scholarly journals Optimization of Chitosan–Alginate Microparticles for Delivery of Mangostins to the Colon Area Using Box–Behnken Experimental Design

2020 ◽  
Vol 21 (3) ◽  
pp. 873 ◽  
Author(s):  
Kamarza Mulia ◽  
Ameninta Cesanina Singarimbun ◽  
Elsa Anisa Krisanti
Keyword(s):  
Calcium Chloride ◽  
Sodium Tripolyphosphate ◽  
Chloride Concentration ◽  
Release Profile ◽  
Significant Variable ◽  
Mass Ratio ◽  
Box Behnken Design ◽  
Cumulative Release ◽  
Independent Variables ◽  
Sequential Release

Chitosan-alginate microparticles loaded with hydrophobic mangostins present in the mangosteen rind extract have been formulated and optimized for colon-targeted bioactive drug delivery systems. The chitosan–mangostin microparticles were prepared using the ionotropic gelation method with sodium tripolyphosphate as the cross-linking agent of chitosan. The chitosan–mangostin microparticles were then encapsulated in alginate with calcium chloride as the linking agent. The mangostin release profile was optimized using the Box–Behnken design for response surface methodology with three independent variables: (A) chitosan–mangostin microparticle size, (B) alginate:chitosan mass ratio, and (C) concentration of calcium chloride. The following representative equation was obtained: percent cumulative release of mangostins (10 h) = 59.51 − 5.16A + 20.00B − 1.27C − 1.70AB − 5.43AC − 5.04BC + 0.0579A2 + 10.25B2 + 1.10C2. Cumulative release of 97% was obtained under the following optimum condition for microparticle preparation: chitosan–mangosteen particle size < 100 µm, alginate:chitosan mass ratio of 0.5, and calcium chloride concentration of 4% w/v. The alginate to chitosan mass ratio is the statistically significant variable in the optimization of sequential release profile of mangostins in simulated gastrointestinal fluids. Furthermore, a sufficient amount of alginate is necessary to modify the chitosan microparticles and to achieve a complete release of mangostins. The results of this work indicate that the complete release of mangostins to the colon area can be achieved using the chitosan–alginate microparticles as the bioactive delivery system.

scholarly journals PRELIMINARY FORMULATION STUDY OF LYCOPENE SELF-ASSEMBLE NANOPARTICLES VIA BOX-BEHNKEN DESIGN IMPARTING AN EFFICIENT DRUG DELIVERY: STATISTICAL AND ILLUSTRATIVE APPROACH

2020 ◽  
Vol 8 (12) ◽  
pp. 455-463
Author(s):  
Mohammad Yusuf ◽  
Keyword(s):  
Drug Delivery ◽  
Zeta Potential ◽  
Clinical Outcomes ◽  
Self Assembly ◽  
Intrinsic Property ◽  
Box Behnken Design ◽  
Cumulative Release ◽  
Independent Variables ◽  
Chitosan Concentration ◽  
Dependent Variables

Lycopene, a structurally polyene conjugated antioxidant,is frequentlyutilized for the treatment of ailments induced by augmentedoxidative stress.Its colossal structure and poor water-solubilityfailed to show the requisite clinical outcomes. To overcome these drawbacks a formulation study introducing Lycopene as Chitosan-phosphatidylserineself-assembled nanoparticles (LNP)to correlatethe dependent and independent variables employing Box-Behnken design has been performed. LNP formulation was achieved byinjection technique, using chitosan’s intrinsic property of towards Phosphatidylserine for self-assembly. Independent variables, i.e., chitosan concentration (X1), Phosphatidylserine (X2), and injecting rate (X3) were correlatedagainst dependent variables (responses) nanoparticle size, cumulative release,and lycopene encapsulation. Prepared nanocrops were stable, under 300 nmparticle size, Zeta potential below +30 mV, close PDI to 0.3, and exhibited invitro 69-76% cumulative release. Overall, the formulation strategy was fruitful to develop a formulation in the future for efficient drug delivery.

scholarly journals Influence of Pregelatinized Breadfruit Starch-Alginate Blend as a Sustained Release Polymer in Theophylline Microbeads Using Box Behnken Design

2021 ◽  
Vol 16 (2) ◽  
pp. 143-151
Author(s):  
A. Okunlola ◽  
S. T. Oloye
Keyword(s):  
Sustained Release ◽  
Calcium Chloride ◽  
Entrapment Efficiency ◽  
Ionic Gelation ◽  
Natural Polymers ◽  
Box Behnken Design ◽  
Artocarpus Altilis ◽  
Independent Variables ◽  
Modified Starches ◽  
High Level

Background: Apart from the coating property of modified starches on drugs, these natural polymers also acts as release rate retardants.Objectives: To evaluate the potential of pregelatinized breadfruit (Artocarpus altilis) starch as a carrier in microbead formulations of theophylline using different blend combinations with sodium alginate and to determine the optimized formulation using Box-Behnken design.Method: Theophylline microbeads were prepared using the ionic gelation method. The 3 factor-3 level Box-Behnken design was employed for constructing polynomial models to optimize the microbeads, involving 3 independent variables (polymer type, X1, polymer: drug ratio, X2, and concentration of calcium chloride, X3) and 2 dependent variable (entrapment efficiency and quantity of drug released in 12 h, Q12).Results: Entrapment efficiency was 35 - 71 % while the values of Q12 was 38 - 88 %. The three variables, X1, X2 and X3, were positive for entrapment efficiency but negative for Q12, implying that increase from low to medium and then to high level resulted in an increase in entrapment but a decrease in Q12 (sustained release), both desirable effects. Factor X1 had the most significant influence on entrapment efficiency and Q12 (p = 0.002; p = 0.0001, respectively). The optimized formulation with starch:polymer 2:1, polymer:drug 3:1 and 7.5%w/v calcium chloride solution gave an entrapment efficiency 65% with Q12 of 38.75%.Conclusion: Pregelatinized breadfruit starch enhanced entrapment efficiency while retarding drug release, showing its potential as a polymer for sustained release in microbead formulations. Keywords: Box-Behnken design; Breadfruit starch; Ionic gelation, Microbeads, Pregelatinization

Development, Evaluation and Optimization of Osmotic Controlled Tablets of Aceclofenac for Rheumatoid Arthritis Management

2019 ◽  
Vol 9 (1) ◽  
pp. 29-36
Author(s):  
Bijaya Ghosh ◽  
Niraj Mishra ◽  
Preeta Bose ◽  
Moumita D. Kirtania
Keyword(s):  
Rheumatoid Arthritis ◽  
Polyethylene Glycol ◽  
Sodium Chloride ◽  
Cellulose Acetate ◽  
Hydroxypropyl Methylcellulose ◽  
Release Profile ◽  
Polyethylene Glycol 400 ◽  
Permeable Membrane ◽  
Cumulative Release ◽  
The Core

Objective: Rheumatoid arthritis is a dreaded disease, characterized by pain, inflammation and stiffness of joints, leading to severe immobility problems. The disease shows circadian variation and usually gets aggravated in early morning hours. Aceclofenac, a BCS Class II compound is routinely used in the treatment of pain and inflammation associated with rheumatoid arthritis. The objective of this study was to develop an osmotic delivery system of Aceclofenac that after administration at bedtime would deliver the drug in the morning hours. </P><P> Methods: A series of osmotically controlled systems of aceclofenac was developed by using lactose, sodium chloride and hydroxypropyl methylcellulose K100M as osmogens. Cellulose acetate (2% w/v in acetone) with varying concentrations of polyethylene glycol-400 was used as the coating polymer to create semi permeable membrane and dissolution was carried out in 290 mOsm phosphate buffer. Formulation optimization was done from four considerations: cumulative release at the end of 6 hours (lag time), cumulative release at the end of 7 hours (burst time), steady state release rate and completeness of drug release. </P><P> Results: A formulation having swelling polymer hydroxypropyl methylcellulose in the core and lactose and sodium chloride as osmogens, polyethylene glycol-400 (16.39 %) as pore former, with a coating weight of 5% was a close fit to the target release profile and was chosen as the optimum formulation. Conclusion: Aceclofenac tablets containing lactose, HPMC and sodium chloride in the core, given a coating of cellulose acetate and PEG-400 (5% wt gain), generated a release profile for optimum management of rheumatoid arthritic pain.

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.

scholarly journals Chitosan Nanocarrier Entrapping Hydrophilic Drugs as Advanced Polymeric System for Dual Pharmaceutical and Cosmeceutical Application: A Comprehensive Analysis Using Box-Behnken Design

Polymers ◽  
2021 ◽  
Vol 13 (5) ◽  
pp. 677
Author(s):  
Sara A. Abosabaa ◽  
Aliaa N. ElMeshad ◽  
Mona G. Arafa
Keyword(s):  
Particle Size ◽  
Sodium Tripolyphosphate ◽  
Chitosan Nanoparticles ◽  
Optimization Procedure ◽  
Entrapment Efficiency ◽  
Chitosan Solution ◽  
Polydispersity Index ◽  
Successful Implementation ◽  
Solution Ph ◽  
Box Behnken Design

The objective of the present research is to propose chitosan as a nanocarrier for caffeine—a commonly used drug in combating cellulite. Being a hydrophilic drug, caffeine suffers from insufficient topical penetration upon application on the skin. Chitosan nanoparticles loaded with caffeine were prepared via the ionic gelation technique and optimized according to a Box–Behnken design. The effect of (A) chitosan concentration, (B) chitosan solution pH, and (C) chitosan to sodium tripolyphosphate mass ratio on (Y1) entrapment efficiency percent, (Y2) particle size, (Y3) polydispersity index, and (Y4) zeta potential were studied. Subsequently, the desired constraints on responses were applied, and validation of the optimization procedure was confirmed by the parameters exhibited by the optimal formulation. A caffeine entrapment efficiency percent of 17.25 ± 1.48%, a particle size of 173.03 ± 4.32 nm, a polydispersity index of 0.278 ± 0.01, and a surface charge of 41.7 ± 3.0 mV were attained. Microscopical evaluation using transmission electron microscope revealed a typical spherical nature of the nanoparticles arranged in a network with a further confirmation of the formation of particles in the nano range. The results proved the successful implementation of the Box–Behnken design for optimization of chitosan-based nanoparticles in the field of advanced polymeric systems for pharmaceutical and cosmeceutical applications.

A Novel Application of Refinery Merox Unit Wastewater for Bovine Hide Unhairing

2020 ◽  
Vol 115 (8) ◽  
pp. 301-308
Author(s):  
Asgarifard Pourya ◽  
Tafreshi Navid ◽  
Sharifi Akbar
Keyword(s):  
Optimum Condition ◽  
Polynomial Equation ◽  
Process Time ◽  
P Value ◽  
Environment Pollution ◽  
Box Behnken Design ◽  
Independent Variables ◽  
Order Polynomial ◽  
Tanning Process ◽  
Bovine Hide

Unhairing is one of the major steps of the leather tanning process which removes the hairs, epidermis and to some degree inter-fibrillary proteins. This process needs high amounts of chemicals that cause environmental difficulties. On the other hand, these chemicals are available in the wastewater of the Merox unit of Kermanshah Refinery. For reducing chemical consumption and decreasing environment pollution, we used the aforementioned wastewater for bovine unhairing. A unhairing liquor was prepared in order to unhair skins and different parameters such as the concentration of CaCO3 and Na2S, process time, and temperature were considered to evaluate their impact on the unhairing process and to obtain optimum condition. Response surface methodology based on Box-Behnken design was applied to model the unhairing efficiency in terms of four independent variables. A second-order polynomial equation was suggested to predict the response with high certainty. ANOVA revealed the validity and importance of that model by P-value of < 0.0001, large F-values, and, R2 of 98.8. The maximum unhairing efficiency of about 98.5 % was obtained under the optimum condition of 1.7 wt% Na2S, 5.8 wt% CaCO3, 114 min process time and 29.5 ºC.

scholarly journals Ranitidine Loaded Biopolymer Floats: Designing, Characterization, and Evaluation

2017 ◽  
Vol 2017 ◽  
pp. 1-12
Author(s):  
Abdul Karim ◽  
Muhammad Ashraf Shaheen ◽  
Tahir Mehmood ◽  
Abdul Rauf Raza ◽  
Musadiq Aziz ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Lag Time ◽  
Zero Order ◽  
Release Profile ◽  
Drug Release Profile ◽  
Independent Variables ◽  
Zero Order Kinetics ◽  
Model Drug ◽  
Predicted Values

The float formulation is a strategy to improve the bioavailability of drugs by gastroretentive drug delivery system (GRDDS). A drug delivery model based on swellable and reswellable low density biopolymers has been designed to evaluate its drug release profile using ranitidine (RNT) as a model drug and formulations have been prepared utilizing 32factorial designs. The drug release (DR) data has been subjected to various kinetic models to investigate the DR mechanism. A reduction in rate has been observed by expanding the amounts of PSG and LSG parts, while an expansion has been noted by increasing the concentration of tragacanth (TG) and citric acid (CA) with an increment in floating time. The stearic acid (SA) has been used to decrease the lag time because a decrease in density of system was observed. The kinetic analysis showed that the optimized formulation (S4F3) followed zero-order kinetics and power law was found to be best fitted due to its minimum lag time and maximum floating ability. The resemblance of observed and predicted values indicated the validity of derived equations for evaluating the effect of independent variables while kinetic study demonstrated that the applied models are feasible for evaluating and developing float for RNT.

scholarly journals PREPARATION OF ORAL CURCUMIN DELIVERY FROM 3D-NANO-CELLULOSE NETWORKS MATERIAL PRODUCED BY ACETOBACTER XYLINUM USING OPTIMIZATION TECHNIQUE

2020 ◽  
pp. 47-52
Author(s):  
THANH XUAN NGUYEN ◽  
HUONG LAN THI PHAM ◽  
THUONG THI NGO ◽  
PHONG XUAN ONG
Keyword(s):  
Oral Delivery ◽  
Positive Impact ◽  
Optimization Technique ◽  
Box Behnken Design ◽  
Independent Variables ◽  
3D Network ◽  
Nano Cellulose ◽  
Optimized Conditions ◽  
The Impact

Objective: To prepare oral curcumin delivery and optimize curcumin loading of 3D-nano-cellulose networks material (3DCM) by looking into the impact of process variables on the response utilizing response surface methodology (RSM) and Box-Behnken design. Methods: Optimization of curcumin loading of 3DCM was conducted using RSM and Box-Behnken model. Impact of four independent variables, including, the concentration of curcumin (X1), temperature (X2), shaking speed (X3), and time of loading (X4), was studied on one dependent response, that is, an amount of loaded curcumin (Y). Characterization of optimized 3DCM including curcumin was examined by Scanning Electron Microscopy (SEM) and Fourier Transform Infrared (FTIR) analysis . Results: R2 value for Y was approximately 0.94. X1 possessed the biggest positive impact compared to X2, X3 and X4. Optimized conditions for curcumin loading of 3DCM were X1 at 3 mg/ml, X2 at 40 °C, X3 at 120 rpm and X4 at 120 min. SEM photograph of 3DCM surfaces were found including fibers creating a 3D network structure. FTIR spectra studies depicted that there was no interaction between curcumin and 3DCM. Conclusion: The data obtained in this study thus suggest that curcumin loaded 3DCM was successfully fabricated to give a potential oral delivery system of curcumin.

scholarly journals Fluoride removal efficiencies of Al-EC and Fe-EC reactors: process optimization using Box–Behnken design of the surface response methodology

2020 ◽  
Vol 10 (9) ◽  
Author(s):  
Magori J. Nyangi ◽  
Yonas Chebude ◽  
Kessy F. Kilulya
Keyword(s):  
Treatment Time ◽  
Fluoride Concentration ◽  
Fluoride Removal ◽  
Reactor Model ◽  
Optimal Operating ◽  
Surface Response Methodology ◽  
Box Behnken Design ◽  
Surface Response ◽  
Independent Variables ◽  
Initial Ph

Abstract In this study, surface response methodology was employed to investigate the effect of different interacting factors on the removal of fluoride from synthetic water using aluminum electrocoagulation (Al-EC) and iron electrocoagulation (Fe-EC) in different reactors. Box–Behnken design of a Design Expert version 11 was used for the optimization and evaluation of the process independent variables: applied electric density, initial pH, initial fluoride concentration and treatment time on the efficiency of fluoride removal as a response. Results showed that the effect of current density and initial fluoride concentration was significant model terms for fluoride reduction in Fe-EC and Al-EC reactors, respectively. The Al-EC reactor model presented the R2 value of 79.2% while Fe-EC presented R2 value of 75.8%, showing that both models can predict the response well. The reduction by 94% (initial concentration of 16 mgF/L) was established at optimal operating parameters of 18.5 mAcm−2, pH 6.80 in 50 min using Al-EC. On the other hand, 16 mgF/L was reduced by 92% to 1.28 mgF/L in Fe-EC reactor at optimal condition of 6.5 mAcm−2, pH 6.50 in 50 min. Experimental results correlated well to the model predicted results that were 95 and 94% for Al-EC and Fe-EC, respectively. Both reactors manage to reduce fluoride to a level recommended by WHO (≤ 1.5 mg/L) for drinking purpose.

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