scholarly journals Chitosan-Alginate Nanoparticle System Efficiently Delivers Doxorubicin to MCF-7 Cells

2016 ◽  
Vol 2016 ◽  
pp. 1-12 ◽  
Author(s):  
Nuwanthi P. Katuwavila ◽  
A. D. L. Chandani Perera ◽  
Sameera R. Samarakoon ◽  
Preethi Soysa ◽  
Veranja Karunaratne ◽  
...  
Keyword(s):  
Sustained Release ◽  
Slow Release ◽  
Sodium Tripolyphosphate ◽  
Chitosan Nanoparticles ◽  
Time Dependency ◽  
Initial Release ◽  
Nanoparticle System ◽  
Dose Dependent ◽  
Mcf 7

A chitosan-alginate nanoparticle system encapsulating doxorubicin (DOX) was prepared by a novel ionic gelation method using alginate as the crosslinker. These nanoparticles were around 100 nm in size and more stable with higher positive zeta potential and had higher % encapsulation efficiency (95%) than DOX loaded chitosan nanoparticles (DOX Csn NP) crosslinked with sodium tripolyphosphate (STPP). FTIR spectroscopy and thermogravimetric analysis revealed successful loading of DOX.In vitrodrug release showed an initial release phase followed by slow release phase with higher cumulative release obtained with DOX loaded chitosan-alginate nanoparticles (DOX Csn-Alg NP). Thein vitrocytotoxicity of DOX released from the two nanoparticle systems showed a notable difference on comparison with that of free DOX on the MCF-7 cell line. The SRB assay, AO/EB staining, and fluorescence uptake study indicated that free DOX only showed dose dependent cytotoxicity, whereas both dose and time dependency were exhibited by the two sets of NPs. While both systems show sustained release of DOX, from the cell viability plots, DOX Csn-Alg NPs showed their superiority over DOX Csn NPs. The results obtained are useful for developing DOX Csn-Alg NPs as a sustained release carrier system for DOX.

scholarly journals Formulation of Quaternized Aminated Chitosan Nanoparticles for Efficient Encapsulation and Slow Release of Curcumin

Molecules ◽  
2021 ◽  
Vol 26 (2) ◽  
pp. 449
Author(s):  
Ahmed M. Omer ◽  
Zyta M. Ziora ◽  
Tamer M. Tamer ◽  
Randa E. Khalifa ◽  
Mohamed A. Hassan ◽  
...  
Keyword(s):  
Slow Release ◽  
Sodium Tripolyphosphate ◽  
Chitosan Nanoparticles ◽  
Gastric Fluid ◽  
Release Profile ◽  
Simulated Gastric Fluid ◽  
Maximum Value ◽  
Structure Surface ◽  
Drug Encapsulation Efficiency

An effective drug nanocarrier was developed on the basis of a quaternized aminated chitosan (Q-AmCs) derivative for the efficient encapsulation and slow release of the curcumin (Cur)-drug. A simple ionic gelation method was conducted to formulate Q-AmCs nanoparticles (NPs), using different ratios of sodium tripolyphosphate (TPP) as an ionic crosslinker. Various characterization tools were employed to investigate the structure, surface morphology, and thermal properties of the formulated nanoparticles. The formulated Q-AmCs NPs displayed a smaller particle size of 162 ± 9.10 nm, and higher surface positive charges, with a maximum potential of +48.3 mV, compared to native aminated chitosan (AmCs) NPs (231 ± 7.14 nm, +32.8 mV). The Cur-drug encapsulation efficiency was greatly improved and reached a maximum value of 94.4 ± 0.91%, compared to 75.0 ± 1.13% for AmCs NPs. Moreover, the in vitro Cur-release profile was investigated under the conditions of simulated gastric fluid [SGF; pH 1.2] and simulated colon fluid [SCF; pH 7.4]. For Q-AmCs NPs, the Cur-release rate was meaningfully decreased, and recorded a cumulative release value of 54.0% at pH 7.4, compared to 73.0% for AmCs NPs. The formulated nanoparticles exhibited acceptable biocompatibility and biodegradability. These findings emphasize that Q-AmCs NPs have an outstanding potential for the delivery and slow release of anticancer drugs.

ROSUVASTATIN CALCIUM LOADED CHITOSAN NANOPARTICLES: PREPARATION EVALUATION AND IN VITRO RELEASE STUDIES

2020 ◽  
pp. 95-102
Author(s):  
SUVARNA G. BHOKARE ◽  
RAJENDRA P. MARATHE
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Sustained Release ◽  
Sodium Tripolyphosphate ◽  
Chitosan Nanoparticles ◽  
In Vitro Release ◽  
Particle Diameter ◽  
Vitro Release ◽  
Rosuvastatin Calcium

Objective: The objective of the present study was to develop sustained release biodegradable polymeric nanoparticles of rosuvastatin calcium. Methods: Nanoparticles were prepared by modified ionotropic gelation method using 3² full factorial designs. From the preliminary trials, the constraints for independent variables X1 (concentration. of chitosan) and X2 (concentration. of sodium tripolyphosphate) have been fixed. Factors included concentration of chitosan and sodium tripolyphosphate, have been examined to investigate effect on particle size, encapsulation efficiency, zeta potential, % release, scanning electron microscopy, Fourier transfer infrared study and X-ray diffraction and release study of rosuvastatin calcium nanoparticles. 0 Results: The prepared nanoparticles were white, free-flowing and spherical in shape. The infrared spectra showed stable character of rosuvastatin calcium in the drug-loaded nanoparticles and revealed the absence of drug polymer interactions. The chitosan nanoparticles have a particle diameter ranging approximately 114.5±3.61 to 724±.2.51 nm and a zeta potential-13.12 to-52.63 mV. The in vitro release behavior from all the drug loaded batches were found to follow first order and provided sustained release over a period of 10 h. The Zeta potential of all the batches were in the range of-13.12 to-52.63 mv. The release profiles of all batches were very well fitted by Korsmeyer Peppas model. Conclusion: The best-fit release kinetics was achieved with Korsmeyer peppas model. The release of rosuvastatin calcium was influenced by the drug to polymer ratio and particle size. These results indicate that rosuvastatin calcium nanoparticles could be effective in sustaining drug release for a prolonged period.

scholarly journals Design of Guggul Lipid Loaded Chitosan Nanoparticles Using Box-Behnken Design – An Evaluation Study

2021 ◽  
pp. 53-67
Author(s):  
B. R. Srinivas Murthy ◽  
Prasanna Raju Yelavarthi ◽  
N. Devanna ◽  
D. Jamal Basha
Keyword(s):  
Sustained Release ◽  
Lipid A ◽  
Sodium Tripolyphosphate ◽  
Desirability Function ◽  
Chitosan Nanoparticles ◽  
Entrapment Efficiency ◽  
Polynomial Equation ◽  
Ionic Gelation ◽  
Box Behnken Design

Aim: Guggul lipid, a lipophillic antihyperlipidemic moiety, undergoes extensive first-pass metabolism and has low bioavailability. In order to address this limitation, guggul lipid loaded chitosan nanoparticles (GNPs) were designed, optimized and processed by 3- factor 3- level Box- Behnken design (BBD). Methodology: A 3-factor 3-level BBD was employed to investigate combined influence of formulation variables on percent entrapment efficiency (EE) and percent drug release (DR) of GNPs prepared by ionic gelation method. The generated polynomial equation was validated and desirability function was utilized for optimization. Optimized GNPs were evaluated for physicochemical, morphological, release characteristics, solid state characterization and in-vitro cell line studies. Results: Amounts of chitosan, sodium tripolyphosphate and guggul were selected as independent variables had variably influenced EE and DR. Optimized GNPs were produced with an average size of 96.5 nm, electro kinetic potential of -15.4 mV, EE of 92.98% and DR of 95.12% in 24 h with sustained release. Physicochemical and in-vitro characterization revealed existence of guggul in amorphous form in GNPs without interaction and exhibited sustained release profile following first order with Higuchi kinetics. GNPs possessed lipase inhibition activity with IC50 value of 14.72 µg/ml and better viability against various cell lines with CTC50 values (256.24 to 321.27 µg/ml). Conclusions: Design and optimization of GNPs by BBD proved to be an effective and promising approach. High entrapment of guggul followed controlled release were the outcomes of GNPs prepared by ionic gelation with improved cell viability.

scholarly journals Synthesis and In Vitro Antitumor Activity of Novel Bivalent β-Carboline-3-carboxylic Acid Derivatives with DNA as a Potential Target

2018 ◽  
Vol 19 (10) ◽  
pp. 3179 ◽  
Author(s):  
Hongling Gu ◽  
Na Li ◽  
Jiangkun Dai ◽  
Yaxi Xi ◽  
Shijun Wang ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Cell Apoptosis ◽  
Docking Studies ◽  
In Vitro Cytotoxicity ◽  
Dependent Manner ◽  
Cycle Arrest ◽  
Dna Binding Affinity ◽  
Dose Dependent ◽  
Mcf 7

A series of novel bivalent β-carboline derivatives were designed and synthesized, and in vitro cytotoxicity, cell apoptosis, and DNA-binding affinity were evaluated. The cytotoxic results demonstrated that most bivalent β-carboline derivatives exhibited stronger cytotoxicity than the corresponding monomer against the five selected tumor cell lines (A549, SGC-7901, Hela, SMMC-7721, and MCF-7), indicating that the dimerization at the C3 position could enhance the antitumor activity of β-carbolines. Among the derivatives tested, 4B, 6i, 4D, and 6u displayed considerable cytotoxicity against A549 cell line. Furthermore, 4B, 6i, 4D, and 6u induced cell apoptosis in a dose-dependent manner, and caused cell cycle arrest at the S and G2/M phases. Moreover, the levels of cytochrome C in mitochondria, and the expressions of bcl-2 protein, decreased after treatment with β-carbolines, which indicated that 6i and 6u could induce mitochondria-mediated apoptosis. In addition, the results of UV-visible spectral, thermal denaturation, and molecular docking studies revealed that 4B, 6i, 4D, and 6u could bind to DNA mainly by intercalation.

scholarly journals DEVELOPMENT, CHARACTERIZATION AND IN VITRO RELEASE KINETIC STUDIES OF IBANDRONATE LOADED CHITOSAN NANOPARTICLES FOR EFFECTIVE MANAGEMENT OF OSTEOPOROSIS

2021 ◽  
pp. 120-125
Author(s):  
S. PATHAK ◽  
S. P. VYAS ◽  
A. PANDEY
Keyword(s):  
Electron Microscopy ◽  
Particle Size ◽  
Sodium Tripolyphosphate ◽  
Release Kinetics ◽  
Ph Effect ◽  
Chitosan Nanoparticles ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Release Kinetic

Objective: The objective of the present study was to develop, optimize, and evaluate Ibandronate-sodium loaded chitosan nanoparticles (Ib-CS NPs) to treat osteoporosis. Methods: NPs were prepared by the Ionic gelation method and optimized for various parameters such as the effect of concentration of chitosan, sodium tripolyphosphate (TPP), and pH effect on particle size polydispersity index (PDI), zeta potential, and entrapment efficiency. The prepared nanoparticles were characterized using particle size analyzer (DLS), transmission electron microscopy (TEM), scanning electron microscopy (SEM), and Fourier-Transform Infrared spectroscopy (FTIR).  Results: Formulated NPs were obtained in the average nano size in the range below 200 nm in TEM, SEM, and DLS studies. The particle size and encapsulation efficiency of the optimized formulation were 176.1 nm and 63.28%, respectively. The release profile of NPs was depended on the dissolution medium and followed the First-order release kinetics. Conclusion: Bisphosphonates are the most commonly prescribed drugs for treating osteoporosis in the US and many other countries, including India. Ibandronate is a widely used anti-osteoporosis drug, exhibits a strong inhibitory effect on bone resorption performed by osteoclast cells. Our results indicated that Ibandronate sodium-loaded chitosan nanoparticles provide an effective medication for the treatment of osteoporosis.

scholarly journals Chitosan-based nanoparticles sustenance and potentiation of the antibacterial effect of ampicillin against drug resistance among strains of Escherichia coli

Bio-Research ◽  
2020 ◽  
Vol 18 (2) ◽  
Author(s):  
EB Onuigbo ◽  
C Anozie-Ikeanyi ◽  
NE Edeh ◽  
CO Eze ◽  
TH Gugu
Keyword(s):  
Drug Resistance ◽  
Drug Release ◽  
Encapsulation Efficiency ◽  
Antibacterial Effect ◽  
Sodium Tripolyphosphate ◽  
Chitosan Nanoparticles ◽  
In Vitro Drug Release ◽  
E Coli ◽  
Ampicillin Trihydrate

The study seeks to evaluate nanoparticles based on chitosan for enhanced delivery of ampicillin in plasmid-mediated drug resistance. Serial dilutions of a mixed population of E. coli was plated on nutrient agar and streaked on Replica-plate 25 random colonies using MacConkey agar with or without ampicillin (100 µg/ml) daily for 96 h. Nanoparticles were prepared by cross-linking chitosan with sodium tripolyphosphate with ampicillin trihydrate adsorbed. Three different batches were prepared for optimization. The nanoparticles were optimized based on encapsulation efficiency, in vitro drug release, pH stability and microbiological assay using two laboratory strains of E. coli. Increased resistance to ampicillin due to possible plasmid transfer was established in vitro after 96 h. The encapsulation efficiency of the three batches was between 21-57 %. The drug release showed a burst effect and slow extended release over 8 h and reached a peak of about 19 % release at the 6 and 7 h in Batch A, B and C. The pH of the particles was stable over a period of 6 d. The nanoparticles containing only 0.075 mg of ampicillin dropped in an agar well plate inoculated with 1 ml of E. coli J62 lac pro trp hispFlac::Tn3 (AmpR) gave an IZD of ≥ 25 mm. Chitosan nanoparticles holds good potentials in potentiating the antibacterial effect of ampicillin against possible plasmid-mediated drug resistance

scholarly journals Preparation of 5-fluorouracil-loaded chitosan nanoparticles and study of the sustained release in vitro and in vivo

2017 ◽  
Vol 12 (5) ◽  
pp. 418-423 ◽  
Author(s):  
Li Sun ◽  
Yunna Chen ◽  
Yali Zhou ◽  
Dongdong Guo ◽  
Yufan Fan ◽  
...  
Keyword(s):  
Sustained Release ◽  
Chitosan Nanoparticles ◽  
Release In Vitro

Preparation, Characterization, and In Vitro Evaluation of EGCG-Loaded Chitosan Nanoparticles

2011 ◽  
Vol 282-283 ◽  
pp. 539-544 ◽  
Author(s):  
Jia Lei Li ◽  
Yuan Gang Zu ◽  
Xiu Hua Zhao ◽  
Zhi Gang An ◽  
Xiao Yu Sui ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Drug Delivery Systems ◽  
Room Temperature ◽  
Active Component ◽  
Sodium Tripolyphosphate ◽  
Chitosan Nanoparticles ◽  
Entrapment Efficiency ◽  
Release Drug

Epigallocatechin-3-gallate (EGCG), a principal polyphenolic, which is most abundant and active component in tea. It is considered key to these healthful qualities. However, EGCG used in clinical application which is still shortcomings of short half-life and low bioavailability. Chitosan (CS) has been widely used in pharmaceutical and medical areas, particularly for its potential in the development of controlled release drug delivery systems due to its well properties. In this study, we prepared EGCG-loaded chitosan nanoparticles by ionic polymeric method using sodium tripolyphosphate(TPP) as ionic polymeric agent successfully. Results controlled conditions (concentration of CS, 2 mg/mL; pH = 5.4; volume of TPP(0.5 mg/mL), 6.6 mL; amount of EGCG, 15 mg; ionic polymeric time, 24 h at room temperature (0.5 mL/min))volume of TPP(0.5 mg/mL), 6.6 mL; amount of EGCG, 15 mg; ionic polymeric time, 24 h at room temperature (0.5 mL/min)) for entrapment efficiency, loading efficiency, mean particle size and Zeta potential, were found to be 62.3 %, 33.8 %, 141.5 ± 0.4 nm and -31.21 ± 0.54 mV, respectively, and CS-EGCG-NPS have well property of sustained release.

scholarly journals Control of Anthracnose Disease (Colletotrichum gloeosporioides) Using Nano Chitosan Hydrolyzed by Chitinase Derived from Burkholderia cepacia Isolate E76

2018 ◽  
Vol 13 (2) ◽  
pp. 111 ◽  
Author(s):  
Yadi Suryadi ◽  
Tri Puji Priyatno ◽  
I Made Samudra ◽  
Dwi Ningsih Susilowati ◽  
Tuti Septi Sriharyani ◽  
...  
Keyword(s):  
Burkholderia Cepacia ◽  
Colletotrichum Gloeosporioides ◽  
Sodium Tripolyphosphate ◽  
Average Particle Size ◽  
Chitosan Nanoparticles ◽  
Average Particle ◽  
Coating Application ◽  
Anthracnose Disease

<p>Anthracnose (Colletotrichum gloeosporioides) is one of the important diseases of fruit crops that need to be controlled. This study was aimed to obtain the best formula of hydrolyzed nano chitosan and its potensial in controlling anthracnose. The hydrolyzed chitosan was prepared using chitinase enzyme extracted from Burkholderia cepacia isolate E76. Chitosan nanoparticles were synthesized using ionic gelation method by reacting hydrolyzed chitosan (0.2%) with Sodium tripolyphosphate (STPP) (0.1%) as cross-linking agent using 30&amp;ndash;60 minutes stirring condition. The bioactivity of the nano chitosan formula was tested to C. gloeosporioides under in vitro and in vivo assays. The specific enzymatic activity of the purified chitinase was higher (0.19 U/mg) than that of crude enzyme (supernatant) with the purity increased by 3.8 times. Of the four formula tested, Formula A (hydrolyzed chitosan to STPP volume ratio of 5 : 1 with 60 minutes stirring condition) was found good in terms of physical characteristic of the particle. The formula nano chitosan particle had the spherical-like shape with an average particle size of 126.2+3.8 nm, polydispersity index (PI) of 0.4+0.02, and zeta potential (ZP) value of 27.8+0.2 mV. Nano chitosan had an inhibitory activity to C. gloeosporioides in vitro up to 85.7%. Moreover, it could inhibit 61.2% of C. gloeosporioides spores germination. It was shown that nano chitosan was also effective to reduce anthracnose disease severity in vivo when applied as a preventive measure on chili and papaya fruits. This study could be used as a reference for further fruit coating application using nano chitosan as a promising postharvest biocontrol agent to C. gloeosporioides.</p>

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