scholarly journals Effect of Temperature on Drug Release: Production of 5-FU-Encapsulated Hydroxyapatite-Gelatin Polymer Composites via Spray Drying and Analysis of In Vitro Kinetics

2020 ◽  
Vol 2020 ◽  
pp. 1-13
Author(s):  
Nalan Erdöl Aydin
Keyword(s):  
Drug Release ◽  
Polymer Composites ◽  
Drug Loading ◽  
Effect Of Temperature ◽  
Release Mechanism ◽  
Gravimetric Analysis ◽  
X Ray Diffraction ◽  
In Vitro Kinetics ◽  
Best Fit

In this study, 5-fluorouracil- (5-FU-) loaded hydroxyapatite-gelatin (HAp-GEL) polymer composites were produced in the presence of a simulated body fluid (SBF) to investigate the effects of temperature and cross-linking agents on drug release. The composites were produced by wet precipitation at pH 7.4 and temperature 37°C using glutaraldehyde (GA) as the cross-linker. The effects of different amounts of glutaraldehyde on drug release profiles were studied. Encapsulation (drug loading) was performed with 5-FU using a spray drier, and the drug release of 5-FU from the HAp-GEL composites was determined at temperatures of 32°C, 37°C, and 42°C. Different mathematical models were used to obtain the release mechanism of the drug. The morphologies and structures of the composites were analyzed by X-ray diffraction, thermal gravimetric analysis, Fourier transform infrared spectroscopy, and scanning electron microscopy. The results demonstrated that for the HAp-GEL composites, the initial burst decreased with increasing GA content at all three studied temperatures. Further, three kinetic models were investigated, and it was determined that all the composites best fit the Higuchi model. It was concluded that the drug-loaded HAp-GEL composites have the potential to be used in drug delivery applications.

scholarly journals Development and In-Vitro Evaluation of pH Responsive Polymeric Nano Hydrogel Carrier System for Gastro-Protective Delivery of Naproxen Sodium

2019 ◽  
Vol 2019 ◽  
pp. 1-13
Author(s):  
Rai Muhammad Sarfraz ◽  
Muhammad Rouf Akram ◽  
Muhammad Rizwan Ali ◽  
Asif Mahmood ◽  
Muhammad Usman Khan ◽  
...  
Keyword(s):  
Drug Release ◽  
Naproxen Sodium ◽  
Research Work ◽  
Entrapment Efficiency ◽  
Gravimetric Analysis ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
Swelling Behaviour ◽  
X Ray

Current research work was carried out for gastro-protective delivery of naproxen sodium. Polyethylene glycol-g-poly (methacrylic acid) nanogels was developed through free radical polymerization technique. Formulation was characterized for swelling behaviour, entrapment efficiency, Fourier transform infrared (FTIR) spectroscopy, Differential scanning calorimetry (DSC), and Thermal Gravimetric Analysis (TGA), Powder X-ray diffraction (PXRD), Zeta size distribution, and Zeta potential measurements, and in-vitro drug release. pH dependent swelling was observed with maximum drug release at higher pH. PXRD studies confirmed the conversion of loaded drug from crystalline to amorphous form while Zeta size measurement showed size reduction. On the basis of these results it was concluded that prepared nanogels proved an effective tool for gastro-protective delivery of naproxen sodium.

scholarly journals Synthesis and Characterization of Lyophilized Chitosan-Based Hydrogels Cross-Linked with Benzaldehyde for Controlled Drug Release

2020 ◽  
Vol 2020 ◽  
pp. 1-10 ◽  
Author(s):  
Fouad Damiri ◽  
Yahya Bachra ◽  
Chaimaa Bounacir ◽  
Asmae Laaraibi ◽  
Mohammed Berrada
Keyword(s):  
Ascorbic Acid ◽  
Drug Release ◽  
Drug Loading ◽  
In Vitro Release ◽  
Controlled Drug Release ◽  
Tween 20 ◽  
Release Mechanism ◽  
Synthetic Process ◽  
Chitosan Salt

In this study, chitosan-based hydrogels were produced by incorporating three drugs with a different solubility into a polymer matrix. The lyophilized chitosan salt was prepared using an innovative and less-expensive synthetic process by the freeze-drying technique. Firstly, the three drugs (caffeine, ascorbic acid, and 5-fluorouracil (5-FU)) were selected as model drugs to test the in vitro release behavior of the hydrogel. The drugs were solubilized in chitosan salt, lyophilized, and cross-linked with benzaldehyde involving the formation of a Schiff base with (–C=N-) linkage to produce a physical hydrogel. Subsequently, the physicochemical properties of N-benzyl chitosan and lyophilized chitosan salt were evaluated by Fourier-transform infrared (FTIR) spectra, scanning electron microscopy (SEM), and thermogravimetric analysis (TGA). The intrinsic viscosity of the conventional chitosan was determined by the Mark–Houwink–Sakurada equation. Moreover, the kinetics of hydrogel swelling and drug release were studied by the UV-visible method at physiological conditions (pH = 7.4 at 37°C). The results show that lyophilized N-benzyl chitosan had a maximum swelling ratio of 720 ± 2% by immersion in phosphate-buffered saline solutions (PBS) (pH = 7.4 at 37°C). In vitro drug releases were evaluated in PBS, and the obtained results show that the maximum drug release after 24 h was 42% for caffeine, 99% for 5-FU, and 94% for ascorbic acid. Then, to optimize the cumulative release of caffeine, Tween 20 was added and 98% as a release percentage was obtained. The drug-loading results were investigated with the Korsmeyer–Peppas kinetic model and applied to determine the drug release mechanism.

scholarly journals IN VITRO ENTRAPMENT AND RELEASE STUDIES OF LEVOFLOXACIN USING EPICHLOROHYDRIN-CROSSLINKED HYDROGEL

2019 ◽  
pp. 138-144
Author(s):  
ANGELI ANN S RESCOBER
Keyword(s):  
New Zealand ◽  
Drug Release ◽  
Release Rate ◽  
Drug Loading ◽  
Ophthalmic Solution ◽  
Antimicrobial Activities ◽  
Release Mechanism ◽  
Scanning Calorimetry ◽  
Polymer Ratio

Objective: This study aimed to optimize and evaluate the controlled release rate, ocular irritancy, and in vitro antimicrobial properties of levofloxacinentrapped in the epichlorohydrin-crosslinked hydrogel of sodium carboxymethyl cellulose (NaCMC) and gelatin.Materials and Methods: Various parameters such as polymer ratio, amount of crosslinker, temperature, reaction time, swelling capacity, and percentdrug loading were considered in Optimized levofloxacin hydrogel. Hydrogel preparations with higher amount of drug loaded were further analyzedto determine its in vitro drug release rate, ocular irritancy on New Zealand rabbits, and antimicrobial activities against Pseudomonas aeruginosaand Staphylococcus aureus. Optimized levofloxacin hydrogel (OLH) was then subjected to 3-month stability testing at 40 ± 2°C and 75 ± 5% relativehumidity in which samples were withdrawn at the end of each month for analysis.Results: Polymer groups with higher concentrations of NaCMC have higher swelling and drug loading capacities than those with higher gelatinconcentrations. Meanwhile, qualitative analysis using differential scanning calorimetry, Fourier-transform infrared spectroscopy, and scanningelectron microscopy verified the presence of levofloxacin in the epichlorohydrin-cross-linked hydrogel. Among the four polymer ratio, F3 was theoptimized hydrogel with drug-loaded concentration of 99.50%, which was within the acceptable assay limit of 0.5% levofloxacin solution based onUnited States Pharmacopeia monograph. It followed the Higuchi kinetic model with a drug release mechanism of super case 2 transport indicatinghydrogel swelling as a key factor for its controlled drug release. In vitro, antibacterial test against P. aeruginosa and S. aureus was sensitive to optimizedlevofloxacin hydrogel (OLH) with inhibitory diameter zones of 31.68 and 37.05 mm, respectively. Ocular irritancy test also showed that the OLH isnon-irritating on installation in the cul-de-sac of New Zealand rabbits.Conclusion: Optimized levofloxacin hydrogel was effective, non-irritating, and stable, which can be used as an alternative to conventional 0.5%levofloxacin ophthalmic solution.

scholarly journals Porous nanoparticles of metoprolol tartrate produced by spray-drying: development, characterization and in vitro evaluation

2012 ◽  
Vol 62 (3) ◽  
pp. 383-394 ◽  
Author(s):  
Mohammed S. Khan ◽  
Gowda D. Vishakante ◽  
H. G. Shivakumar
Keyword(s):  
Drug Release ◽  
Spray Drying ◽  
Release Kinetics ◽  
Drug Loading ◽  
Release Mechanism ◽  
Metoprolol Tartrate ◽  
Pore Former ◽  
Porous Nanoparticles ◽  
Zero Order Release

The present investigation was undertaken to fabricate porous nanoparticles of metoprolol tartrate by spray-drying using ammonium carbonate as pore former. Prepared nanoparticles were coated with Eudragit S100 polymer in order to prevent the release of metoprolol tartrate in the upper GI tract. It was shown that nanoparticles with low size ranges can be obtained with a low feed inlet rate. Micromeritic studies confirmed that nanoparticle batches are discrete and free flowing. Effects of the pore former on drug loading, porosity and in vitro release were studied. It was found that there was an increase in drug loading and porosity with increasing the amount of pore former. In vitro drug release studies showed that an increase in pore former made drug release faster. Release kinetics proved that nanoparticles follow a zero-order release mechanism.

scholarly journals Cytocompatibility and Dielectric Properties of Sr2+ Substituted Nano-Hydroxyapatite for Triggered Drug Release

2019 ◽  
Vol 1 (1) ◽  
pp. 18-24
Author(s):  
Lakshmanaperumal Sundarabharathi ◽  
Mahendran Chinnaswamy ◽  
Hemalatha Parangusan ◽  
Deepalekshmi Ponnamma ◽  
Mariam Al Ali Al-Maadeed
Keyword(s):  
Dielectric Properties ◽  
Drug Release ◽  
Drug Loading ◽  
Sol Gel ◽  
X Ray Diffraction ◽  
Sustained Drug Release ◽  
Model Drug ◽  
Dielectrical Properties ◽  
Living Tissues

Hydroxyapatite (Ca5(PO4)3OH) is a well-known bioceramics material used in medical applications because of its ability to form direct chemical bonds with living tissues. In this context, we investigate the biocompatibility and dielectric properties of Sr2+-substituted hydroxyapatite nanoparticles were synthesized by sol-gel method. The influence of strontium on the crystal structure, functional group, morphological, electrical properties, and biocompatibility of as-synthesized nano-hydroxyapatite samples was analyzed using X-ray diffraction (XRD), Fourier transform infrared (FTIR) spectroscopy and field emission scanning electron microscopy (FE-SEM). Dielectrical properties of the bioactive Sr-HA sample were investigated by a dielectric impedance spectroscopy method. The observed results illustrate the incorporation of Sr2+ ions in the apatite lattice could influence the pure HA properties, by reducing the crystallite size and crystallinity quite consistent with the morphology variation. The ac conductivity (σac) increased with an increasing applied frequency confirmed that prepared HA sample exhibited the universal power law nature. Further, the in vitro drug loading and release studies using doxycycline as a model drug demonstrate that the Sr2+ -HA nanoparticles show high drug adsorption capacity and sustained drug release. Thus, the improved bioceramics system could be a promising candidate for future biomedical applications.

scholarly journals Formulation and In vitro Evaluation of Eudragit RL 100 Loaded Fexofenadine HCl Microspheres

2016 ◽  
Vol 19 (1) ◽  
pp. 58-67
Author(s):  
Paroma Arefin ◽  
Ikramul Hasan ◽  
Md Shfiqul Islam ◽  
Md Selim Reza
Keyword(s):  
Drug Release ◽  
Release Rate ◽  
Encapsulation Efficiency ◽  
Release Kinetics ◽  
Drug Loading ◽  
Release Mechanism ◽  
Order Release ◽  
Eudragit Rl ◽  
Fexofenadine Hcl

The present study deals with the formulation and evaluation of Fexofenadine hydrochloride (HCl) loaded sustained release microspheres by emulsion solvent evaporation method with Eudragit RL 100. The effects of percent drug loading on drug encapsulation efficiency, drug content and drug release rate were assessed. In vitro dissolution study was performed spectrophotometrically according to USP paddle method using phosphate buffer (pH 6.8) for 10 hours. The release rate of Fexofenadine HCl from the microspheres was significantly increased with the increase of drug loading. The drug release patterns were simulated in different kinetic orders such as zero order release kinetics, first order release kinetics, Higuchi release kinetics, Korsmeyer-Peppas release kinetics and Hixson-Crowell release kinetics to assess the release mechanism and Higuchi release kinetics was found to be the predominant release mechanism. Morphological changes due to different drug loading were assessed by scanning electron microscopic (SEM) technique. Differential scanning calorimetry and fourier transform infra-red (FT-IR) spectroscopy was performed to evaluate compatibility of drug with the polymer. A statistically significant variation indrug encapsulation efficiency and release rate was observed for variation in drug loading.Bangladesh Pharmaceutical Journal 19(1): 58-67, 2016

scholarly journals DEVELOPMENT AND EVALUATION OF SUSTAIN RELEASE MICROPARTICLES OF METOPROPROPROLOL SUCCINATE

2019 ◽  
pp. 166-172
Author(s):  
Suma Oommen Sen ◽  
PRITESH DEVBHUTI ◽  
KALYAN KUMAR SEN ◽  
AMITAVA GHOSH
Keyword(s):  
Drug Release ◽  
Xanthan Gum ◽  
Drug Loading ◽  
Crosslinking Agent ◽  
Periodate Oxidation ◽  
Release Mechanism ◽  
Equilibrium Studies ◽  
In Vitro Drug Release ◽  
Metoprolol Succinate

Objective: In this study, xanthan gum was oxidized by sodium periodate to form xanthan dialdehyde. This oxidized gum was used as crosslinking agent as an alternative to somewhat toxic glutaraldehyde, the basis of which is the reaction between the Schiff reagent and the aldehydes formed by periodate oxidation. Methods: Formation of aldehyde groups were confirmed by Fourier Transform Infrared Spectroscopy (FTIR). Microparticles of metoprolol succinate were fabricated using crosslinking of a chitosan/gelatin mix system by dialdehyde Xanthan gum. The properties of the developed microparticles were investigated with swelling equilibrium studies, differential scanning calorimeter (DSC), in vitro drug release studies and scanning electron microscopy (SEM). Results: The in vitro drug release from these microparticles was affected by total polymer amount, oxidation reaction time and chitosan to gelatin ratio. The cumulative percent release of metoprolol succinate was observed within the range of 46 to 95% at 8 h from different formulations studied. The factors identified as significant to produce any impact on drug loading as well as drug release were both the polymer and inter actions of polymer and Xanthan gum dialdehyde. Conclusion: The release mechanism followed the super case II model kinetics.

In vitro drug release mechanism and drug loading studies of cubic phase gels

2005 ◽  
Vol 293 (1-2) ◽  
pp. 241-250 ◽  
Author(s):  
Marilisa G. Lara ◽  
M. Vitória L.B. Bentley ◽  
John H. Collett
Keyword(s):  
Drug Release ◽  
Drug Loading ◽  
Release Mechanism ◽  
Cubic Phase ◽  
In Vitro Drug Release ◽  
Drug Release Mechanism

scholarly journals THE ROLE OF NEEDLE IN FORMULATION OF pH SENSITIVE SWELLABLE MICROBEADS PREPARED WITH HYDROPHILIC POLYMERS FOR ATORVASTATIN AND THEIR CHARACTERIZATION STUDIES

2017 ◽  
Vol 9 (3) ◽  
pp. 20
Author(s):  
K.v. Ramana Reddy ◽  
M. V. Nagabhushanam
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Drug Loading ◽  
In Vitro Release ◽  
Process Variable ◽  
Ph Sensitive ◽  
Hydrophilic Polymers ◽  
Release Mechanism ◽  
Curing Agents

Objective: The aim of the study was to develop and characterize mucoadhesive microbeads for oral sustained release of atorvastatin by using hydrophilic polymers and application of different process variables in designing of pH sensitive swellable microbeads.Methods: Microbeads were prepared by ionic gelation method. The compatibility studies of atorvastatin with polymers were investigated by differential scanning calorimeter and fourier transform infrared spectroscopy studies. In this work process variable like optimization of curing agents and their quantity, effect of rpm, and their influence in drug entrapment were studied. Prepared beads were characterized for particle size, swelling index, erosion studies and drug release studies.Results: Mixture of alginate and carbopol 934 P at 3.3 % w/v shows sustained release and good mucoadhesive capacity. Furthermore, drug loading and swelling increased with the use of a combination of polymers. On basis of in vitro release studies and swelling studies, it was observed that sodium alginate coated with carbopol 934 P showed sustained release of 84.5 % at end of 10 h in 6.8 phosphate buffer. The optimised batch followed peppas and higuchi release mechanism and releasing the drug by non-fickian transport.Conclusion: The alginate beads with a combination of carbopol 934P showed a sustain release pattern. The release rate and swelling of atorvastatin beads could be adjusted by adding other hydrophilic polymers or by optimising curing agents, curing time and their volume. The zero order of drug release was confirmed for all the batches. The in vitro data was better fit to Higuchi’s diffusion model and diffusion rate limited.

scholarly journals A Statistical Study on the Development of Metronidazole-alginate-chitosan Nanocomposite Formulations using Full Factorial Designs

2020 ◽  
Author(s):  
Hazem Sabbagh ◽  
Samer Hussein Al Ali ◽  
Mohd Zobir Hussein ◽  
Zead Abudayeh ◽  
Rami Ayoub ◽  
...  
Keyword(s):  
Statistical Study ◽  
Drug Loading ◽  
Gravimetric Analysis ◽  
X Ray Diffraction ◽  
In Vitro Drug Release ◽  
X Ray ◽  
Release Studies ◽  
Statistical Equation ◽  
Full Factorial

The purpose of this study was to investigate the effect of chitosan (CS) and Alginate (Alg) polymers concentrations and CaCl2 concentration on metronidazole (MET) drug loading (LE), size particles and zeta potential. Nanocomposites were prepared by ionotropic pregelation method. A (21 *31 *21) *3= 36 full factorial design (FFD) was used to predict statistical equation and responses. The MET-CS-AlgNPs nanocomposites were characterized by X-ray diffraction, Fourier-transform infrared spectroscopy, thermal gravimetric analysis, scanning electron microscope and in vitro drug release studies. All data indicated the presence of drug into MET-CS-AlgNPs nanocomposites. The release profile of MET-CS-AlgNPs nanocomposites was found to be sustained

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