scholarly journals Synthesis and Characterization of Folate-Targeted Dextran/Retinoic Acid Micelles for Doxorubicin Delivery in Acute Leukemia

2014 ◽  
Vol 2014 ◽  
pp. 1-14 ◽  
Author(s):  
J. Varshosaz ◽  
F. Hassanzadeh ◽  
H. Sadeghi Aliabadi ◽  
M. Nayebsadrian ◽  
M. Banitalebi ◽  
...  
Keyword(s):  
Particle Size ◽  
Retinoic Acid ◽  
Zeta Potential ◽  
Targeted Delivery ◽  
Drug Loading ◽  
Myelogenous Leukemia ◽  
Xps Spectra ◽  
H Nmr ◽  
Loading Efficiency ◽  
Drug Loading Efficiency

Folate and retinoic acid grafted/dextran (FA-RA/DEX) copolymers with different molecular weight of DEX were synthesized using carbonyldiimidazole and dimethylaminopyridine for targeted delivery of doxorubicin (DOX) in acute myelogenous leukemia (AML). The copolymers structure was confirmed by1H NMR and FTIR. Critical micelle concentration (CMC) of each copolymer was determined using pyrene as a fluorescent probe. DOX was loaded in micelles by the direct dissolution method. Physical properties of micelles, including particle size, zeta potential, drug loading efficiency, and drug release profiles, were examined. The orientation of the folate ligand on the surface of the micelles was studied by X-ray photoelectron spectroscopy (XPS) technique. The cytotoxicity of micelles loaded with DOX at different concentrations was studied in KG1 cells using MTT assay and their cellular uptake by flow cytometry technique. FTIR and1H NMR spectra confirmed successful production of the targeted micelles and XPS spectra showed the surface orientation of folate. R15D10F7copolymer produced micelles with particle size of 82.86 nm, polydispersity index of 0.3, zeta potential of −4.68 mV, drug loading efficiency of 96%, and release efficiency of 63%. DOX loaded in folate-targeted micelles of RA/DEX was more toxic than that in nontargeted micelles and free drug and seems promising in reducing drug resistance in AML.

scholarly journals Screening the Most Effective Variables on Physical Properties of Folate-Targeted Dextran/Retinoic Acid Micelles by Taguchi Design

2012 ◽  
Vol 2012 ◽  
pp. 1-7 ◽  
Author(s):  
M. Nayebsadrian ◽  
J. Varshosaz ◽  
F. Hassanzadeh ◽  
H. Sadeghi ◽  
M. Banitalebi ◽  
...  
Keyword(s):  
Particle Size ◽  
Retinoic Acid ◽  
Zeta Potential ◽  
Drug Concentration ◽  
Drug Loading ◽  
Taguchi Design ◽  
Amphiphilic Copolymers ◽  
Effective Parameters ◽  
Self Assembling ◽  
Stirring Time

Amphiphilic copolymers with self-assembling properties produce micelles in aqueous solutions and are made of two hydrophilic and hydrophobic segments. The objective of this study was optimization of the production of folate-conjugated dextran/retinoic acid (DEX/RA) micelles of doxorubicin. Micelles were prepared by direct dissolution method, and different effective parameters on their production were studied by a Taguchi design. The studied variables included CMC of the copolymer, polymer and drug contents, DEX Mw, stirring time, and rate and temperature. The effects of variables on responses of particle size, polydispersity index, zeta potential, drug loading, and release efficiency were studied. The most effective factors on particle size were DEX Mw, CMC of the copolymer, and stirring rate. Zeta potential and drug loading were more affected by the polymer content, DEX Mw, stirring time, and drug concentration. Stirring time and rate and also temperature of water were more effective variables on drug release rate. The optimum processing situation for micelles formation was obtained by copolymers with CMC <17 μg/mL and prepared from 20.1 mg copolymers of DEX Mw of 10000 and drug concentration of 15.9%. The optimized temperature for micelles formation was 40.7°C, and stirring time was 1 hr at a rate of 560 rpm.

scholarly journals A Statistical Study on the Development of Metronidazole-Chitosan-Alginate Nanocomposite Formulation Using the Full Factorial Design

Polymers ◽  
2020 ◽  
Vol 12 (4) ◽  
pp. 772 ◽  
Author(s):  
Hazem Abdul Kader Sabbagh ◽  
Samer Hasan Hussein-Al-Ali ◽  
Mohd Zobir Hussein ◽  
Zead Abudayeh ◽  
Rami Ayoub ◽  
...  
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Factorial Design ◽  
Drug Loading ◽  
Spherical Shape ◽  
Full Factorial Design ◽  
Gravimetric Analysis ◽  
Loading Efficiency ◽  
Full Factorial

The goal of this study was to develop and statistically optimize the metronidazole (MET), chitosan (CS) and alginate (Alg) nanoparticles (NP) nanocomposites (MET-CS-AlgNPs) using a (21 × 31 × 21) × 3 = 36 full factorial design (FFD) to investigate the effect of chitosan and alginate polymer concentrations and calcium chloride (CaCl2) concentration ondrug loading efficiency(LE), particle size and zeta potential. The concentration of CS, Alg and CaCl2 were taken as independent variables, while drug loading, particle size and zeta potential were taken as dependent variables. The study showed that the loading efficiency and particle size depend on the CS, Alg and CaCl2 concentrations, whereas zeta potential depends only on the Alg and CaCl2 concentrations. The MET-CS-AlgNPs nanocomposites were characterized by X-ray diffraction (XRD), Fourier-transform infrared spectroscopy (FTIR), thermal gravimetric analysis (TGA), scanning electron microscopy (SEM) and in vitro drug release studies. XRD datashowed that the crystalline properties of MET changed to an amorphous-like pattern when the nanocomposites were formed.The XRD pattern of MET-CS-AlgNPs showed reflections at 2θ = 14.2° and 22.1°, indicating that the formation of the nanocompositesprepared at the optimum conditions havea mean diameter of (165±20) nm, with a MET loading of (46.0 ± 2.1)% and a zeta potential of (−9.2 ± 0.5) mV.The FTIR data of MET-CS-AlgNPs showed some bands of MET, such as 3283, 1585 and 1413 cm−1, confirming the presence of the drug in the MET-CS-AlgNPs nanocomposites. The TGA for the optimized sample of MET-CS-AlgNPs showed a 70.2% weight loss compared to 55.3% for CS-AlgNPs, and the difference is due to the incorporation of MET in the CS-AlgNPs for the formation of MET-CS-AlgNPs nanocomposites. The release of MET from the nanocomposite showed sustained-release properties, indicating the presence of an interaction between MET and the polymer. The nanocomposite shows a smooth surface and spherical shape. The release profile of MET from its MET-CS-AlgNPs nanocomposites was found to be governed by the second kinetic model (R2 between 0.956–0.990) with more than 90% release during the first 50 h, which suggests that the release of the MET drug can be extended or prolonged via the nanocomposite formulation.

Preparation and In Vitro Evaluation of a Nano Ultrasound Contrast Agent Targeting Pancreatic Cancer

2021 ◽  
Vol 21 (3) ◽  
pp. 1413-1418
Author(s):  
Wu Chen ◽  
Xiaofang Liu ◽  
Yiying Li ◽  
Yongsheng Yang ◽  
Kun Xu ◽  
...  
Keyword(s):  
Pancreatic Cancer ◽  
Particle Size ◽  
Contrast Agent ◽  
Drug Loading ◽  
Ultrasound Contrast Agent ◽  
Ultrasound Contrast ◽  
Loading Efficiency ◽  
Targeted Ultrasound ◽  
Drug Loading Efficiency

To prepare a nano-sized ultrasound contrast agent that specifically targets pancreatic cancer cells and to evaluate its targeting effect In Vitro. PLGA-PEG-NHS was synthesized using PLGA, NHS, and PEG and detected using 1H-NMR. PLGA-PEG-NHS and PFOB were used to prepare PLGA nano contrast agent coated with PFOB by emulsification and volatilization, and then a hedgehog antibody was conjugated. The morphology of the nano contrast agent was observed using a transmission electron microscope, and its particle size and potential were measured using the dynamic light scattering method. The entrapment and drug loading efficiency of the nano contrast agent was measured using gas chromatography-mass spectrometry. The In Vitro release characteristics of the nano contrast agent was measured using the dialysis method. Human pancreatic cancer cell lines SW1990 and CFPAC1 were cultured in medium containing the nano contrast agent. The targeting ability of the nano contrast agent was qualitatively and quantitatively verified using fluorescence microscopy and flow cytometry. The average particle size of the targeted ultrasound contrast agent was 198.9 nm, zeta potential was −31.8 mv, entrapment rate was 63.7±3.9%, drug loading efficiency was 14.3±0.9%, and drug release was 85.3% in 48 h. In Vitro cell experiments showed that the targeted ultrasound contrast agent strongly bound to SW1990 cells with high expression of hedgehog antigen, but no specific binding was detected in CFPAC-1 cells which lack the hedgehog antigen. The nano ultrasound contrast agent prepared by emulsification and volatilization method can be potentially used for the diagnosis of pancreatic cancer.

scholarly journals Solvent Diffusion Method: An Effective Approach to Formulate Nanosponges Loaded with Naproxen Sodium

2020 ◽  
Vol 8 (2) ◽  
pp. 74-80
Author(s):  
Fizza Ilyas ◽  
Muhammad Jamsahid ◽  
Irfan Bashir ◽  
Rabia Aslam ◽  
Tooba Mehboob ◽  
...  
Keyword(s):  
Zeta Potential ◽  
Naproxen Sodium ◽  
Active Drug ◽  
Drug Loading ◽  
Study Drug ◽  
Diffusion Method ◽  
Diffusion Study ◽  
Franz Cell ◽  
Loading Efficiency ◽  
Drug Loading Efficiency

Objective: Solubility of naproxen sodium is limited. In conventional dosage form it causes different gastro intestinal problems. To overcome these difficulties naproxen sodium loaded nano sponges were designed. Methodology: Nanosponges were formulated by using emulsion solvent evaporation technique. To obtain dispersion of nanosponges, homogenization of active drug, with specified quantities of polyvinyl alcohol, dichloromethane, ethyl cellulose and distilled, water was done. Compatibility among excipients and active drug was checked by FTIR and results didn’t show any interaction between them. 11 trial formulations were tested for poly dispersity, zeta potential, particle size and viscosity. Results: Results showed all formulations except NS9, NS10 and NS11 were in nano range. Formulation NS1 to NS6 fall in category of “mid poly dispersity” and formulation NS7 to NS11 were in the category of “very poly dispersity”. Values of Zeta potential of all formulations were in negative range -0.106 to -9.75 mV. The value of viscosity of all formulations were 0.8872. NS2 and NS3 were selected for further testing like Franz cell diffusion study, stability testing and drug loading efficiency. In Franz cell diffusion study, drug release for NS2= 89.62%, for NS3= 89.10% at 50 minutes’ time. Stability studies performed for the 21 days, NS2 and NS3 revealed slight change in percentage drug content at 4°C and 25°C, and major changes were observed at 45°C temperature. Drug loading efficiency was found in NS2= 97.659 % and for NS3= 98.901%. Conclusion: Nanosponges formulations loaded with naproxen sodium have successfully been prepared.

Novel Formulation Development and Evaluation of Nanoparticles Based in Situ Gelling System for The Ophthalmic Delivery of Ciprofloxacin Hydrochloride

2015 ◽  
Vol 5 (4) ◽  
Author(s):  
Kranti Singh ◽  
Surajpal Verma ◽  
Shyam Prasad ◽  
Indu Bala
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Drug Loading ◽  
In Vitro Release ◽  
Formulation Development ◽  
Ciprofloxacin Hydrochloride ◽  
Potential Value ◽  
The Mean ◽  
In Situ Gelling

Ciprofloxacin hydrochloride loaded Eudragit RS100 nanoparticles were prepared by using w/o/w emulsification (multiple emulsification) solvent evaporation followed by drying of nanoparticles at 50°C. The nanoparticles were further incorporated into the pH-triggered in situ gel forming system which was prepared using Carbopol 940 in combination with HPMC as viscosifying agent. The developed nanoparticles was evaluated for particle size, zeta potential value and loading efficiency; nanoparticle incorporated in situ gelling system was evaluated for pH, clarity, gelling strength, rheological studies, in-vitro release studies and ex-vivo precorneal permeation studies. The nanopaticle showed the mean particle size varying between 263.5nm - 325.9 nm with the mean zeta potential value of -5.91 mV to -8.13 mV and drug loading capacity varied individually between 72.50% to 98.70% w/w. The formulation was clear with no suspended particles, showed good gelling properties. The gelling was quick and remained for longer time period. The developed formulation was therapeutically efficacious, stable and non-irritant. It provided the sustained release of drug over a period of 8-10 hours.

Improving drug loading efficiency and delivery performance of micro- and nanoparticle preparations through optimising formulation variables

2013 ◽  
Vol 10 (10/11) ◽  
pp. 996 ◽  
Author(s):  
Chiao Hsi Chiang ◽  
Hossein Hosseinkhani ◽  
Wen Sheng Cheng ◽  
g Wei Chen ◽  
Chun Hsiang Wang ◽  
...  
Keyword(s):  
Drug Loading ◽  
Delivery Performance ◽  
Loading Efficiency ◽  
Drug Loading Efficiency ◽  
Formulation Variables

scholarly journals FORMULATION, OPTIMIZATION AND IN VITRO EVALUATION OF 5-FLUOROURACIL LOADED LIQUORICE CRUDE PROTEIN NANOPARTICLES FOR SUSTAINED DRUG DELIVERY USING BOX-BEHNKEN DESIGN

2021 ◽  
pp. 216-226
Author(s):  
GEETHA V. S. ◽  
MALARKODI VELRAJ
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Drug Release ◽  
Crude Protein ◽  
Drug Loading ◽  
Entrapment Efficiency ◽  
Box Behnken Design ◽  
Sustained Drug Delivery ◽  
Drug Loading Efficiency

Objective: To formulate, optimize and evaluate 5-fluorouracil loaded liquorice crude protein nanoparticles for sustained drug delivery using Box-Behnken design. Methods: 5-fluorouracil (5-FU) loaded liquorice crude protein (LCP) nanoparticles were prepared by desolvation method using ethanol-water (1:2 ratio), Tween-80 (2%v/v) as stabilizing agent and gluteraldehyde (8% v/v) as cross linking agent. The optimization of prepared nanoparticles was carried out using Box-Behnken design with 3 factors 2 levels and 3 responses. The independent variables were A)5-FU concentration B)LCP concentration and C) sonication time while the responses were R1) Drug entrapment efficiency R2) Drug loading efficiency and R3) Particle size. The correlation between factors and responses were studied through response surface plots and mathematical equations. The nanoparticles were evaluated for FTIR, physicochemical properties like particle size and zeta potential by Photon correlation spectroscopy (PCS) and surface morphology by TEM. The entrapment efficiency, drug loading efficiency and in vitro drug release studies in PBS pH 7.4 (24 h) were carried out. The observed values were found to be in close agreement with the predicted value obtained from the optimization process. Results: 5-fluorouracil loaded LCP nanoparticles were prepared by desolvation method, the optimization was carried out by Box-Behnken design and the final formulation was evaluated for particle size (301.1 nm), zeta-potential (-25.8mV), PDI(0.226), with entrapment efficiency (64.07%), drug loading efficiency (28.54%), in vitro drug release (65.2% in 24 h) respectively. The formulated nanoparticles show Higuchi model drug release kinetics with sustained drug delivery for 24 h in pH7.4 buffer. Conclusion: The results were proved to be the most valuable for the sustained delivery of 5-Fluorouracil using liquorice crude protein as carrier. 5-FU–LCP nanoparticles were prepared using Tween-80 as stabilizing agent and gluteraldehyde as cross-linking agent to possess ideal sustained drug release characteristics.

scholarly journals OPTIMIZATION AND CHARACTERIZATION OF FORMULATION SELF-NANOEMULSIFYING DRUG DELIVERY SYSTEM ETHANOL EXTRACT OF ROMANG PARANG LEAVES (BOEHMERIA VIRGATA)

2021 ◽  
pp. 207-212
Author(s):  
MAGFIRAH ◽  
INDAH KURNIA UTAMI
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Secondary Metabolites ◽  
Zeta Potential ◽  
Drug Delivery System ◽  
Delivery System ◽  
Drug Loading ◽  
Ethanol Extract ◽  
Polydispersity Index ◽  
Lattice Design

Objective: Parang romang (Boehmeria virgata) is one of the traditional medicines that are used empirically by Makassar tribal healers, South Sulawesi, as an antitumor drug. This traditional medicine contains secondary metabolites such as alkaloids, flavonoids, tannins, and saponins. However, secondary metabolites of those leaves extract have low solubility in water. Hence, to be formula, self-nanoemulsifying drug delivery system (SNEDDS) is one of the solutions to increase the extract solubility. Methods: The optimization of two formula optimum SNEDDS parang romang leaves (T80PGMZ and T20PGMZ) was using the simple lattice design (SLD) method which will give 28 SNEDDS formula parang romang leaves each of which the formula is tested for its characteristics as a critical point include emulsification time, % transmittance, drug loading, particle size, zeta potential, polydispersity index, and morphology particle. Results: The results of SNEDDS characterization obtained the optimum formula T80PGMZ with emulsification time 12.6 s, % transmittance 92.21%, drug loading 68.21 ppm, particle size 370.26 nm, zeta potential −31.4 mV, polydispersity index of 0.615, and regular particle morphology with spherical chunks at a magnification of 10,000 times with a particle size of 10 μm. Conclusion: SNEDDS of parang romang leaves extracts that used olive oil as oil phase, Tween 80 as a surfactant, and propylene glycol as the cosurfactant provided nanoemulsion with good characteristics.

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