Chitosan Nanoparticles as a Carrier for Indigofera intricata Plant Extract: Preparation, Characterization and Anticancer Activity

2019 ◽  
Vol 15 (2) ◽  
pp. 162-169
Author(s):  
Aliasgar Shahiwala ◽  
Naglaa G. Shehab ◽  
Maryam Khider ◽  
Rawoof Khan
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Plant Extract ◽  
Anticancer Agents ◽  
Proliferative Activity ◽  
Chitosan Nanoparticles ◽  
Cancer Cell Line ◽  
Alcoholic Extract ◽  
Cell Proliferative Activity ◽  
Phenolic And Flavonoid

Background: Cancer is one of the major causes of the death and affects people of all ages throughout the world. The drugs that are currently available to treat cancer have many side effects. Hence, there is considerable scientific interest in the continuing discovery of new anticancer agents from natural sources. The aim of this study was to prepare and characterize nanoparticles combining Indigofera intricata crude alcoholic extract and chitosan and to evaluate the anticancer cell proliferative activity for both extract and nanoparticles. Methods: Dried alcoholic extract was prepared and characterized for its phenolic and flavonoid contents. Chitosan extract nanoparticles was prepared by ionic gelation method and characterized by thin layer chromatography (TLC), Fourier-transform infrared spectroscopy (FTIR), particle size and zeta-potential analysis. The anticancer cell proliferative activities of both plant extract and nanoparticles at different concentrations were evaluated using breast cancer cell line (MCF 7). Results: The alcoholic extract showed high contents from both phenolic and flavonoid constituents (15 % and 22 % respectively). The interaction of polyphenolic compounds of the extract with chitosan was confirmed by the TLC and FTIR results. The particle size and zeta-potential of nanoparticles found to be 400.6nm ± 101.8 nm and +42.1 mV ± 9.27 mV respectively. The plant extract showed the lowest cell viability of 45.21% ± 4.8% at the highest dose (250 mg) tested in this investigation. Almost 500-fold reduction (from 250 mg to 0.5 mg) in the extract concentration required to achieve same anticancer cell proliferative activity when formulated as nanoparticles. Also 2.5 mg extract containing nanoparticles showed similar anticancer cell proliferative activity as 5 mg 5-FU. Conclusion: Our results revealed that traditional medicinal plants could be an excellent source of natural anticancer agents and the chitosan-extract nanoparticles is a promising formulation strategy to enhance their clinical effectiveness.

Synthesis, Characterization, Anti-proliferative Evaluation, and DNA Flow Cytometry Analysis of Some 2-Thiohydantoin Derivatives

2020 ◽  
Vol 20 (18) ◽  
pp. 1929-1941
Author(s):  
Heba A. Elhady ◽  
Hossa F. Al-Shareef
Keyword(s):  
Anticancer Activity ◽  
Schiff Bases ◽  
Anticancer Agents ◽  
Proliferative Activity ◽  
Cancer Cell Line ◽  
Aromatic Aldehydes ◽  
Pharmaceutical Chemistry ◽  
Dna Flow Cytometry ◽  
Quinazoline Derivative ◽  
Reference Drug

Background and Objective: Due to the well-documented anti-proliferative activity of 2-thiohydantoin incorporated with pyrazole, oxadiazole, quinazoline, urea, β-naphthyl carbamate and Schiff bases, they are noteworthy in pharmaceutical chemistry. Methods: An efficient approach for the synthesis of a novel series of 2-thiohydantoin derivatives incorporated with pyrazole and oxadiazole has proceeded via the reaction of the acyl hydrazide with chalcones and/or triethyl orthoformate. Schiff bases were synthesized by the reaction of the acyl hydrazide with different aromatic aldehydes. Moreover, Curtius rearrangement was applied to the acyl azide to obtain the urea derivative, quinazoline derivative, and carbamate derivative. Results: The synthesized compounds structures were discussed and confirmed depending on their spectral data. The anticancer activity of these heterocyclic compounds was evaluated against the breast cancer cell line (MCF-7), where they showed variable activity. Compound 5d found to have a superior anticancer activity, where it has (IC50 = 2.07 ± 0.13 μg/mL) in comparison with the reference drug doxorubicin that has (IC50 = 2.79 ± 0.07 μg / mL). Then compound 5d subjected to further studies such as cell cycle analysis and apoptosis. Apoptosis was confirmed by the upregulation of Bax, downregulation of Bcl-2, and the increase of the caspase 3/7percentage. Conclusion: Insertion of pyrazole, oxadiazole and, quinazoline moieties with 2-thiohydantoin moiety led to the enhancement of its anti-proliferative activity. Hence they can be used as anticancer agents.

scholarly journals Atorvastatin calcium loaded chitosan nanoparticles: in vitro evaluation and in vivo pharmacokinetic studies in rabbits

2015 ◽  
Vol 51 (2) ◽  
pp. 467-477 ◽  
Author(s):  
Abdul Baquee Ahmed ◽  
Ranjit Konwar ◽  
Rupa Sengupta
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Oral Bioavailability ◽  
Chitosan Nanoparticles ◽  
Rabbit Model ◽  
Pharmacokinetic Studies ◽  
Release Formulation ◽  
Atorvastatin Calcium

<p>In this study, we prepared atorvastatin calcium (AVST) loaded chitosan nanoparticles to improve the oral bioavailability of the drug. Nanoparticles were prepared by solvent evaporation technique and evaluated for its particle size, entrapment efficiency, zeta potential, <italic>in vitro</italic> release and surface morphology by scanning electron microscopy (SEM). In addition, the pharmacokinetics of AVST from the optimized formulation (FT5) was compared with marketed immediate release formulation (Atorva<sup>(r))</sup> in rabbits. Particle size of prepared nanoparticles was ranged between 179.3 ± 7.12 to 256.8 ± 8.24 nm with a low polydispersity index (PI) value. Zeta potential study showed that the particles are stable with positive values between 13.03 ± 0.32 to 46.90 ± 0.49 mV. FT-IR studies confirmed the absence of incompatibility of AVST with excipient used in the formulations. <italic>In vitro</italic> release study showed that the drug release was sustained for 48 h. Results of pharmacokinetics study showed significant changes in the pharmacokinetic parameter (2.2 fold increase in AUC) of the optimized formulation as compared to marketed formulation (Atorva<sup>(r))</sup>. Thus, the developed nanoparticles evidenced the improvement of oral bioavailability of AVST in rabbit model.</p>

scholarly journals Controlling the Antioxidant Activity of Green Tea Extract through Encapsulation in Chitosan-Citrate Nanogel

2020 ◽  
Vol 2020 ◽  
pp. 1-9
Author(s):  
F. Piran ◽  
Z. Khoshkhoo ◽  
S. E. Hosseini ◽  
M. H. Azizi
Keyword(s):  
Antioxidant Activity ◽  
Particle Size ◽  
Zeta Potential ◽  
Green Tea ◽  
Chitosan Nanoparticles ◽  
Green Tea Extract ◽  
X Ray Diffraction ◽  
Bioactive Ingredients ◽  
Ft Ir ◽  
Tea Extract

Applying bioactive ingredients in the formulation of foods instead of artificial preservatives is problematic because bioactive ingredients are unstable and sensitive to environmental conditions. The present study aimed to control the antioxidant activity of green tea extract (GT) through encapsulating in chitosan nanoparticles (CS-NP). The synthesized nanoparticles were analyzed by using scanning electron microscopy (SEM), Fourier transform infrared spectroscopy (FT-IR), and X-ray diffraction (XRD). The encapsulation efficiency (EE), particle size, zeta potential, and polydispersity index (PDI) of GT-loaded CS-nanoparticles (CS-NP-GT) were assessed. Based on the results, the particle size and zeta potential related to the ratio of CS to GT of 1 : 0.5 were obtained as 135.43 ± 2.52 nm and 40.40 ± 0.2 mV, respectively. Furthermore, the results of FT-IR and XRD confirmed the validity of encapsulating GT in CS-NP. In addition, the antioxidant activity of GT increased after nanoencapsulation since the IC50 value of CS-NP-GT decreased to 6.13 ± 0.12 μg/ml. Finally, applying these particles for delivering GT polyphenols in foods is regarded as promising.

scholarly journals PHYSICOCHEMICAL CHARACTERIZATION OF PROPRANOLOL-LOADED CHITOSAN NANOPARTICLES FOR A BUCCAL DRUG DELIVERY SYSTEM

2020 ◽  
pp. 243-247
Author(s):  
SIRIPORN KITTIWISUT ◽  
PAKORN KRAISIT
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Zeta Potential ◽  
Drug Delivery System ◽  
Delivery System ◽  
Chitosan Nanoparticles ◽  
Particle Sizes ◽  
Zeta Potentials ◽  
Ph Values ◽  
Buccal Drug Delivery

Objective: This study aimed to characterize the physicochemical properties, including pH, zeta potential, and particle size of propranolol-loaded nanoparticles that were incorporated into a buccal transmucosal drug-delivery system. Methods: An ionotropic gelation technique was used to formulate propranolol-loaded chitosan nanoparticles. Chitosan used as the nanoparticle base, using tripolyphosphate (TPP) as a cross-linking agent. The effects on nanoparticle physical properties, including pH, zeta potential, and particle size were examined when various chitosan [0.150-0.300 % (w/v)] and propranolol contents (0-40 mg) were used during the preparation. The effects of using chitosan solutions with different pH values on nanoparticle properties were also determined. Results: The pH values of all nanoparticles ranged between 4.14–4.55. The zeta potentials of the prepared nanoparticles ranged between 22.6–52.6 mV, with positive charges. The nanoparticle sizes ranged from 107–140 nm, which are within the range of suitable particle sizes for transmucosal preparations. Conclusion: The pH values, zeta potentials, and particle sizes of the nanoparticle formulations were influenced by the concentrations of chitosan and propranolol and by the pH of the initial chitosan solution. The relationships between nanoparticle properties and all factors primarily depended on the ionic charges of the components, especially chitosan. Our study provides beneficial physicochemical knowledge for the further development of chitosan-based nanoparticles containing propranolol for buccal drug delivery systems.

scholarly journals PENGARUH WAKTU ULTRASONIKASI TERHADAP KARAKTERISTIK FISIKA NANOPARTIKEL KITOSAN EKSTRAK ETANOL DAUN SUJI (Pleomele angustifolia) DAN UJI STABILITAS FISIKA MENGGUNAKAN METODE CYCLING TEST

2019 ◽  
Vol 16 (02) ◽  
pp. 40
Author(s):  
Malinda Prihantini ◽  
Elya Zulfa ◽  
Listyana Dewi Prastiwi ◽  
Ikha Dyah Yulianti
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Physical Stability ◽  
Chitosan Nanoparticles ◽  
Ethanol Extract ◽  
Physical Characteristics ◽  
Test Method ◽  
Polydispersity Index ◽  
Cycling Test ◽  
Ultrasonication Time

ABSTRACT The nanoparticle system encapsulates and protects flavonoids of suji leaves from photolysis and oxidation instability. Chitosan is a biocompatible, biodegradable and non-toxic nanoparticles forming polymer. Ultrasonication is a materials mixing technique under high vibration energy. The ultrasonication time affects the particle size. The aim of this study was to determine the effect of the ultrasonication time on physical characteristics of chitosan nanoparticles of suji (Pleomele angustifolia) leaf ethanol extract and its physical stability after cycling test. Ethanol extract of suji leaves (EEDS) was obtained by maceration using 70% ethanol. Chitosan EEDS nanoparticles were made under ionic gelation method using an ultrasonication time of 3 minutes (FI), 6 minutes (FII), and 9 minutes (FIII). The physical characterization of nanoparticles includes particle size, polydispersity index, and zeta potential. Chitosan EEDS nanoparticles with the best physical characteristics (FIII) were tested for stability using cycling test method. The data obtained were analyzed using the Anova statistical method with a 95% confidence level. The size of EEDS chitosan nanoparticles (nm) was significantly different in all formulas, FI (374.47), FII (288.43), and FIII (233.37). The polydispersity index of FI (0.38) and FIII (0.65) were significantly different, while FII (0.41) was not significantly different. The zeta potential (mV) FI (51.70), FII (46.10), and FIII (48.60) were not significantly different in all formulas. The physical characteristics of Formula III after Cycling Test showed a particle size of 455.0 nm, a polydispersity index of 0.174, and a zeta potential of 20.1 mV. Keywords: ultrasonication, nanoparticles, chitosan, cycling test, suji leaf (Pleomele angustifolia)

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.

Poloxamer Modified Chitosan Nanoparticles for Vaginal Delivery of Acyclovir

2021 ◽  
Vol 08 ◽  
Author(s):  
Sanjeevani Deshkar ◽  
Sumit Sikchi ◽  
Anjali Thakre ◽  
Rupali Kale
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Sodium Tripolyphosphate ◽  
Chitosan Nanoparticles ◽  
Drug Uptake ◽  
Mass Ratio ◽  
Modified Chitosan ◽  
Chitosan Nanoparticle ◽  
Nanoparticle Formulation

Objective: The aim of the present study was to design a surface modified chitosan nanoparticle system for vaginal delivery of Acyclovir for effective drug uptake into vaginal mucosa. Method: Acyclovir loaded chitosan nanoparticles, with and without modification by poloxamer 407, were prepared by ionic gelation method. The effects of two independent variables, chitosan to sodium tripolyphosphate mass ratio (X1) and acyclovir concentration (X2), on drug entrapment in nanoparticles, were studied using 32 full factorial design. The surface response and counter plots were drawn to facilitate an understanding of the contribution of the variables and their interaction. The nanoparticles were evaluated for drug entrapment, size with zeta potential, morphological analysis by TEM, solid state characterization by FTIR, DSC, XRD, in vitro dissolution, in vitro cell uptake using HeLa cell line and in vivo vaginal irritation test in Wistar rats. Results: Chitosan nanoparticle formulation with chitosan to sodium tripolyphosphate mass ratio of 2:1 and acyclovir concentration of 2 mg/mL resulted in highest entrapment efficiency. Resulting nanoparticles revealed spherical morphology with particle size of 191.2 nm. The surface modification of nanoparticles with Poloxamer resulted in higher drug entrapment (74.3±1.5%), higher particle size (391.1 nm) as a result of dense surface coating, lower zeta potential and sustained drug release compared to unmodified nanoparticles. The change in the crystallinity of drug during nanoparticle formulation was observed in DSC and XRD study. Cellular uptake of Poloxamer modified chitosan nanoparticles was found to be higher than chitosan nanoparticles in HeLa cells. Safety of nanoparticle formulations by vaginal route was evident when tested in female rats. Conclusion: Conclusively, Poloxamer modified CH NP could serve as a promising and safe delivery system with enhanced cellular drug uptake.

scholarly journals PREPARATION AND CHARACTERIZATION OF CEFTRIAXONE SODIUM ENCAPSULATED CHITOSAN NANOPARTICLES

2017 ◽  
Vol 9 (6) ◽  
pp. 10 ◽  
Author(s):  
P. Manimekalai ◽  
R. Dhanalakshmi ◽  
R. Manavalan
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Zeta Potential ◽  
Chitosan Nanoparticles ◽  
Cross Linking ◽  
Burst Release ◽  
In Vitro Drug Release ◽  
Cumulative Percentage ◽  
Ceftriaxone Sodium

Objective: The objective of this study was to prepare ceftriaxone sodium chitosan nanoparticles (CS-NP) from different drug and polymer ratios and analyze their physicochemical characteristics.Methods: Ceftriaxone sodium loaded chitosan nanoparticles were prepared using chitosan as a polymer and tri sodium polyphosphate (TPP) as cross linking agent by ionic cross linking and coacervation with the aid of sonication. Various trials have been carried out for the confirmation of nanoformulation. Parameters such as the zeta potential, polydispersity, particle size, entrapment efficiency, in vitro drug release Thermo gravimetric analysis and scanning electron microscope of the nanoparticles were assessed for confirmation of nanoformulation.Results: The formulated nanoparticles showed mean particle size, polydispersity index and zeta potential to be 183.1±8.42 nm, 0.212±0.05, +38.5±1.6 mV respectively and the drug loading was found to be 46.42±10 %. In vitro drug release was showed a biphasic release pattern with initial burst release followed by sustained release of formulated nanoparticles. The cumulative percentage of drug release was about 83.08 %.Conclusion: Formulation F2 was found to be the best formulation with a higher cumulative percentage of drug release. Modified ionic gelation method can be utilized for the development of chitosan nanoparticles of ceftriaxone sodium. Polymer and crosslinking agent concentrations and sonication time are rate-limiting factors for the development of the optimized formulation. The chitosan nanoparticles developed would be capable of sustained delivery of ceftriaxone sodium.

scholarly journals Design, Synthesis and Potential Anti-Proliferative Activity of Some Novel 4-Aminoquinoline Derivatives

2014 ◽  
Vol 64 (3) ◽  
pp. 285-297 ◽  
Author(s):  
Mostafa M. Ghorab ◽  
Mansour S. Al-Said ◽  
Reem K. Arafa
Keyword(s):  
Anticancer Agents ◽  
Proliferative Activity ◽  
Cancer Cell Line ◽  
The Novel ◽  
Design Synthesis ◽  
Reference Drug ◽  
Antiproliferative Agents ◽  
New Compounds ◽  
Mcf 7

Abstract Novel nineteen compounds based on a 4-aminoquinoline scaffold were designed and synthesized as potential antiproliferative agents. The new compounds were N-substituted at the 4-position by aryl or heteroaryl (1-9), quinolin- 3-yl (10), 2-methylquinolin-3-yl (11), thiazol-2-yl (12), and dapsone moieties (13, 14 and 18). Bis-compounds 15, 16 and 19 were also synthesized to assess their biological activity. All the newly synthesized comounds were tested for in vitro antiproliferative activity against the MCF-7 breast cancer cell line. Seventeen of the novel compounds showed higher activity than the reference drug doxorubicin. The corresponding 7-(trifluoromethyl)-N-(3,4,5-trimethoxyphenyl)quinolin-4- amine 1, N-(7-(trifluoromethyl)quinolin-4-yl)quinolin- 3- amine (10), 2-methyl-N-(7-trifluorome-thyl)quinolin-4-yl) quinolin-3-amine (11) and N-(4-(4-aminophenylsulfonyl) phenyl)-7-chloroquinolin-4-amine (13) were almost twice to thrice as potent as doxorubicin. Biological screening of the tested compounds could offer an encouraging framework in this field that may lead to the discovery of potent anticancer agents.

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