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

scholarly journals Formulation and Evaluation of Acyclovir Microspheres

2018 ◽  
Vol 27 (1) ◽  
pp. 1-7
Author(s):  
Pavani S ◽  
Mounika K ◽  
Naresh K
Keyword(s):  
Particle Size ◽  
Sustained Release ◽  
Sodium Alginate ◽  
Calcium Chloride ◽  
Polymer Concentration ◽  
Entrapment Efficiency ◽  
In Vitro Dissolution ◽  
Release Mechanism ◽  
Natural Polymers

The present study is to formulate and evaluate Acyclovir (ACV) microspheres using natural polymers like chitosan and sodium alginate. ACV is a DNA polymerase inhibitor used in treating herpes simplex virus infection and zoster varicella infections. Acyclovir is a suitable candidate for sustained-release (SR) administration as a result of its dosage regimen twice or thrice a day and relatively short plasma half-life (approximately 2 to 4 hours). Microspheres of ACV were prepared by an ionic dilution method using chitosan and sodium alginate as polymers. The prepared ACV microspheres were then subjected to FTIR, SEM, particle size, % yield, entrapment efficiency, in vitro dissolution studies and release kinetics mechanism. The FTIR spectra’s revealed that, there was no interaction between polymer and ACV. ACV microspheres were spherical in nature, which was confirmed by SEM. The particle size of microspheres was in the range of 23.8µm to 39.4µm. 72.9% drug entrapment efficiency was obtained in the formulation F3 (1:3 ratio) with a high concentration of calcium chloride (4% w/v). The in vitro performance of ACV microspheres showed sustained release depending on the polymer concentration and concentration of calcium chloride.   The release data was best fitted with zero order kinetics and Korsemeyer -Peppas release mechanism and diffusion exponent ‘n’ value of was found to be Non-Fickian.

scholarly journals Design of Guggul Lipid Loaded Chitosan Nanoparticles Using Box-Behnken Design – An Evaluation Study

2021 ◽  
pp. 53-67
Author(s):  
B. R. Srinivas Murthy ◽  
Prasanna Raju Yelavarthi ◽  
N. Devanna ◽  
D. Jamal Basha
Keyword(s):  
Sustained Release ◽  
Lipid A ◽  
Sodium Tripolyphosphate ◽  
Desirability Function ◽  
Chitosan Nanoparticles ◽  
Entrapment Efficiency ◽  
Polynomial Equation ◽  
Ionic Gelation ◽  
Box Behnken Design

Aim: Guggul lipid, a lipophillic antihyperlipidemic moiety, undergoes extensive first-pass metabolism and has low bioavailability. In order to address this limitation, guggul lipid loaded chitosan nanoparticles (GNPs) were designed, optimized and processed by 3- factor 3- level Box- Behnken design (BBD). Methodology: A 3-factor 3-level BBD was employed to investigate combined influence of formulation variables on percent entrapment efficiency (EE) and percent drug release (DR) of GNPs prepared by ionic gelation method. The generated polynomial equation was validated and desirability function was utilized for optimization. Optimized GNPs were evaluated for physicochemical, morphological, release characteristics, solid state characterization and in-vitro cell line studies. Results: Amounts of chitosan, sodium tripolyphosphate and guggul were selected as independent variables had variably influenced EE and DR. Optimized GNPs were produced with an average size of 96.5 nm, electro kinetic potential of -15.4 mV, EE of 92.98% and DR of 95.12% in 24 h with sustained release. Physicochemical and in-vitro characterization revealed existence of guggul in amorphous form in GNPs without interaction and exhibited sustained release profile following first order with Higuchi kinetics. GNPs possessed lipase inhibition activity with IC50 value of 14.72 µg/ml and better viability against various cell lines with CTC50 values (256.24 to 321.27 µg/ml). Conclusions: Design and optimization of GNPs by BBD proved to be an effective and promising approach. High entrapment of guggul followed controlled release were the outcomes of GNPs prepared by ionic gelation with improved cell viability.

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 FORMULATION AND CHARACTERISATION OF SUSTAINED RELEASE MICROBEADS LOADED WITH ZALTOPROFEN

2019 ◽  
pp. 173-180
Author(s):  
H. C. KIRAN ◽  
DHANDAPANI NAGASAMY VENKATESH ◽  
RAMAN RAJESHKUMAR
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Calcium Chloride ◽  
Oral Bioavailability ◽  
Half Life ◽  
Elimination Rate ◽  
Entrapment Efficiency ◽  
Sustained Drug Release ◽  
Scanning Calorimetry ◽  
Drug Entrapment Efficiency

Objective: The main aim of the present investigation was to formulate and evaluate microbeads of zaltoprofen. Zaltoprofen, a BCS class II drug used in the treatment of rheumatoid arthritis. Zaltoprofen has a shorter half-life of 2.8 h, and it is administered at a dose of 80 mg thrice a day. By encapsulating the drug into microbeads, it is expected that the release of the drug would be prolonged and thereby, it reduces the frequency of administration and better patient compliance may be improved. Methods: Gellan-chitosan and calcium chloride beads of zaltoprofen were prepared employing ionotropic gelation method using different concentrations of gellan, chitosan, calcium chloride and zaltoprofen. The microbeads were evaluated for its various Physico-chemical parameters such as particle size determination, drug entrapment efficiency, infrared spectroscopy study, differential scanning calorimetry, X-ray diffraction analysis, scanning electron microscopy, in vitro drug release study and in vivo oral bioavailability studies. Results: The results suggested that the batch FG-II exhibited higher drug entrapment efficiency (72.42±0.013), a sustained drug release for a period of 24 h. The pharmacokinetic profile of the drug from microbeads exhibited an enhanced oral bioavailability (2.4 times higher than that of pure drug), lower elimination rate (1.14 times lesser for the drug in microbeads) with prolonged elimination half-life (2.561 times higher than pure zaltoprofen). Conclusion: Zaltoprofen entrapped microbeads demonstrated as a better delivery system for the sustained release of drug and also to circumvent the drawbacks associated with conventional therapy.

scholarly journals FORMULATION AND OPTIMIZATION OF MUCOADHESIVE MICROSPHERES OF VALSARTAN BY USING BOX-BEHNKEN DESIGN

2019 ◽  
pp. 371-379
Author(s):  
CHIMAN LAL ◽  
RAJEEV GARG ◽  
GHANSHYAM DAS GUPTA
Keyword(s):  
Ethyl Cellulose ◽  
Entrapment Efficiency ◽  
Sem Analysis ◽  
Stability Study ◽  
Box Behnken Design ◽  
Independent Variables ◽  
Dependent Variables ◽  
Evaporation Technique ◽  
Drug Entrapment Efficiency ◽  
Carbopol 934P

Objective: The purpose of this study was to formulate and optimize mucoadhesive microspheres of antihypertensive drug (valsartan) within ethyl cellulose as a carrier polymer and carbopol 934P as a mucoadhesive polymer for controlling the release of valsartan. Methods: The emulsion solvent evaporation technique was used for preparation of microspheres of valsartan and the Box-Behnken design was employed with thee independent variables that is amount of ethyl cellulose (X1) and amount of carbopol 934P (X2) and stirring speed (X3) and evaluate four dependent variables such as percentage mucoadhesion, Q1 h, t90% and drug entrapment efficiency. Results: The optimum conditions were found to be X1= 200 mg, X2= 107 mg and X3= 1200rpm. The optimized batch exhibited a high drug entrapment efficiency of 85.63±1.384%, percentage mucoadhesion was 66.76±0.986% and drug release was also sustained for more than 12 h. Conclusion: The analysis of variance showed a significant effect of independent variables. The scaning electron microscopy (SEM) analysis showed that the microspheres were spherical and free-flowing. The microspheres of valsartan were stable after thee month stability study at accelerated condition.

scholarly journals Design of Lipid Nanoparticles Containing Fenugreek Seed Extract

2021 ◽  
pp. 268-278
Author(s):  
P. Ananth ◽  
Marina Koland ◽  
Sridhar Deshpande ◽  
G. S. Mahendra
Keyword(s):  
Entrapment Efficiency ◽  
Lipid Nanoparticles ◽  
Quality Parameters ◽  
Seed Extract ◽  
Box Behnken Design ◽  
Independent Variables ◽  
Fenugreek Seed ◽  
Mathematical Equations

Background: The main purpose of this study was to maximize the efficacy of fenugreek seed extract by loading it in an optimised solid lipid nanoparticles (SLNs) formula. Methods: To achieve an effective extraction method, preliminary studies were carried out to confirm the extract, and the extract was standardised using trigonelline. The influence of independent variables lipid concentration (X1), surfactant concentration (X2), and cosurfactant concentration (X3) on dependent variables particle size (Y1) and entrapment efficiency (Y2) was also studied and optimised using the Box–Behnken design. Melt emulsification followed by ultrasonication was used to prepare SLN formulations. To understand the effect of independent variables on the dependent quality parameters, response surface plots and mathematical equations were produced. Results: The results confirmed that soxhalation was the most suitable method for extraction of fenugreek seeds, confirmed by standardization. Further optimization revealed that particle sizes ranged from 193.4 to 312.3 nm, with entrapment efficiencies ranging from 61.2 to 74.32 percent. This implies that the developed formulations can be used for further in vitro and in vivo characterizations.

scholarly journals PREPARATION AND CHARACTERIZATION OF ETODOLAC BEARING EMULSOMES

2020 ◽  
pp. 166-172
Author(s):  
VIVEK GILL ◽  
ARUN NANDA
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Drug Release ◽  
Zeta Potential ◽  
Sustained Release ◽  
Entrapment Efficiency ◽  
Box Behnken Design ◽  
Phospholipid Ratio ◽  
Predicted Values ◽  
Experimental Values

Objective: Emulsomes are novel vesicular drug delivery system with an internal solid lipid core surrounded by one or more bilayers of phospholipids. Etodolac is a potent anti-inflammatory drug and is a drug of choice for the treatment of various diseases. The present study is focused on the development of emulsomes using etodolac as drug candidates having improved drug loading with sustained-release effect for patient compliance. Methods: Emulsomes formulation composed of solid lipids (tristearin), phospholipids, cholesterol, stearylamine, and drug (etodolac) were prepared by lipid film hydration method followed by sonication to produce emulsomes of the nanometric size range. All the formulations were optimized by using box-behnken design of experiment considering 3 factors viz. drug to phospholipid ratio (A), tristearin to phospholipid ratio (B), stearylamine to phospholipid ratio (C) at 3 levels lower (-1), middle (0) and upper (+1). The response of the independent variables (A, B, C) was studied on the dependent variable viz. particle size (Y1), zeta potential (Y2), and entrapment efficiency (Y3). The responses were analyzed by design expert software to find out the optimized values of variables within the design space. Results: Compatibility with excipients was established by FTIR studies. The developed emulsomes were spherical shape vesicles as analyzed by TEM. The optimized batch (OB) was evaluated for particle size, zeta potential, and entrapment efficiency with experimental values 383.1 ± 11.7 nm, 47.2 ± 1.3 mV and 80.1 ± 3.2% and predicted values 390.394 nm, 45.000 mV and 81.642 %, respectively. The experimental values were found in reasonable agreement with predicted values by the design of the experiment. In vitro drug release study showed sustained release of the drug (88.69 % after 24 h). Conclusion: Etodolac loaded emulsomes is a novel drug delivery system and found to reliable in terms of various characteristic parameters like particle size, zeta potential, entrapment efficiency, and drug release. 3-factors 3-levels Box-behnken design of the experiment is a suitable design for the optimization of emulsomes.

scholarly journals SUSTAINED RELEASE MUCOADHESIVE MICROCAPSULES OF RAMIPRIL BY IONIC GELATION TECHNIQUE: FORMULATION DESIGN, OPTIMIZATION AND CHARACTERIZATION

2017 ◽  
Vol 9 (2) ◽  
pp. 128
Author(s):  
Korlapati Venkateswara Rao ◽  
V. V. Venkatchalam
Keyword(s):  
Sustained Release ◽  
Desirability Function ◽  
Research Work ◽  
Entrapment Efficiency ◽  
Spectral Studies ◽  
Antihypertensive Activity ◽  
Ionic Gelation ◽  
Scanning Calorimetry

<p><strong>Objective: </strong>The major objective of the research work was to design, optimise and characterise sodium alginate based sustained release mucoadhesive microcapsules of ramipril by ionic gelation method.</p><p><strong>Methods: </strong>An experimental set-up was designed to investigate the optimal combination of mucoadhesive polymers such as carbopol 974P, HPMC (K4M and K100M), Na CMC and chitosan and their drug compatibility with respect to reliabilities. Preliminary screening of the formulation variables was accomplished by Taguchi design followed by Box-Behnken design for systematic optimisation. The suitable mathematical model was selected, response surface analysis was performed and optimised formulation was chosen by numerical optimization and desirability function method. Characterization of the prepared microcapsules for several inherent properties like particle size, drug content, sphericity, entrapment efficiency, loose surface crystal study, swelling index, micromeritic properties, moisture content, <em>in vitro</em> drug release, mucoadhesive strength and <em>in vivo</em> antihypertensive activity was performed.</p><p><strong>Results: </strong>Differential Scanning Calorimetry (DSC) thermograms and Fourier Transform Infra-Red (FT-IR) spectral studies revealed no incompatibility between the pure drug and selected polymers. The spherical nature of the prepared microcapsules was established by surface morphology studies.</p><p><strong>Conclusion: </strong>The resultant sustained release mucoadhesive microcapsules of ramipril remained stable when subjected to stress conditions unveiling it as a better alternative delivery system with superior therapeutic efficacy.</p>

scholarly journals SUSTAINED RELEASE MICROBEADS OF RITONAVIR: IN VITRO AND IN VIVO EVALUATION

2019 ◽  
pp. 189-198
Author(s):  
D. NAGASAMY VENKATESH ◽  
S. SHASHI KUMAR ◽  
RAMAN RAJESHKUMAR
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Calcium Chloride ◽  
Half Life ◽  
Elimination Rate ◽  
Entrapment Efficiency ◽  
Drug Entrapment Efficiency ◽  
Pure Drug

Objective: The main aim of the present investigation was to develop sustained release microbeads of ritonavir that has a shorter half-life (3-5 h) and requires twice a day administration. These formulations exhibit a sustained release of ritonavir that would expect to improve the therapy, better drug utilization, and patient compliance. Methods: Gellan-chitosan and calcium chloride reinforced beads of ritonavir were prepared by ionotropic gelation method employing different concentrations of gellan, chitosan, calcium chloride and drug. The prepared beads were evaluated for various physicochemical parameters such as particle size determination, drug entrapment efficiency, swelling studies, infrared spectroscopy study, differential scanning calorimetry, x-ray diffraction analysis, scanning electron microscopy, in vitro drug release study and in vivo bioavailability studies. Results: From the results, formulation GC-II exhibited higher drug entrapment efficiency (79.65±0.012), higher swelling index, sustained drug release over a period of 24 h, increased oral bioavailability (2.07 times higher than that of pure drug) and decreased elimination rate (2.15 times lesser for ritonavir microbeads) with prolonged elimination half-life (2.15 times more than pure drug) as compared to pure drug. Conclusion: Ritonavir microbeads have demonstrated as a better delivery system for the sustained release of the drug; which may in turn circumvent the drawbacks associated with the conventional therapy.

scholarly journals FORMULATION AND EVALUATION OF RACECADOTRIL MUCOADHESIVE MICROSPHERES

2019 ◽  
pp. 55-61
Author(s):  
KANCHAN JAMKAR ◽  
SWATI MUTHA ◽  
SHARWAREE HARDIKAR ◽  
NIKHIL KUMBHAR
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Xanthan Gum ◽  
Entrapment Efficiency ◽  
Cross Linking ◽  
Natural Polymers ◽  
In Vitro Drug Release ◽  
Mucoadhesive Microsphere ◽  
Chemical Cross Linking

Objective: To develop and evaluate the mucoadhesive microsphere using combinations of natural polymers chitosan and xanthan gum for sustained release. Methods: In the present work mucoadhesive microspheres were prepared by using natural polymers like chitosan and xanthan gum by using the emulsion chemical cross-linking method. Chemical cross-linking was done by using glutaraldehyde. The 22 factorial design was employed to show the effect of cross-linking agent and processing factor-like stirring and speed. Prepared microspheres were evaluated for their particle size, surface morphology, drug entrapment efficiency, in vitro drug release, swelling index, and mucoadhesive strength. Results: The size of microspheres of factorial batches were in the range of 26-46 µm. The swelling index was showed in the range of 1.51-1.66 percentage. The equation of multiple regression revealed that there was significant interaction among factors. The glutaraldehyde concentration had a positive effect on % entrapment efficiency, % cumulative drug release and % mucoadhesion. Stirring speed showed a negative impact on % entrapment efficiency, % cumulative drug release and % mucoadhesion. The interactive effect of glutaraldehyde concentration and the stirring speed was found to be positive for % entrapment efficiency and % cumulative drug release. In vitro drug release study of optimized formulation F2 show 96 % of drug release with 6 h indicating sustained release behavior with diffusion mechanism. The SEM image of the optimized batch was spherical with a porous surface. Conclusion: The results obtained in this research work indicated that a promising potential of chitosan and xanthan gum combination for the preparation of the mucoadhesive microsphere of Racecadotril.

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