Development of Apigenin-Loaded Niosomes Using Ecological Probe Sonication Technique for enhanced oral delivery: Application of Box-Behnken Design

2021 ◽  
Vol 22 ◽  
Author(s):  
Md. Ali Mujtaba
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Oral Delivery ◽  
Aqueous Solubility ◽  
Polydispersity Index ◽  
Antioxidant Potential ◽  
Box Behnken Design ◽  
Sonication Technique ◽  
Probe Sonication

Background: Apigenin (APG), a natural bioactive flavonoid, has multiple pharmacological effects. However, its poor aqueous solubility hinders its clinical benefits. Objective and Methods: The work aimed to develop novel apigenin-loaded niosomes (APG-NIO) with ecological probe sonication techniques. The formulation was statistically optimized by Box-Behnken design (BBD), and the independent variables were selected as Span 80 (X1), Poloxamer 188 (X2), and Tween 80 (X3) at three levels, and the dependent variables were identified as: particle size (Y1), polydispersity index (Y2), and % entrapment efficiency (Y3). The formulation was characterized for various parameters such as vesicle shape, size, PDI, %EE, solubility, in vitro drug release, and antioxidant potential. Results: The optimized APG-NIO formulation was found to have a spherical shape with homogenous distribution and a low polydispersity index. It has a particle size of 425.77 nm, zeta potential -17.1±0.9 mV, and %EE of 89.63. The aqueous solubility of APG-NIO was found approximately 45 times higher than that of pure APG. The formulation showed a higher drug release rate as compared to pure APG in phosphate buffer pH 7.4 and followed the Higuchi release model with a non-Fickian transport mechanism. The stability was found at 4°C for 3 months. The antioxidant potential of APG-NIO was significantly increased in comparison to the pure drug suspension in the DPPH• assay. Conclusion: These findings suggest that the probe sonication technique is an alternative, cost-effective, simple, and green method for the development of niosomes, and BBD is a useful optimization tool for identifying the effect of 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 Development of Dry Powder Inhaler Containing Prothionamide-PLGA Nanoparticles Optimized Through Statistical Design: In-vivo Study

2017 ◽  
Vol 4 (1) ◽  
pp. 30-40 ◽  
Author(s):  
Sujit K. Debnath ◽  
Saisivam Srinivasan ◽  
Monalisha Debnath
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Dry Powder Inhaler ◽  
Burst Release ◽  
Dry Powder ◽  
Box Behnken Design ◽  
Pulmonary Administration ◽  
Aerodynamic Particle Size

Objective:The objective of the present work was to formulate Prothionamide (PTH) nanoparticles using Poly lactic co-glycolic acid (PLGA), optimized by Box-Behnken Design and further modification to dry powder inhaler followed byin-vivostudy.Methods:Poly-lactic co-gycolic acid (PLGA), a biodegradable polymer was used to coat Prothionamide by solvent evaporation technique. Formulation was optimized using Box-Behnken Design. Response surface curve and desirability factors helped in the selection of optimum formulation of PTH nanoparticles. Dry powder inhaler was prepared by adding inhalable grade lactose to optimize PTH nanoparticles. Mass median aerodynamic diameter (MMAD) was carried out using Andersen Cascade Impactor (ACI) to demonstrate its suitability in the pulmonary administration.In-vitrodrug release of dry powder inhaler was carried out in simulated lungs fluid. Correlationin-vitrotoin-vivowas established after performing animal experiment.Results:FTIR study reveals no chemical interaction between PTH, lactose and PLGA as the principle peaks was retained with same intensity in the physical mixture. Scanning electron microscope showed the spherical shape and aerodynamic particle size was found to be 1.69µm. Drug release study showed initial burst release followed by zero order release.In-vivomodel confirmed the presence of PTH after 24h. Aerodynamic particle size and the release profile revealed the suitability of PTH loaded nanoparticles containing dry powder inhaler for the pulmonary administration.Conclusion:Prepared DPI containing PTH nanoparticles can improve in the management of tuberculosis by increasing PTH residency in the lungs tissue for prolong period of time.

scholarly journals Microemulsion Drug Delivery System: For Bioavailability Enhancement of Ampelopsin

2012 ◽  
Vol 2012 ◽  
pp. 1-4 ◽  
Author(s):  
Shailendra Singh Solanki ◽  
Brajesh Sarkar ◽  
Rakesh Kumar Dhanwani
Keyword(s):  
Drug Release ◽  
Delivery System ◽  
Oral Delivery ◽  
Aqueous Solubility ◽  
Water Soluble ◽  
Cremophor El ◽  
Bioavailability Enhancement ◽  
Capmul Mcm ◽  
Drug Solution

Ampelopsin, one of the most common flavonoids, reported to possess numerous pharmacological activities and shows poor aqueous solubility. The purpose of this study was to enhance the dissolution rate and bioavailability of this drug by developing a novel delivery system that is microemulsion (ME) and to study the effect of microemulsion (ME) on the oral bioavailability of ampelopsin. Capmul MCM-based ME formulation with Cremophor EL as surfactant and Transcutol as cosurfactant was developed for oral delivery of ampelopsin. Optimised ME was evaluated for its transparency, viscosity, percentage assay and so forth. Solubilisation capacity of the ME system was also determined. The prepared ME was compared with the pure drug solution and commercially available tablet for in vitro drug release. The optimised ME formulation containing ampelopsin, Capmul MCM (5.5%), Cremophor EL (25%), Transcutol P (8.5%), and distilled water showed higher in vitro drug release, as compared to plain drug suspension and the suspension of commercially available tablet. These results demonstrate the potential use of ME for improving the bioavailability of poor water soluble compounds, such as ampelopsin.

scholarly journals FORMULATION AND EVALUATION OF ALLOPURINOL LOADED CHITOSAN NANOPARTICLES

2019 ◽  
pp. 49-52 ◽  
Author(s):  
Gurpreet Kandav ◽  
D.c. Bhatt ◽  
Deepak Kumar Jindal
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Sustained Release ◽  
Release Kinetics ◽  
Chitosan Nanoparticles ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Polydispersity Index ◽  
Sustained Release Formulation

Objective: The objective of the present investigation was to fabricate and characterize allopurinol loaded chitosan nanoparticles (A-CNPs) for sustained release of drug. Methods: The allopurinol loaded chitosan nanoparticles were successfully prepared by employing the ionotropic gelation method. Further, particle size (PS), polydispersity index (PDI), zeta potential (ZP), Differential Scanning Calorimetry (DSC), entrapment efficiency (EE), Transmission Electron Microscopy (TEM), in vitro drug release, X-Ray Diffraction (XRD) and Fourier transform infrared (FTIR) were used for evaluating formulated A-CNPs Results: A-CNPs was successfully prepared and the particle size, polydispersity index, ZP and entrapment efficiency were found to be 375.3±10.1 nm, 0.362±0.01 and 32.5±2.7 mV and 52.56±0.10% respectively. In vitro release profile of A-CNPs showed sustained release and Higuchi model was found to be best fit for drug release kinetics. FTIR study depicted no chemical interaction between pure drug allopurinol (AL) and other excipients. Conclusion: The sustained release formulation of allopurinol was successfully prepared using HMW chitosan and evaluated for different parameters.

scholarly journals SMART INNOVATIVE APPROACH FOR DESIGNING FLUVOXAMINE LOADED BIO-NANOSUSPENSION FOR THE MANAGEMENT OF DEPRESSION

2019 ◽  
Vol 11 (1) ◽  
pp. 191 ◽  
Author(s):  
Yogita Tyagi ◽  
N. V. Satheesh Madhav
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Zeta Potential ◽  
Release Kinetics ◽  
Polydispersity Index ◽  
Fickian Diffusion ◽  
Santalum Album ◽  
Improved Stability ◽  
Ophthalmic Delivery

Objective: Design and evaluation of fluvoxamine loaded bio-nanosuspensions using biopolymer which was isolated from the wood of Santalum album used as the stabilizer.Methods: The main aim of the present investigation was to obtain an ocular drug delivery system with improved stability using biopolymer. The fluvoxamine loaded Bio-nanosuspension was prepared using novel biopolymer isolated from Santalum album by sonication solvent evaporation method with different ratios (1%, 2%, 3%, 4% and 5%) and evaluated for particle size, polydispersity index, zeta potential, pH stability studies, %entrapment efficacy, in vitro drug release, stability studies.Results: The prepared bio-nanosuspension was subjected to the best formulation based on the comparison of above-mentioned evaluation parameters, so Fb3 (3%) formulation was found to be the best formulation showing an R2 value of 0.9744, T50% of 31.3 h and T80% of 50.1 h respectively. According to the release kinetics, the best fit model was found to be Peppas Korsmeyer with Fickian Diffusion (Higuchi Matrix) as the mechanism of drug release. Santalum album provided excellent stability for the formulation, and resulting particle size for the best formulation was found to be 196 nm. The bio-nanosuspension had Polydispersity Index (PDI) of 0.19 with zeta potential of-20mV.Conclusion: The prepared bio-nanosuspension was found to be safe and compatible with the ophthalmic delivery for treatment of depression.

scholarly journals DESIGN, DEVELOPMENT AND IN VITRO EVALUATION OF ERLOTINIB LOADED LIQUORICE CRUDE PROTEIN NANOPARTICLES BY BOX BEHNKEN DESIGN

2021 ◽  
pp. 94-101
Author(s):  
GEETHA V. S. ◽  
MALARKODI VELRAJ
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Crude Protein ◽  
Entrapment Efficiency ◽  
In Vitro Cytotoxicity ◽  
In Vitro Drug Release ◽  
Box Behnken Design ◽  
Prepared Nanoparticles ◽  
Drug Entrapment Efficiency

Objective: To formulate and evaluate Erlotinib loaded Liquorice crude protein (LCP) nanoparticles from the powdered liquorice root (Glycyrrhiza glabra) using Box-Behnken design. Methods: Erlotinib loaded liquorice crude protein nanoparticles were prepared by desolvation method using ethanol-water (1:2 ratio), Tween-80 (2%v/v) and gluteraldehyde (8% v/v) as cross linking agent. Box-Behnken design with 3 factors, 3 levels and 3 responses was used to optimize the prepared nanoparticles. The independent variables were taken as A) Erlotinib concentration B) LCP concentration and C) Incubation time with responses R1) Drug entrapment efficiency R2) Drug Release 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, particle size and zeta potential by Photon correlation spectroscopy (PCS) and surface morphology by TEM. The entrapment efficiency, and in vitro drug release studies in PBS pH 7.4 (26 h) were carried out. The experimental values were found to be in close resemblance with the predicted value obtained from the optimization process. The in vitro cytotoxicity studies of the prepared nanoparticles in lung cancer cell line (A 549) were studied with different concentrations for 24h. Results: The average particle size, zeta potential, Polydispersity index (PDI) were found to be 292.1 nm,-25.8 mV and 0.384 respectively. TEM image showed that the nanoparticles dispersed well with a uniform shape and showed not much change during storage. The in vitro drug release showed 41.23% for 26 h in PBS (7.4) and release kinetics showed highest R2value (0.982) for Korsmeyer-Peppas model, followed by 0.977 for Higuchi model. The in vitro cytotoxicity of prepared nanoparticles in A 549 cell line showed good results with different concentrations for 24h. Conclusion: Erlotinib (Erlo) is a BCS class II drug with poor solubility, poor bioavailability and selective tyrosine kinase inhibitor for non small-cell lung cancer (NSCLC) through oral administration. To improve the oral bioavailability and absorption of molecules, plant protein as carriers is used for developing drug delivery systems due to their proven safety. The optimization variables were Conc of Erlo, Conc. of LCP and Incubation time to get responses as drug entrapment efficiency, drug release and particle size. The compatibility between drug and LCP were evaluated by FTIR.

scholarly journals FORMULATION AND QBD BASED OPTIMIZATION OF METHOTREXATE-LOADED SOLID LIPID NANOPARTICLES FOR AN EFFECTIVE ANTI-CANCER TREATMENT

2021 ◽  
pp. 132-143
Author(s):  
CHAITALI SURVE ◽  
RUCHI SINGH ◽  
ANANYA BANERJEE ◽  
SRINIVAS PATNAIK ◽  
SUPRIYA SHIDHAYE
Keyword(s):  
Particle Size ◽  
Solid Lipid Nanoparticles ◽  
Oral Delivery ◽  
Entrapment Efficiency ◽  
Lipid Nanoparticles ◽  
Polydispersity Index ◽  
In Vivo Studies ◽  
Solid Lipid

Objective: In the current study, the Quality by Design method was utilized for the formulation of solid lipid nanoparticles of Methotrexate (MTX SLNs). Methods: MTX SLNs formulated by melt emulsification method were studied for the effect of independent variables viz. concentration of lipid and surfactants on quality attributes viz. particle size, polydispersity index, and entrapment efficiency of SLNs using 32 factorial design. Results: The optimal formulation was spherical, had a particle size of 147.6±4.1 nm (z-average), a polydispersity index of 0.296±0.058, a zeta potential of −19±0.98 mV, encapsulation efficiency of 98.7±1.55%, and a cumulative drug release of 95.59±0.918% in 5 h. Conclusion: The  in vitro and in vivo studies revealed that SLNs provide a promising oral delivery system to improve the bioavailability of MTX.

scholarly journals DEVELOPMENT, CHARACTERIZATION, AND EVALUATION OF SELEGILINE BIONANOSUSPENSIONS USING BUCHANANIA LANZAN AS BIOSTABILIZER

2019 ◽  
pp. 248-255
Author(s):  
YOGITA TYAGI ◽  
N. V. SATHEESH MADHAV
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Zeta Potential ◽  
Release Kinetics ◽  
Hydroxypropyl Methylcellulose ◽  
Polydispersity Index ◽  
Fickian Diffusion ◽  
Stability Studies ◽  
Best Fit

Objective: Development and evaluation of selegiline-loaded bio-nanosuspensions using biopolymer which was isolated from seeds of Buchanania lanzan (Chironji), used as biostabilizer and compared with standard polymer. Methods: The selegiline-loaded bio-nanosuspensions were prepared using novel biopolymer and standard stabilizer (hydroxypropyl methylcellulose) by sonication solvent evaporation method with different ratios (1%, 2%, 3%, 4%, and 5%) and evaluated for particle size, polydispersity index, zeta potential, pH stability studies, percentage entrapment efficacy, in vitro drug release, and stability studies. Results: The prepared selegiline bio-nanosuspensions were subjected to the best formulation based on comparison of above-mentioned evaluation parameters, so Fb2 (2%) formulation was found to be the best formulation showing an R2=0.9842, T50% of 32 h and T80% of 70 h, respectively. According to the release kinetics, the best fit model was found to be Peppas-Korsmeyer with Fickian diffusion (Higuchi matrix) as the mechanism of drug release, and Fs5 (5%) formulation was found to be the best formulation showing an R2=0.9564, T50% of 25 h and T80% of 60 h, respectively. According to the release kinetics, the best fit model was found to be Peppas-Korsmeyer with Fickian diffusion (Higuchi matrix) as the mechanism of drug release. The biopolymer provided excellent stability for the formulation and resulting particle size for the best formulation was found to be 360 nm. The best formulation was found to be polydispersity index of 0.43 with zeta potential of −5.12 mV. Conclusion: The prepared bio-nanosuspensions using biopolymer were found to be safe and compatible with the novel drug delivery for the treatment of depression in comparison of standard polymer.

scholarly journals Optimization of Site-Specific Drug Delivery System of Tyrosine Kinase Inhibitor Using Response Surface Methodology

2021 ◽  
pp. 273-286
Author(s):  
S. Parimala Krishnan ◽  
Cinnayyagari Mahesh Reddy ◽  
Challa Balashekar Reddy
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Sodium Alginate ◽  
Calcium Chloride ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Site Specific ◽  
Box Behnken Design ◽  
Specific Formulation

Aims: The aim of present study was to develop a stomach specific formulation of Imatinibmesylate to increase the fraction of drug absorbed in stomach. Study Design: Development and Optimization of Microspheres for site specific delivery.. Place and Duration of Study: The study was carried out in Department of Pharmacy, Annamalai University, between October 2020 and July 2021. Methodology: Ionotropic gelation method with Sodium alginate and Chitosan were used to formulate the mucoadhesive microspheres with calcium chloride. The formulation was optimized using Box – Behnken design to study the effect of independent variables, Amount of Sodium Alginate (X1), Amount of Chitosan (X2) and concentration of Calcium Chloride (X3) on dependent variables Particle Size (Y1), Entrapment Efficiency (Y2) and In-vitro drug release (Y3). Results: Particle size of prepared microspheres varied from 458.25 to 810.75 μm, entrapment efficiency from 64.87 to 82.63% and in-vitro release from 69.22 to 83.50%. The optimized formulation was found using point prediction, and formulation showed optimum results. The drug release was controlled for more than 12 h. Conclusion: Stomach specific formulation of Imatinibmesylate was successfully optimized by a three-factor, three level Box – Behnken design.

Fenofibrate Solid Dispersion for Improving Oral Bioavailability: Preparation, and Characterization and in vivo Evaluation

2020 ◽  
Vol 13 (5) ◽  
pp. 5102-5109
Author(s):  
Venu Madhav K ◽  
Somnath De ◽  
Chandra Shekar Bonagiri ◽  
Sridhar Babu Gummadi
Keyword(s):  
Oral Bioavailability ◽  
Oral Delivery ◽  
Solid Dispersions ◽  
In Vitro Release ◽  
Aqueous Solubility ◽  
Water Soluble ◽  
Scanning Calorimetry ◽  
In Vivo Evaluation

Fenofibrate (FN) is used in the treatment of hypercholesterolemia. It shows poor dissolution and poor oral bioavailability after oral administration due to high liphophilicity and low aqueous solubility. Hence, solid dispersions (SDs) of FN (FN-SDs) were develop that might enhance the dissolution and subsequently oral bioavailability. FN-SDs were prepared by solvent casting method using different carriers (PEG 4000, PEG 6000, β cyclodextrin and HP β cyclodextrin) in different proportions (0.25%, 0.5%, 0.75% and 1% w/v). FN-SDs were evaluated solubility, assay and in vitro release studies for the optimization of SD formulation. Differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD) and scanning electron microscopy (SEM) analysis was performed for crystalline and morphology analysis, respectively. Further, optimized FN-SD formulation evaluated for pharmacokinetic performance in Wistar rats, in vivo in comparison with FN suspension.  From the results, FN-SD3 and FN-SD6 have showed 102.9 ±1.3% and 105.5±3.1% drug release, respectively in 2 h. DSC and PXRD studies revealed that conversion of crystalline to amorphous nature of FN from FT-SD formulation. SEM studies revealed the change in the orientation of FN when incorporated in SDs. The oral bioavailability FN-SD3 and FN-SD6 formulations exhibited 2.5-folds and 3.1-folds improvement when compared to FN suspension as control. Overall, SD of FN could be considered as an alternative dosage form for the enhancement of oral delivery of poorly water-soluble FN.

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