Cisplatin Nanoparticles for Folate Targeted Delivery in Ovarian Cancer: Study in SKOV-3 Cancer Cells

2020 ◽  
Vol 10 (7) ◽  
pp. 939-944
Author(s):  
Ruijing Wang ◽  
Guohong Shen ◽  
Qingfeng Lv ◽  
Min Pan

Tumor targeting of drug to specific site via use of folate is one the choicest method for enhancing specificity of Cisplatin. Chitosan was conjugated with folate via amino acylation method and Folate-chitosan-Cisplatin-nanoparticles (FA-CS-Cis-NP's) were prepared using ionotropic gelation method. Thus prepared nanoparticles were evaluated for various parameters such as particles size, % encapsulation efficiency, % drug release, cytotoxic assay, cellular uptake. The average particle size of nanoparticles was found to be 265 nm with encapsulation efficiency of 89.43%. The cumulative release of drug from dosage form was found to be 82.31% for 240 min. The higher level of intra-cellular accumulation of Cisplatin was found to be in case of FA-CS-Cis-NP's than conventional drug delivery when cultured with folate. The results indicate that targeting of FA-CSCis-NP's is possible with folate targeting and are proved as potential folate receptor positive tumor cell targeting drug delivery system.

Pharmaceutics ◽  
2019 ◽  
Vol 11 (9) ◽  
pp. 430 ◽  
Author(s):  
Xiaoxiao Sun ◽  
Nan Wang ◽  
Li-Ye Yang ◽  
Xiao-Kun Ouyang ◽  
Fangfang Huang

Nano anti-cancer drug carriers loaded with antineoplastic drugs can achieve targeted drug delivery, which enriches drugs at tumor sites and reduces the toxic side effects in normal tissues. Mesoporous silica nanoparticles (MSN) are good nano drug carriers, as they have large specific surface areas, adjustable pore sizes, easily modifiable surfaces, and good biocompatibility. In this work, polyethyleneimine (PEI) grafted MSN were modified with folic acid (FA) as an active target molecule using chemical methods. The product was characterized by SEM, TEM, Zetasizer nano, FTIR, and an N2 adsorption and desorption test. MSN-PEI-FA are porous nano particles with an average particle size of approximately 100 nm. In addition, the loading rate and release behavior of MSN-PEI-FA were studied with curcumin as a model drug. The results show that when loading curcumin to MSN-PEI-FA at 7 mg and 0.1 g, respectively, the encapsulation efficiency was 90% and the cumulative release rate reached more than 50% within 120 h at pH = 5. This drug delivery system is suitable for loading fat-soluble antineoplastic drugs for sustained release and pH sensitive delivery.


2020 ◽  
Vol 27 (22) ◽  
pp. 3623-3656 ◽  
Author(s):  
Bruno Fonseca-Santos ◽  
Patrícia Bento Silva ◽  
Roberta Balansin Rigon ◽  
Mariana Rillo Sato ◽  
Marlus Chorilli

Colloidal carriers diverge depending on their composition, ability to incorporate drugs and applicability, but the common feature is the small average particle size. Among the carriers with the potential nanostructured drug delivery application there are SLN and NLC. These nanostructured systems consist of complex lipids and highly purified mixtures of glycerides having varying particle size. Also, these systems have shown physical stability, protection capacity of unstable drugs, release control ability, excellent tolerability, possibility of vectorization, and no reported production problems related to large-scale. Several production procedures can be applied to achieve high association efficiency between the bioactive and the carrier, depending on the physicochemical properties of both, as well as on the production procedure applied. The whole set of unique advantages such as enhanced drug loading capacity, prevention of drug expulsion, leads to more flexibility for modulation of drug release and makes Lipid-based nanocarriers (LNCs) versatile delivery system for various routes of administration. The route of administration has a significant impact on the therapeutic outcome of a drug. Thus, the non-invasive routes, which were of minor importance as parts of drug delivery in the past, have assumed added importance drugs, proteins, peptides and biopharmaceuticals drug delivery and these include nasal, buccal, vaginal and transdermal routes. The objective of this paper is to present the state of the art concerning the application of the lipid nanocarriers designated for non-invasive routes of administration. In this manner, this review presents an innovative technological platform to develop nanostructured delivery systems with great versatility of application in non-invasive routes of administration and targeting drug release.


Author(s):  
Sumit Kumar ◽  
Dinesh Chandra Bhatt

Fabrication and evaluation of the Isoniazid loaded sodium alginate nanoparticles (NPs) was main objective of current investigation. These NPs were engineered using ionotropic gelation technique. The NPs fabricated, were evaluated for average particle size, encapsulation efficiency, drug loading, and FTIR spectroscopy along with in vitro drug release. The particle size, drug loading and encapsulation efficiency of fabricated nanoparticles were ranging from 230.7 to 532.1 nm, 5.88% to 11.37% and 30.29% to 59.70% respectively. Amongst all batches studied formulation F-8 showed the best sustained release of drug at the end of 24 hours.


2019 ◽  
Vol 99 (4) ◽  
pp. 713-723 ◽  
Author(s):  
Gabriela Tasso Pinheiro Machado ◽  
Maria Beatriz Veleirinho ◽  
Letícia Mazzarino ◽  
Luiz Carlos Pinheiro Machado Filho ◽  
Marcelo Maraschin ◽  
...  

This study describes the development of propolis nanoparticles (PNP) to treat bovine mastitis. Three PNP prepared with varying concentrations of propolis (5% and 7%, w/v) and the surfactants [poloxamer (1%, 3%, and 4%, w/v) and soy lecithin (0.25%, 0.7%, and 1%, w/v)]. PNP were characterized according to their size, polydispersity, zeta potential, pH, morphology, and physical stability. PNP were evaluated for their in vitro antimicrobial and cytotoxic effects. PNP obtained were spherical with a monodisperse distribution (polydispersity index < 0.2) and an average particle size between 181 and 201 nm. Stability studies showed that PNP were stable over 150 d. The encapsulation efficiency of total phenolic content varied between 73% and 91%. The chromatographic profile of phenolic compounds from PNP showed selective encapsulation efficiency according to the polarity of compounds. All PNP showed antimicrobial activity against Staphylococcus aureus with a minimum inhibitory concentration ranging from 156 to 310 μg mL−1. The IC50 (the concentration responsible for reduction of cellular viability by half) for epithelial cells of bovine mammary gland (MAC-T, mammary alveolar cell-T) varied from 122.2 to 268.4 μg mL−1. Results showed that PNP represent a promising nanocarrier for high concentrations of propolis extract in a stable aqueous medium, while, at the same time, presenting antimicrobial activity accompanied by moderate cytotoxicity to the MAC-T cells.


2013 ◽  
Vol 684 ◽  
pp. 57-62 ◽  
Author(s):  
Zhi Hua Xing

Folic acid-chitosan (FA-CTS) and 10-hydroxycamptothecin (HCPT)-loaded folate-conjugated chitosan (FA-CTS/HCPT) microspheres were prepared by the ionic crosslinking method.The morphological characteristics of microspheres were examined using a scanning electron microscope (SEM). The average particle size and size distribution were determined by dynamic light scattering. The drug encapsulation efficiency (EE) , loading capacity (LC)and release characteristics in vitro were determined using ultraviolet spectrophotometer.The results shown that the microspheres are uniform spherical and regular with a size between 19.79 and81.40μm.Optimized preparation parameters lead to the successful preparation of hydroxycamptothecin-loaded folate-conjugated chitosan microspheres characterized with encapsulation efficiency and loading capacity up to (86.8±0.1)% and 20.6±0.3 % respectively. More then 90% of 10-hydroxycamptothecin was released from microspheres in 4 h at artificial gastric juice, 8h at artificial small intestinal fluid with a good delayed release effect.


2021 ◽  
Vol 9 ◽  
Author(s):  
Suchetan Pal ◽  
Tatini Rakshit

DNA origami has emerged as a versatile platform for diverse applications, namely, photonics, electronics, (bio) sensing, smart actuator, and drug delivery. In the last decade, DNA origami has been extensively pursued for efficient anticancer therapy. However, challenges remain to develop strategies that improve the targeting efficiency and drug delivery capability of the DNA origami nanostructures. In this direction, we developed folate-functionalized DNA origami that effectively targets and delivers doxorubicin (DOX), a well-known anticancer drug to the folate receptor alpha (FOLR1) expressing triple-negative breast cancer (TNBC) cells in vitro. We show that folate-functionalized DNA origami structure targets and kills FOLR1 overexpressing cells with better efficacy than nontargeted origami. We envision that this study will open up the possibility of target specific delivery of anticancer drug combinations using the versatile DNA origami nanostructures to the drug resistant cancer cells.


Polymers ◽  
2020 ◽  
Vol 12 (11) ◽  
pp. 2716
Author(s):  
Mona Ebadi ◽  
Kalaivani Buskaran ◽  
Saifullah Bullo ◽  
Mohd Zobir Hussein ◽  
Sharida Fakurazi ◽  
...  

In the last two decades, the development of novel approaches for cancer treatment has attracted intense attention due to the growing number of patients and the inefficiency of the available current conventional treatments. In this study, superparamagnetic iron oxide nanoparticles (SPIONs) were synthesized by the co-precipitation method in an alkaline medium. Then the nanoparticles were chemically modified by coating them with polyethylene glycol (PEG) and sorafenib (SO)–zinc/aluminum layered double hydroxide (ZLDH) to improve their biocompatibility. The SPIONs and their coated and drug-loaded nanoparticles, M-PEG–SO–ZLDH are of the crystalline phase with the presence of C, O, Al, Fe, Cl, Zn in the latter, indicating the presence of the coating layers on the surface of the SPIONs. The superparamagnetic properties of the bare SPIONs were found to be reduced but retained in its coated drug delivery nanoparticles, M-PEG–SO–ZLDH. The latter has an average particle size of 16 nm and the release of the drug from it was found to be governed by the pseudo-second-order kinetic. The cytotoxicity and biocompatibility evaluation of the drug-loaded magnetic nanoparticles using 3T3 and HepG2 cells using the diphenyltetrazolium bromide (MTT) assays shows that the synthesized nanoparticles were less toxic than the pure drug. This preliminary study indicates that the prepared nanoparticles are suitable to be used for the drug delivery system.


2020 ◽  
Vol 20 (9) ◽  
pp. 5313-5321
Author(s):  
Burcu Turkoglu ◽  
Banu Mansuroglu

Here we evaluate the cytotoxic and antioxidant properties of Catechin (Cat) loaded nanoparticles (CatNps) on breast cancer cell lines. CatNps were prepared by the modified single emulsion solvent evaporation method. The structural, physical and chemical properties of the CatNps including PLGA-Cat interactions, and surface characteristics, were analyzed by dynamic light scattering (DLS), Fourier transform infrared (FT-IR), and Scanning Electron Microscopy (SEM). The average particle size of CatNps was 190.5±1.762 nm with an encapsulation efficiency of 10% and zeta potential value of 13.7±1.258 mV. The CatNps had reaction yield of 43.47±1.1% and loading capacity of 3.710±2.6% Treating MCF-7 cells with CatNps for 48 h led to a decrease in cell viability with an of IC50 22.59 μg/mL. The antioxidant behavior of CatNps was evaluated by the DPPH method in various pH environments (pH 3-, 6-, 7.4-, 9- and 12). Despite the low encapsulation efficiency, CatNps showed significant antioxidant efficacy against DPPH radicals relative to Cat. Our results revealed that CatNps could be used as promising anti-cancer agents due to their enhanced cytotoxic activity, increased bioavailability, and antioxidant properties.


Author(s):  
Ling Zhao ◽  
Leyi Liang ◽  
Mimi Guo ◽  
Ming Li ◽  
Xuesong Yu ◽  
...  

Aims: Research on developing targeted delivery of anticancer drugs for the treatment of hepatocellular carcinoma (HCC) is ongoing. This study aimed at synthesizing nanoliposomes modified by glycyrrhetinic acid (GA) and ferric tetroxide (Fe3O4) for targeted delivery of paclitaxel for selective and specific therapy of HCC. Objective: During this project, GA and Fe3O4 were used to jointly modify the active targeting and magnetic orientation of paclitaxel nanoliposomes for enhanced targeting of HCC to improve the efficacy, while reducing the systemic toxicity and side effects of the drug. Methods: In this study, liposomes were prepared to utilize a thin film dispersion method, in which the average particle size of GA/Fe3O4-PTX-LP was 148.9 ± 2.3 nm, and the average Zeta potential was -23.2 ± 3 mV. Based on the TEM characterization, GA/Fe3O4-PTX-LP is a closed particle with bilayer membranes. In vitro release assessments of the drug indicated that the release of GA/Fe3O4-PTX-LP was sustained. Results: In vitro cell tests have demonstrated that GA/Fe3O 4-PTX-LP can inhibit the proliferation, affect the morphology, migration and invasion, and interfere with the cycle of HCC cells. Uptake tests have confirmed that GA/Fe3O4-PTX-LP can promote the uptake of the drug in HCC cells. Conclusion: In vivo targeting experiments have shown that GA/Fe3O4-PTX-LP has a strong ability to target tumors. In vivo antitumor assessments have proven that GA/Fe3O4-PTX-LP can inhibit tumor growth without obvious toxicity. This project provides a promising nano-targeted drug delivery system for the treatment of HCC.


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