scholarly journals Designing of nanosized bioflavonoids using biodegradable polymeric nanoparticles by Plackett Burman method

2017 ◽  
Vol 6 (2) ◽  
pp. 9-15 ◽  
Author(s):  
Nandhakumar Loganathan ◽  
Mohan Sellappan
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Oral Delivery ◽  
Polymeric Nanoparticles ◽  
Pharmaceutical Journal ◽  
Critical Parameters ◽  
Antidiabetic Activity ◽  
Independent Variables ◽  
Method Optimization ◽  
Nanoparticulate Systems

In this present study, dual loaded flavono nanoparticulate systems have been developed for oral delivery of Naringin and Hesperidin to enhance its antioxidant and antidiabetic activities. The fabrication of Dual Loaded Flavono Nanoparticles by suitable method was optimized by Plackett Burman method. Optimization of the formulation requires proper designing of the experiments. For this reason, only in our current study, the placket burman method has been projected for the formulation of nanoparticles biodegradable polymers encompass bioflavonoid isolates for the antidiabetic activity. Ten critical parameters influencing the formulation has been selected and designed in Plackett Burman method of experimentation for 12 runs to assess independent variables influencing the result outcome. The results revealed that the 9th run shows the optimum particle size of 126.1 nm with zeta potential of 29.9 mV. Remarkably significant nanoparticles were obtained by exploiting the Plackett Burman method as designing tool.Loganathan and Sellappan, International Current Pharmaceutical Journal, January 2017, 6(2): 9-15http://www.icpjonline.com/documents/Vol6Issue2/01.pdf

scholarly journals Development of NIPAAm-PEG acrylate polymeric nanoparticles for co-delivery of paclitaxel with ellagic acid for the treatment of breast cancer

2019 ◽  
Vol 39 (3) ◽  
pp. 271-278 ◽  
Author(s):  
Suruchi Suri ◽  
Mohd. Aamir Mirza ◽  
Md. Khalid Anwer ◽  
Abdullah S. Alshetaili ◽  
Saad M. Alshahrani ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Particle Size ◽  
Ellagic Acid ◽  
Oral Delivery ◽  
Polymeric Nanoparticles ◽  
Entrapment Efficiency ◽  
Shell Nanoparticles ◽  
Transmission Electron ◽  
Core Shell Nanoparticles

Abstract The aim of the current study was to develop a dual-loaded core shell nanoparticles encapsulating paclitaxel (PTX) and ellagic acid (EA) by membrane dialysis method. Based on particle size, polydispersity index (PDI), and entrapment efficiency, the dual drug-loaded nanoparticles (F2) was optimized. The optimized nanoparticles (F2) showed a particle size of 140±2 nm and a PDI of 0.23±3. The size and the morphology were confirmed by transmission electron microscopy (TEM) and found agreement with the results of dynamic light scattering. The entrapment efficiencies of total drug (PTX and EA), PTX, and EA in the nanoparticles (F2) were measured as 80%, 62.3%, and 37.7%, respectively. The in vitro release profile showed a controlled release pattern for 48 h. A higher cytotoxicity was observed with nanoparticles (F2) in comparison to free PTX. The results revealed that co-delivery of PTX and EA could be used for its oral delivery for the effective treatment of breast cancer.

scholarly journals FORMULATION AND EVALUATION OF ETHAMBUTOL POLYMERIC NANOPARTICLES

2020 ◽  
pp. 207-217
Author(s):  
MONOWAR HUSSAIN ◽  
ANUPAM SARMA ◽  
SHEIKH SOFIUR RAHMAN ◽  
ABDUL MATIN SIDDIQUE ◽  
TANUKU PAVANI EESWARI
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Zeta Potential ◽  
Polymeric Nanoparticles ◽  
Release Kinetics ◽  
Drug Loading ◽  
Entrapment Efficiency ◽  
Compatibility Study ◽  
Bacterial Disease ◽  
Dose Frequency

Objective: Tuberculosis (TB) is an infectious bacterial disease caused by Mycobacterium tuberculosis which most commonly affects the lungs. TB has the highest mortality rate than any other infectious disease occurs worldwide. The main objective of the present investigation was to develop polymeric nanoparticles based drug delivery system to sustain the ethambutol (ETB) release by reducing the dose frequency. Methods: The Preformulation studies of drug ETB were done by physical characterization, melting point determination, and UV spectrophotometric analysis. The ETB loaded nanoparticles were prepared by double-emulsion (W/O/W) solvent evaporation/diffusion technique. The prepared polymeric nanoparticles were evaluated for particle size, polydispersity index, zeta potential, drug entrapment efficiency, drug loading, drug-polymer compatibility study, surface morphology, in vitro drug release, and release kinetics. Results: Based on the result obtained from the prepared formulations, F11 showed the best result and was selected as the optimized formulation. Optimized batch (F11) showed better entrapment efficiency (73.3%), good drug loading capacity (13.21%), optimum particle size (136.1 nm), and zeta potential (25.2 mV) with % cumulative drug release of 79.08% at the end of 24 h. Conclusion: These results attributed that developed polymeric nanoparticles could be effective in sustaining the ETB release over 24 h. Moreover, the developed nanoparticles could be an alternate method for ETB delivery with a prolonged drug release profile and a better therapeutic effect can be achieved for the treatment of tuberculosis.

Development of Lipid-Drug Conjugate Nanoparticles for Hydrophilic and Lipophilic Drug: A Comparative Ex vivo Gut and Caco-2 Cell Permeability Study

2020 ◽  
Vol 16 ◽  
Author(s):  
Arehalli Manjappa ◽  
Popat Kumbhar ◽  
John Disouza ◽  
Abhijeet D. Shete
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Stearic Acid ◽  
Oral Delivery ◽  
Ex Vivo ◽  
Diffusion Mechanism ◽  
Cell Permeability ◽  
Permeability Characteristics ◽  
Drug Conjugate ◽  
Mean Particle Size

Background: The lipid-drug conjugate nanoparticles (LDC NPs), amongst other lipid-based nanoparticles, are the most accepted one for the oral delivery of both hydrophilic and hydrophobic drugs with poor bioavailability. Besides, the LDC NPs show altered physicochemical properties of the drug and has the potential applications in targeting the drug to a specific organ. Objective: To synthesize hydrophilic Valacyclovir (VACV)-stearic acid (SA) and lipophilic Acyclovir (ACV)-stearic acid conjugates (VACV-SAC and ACV-SAC), and develop their nanoparticles (VACV-LDC-NPs and ACV-LDC-NPs) for improved intestinal permeability. Methods: Both VACV-SAC and ACV-SAC were synthesized and confirmed using FTIR, NMR, and DSC techniques and characterized for assay. The lipid drug conjugate nanoparticles (LDC NPs) were prepared using cold high-pressure homogenization technique and characterized for drug content, mean particle size, zeta potential, ex vivo gut permeability using rat gut sac model, and Caco-2 cell permeability. Results: The FTIR, NMR, and DSC results confirmed the successful synthesis of LDCs. The assay of VACV-SAC and ACV-SAC is found to be 51.48±5.6% and 41.2±6.2% respectively. The VACV-LDC-NPs and ACV-LDC-NPs showed %EE of 99.10±6.71% and 86.84±5.32%, the mean particle size of 338.7±8nm and 251.3±7nm and zeta potential of -10.8±2.31mV and -11.2±3.52mV respectively. About 91±5.2% of VACV and 84±6.5% of ACV is found permeated across the rat intestine after 480 minutes from their respective NPs. Further, the VACV-LDC-NPs and ACV-LDC-NPs displayed significantly higher permeability coefficient (61.5×10-6 and 59.8×10-6 cm/s respectively) than their plain solutions. Conclusion: The obtained remarkable permeability characteristics indicate developed LDC NPs are the potential, promising and translational approaches for effective oral delivery of poorly bio-available hydrophilic and lipophilic drugs. Further, this approach may result in moderately to significantly enhanced oral bioavailability of hydrophilic drugs as the conjugation results in amphiphilic molecules which are further absorbed through different mechanisms across the intestinal mucosa (mainly through passive diffusion mechanism).

FORMULATION AND EVALUATION OF STABILIZED EPROSARTAN NANOSUSPENSION

2020 ◽  
pp. 83-87
Author(s):  
M. SANTHOSH RAJA ◽  
K. VENKATARAMANA
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Polymeric Nanoparticles ◽  
Precipitation Method ◽  
Dissolution Testing ◽  
Potential Drug ◽  
Dsc Analysis ◽  
Scanning Calorimetry ◽  
Bcs Class Ii ◽  
Pvp K30

Objective: The objective of the current study is to enhance the solubility of Eprosartan mesylate a BCS Class II drug by employing the nanoprecipitation technique. Methods: Polymeric nanoparticles of Eprosartan mesylate were prepared by precipitation technique with various polymers like PVP K30, HPMC K15M, and Eudragit L100 in various ratios. The incompatibility issues which may arise between the drug and polymers were tested by differential scanning calorimetry (DSC). The formed nanosuspensions were evaluated for various parameters like particle size, zeta potential, drug content, and dissolution testing. Results: Among all the nanosuspension formulations, E12 formulation prepared with Eudragit L 100 showed better evaluation characteristics. SEM and DSC analysis showed no major interactions with the excipients. The maximum drug release was showed at 12h. The formulation E12 showed the particle size of 81.5±5.5 nm and zeta potential of-55.1mv. Conclusion: The nano-precipitation method improved the dissolution as well as the bioavailability of Eprosartan mesylate nanosuspension.

scholarly journals Development and evaluation of bio-nanoparticles as novel drug carriers for the delivery of Selegiline

2016 ◽  
Vol 5 (4) ◽  
pp. 33-37 ◽  
Author(s):  
Laxmi Goswami ◽  
N.V. Satheesh Madhav ◽  
Kumud Upadhyaya
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Evaluation Studies ◽  
Drug Carriers ◽  
Pharmaceutical Journal ◽  
Chemical Test ◽  
Economic Method ◽  
Novel Drug ◽  
Luffa Acutangula

The purpose of the present study was to formulate and evaluate Selegiline loaded bio-nanoparticles for effective treatment of Depression. For the preparation of bio-nanoparticles biomaterial was isolated from fruits of Luffa acutangula by an economic method. The biomaterial recovered from the concentrate was subjected for various physicochemical properties like color, solubility, color changing point and chemical test. Bio-nanoparticles were prepared by modified solvent evaporation method in different batches with variable drug/biomaterial ratio. Prepared batches were subjected for various evaluation studies like particle size, zeta potential, SEM, TEM, surface entrapment, in-vitro diffusion, DSC and stability. Particle size and zeta potential result revealed that all nanoformulation were within range of 110 to 152.7 with slight negative in charge. SEM and TEM study report indicate that formulations were spherical in shape with less or no aggregation. Less surface entrapment leads to better drug entrapped inside nanomatrix. Bio-nanoformulations were capable of releasing the drug in a slow sustained manner. From the present investigation, it may be concluded that biomaterial isolated from fruits of Luffa acutangula used in the preparation of bio-nanoparticle act as an efficient carriers for deliver selegiline at a controlled rate. It may significantly improve the ability to cross blood-brain barrier and serve as an effective tool to treat Depression disease.Goswami et al., International Current Pharmaceutical Journal, March 2016, 5(4): 33-37http://www.icpjonline.com/documents/Vol5Issue4/01.pdf

scholarly journals Determination of Critical Parameters of Drug Substance Influencing Dissolution: A Case Study

2014 ◽  
Vol 2014 ◽  
pp. 1-9 ◽  
Author(s):  
Erika Bojnanska ◽  
Michal Kalina ◽  
Ladislav Parizek ◽  
Eva Bartonickova ◽  
Tomas Opravil ◽  
...  
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Particle Size Distribution ◽  
Dissolution Rate ◽  
Size Distribution ◽  
Drug Product ◽  
Drug Formulation ◽  
Drug Substance ◽  
Critical Parameters ◽  
Dissolution Profile

The purpose of this study was to specify critical parameters (physicochemical characteristics) of drug substance that can affect dissolution profile/dissolution rate of the final drug product manufactured by validated procedure from various batches of the same drug substance received from different suppliers. The target was to design a sufficiently robust drug substance specification allowing to obtain a satisfactory drug product. For this reason, five batches of the drug substance and five samples of the final peroral drug products were analysed with the use of solid state analysis methods on the bulk level. Besides polymorphism, particle size distribution, surface area, zeta potential, and water content were identified as important parameters, and the zeta potential and the particle size distribution of the drug substance seem to be critical quality attributes affecting the dissolution rate of the drug substance released from the final peroral drug formulation.

scholarly journals Design expert as a statistical tool for optimization of 5-ASA-loaded biopolymer-based nanoparticles using Box Behnken factorial design

2021 ◽  
Vol 7 (1) ◽  
Author(s):  
Wasim Akram ◽  
Navneet Garud
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Entrapment Efficiency ◽  
Statistical Tool ◽  
Design Expert ◽  
Independent Variables ◽  
Dsc Studies ◽  
Morphological Studies ◽  
Quality Aspects ◽  
Response Surface Designs

Abstract Background The overall objective was to prepare a highly accurate nanocarrier system of mesalamine for the treatment of ulcerative colitis with increased therapeutic efficacy and targeting. In the formulation of nanocarrier systems, optimization is a critical process for understanding nanoformulation variables and quality aspects. The goal of the present work was to determine the effect of independent variables, i.e., the concentrations of chitosan, carboxymethyl inulin (CMI), and the drug on the response variables, i.e., particle size and percent entrapment efficiency of the mesalamine-loaded nanoparticle using the Box Behnken design (BBD). The correlation between the independent and dependent variables was investigated using the Design Expert generated mathematical equations, contour, and response surface designs. Result An optimized batch was developed using the ionotropic gel method with selected independent variables (A: + 1 level, B: 0 level, C: − 1 level) and the developed nanoparticles had a particle size of 184.18 nm, zeta potential 26.54 mV, and entrapment efficiency 88.58%. The observed responses were remarkably similar to the predicted values. The morphological studies revealed that the formulated nanoparticles were spherical, and the results of the FTIR and DSC studies indicated the drug-polymer compatibility. The nanoparticle showed less than 5% release in the pH 1.2. In the colonic region (pH 7.4), more than 80 % of the medication was released after 24 h. The kinetics study showed that the Higuchi and Korsemeyer-Peppas models had R2 values of 0.9426 and 0.9784 respectively, for the developed formulation indicating linearity, as revealed by the plots. This result justified the sustained release behavior of the formulation. Conclusion The mesalamine-loaded chitosan-CMI nanoparticle has been successfully developed using the ionotropic gelation method. The nanoparticles developed in this study were proposed to deliver the drug to its desired site. The developed nanoparticles were likely to have a small particle size with positive zeta potential and high percent drug entrapment. It could be stated from the results that BBD can be an active way for optimizing the formulation and that nanoparticles can be a potential carrier for delivering therapeutics to the colon.

scholarly journals Determination of Pickering Nanoemulsion by Eudragit Rl-100 Nanoparticle as Oral Drug Delivery for Poorly Soluble

2021 ◽  
pp. 197-208
Author(s):  
Ashish Y. Pawar ◽  
Khanderao R. Jadhav ◽  
Sagar S. Patil ◽  
Pallavi R. Jadhav
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Zeta Potential ◽  
Aqueous Phase ◽  
Oral Drug Delivery ◽  
Polymeric Nanoparticles ◽  
Oral Drug ◽  
In Vitro Drug Release ◽  
Eudragit Rl

Objective: The purpose of this research study was to develop Ketoprofen-loaded Pickering nanoemulsion with the help of polymeric nanoparticles [NPs]. The pickering nanoemulsion  formulation is developed using Eudragit RL 100, which has the greater ability to stabilize the formulation as well as it better controls the  release of drug upon oral administration. Method: In the present study, Ketoprofen - loaded Pickering nanoemulsion were prepared using an ultrasonic emulsification process. For the preparation of the Nanoemulsion, an aqueous phase of the nanodispersion of nanoparticle is used while Captex -300 and drug premix is used as oil phase. The nanoemulsion is formulated by using a probe sonicator with different ratios of aqueous phase and oil phase. The preformulation study of polymer or drug is done by FTIR and DSC and the drug - polymer compatibility was confirmed by FTIR. The prepared formulation was evaluated for physical appearance, pH, Viscosity, In vitro drug release, Particle size, Zeta Potential, Polydispersivity index, and transmission electron microscopy and stability. The Formulation is optimized for the different concentrations of the aqueous phase and oil phase with concentrations of drug and polymer. Results: All the prepared formulations show particle size in between 100-500nm hence it indicats formation of nanoemulsion. The zeta potential is -46mv which indicates good stability of formulation. The In vitro drug release shows maximum drug release i.e. 96.93% in 10 hrs which shows that the release of drug is prolonged due to formation of Polymer NPs. Conclusion: Thus the drug release was significantly controlled and slowed down when nanoemulsion is formulated by using NPs in comparison with control. These results fulfilled the objective of the study. This study opens new prospects on the formulation of Pickering nanoemulsion. 

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