Preparation, Controlled Drug Release and Cell Viability Evaluation of Tenofovir alafenamide‐Loaded Chitosan Nanoparticles

2021 ◽  
pp. 2100144
Author(s):  
Ahmet Ulu ◽  
Selcen Korkmaz Sezer ◽  
Şengül Yüksel ◽  
Ahmet Koç ◽  
Burhan Ateş
2020 ◽  
pp. 088532822095259
Author(s):  
Ke Ma ◽  
Yongbin Cheng ◽  
Xinran Wei ◽  
Daijun Chen ◽  
Xiaoli Zhao ◽  
...  

In this work, gold embedded chitosan nanoparticles (Au@CS NPs) were fabricated by a one-pot method. The benzaldehyde-terminated poly[(2-methacryloyloxy) ethyl phosphorylcholine] (PMPC) was applied to modification of the gold doped chitosan nanoparticles. The obtained Au@CS-PMPC NPs had the diameter of 135 nm with a narrow distribution. The size of the Au@CS-PMPC NPs, as well as the size of the embedded gold NPs, might be well-controlled by adjusting the feeding ratio between chitosan and HAuCl4. Furthermore, the Au@CS-PMPC NPs showed increased colloidal stability, high drug loading content, pH-responsive drug release, excellent biocompatibility and bright fluorescence emission. The results demonstrated that Au@CS-PMPC NPs showed a great potential for tumor therapy via the combination advantages of pH-sensitive controlled drug release and cellular fluorescence imaging.


Pharmaceutics ◽  
2019 ◽  
Vol 12 (1) ◽  
pp. 26 ◽  
Author(s):  
Elisabetta Mazzotta ◽  
Selene De Benedittis ◽  
Antonio Qualtieri ◽  
Rita Muzzalupo

The clinical efficacy of methotrexate (MTX) is limited by its poor water solubility, its low bioavailability, and the development of resistance in cancer cells. Herein, we developed novel folate redox-responsive chitosan (FTC) nanoparticles for intracellular MTX delivery. l-Cysteine and folic acid molecules were selected to be covalently linked to chitosan in order to confer it redox responsiveness and active targeting of folate receptors (FRs). NPs based on these novel polymers could possess tumor specificity and a controlled drug release due to the overexpression of FRs and high concentration of reductive agents in the microenvironment of cancer cells. Nanoparticles (NPs) were prepared using an ionotropic gelation technique and characterized in terms of size, morphology, and loading capacity. In vitro drug release profiles exhibited a glutathione (GSH) dependence. In the normal physiological environment, NPs maintained good stability, whereas, in a reducing environment similar to tumor cells, the encapsulated MTX was promptly released. The anticancer activity of MTX-loaded FTC-NPs was also studied by incubating HeLa cells with formulations for various time and concentration intervals. A significant reduction in viability was observed in a dose- and time-dependent manner. In particular, FTC-NPs showed a better inhibition effect on HeLa cancer cell proliferation compared to non-target chitosan-based NPs used as control. The selective cellular uptake of FTC-NPs via FRs was evaluated and confirmed by fluorescence microscopy. Overall, the designed NPs provide an attractive strategy and potential platform for efficient intracellular anticancer drug delivery.


2012 ◽  
Vol 476-478 ◽  
pp. 1480-1483
Author(s):  
Chih Wei Chou ◽  
Yang Chia Shih ◽  
Te Hsing Wu

In this paper, we prepared and characterized the thiolated chitosan nanoparticles (CS NPs) Through modification. Bridged with a carbodiimide reagent, L-cysteine was therefore covalently bound to CS NPs which are capable of forming double bonds with thiol group and the mucus glycoprotein. A quantitative analysis of the widely used Ellman’s method can obtain the amount of thiol groups in various compounds. The resulted polymer conjugation displayed that the amount of thiol groups attached onto CS NPs, was increased with increasing concentration of cysteine. The method C exhibited greater conjugation ratio of thiol groups attached onto CS NPs. In particular, the evidence of thiol groups attached onto CS NPs was present in the thiolated specimens, can be shown by FTIR spectra.


Molecules ◽  
2021 ◽  
Vol 26 (2) ◽  
pp. 272
Author(s):  
Jhanvi Jhaveri ◽  
Zarna Raichura ◽  
Tabassum Khan ◽  
Munira Momin ◽  
Abdelwahab Omri

Nanotechnology-based development of drug delivery systems is an attractive area of research in formulation driven R&D laboratories that makes administration of new and complex drugs feasible. It plays a significant role in the design of novel dosage forms by attributing target specific drug delivery, controlled drug release, improved, patient friendly drug regimen and lower side effects. Polysaccharides, especially chitosan, occupy an important place and are widely used in nano drug delivery systems owing to their biocompatibility and biodegradability. This review focuses on chitosan nanoparticles and envisages to provide an insight into the chemistry, properties, drug release mechanisms, preparation techniques and the vast evolving landscape of diverse applications across disease categories leading to development of better therapeutics and superior clinical outcomes. It summarizes recent advancement in the development and utility of functionalized chitosan in anticancer therapeutics, cancer immunotherapy, theranostics and multistage delivery systems.


2019 ◽  
Vol 1 (1) ◽  
pp. 7
Author(s):  
R Nahrowi ◽  
A Setiawan ◽  
Noviany Noviany ◽  
I Sukmana ◽  
S D Yuwono

Paclitaxel is one of the cancer drugs that often used. These drug kills cancer cells byinhibiting mitotic cycle. The efficiency of paclitaxel is increased by the use ofnanomaterials as a carrier of paclitaxel. Nanomaterials can enhance encapsulationefficiency, improve the drug release to the target cell following nanomaterialdegradation, and improve local accumulation of drug in the cell through endocytosisreceptor. Nanomaterial that often used forencapsulation of paclitaxel is a polymerderived from natural resources such as cellulose. The advantages of cellulose as acarrier of paclitaxel are nontoxic, biodegradable, and very abundant from varioussources. One of the potential sources of cellulose for drug delivery system is cassavabaggase.Keywords: Paclitaxel, encapsulation, cell viability, nanocellulose


2018 ◽  
Vol 68 (12) ◽  
pp. 2925-2918
Author(s):  
Gabriela Cioca ◽  
Maricel Agop ◽  
Marcel Popa ◽  
Simona Bungau ◽  
Irina Butuc

One of the main challenges in designing a release system is the possibility to control the release rate in order to maintain it at a constant value below a defined limit, to avoid exceeding the toxicity threshold. We propose a method of overcoming this difficulty by introducing the drug into liposomes, prior to its inclusion in the hydrogel. Furthermore, a natural cross linker (as is tannic acid) is used, instead of the toxic cross linkers commonly used, thus reducing the toxicity of the release system as a whole.


2018 ◽  
Vol 14 (5) ◽  
pp. 432-439 ◽  
Author(s):  
Juliana M. Juarez ◽  
Jorgelina Cussa ◽  
Marcos B. Gomez Costa ◽  
Oscar A. Anunziata

Background: Controlled drug delivery systems can maintain the concentration of drugs in the exact sites of the body within the optimum range and below the toxicity threshold, improving therapeutic efficacy and reducing toxicity. Mesostructured Cellular Foam (MCF) material is a new promising host for drug delivery systems due to high biocompatibility, in vivo biodegradability and low toxicity. Methods: Ketorolac-Tromethamine/MCF composite was synthesized. The material synthesis and loading of ketorolac-tromethamine into MCF pores were successful as shown by XRD, FTIR, TGA, TEM and textural analyses. Results: We obtained promising results for controlled drug release using the novel MCF material. The application of these materials in KETO release is innovative, achieving an initial high release rate and then maintaining a constant rate at high times. This allows keeping drug concentration within the range of therapeutic efficacy, being highly applicable for the treatment of diseases that need a rapid response. The release of KETO/MCF was compared with other containers of KETO (KETO/SBA-15) and commercial tablets. Conclusion: The best model to fit experimental data was Ritger-Peppas equation. Other models used in this work could not properly explain the controlled drug release of this material. The predominant release of KETO from MCF was non-Fickian diffusion.


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