scholarly journals Preparation, Optimization, and Evaluation of Epichlorohydrin Cross-Linked Enset (Ensete ventricosum (Welw.) Cheeseman) Starch as Drug Release Sustaining Excipient in Microsphere Formulation

2020 ◽  
Vol 2020 ◽  
pp. 1-19
Author(s):  
Desta Tesfay ◽  
Solomon Abrha ◽  
Zewdu Yilma ◽  
Gebremariam Woldu ◽  
Fantahun Molla
Keyword(s):  
Drug Release ◽  
Central Composite Design ◽  
Release Rate ◽  
Fickian Diffusion ◽  
Cross Linking ◽  
Release Mechanism ◽  
Burst Release ◽  
Drug Release Rate ◽  
Ensete Ventricosum ◽  
Central Composite

Ensete ventricosum (Welw.) cheeseman which belongs to the family of Musaceae is one of the main sources of starch in Ethiopia. This study aimed at evaluating epichlorohydrin cross-linked enset starch as a drug release sustaining excipient in microsphere formulations of theophylline. Extracted enset starch was cross-linked using epichlorohydrin as a cross-linking agent. The effect of cross-linker concentration, cross-linking duration, and cross-linking temperature on the degree of cross-linking and release rate of microspheres prepared by emulsion solvent evaporation method was investigated using the two-level full factorial design. Accordingly, the concentration of epichlorohydrin and duration of cross-linking were the most significant factors affecting both the degree of cross-linking and drug release rate. Thus, the effects of these two factors were further studied and optimized using the central composite design. As per the numerical method of central composite design, the optimal points were obtained at epichlorohydrin concentration of 13.70% and cross-linking time of 3.82 h. Under these optimal conditions, the model predicts the degree of cross-linking of 74.70% and drug release rate of 28.00 h1/2. The validity of these optimal points was confirmed experimentally. The microspheres of the optimum formulation also exhibited minimum burst release with sustained release for 12 h. Besides, the optimized formulation followed the Higuchi square root kinetic model with non-Fickian diffusion release mechanism. The finding of this study suggested that cross-linked enset starch can be used as an alternative drug-release-sustaining pharmaceutical excipient in microsphere formulation.

scholarly journals STUDIES ON CROSS-LINKED CHITOSAN HYDROGEL FOR MATRIX TABLETS OF MONTELUKAST SODIUM

2017 ◽  
Vol 9 (4) ◽  
pp. 22
Author(s):  
Srinivas Hebbar ◽  
Akhilesh Dubey ◽  
Ravi G. S. ◽  
Shanon Ben Mascarenhas
Keyword(s):  
Drug Release ◽  
In Vitro Release ◽  
Matrix Tablets ◽  
Fickian Diffusion ◽  
Cross Linking ◽  
Release Mechanism ◽  
Release Kinetic ◽  
Montelukast Sodium ◽  
Hydrogel Matrix ◽  
Crosslinking Agents

Objective: The aim of the present study was to prepare hydrogel matrix tablets for controlled release of an anti-asthma drug (Montelukast sodium) by modifying the applications of chitosan by crosslinking it with the different cross linking agent.Methods: The hydrogels were prepared by crosslinking chitosan using three different crosslinking agents namely, anhydrous dextrose (DXT), sodium tripolyphosphate (TPP) and glutaraldehyde (GL). Formulations were prepared by direct compression method and pre and post compression parameters were evaluated.Results: FTIR (Fourier transform infrared spectroscopy) studies of tablet formulation indicated that there is no drug-excipient interaction in the prepared formulations. The matrix tablets were capable of releasing the drug for 11 h depending upon the formulation variables. The tablets prepared by plain chitosan discharged the drug quickly, while those prepared by using GL crosslinked-hydrogel released the drug more slowly in a controlled manner. In general, the order of drug release from the crosslinked hydrogel matrix tablets on the basis of crosslinking agents, was found to be DXT>TPP>GL. The type of cross-linking agents affected the drug release rate and in the case of the tablets prepared with CHTPP (95 % to 83 %) it was slower than for the tablets prepared with CHDX (96 % to 88 %) at the end of 11th h. CHGL tablets showed more prolonged drug release profiles (86 % to 74 %) as compared to CHDX and CHTPP at the end of 11th h. In vitro release data was fitted into various release kinetic models to study the release mechanism and showed zero order kinetics and “n” value were found to be less than 0.5 indicated the release mechanism followed fickian diffusion due to swelling of gel matrix and high solubility of montelukast sodium.Conclusion: From the experimental results it can be concluded that hydrogels of chitosan were successfully prepared by using DXT, TPP and GL with different concentration.

scholarly journals Design and evaluation of lornoxicam bilayered tablets for biphasic release

2012 ◽  
Vol 48 (4) ◽  
pp. 609-619
Author(s):  
Songa Ambedkar Sunil ◽  
Meka Venkata Srikanth ◽  
Nali Sreenivasa Rao ◽  
Sakamuri Balaji ◽  
Kolapalli Venkata Ramana Murthy
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Xanthan Gum ◽  
Hydroxypropyl Methylcellulose ◽  
Fickian Diffusion ◽  
Release Mechanism ◽  
Release Kinetic ◽  
Burst Release ◽  
Significant Difference ◽  
Biphasic Release

The objective of the present investigation was to develop bilayered tablets of lornoxicam to achieve biphasic release pattern. A bilayered tablet, consisting of an immediate and controlled release layer, was prepared by direct compression technique. The controlled release effect was achieved by using various hydrophilic natural, semi synthetic and synthetic controlled release polymers such as xanthan gum, hydroxypropyl methylcellulose (HPMC) and polyethylene oxide (PEO) to modulate the release of the drug. The in vitro drug release profiles showed the biphasic release behavior in which the immediate release (IR) layer containing the lornoxicam was released within 15 minutes, whereas the controlled release (CR) layer controlled the drug release for up to 24 h. All the bilayered tablets formulated have followed the zero order release with non-Fickian diffusion controlled release mechanism after the initial burst release. FTIR studies revealed that there was no interaction between the drug and polymers used in the study. Statistical analysis (ANOVA) showed no significant difference in the cumulative amount of drug release after 15 min, but significant difference (p < 0.05) in the amount of drug released after 24 h from optimized formulations was observed. Based on the release kinetic parameters obtained, it can be concluded that xanthan gum polymer was suitable for providing a biphasic release of lornoxicam.

scholarly journals CENTRAL COMPOSITE DESIGN FOR FORMULATION AND OPTIMIZATION OF LONG-ACTING INJECTABLE (LAI) MICROSPHERES OF PALIPERIDONE PALMITATE

2021 ◽  
pp. 87-98
Author(s):  
SANDIP MALI ◽  
NISHANT OZA
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Central Composite Design ◽  
Drug Loading ◽  
Entrapment Efficiency ◽  
Paliperidone Palmitate ◽  
Burst Release ◽  
Mean Particle Size ◽  
Long Acting ◽  
Central Composite

Objective: The aim of the present study was to optimize long-acting injectable (LAI) microspheres of Paliperidone palmitate (PP) for treatment of schizophrenia using face-centered central composite design (FC-CCD). Methods: In this study, poly lactic-co-glycolic acid (PLGA) based LAI microspheres of paliperidone palmitate (PP) were formulated by using FC-CCD. LAI microspheres were developed by using oil in water (O/W) emulsion solvent evaporation technique. On the basis of preliminary trials, FC-CCD was employed to check effect of independent variables such as drug polymer ratio (X1), homogenization speed (X2) and rate of addition (X3). While mean particle size (Y1), drug loading (Y2), entrapment efficiency (Y3), burst release (Y4), and drug release on day 60 (Y5) were considered as dependent variables and statistically evaluation performed by using design expert 12 software. Morphology of prepared microspheres was studied by using the scanning electron microscopy (SEM) technique, while particle size was analyzed by laser diffraction technique. In vitro drug release studies were performed using a controlled temperature shaking water bath apparatus. Fourier transforms infrared spectroscopy (FTIR) and differential scanning calorimetric (DSC) study were performed to analyze any changes in crystal behavior or to detect any chemical bonding between ingredients. 13C NMR and 1H NMR techniques were used to analyze end-capping and monomer ratio in developed microspheres. Results: The factorial batches mean particle size was found to be 38 µm to 104 µm and drug loading were found between 27.2 % to 47.2%. Mathematical modelling of drug release kinetics revealed that near zero-order drug release of checkpoint formulations. Endcap analysis and molar ratio of formulated microspheres were found to be ester end cap and ~75:25, respectively. Morphologically all the prepared samples were found to be spherical in shape and smooth surface. FTIR data showed no significant interactions occurred between drug and excipients. The actual responses of checkpoint formulations were observed within 5% variation of predicted values. Conclusion: The prepared microspheres showed promising results of morphology, particle size, drug loading, entrapment efficiency, burst release and drug release on day 60. The successful predictive designs models were achieved from employed FC-CCD.

scholarly journals Thermosensitive Drug Delivery System SBA-15-PEI for Controlled Release of Nonsteroidal Anti-Inflammatory Drug Diclofenac Sodium Salt: A Comparative Study

Materials ◽  
2021 ◽  
Vol 14 (8) ◽  
pp. 1880
Author(s):  
Lubos Zauska ◽  
Stefan Bova ◽  
Eva Benova ◽  
Jozef Bednarcik ◽  
Matej Balaz ◽  
...  
Keyword(s):  
Drug Release ◽  
Sodium Salt ◽  
Release Rate ◽  
Diclofenac Sodium ◽  
Simulated Gastric Fluid ◽  
Release Mechanism ◽  
Drug Release Rate ◽  
Inflammatory Drug ◽  
Vis Spectroscopy ◽  
Anti Inflammatory

Mesoporous SBA-15 silica material was prepared by the sol–gel method and functionalized with thermosensitive polyethylenimine polymers with different molecular weight (g·mol−1): 800 (SBA-15(C)-800), 1300 (SBA-15(C)-1300) and 2000 (SBA-15(C)-2000). The nonsteroidal anti-inflammatory drug (NSAID) diclofenac sodium was selected as a model drug and encapsulated into the pores of prepared supports. Materials were characterized by the combination of infrared spectroscopy (IR), atomic force microscopy (AFM), transmission electron microscopy (TEM), photon cross-correlation spectroscopy (PCCS), nitrogen adsorption/desorption analysis, thermogravimetry (TG), differential scanning calorimetry (DSC) and small-angle X-ray diffraction (SA-XRD) experiments. The drug release from prepared matrixes was realized in two model media differing in pH, namely small intestine environment/simulated body fluid (pH = 7.4) and simulated gastric fluid (pH = 2), and at different temperatures, namely normal body temperature (T = 37 °C) and inflammatory temperature (T = 42 °C). The process of drug loading into the pores of prepared materials from the diclofenac sodium salt solutions with different concentrations and subsequent quantitative determination of released drugs was analyzed by UV-VIS spectroscopy. Analysis of prepared SBA-15 materials modified with polyethylenimines in solution showed a high ability to store large amounts of the drug, up to 230 wt.%. Experimental results showed their high drug release into the solution at pH = 7.4 for both temperatures, which is related to the high solubility of diclofenac sodium in a slightly alkaline environment. At pH = 2, a difference in drug release rate was observed between both temperatures. Indeed, at a higher temperature, the release rates and the amount of released drug were 2–3 times higher than those observed at a lower temperature. Different kinetic models were used to fit the obtained drug release data to determine the drug release rate and its release mechanism. Moreover, the drug release properties of prepared compounds were compared to a commercially available medicament under the same experimental conditions.

Formulation Design and Optimization of Repaglinide Solid Dispersions by Central Composite Design

2018 ◽  
Vol 11 (6) ◽  
pp. 4337-4348
Author(s):  
Bhikshapathi D. V. R. N. ◽  
Srinivas I
Keyword(s):  
Central Composite Design ◽  
Dissolution Rate ◽  
Solid Dispersion ◽  
Solid Dispersions ◽  
Solvent Evaporation ◽  
Release Mechanism ◽  
Solvent Evaporation Method ◽  
Onset Of Action ◽  
Evaporation Method ◽  
Central Composite

Repaglinide is a pharmaceutical drug used for the treatment of type II diabetes mellitus, it is characterized with poor solubility which limits its absorption and dissolution rate and delays onset of action. In the present study, immediate release solid dispersion of repaglinide was formulated by solvent evaporation technique. Repaglinide solid dispersions were prepared using PEG 8000, Pluronic F 127 and Gelucire 44/14 by solvent evaporation method. A 3-factor, 3-level central composite design employed to study the effect of each independent variable on dependent variables. FTIR studies revealed that no drug excipient interaction takes place. From powder X-ray diffraction (p-XRD) and by scanning electron microscopy (SEM) studies it was evident that polymorphic form of repaglinide has been converted into an amorphous form from crystalline within the solid dispersion formulation. The correlation coefficient showed that the release profile followed Higuchi model anomalous behavior and hence release mechanism was indicative of diffusion. The obtained results suggested that developed solid dispersion by solvent evaporation method might be an efficacious approach for enhancing the solubility and dissolution rate of repaglinide.

scholarly journals Chitosan/Silver Nanoparticle/Graphene Oxide Nanocomposites with Multi-Drug Release, Antimicrobial, and Photothermal Conversion Functions

Materials ◽  
2021 ◽  
Vol 14 (9) ◽  
pp. 2351
Author(s):  
Zheng Su ◽  
Daye Sun ◽  
Li Zhang ◽  
Miaomiao He ◽  
Yulin Jiang ◽  
...  
Keyword(s):  
Silver Nanoparticles ◽  
Graphene Oxide ◽  
Drug Release ◽  
Release Rate ◽  
Composite System ◽  
Methyl Blue ◽  
Burst Release ◽  
Fluorescein Sodium ◽  
Photothermal Conversion ◽  
Dual Drug

In this work, we designed and fabricated a multifunctional nanocomposite system that consists of chitosan, raspberry-like silver nanoparticles, and graphene oxide. The room temperature atmospheric pressure microplasma (RT-APM) process provides a rapid, facile, and environmentally-friendly method for introducing silver nanoparticles into the composite system. Our composite can achieve a pH controlled single and/or dual drug release. Under pH 7.4 for methyl blue loaded on chitosan, the drug release profile features a burst release during the first 10 h, followed by a more stabilized release of 70–80% after 40–50 h. For fluorescein sodium loaded on graphene oxide, the drug release only reached 45% towards the end of 240 h. When the composite acted as a dual drug release system, the interaction of fluorescein sodium and methyl blue slowed down the methyl blue release rate. Under pH 4, both single and dual drug systems showed a much higher release rate. In addition, our composite system demonstrated strong antibacterial abilities against E. coli and S. aureus, as well as an excellent photothermal conversion effect under irradiation of near infrared lasers. The photothermal conversion efficiency can be controlled by the laser power. These unique functionalities of our nanocomposite point to its potential application in multiple areas, such as multimodal therapeutics in healthcare, water treatment, and anti-microbials, among others.

scholarly journals Development of Controlled-Release Carbamide Peroxide Loaded Nanoemulgel for Tooth Bleaching: In Vitro and Ex Vivo Studies

2021 ◽  
Vol 14 (2) ◽  
pp. 132
Author(s):  
Siriporn Okonogi ◽  
Adchareeya Kaewpinta ◽  
Sakornrat Khongkhunthian ◽  
Pisaisit Chaijareenont
Keyword(s):  
Drug Release ◽  
Solid Dispersion ◽  
Solid Dispersions ◽  
Tooth Bleaching ◽  
Polymer Mixture ◽  
Release Mechanism ◽  
Burst Release ◽  
Order Kinetic ◽  
Carbamide Peroxide ◽  
Periodontal Tissues

Burst release of carbamide peroxide (CP) from traditional hydrogels causes severe inflammation to periodontal tissues. The present study explores the development of a novel CP nanoemulgel (CP-NG), an oil-in-water nanoemulsion-based gel in which CP was loaded with a view to controlling CP release. CP solid dispersions were prepared, using white soft paraffin or polyvinylpyrrolidone-white soft paraffin mixture as a carrier, prior to formulating nanoemulsions. It was found that carrier type and the ratio of CP to carrier affected drug crystallinity. Nanoemulsions formulated from the optimized CP solid dispersions were used to prepare CP-NG. It was found that the ratio of drug to carrier in CP solid dispersions affected the particle size and zeta potential of the nanoemulsions as well as drug release behavior and tooth bleaching efficacy of CP-NG. Drug release from CP-NG followed a first-order kinetic reaction and the release mechanism was an anomalous transport. Drug release rate decreased with an increase in solid dispersion carriers. CP-NG obtained from the solid dispersion with a 1:1 ratio of CP to the polymer mixture is suitable for sustaining drug release with high tooth bleaching efficacy and without reduction of enamel microhardness. The developed CP-NG is a promising potential tooth bleaching formulation.

Microorganism-based monodisperse microcapsules: encapsulation of the fungicide tebuconazole and its controlled release properties

RSC Advances ◽  
2015 ◽  
Vol 5 (32) ◽  
pp. 25164-25170 ◽  
Author(s):  
Bo Zhang ◽  
Teng Zhang ◽  
Quanxi Wang ◽  
Tianrui Ren
Keyword(s):  
Controlled Release ◽  
Powdery Mildew ◽  
Drug Release ◽  
Release Rate ◽  
Drug Release Rate ◽  
Burst Effect ◽  
Initial Burst ◽  
Release System ◽  
Controlled Release System ◽  
Monodisperse Microcapsules

A controlled release system was prepared, it based on UF modified PCC cells in which TEB are loaded into cells. It can control the drug release rate, depress the initial “burst effect”, and was efficacious in controlling wheat powdery mildew.

Amoxicillin-loaded polyethylcyanoacrylate nanoparticles: Influence of PEG coating on the particle size, drug release rate and phagocytic uptake

Biomaterials ◽  
2001 ◽  
Vol 22 (21) ◽  
pp. 2857-2865 ◽  
Author(s):  
Giacomo Fontana ◽  
Mariano Licciardi ◽  
Silvana Mansueto ◽  
Domenico Schillaci ◽  
Gaetano Giammona
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Release Rate ◽  
Drug Release Rate ◽  
Peg Coating ◽  
Phagocytic Uptake
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