.21±0.08 µm, and 1085.95±0.03 µm; Water content: 7.28±0.003%, 5.64±0.005%, and 6.84±0.004%; Process efficiency: 29.70%, 28.96%, and 29.70%; Entrapment efficiency: 16.20±0.63%, 17.02±0.37%, and 20.42±0.70% for Formula 1, 2, and 3, respectively. In addition, the results of in vitro cumulative drug release were 67.36%, 76.04%, 83.12%, 83.21%, 40.16%, 37.98%, 45.86%, 41.71% for Formula 3A-3H, respectively.Conclusion: It can be concluded that Formula 3D (CAP 15%) was chosen as a formulation with the best in vitro profile. Moreover, the in vivo targeted test showed that Formula 3D was able to deliver the beads to the intestine compared to the control beads.


2021 ◽  
Vol 19 (1) ◽  
Author(s):  
Fan Li ◽  
Yan Liang ◽  
Miaochen Wang ◽  
Xing Xu ◽  
Fen Zhao ◽  
...  

AbstractSynergistic chemo-photodynamic therapy has garnered attention in the field of cancer treatment. Here, a pH cascade-responsive micellar nanoplatform with nucleus-targeted ability, for effective synergistic chemo-photodynamic cancer treatment, was fabricated. In this micellar nanoplatform, 5-(4-carboxyphenyl)-10,15,20-triphenylporphyrin (Por), a photodynamic therapy (PDT) agent was utilized for carrying the novel anticancer drug GNA002 to construct a hydrophobic core, and cyclic RGD peptide (cRGD)-modified polyethylene glycol (PEG) (cRGD-PEG) connected the cell-penetrating peptide hexaarginine (R6) through a pH-responsive hydrazone bond (cRGD-PEG-N = CH-R6) to serve as a hydrophilic shell for increasing blood circulation time. After passively accumulating in tumor sites, the self-assembled GNA002-loaded nanoparticles were actively internalized into cancer cells via the cRGD ligands. Once phagocytosed by lysosomes, the acidity-triggered detachment of the cRGD-PEG shell led to the formation of R6-coated secondary nanoparticles and subsequent R6-mediated nucleus-targeted drug delivery. Combined with GNA002-induced nucleus-specific chemotherapy, reactive oxygen species produced by Por under 532-nm laser irradiation achieved a potent synergistic chemo-photodynamic cancer treatment. Moreover, our in vitro and in vivo anticancer investigations revealed high cancer-suppression efficacy of this ideal multifunctional nanoplatform, indicating that it could be a promising candidate for synergistic anticancer therapy.


2012 ◽  
Vol 2012 ◽  
pp. 1-7 ◽  
Author(s):  
Elham Khodaverdi ◽  
Ali Golmohammadian ◽  
Seyed Ahmad Mohajeri ◽  
Gholamhossein Zohuri ◽  
Farnaz Sadat Mirzazadeh Tekie ◽  
...  

Traditional drug delivery systems which are based on multiple dosing regimens usually pose many disadvantages such as poor compliance of patients and drug plasma level variation. To overcome the obstacles of traditional drug formulations, novel drug delivery system PCL-PEG-PCL hydrogels have been purposed in this study. Copolymers were synthesized by rapid microwave-assisted and conventional synthesis methods. Polymer characterizations were done using gel permeation chromatography and 1H-NMR. Phase transition behavior was evaluated by inverting tube method and in vitro drug release profile was determined using naltrexone hydrochloride and vitamin B12 as drug models. The results indicated that loaded drug structure and copolymer concentration play critical roles in release profile of drugs from these hydrogels. This study also confirmed that synthesis of copolymer using microwave is the most effective method for synthesis of this kind of copolymer.


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