scholarly journals Formulation of Nano/Micro-Carriers Loaded with an Enriched Extract of Coffee Silverskin: Physicochemical Properties, In Vitro Release Mechanism and In Silico Molecular Modeling

Pharmaceutics ◽  
2022 ◽  
Vol 14 (1) ◽  
pp. 112
Author(s):  
Faezeh Fathi ◽  
Samad N. Ebrahimi ◽  
João A. V. Prior ◽  
Susana M. L. Machado ◽  
Reza Mohsenian Kouchaksaraee ◽  
...  
Keyword(s):  
Surface Charge ◽  
Chlorogenic Acid ◽  
In Vitro Release ◽  
Release Mechanism ◽  
Natural Polymers ◽  
Hydrogen Binding ◽  
Coffee Silverskin ◽  
Coating Layers ◽  
Vitro Release

Designing strategies for an effective transformation of food waste into high-value products is a priority to address environmental sustainability concerns. Coffee silverskin is the major by-product of the coffee roasting industry, being rich in compounds with health benefits. Such composition gives it the potential to be transformed into high-value products. In this study, coffee silverskin extracts were enriched, regarding caffeine and chlorogenic acid contents, by adsorbent column chromatography. The compounds content increased 3.08- and 2.75-fold, respectively, compared to the original extract. The enriched fractions were loaded into nano-phytosomes or cholesterol-incorporated nano-phytosomes (first coating layers) to improve the physiochemical properties and permeation rate. These nano-lipid carriers were also subjected to a secondary coating with different natural polymers to improve protection and stability against degradation. In parallel, and for comparison, different natural polymers were also used as first coating layers. The produced particles were evaluated regarding product yield, encapsulation efficiency, loading capacity, particle size, surface charge, and in vitro release simulating gastrointestinal conditions. All samples exhibited anionic surface charge. FTIR and molecular docking confirmed interactions between the phytoconstituents and lipid bilayers. The best docking score was observed for 5-caffeoylquinic acid (chlorogenic acid) exhibiting a stronger hydrogen binding to the lipid bilayer. Among several kinetic models tested, the particle release mechanism fitted well with the First-order, Korsmeyer–Peppas, and Higuchi models. Moreover, most of the formulated particles followed the diffusion-Fick law and anomalous transport.

Sodium alginate nanoparticles as a new transdermal vehicle of glucosamine sulfate for treatment of osteoarthritis

2017 ◽  
Vol 9 (3-4) ◽  
Author(s):  
Asmaa S. El-Houssiny ◽  
Azza A. Ward ◽  
Dina M. Mostafa ◽  
Salwa L. Abd-El-Messieh ◽  
Kamal N. Abdel-Nour ◽  
...  
Keyword(s):  
Side Effects ◽  
Surface Charge ◽  
Ex Vivo ◽  
In Vitro Release ◽  
Glucosamine Sulfate ◽  
Suspension Stability ◽  
Rat Skin ◽  
Release Studies ◽  
Vitro Release

AbstractGlucosamine sulfate (GS) has been used orally for the treatment of osteoarthritis (OA). However, it may be susceptible to the liver first pass phenomenon, which greatly affects its bioavailability, in addition to its side effects on the gastrointestinal tract. Alginate nanoparticles (Alg NPs) were investigated as a new drug carrier for transdermal delivery of GS to improve its effectiveness and reduce side effects. GS-Alg NPs were characterized by encapsulation efficiency, NP yield, particle size and surface charge properties. The in vitro release studies of GS and the ex vivo permeability through rat skin were determined using a UV-Vis spectrophotometer. GS-Alg NPs are within the nanometer range of size. High negative surface charge values are obtained and indicate the high suspension stability of the prepared formulation. The in vitro release studies showed that GS is released from Alg NPs in a sustained and prolonged manner. The ex vivo permeability of GS through rat skin is enhanced significantly after encapsulation in the negatively charged Alg NPs. We successfully reported a highly stable nanoparticlulate system using Alg NPs that permits the encapsulation of GS for topical administration, overcoming the disadvantages of oral administration.

scholarly journals FABRICATION OF NANO CLAY INTERCALATED POLYMERIC MICROBEADS FOR CONTROLLED RELEASE OF CURCUMIN

2021 ◽  
pp. 206-215
Author(s):  
DHARMENDER PALLERLA ◽  
SUMAN BANOTH ◽  
SUNKARI JYOTHI
Keyword(s):  
Drug Release ◽  
In Vitro Release ◽  
Controlled Drug Release ◽  
Fickian Diffusion ◽  
Simulated Gastric Fluid ◽  
Release Mechanism ◽  
Release Studies ◽  
Swelling Studies ◽  
Vitro Release

Objective: The objective of this study was to formulate and evaluate the Curcumin (CUR) encapsulated sodium alginate (SA)/badam gum (BG)/kaolin (KA) microbeads for controlled drug release studies. Methods: The fabricated microbeads were characterized by fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), thermogravimetric analysis (TGA), X-ray diffraction (X-RD), and scanning electron microscopy (SEM). Dynamic swelling studies and in vitro release kinetics were performed in simulated intestinal fluid (pH 7.4) and simulated gastric fluid (pH 1.2) at 37 °C. Results: FTIR confirms the formation of microbeads. DSC studies confirm the polymorphism of CUR in drug loaded microbeads which indicate the molecular level dispersion of the drug in the microbeads. SEM studies confirmed the microbeads are spherical in shape with wrinkled and rough surfaces. XRD studies reveal the molecular dispersion of CUR and the presence of KA in the developed microbeads. In vitro release studies and swelling studies depend on the pH of test media, which might be suitable for intestinal drug delivery. The % of drug release values fit into the Korsmeyer-Peppas equation and n values are obtained in the range of 0.577-0.664, which indicates that the developed microbeads follow the non-Fickian diffusion drug release mechanism. Conclusion: The results concluded that the CUR encapsulated microbeads are potentially good carriers for controlled drug release studies.

scholarly journals Release Kinetics Study of Azithromycin from Bi-layered Tablets

2017 ◽  
Vol 20 (1) ◽  
pp. 54-63
Author(s):  
FM Shah Noman Ul Bari ◽  
Muhammad Rashedul Islam ◽  
Md Mizanur Rahman Moghal ◽  
Israt Jahan Ira
Keyword(s):  
Release Kinetics ◽  
In Vitro Release ◽  
Methyl Cellulose ◽  
Pharmaceutical Journal ◽  
High Viscosity ◽  
Release Mechanism ◽  
Low Viscosity ◽  
Release Studies ◽  
Vitro Release

The objective of this study was to analysis in vitro release kinetics of Azithromycin from bi-layer tablets prepared by direct compression using high viscosity to low viscosity grades of hydroxypropyl methyl cellulose (HPMC K15M, HPMC K4M, HPMC 50 cps), Carbopol 934p and Carbopol 974p. In addition, it also includes evaluating the effect of formulation variables like polymer proportion and polymer viscosity on the release of Azithromycin. In vitro release studies were performed using USP Type-II (Rotating paddle method) at 100 rpm. The dissolution medium consisted of 0.1N HCl (900 ml) for the first 2 hr and the phosphate buffer (pH 6.0) from 3rd to 10th hour. From twenty five different formulations (F-1 to F-25) based on polymer variation, model-dependent and independent methods were used for data analysis and the best results were observed for HPMC 50cps in Korsmeyer- Peppas (R2=0.995 on F-23) kinetic model. The release mechanism of all formulations was Fickian.Bangladesh Pharmaceutical Journal 20(1): 54-63, 2017

scholarly journals Application of Asymmetrical Flow Field-Flow Fractionation for Characterizing the Size and Drug Release Kinetics of Theranostic Lipid Nanovesicles

2021 ◽  
Vol 22 (19) ◽  
pp. 10456
Author(s):  
Paulina Skupin-Mrugalska ◽  
Philipp A. Elvang ◽  
Martin Brandl
Keyword(s):  
Light Scattering ◽  
Flow Field ◽  
In Vitro Release ◽  
Fickian Diffusion ◽  
Release Mechanism ◽  
Field Flow Fractionation ◽  
Liposome Size ◽  
Flow Fractionation ◽  
Vitro Release

Liposome size and in vitro release of the active substance belong to critical quality attributes of liposomal carriers. Here, we apply asymmetric flow field-flow fractionation (AF4) to characterize theranostic liposomes prepared by thin lipid film hydration/extrusion or microfluidics. The vesicles’ size was derived from multi-angle laser light scattering following fractionation (AF4) and compared to sizes derived from dynamic light scattering measurements. Additionally, we adapted a previously developed AF4 method to study zinc phthalocyanine (ZnPc) release/transfer from theranostic liposomes. To this end, theranostic liposomes were incubated with large acceptor liposomes serving as a sink (mimicking biological sinks) and were subsequently separated by AF4. During incubation, ZnPc was transferred from donor to acceptor fraction until reaching equilibrium. The process followed first-order kinetics with half-lives between 119.5–277.3 min, depending on the formulation. The release mechanism was postulated to represent a combination of Fickian diffusion and liposome relaxation. The rate constant of the transfer was proportional to the liposome size and inversely proportional to the ZnPc/POPC molar ratio. Our results confirm the usefulness of AF4 based method to study in vitro release/transfer of lipophilic payload, which may be useful to estimate the unwanted loss of drug from the liposomal carrier in vivo.

scholarly journals Preparation and characterization of microcapsules of Pterodon pubescens Benth. by using natural polymers

2014 ◽  
Vol 50 (4) ◽  
pp. 919-930 ◽  
Author(s):  
Alexandre Espada Reinas ◽  
Jaqueline Hoscheid ◽  
Priscila Miyuki Outuki ◽  
Mara Lane Carvalho Cardoso
Keyword(s):  
Molecular Weight ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Chemical Degradation ◽  
Release Mechanism ◽  
Natural Polymers ◽  
Alcohol Extract ◽  
Polymeric Systems ◽  
Formulation Parameters

An oleaginous fraction obtained from an alcohol extract of the fruit of Pterodon pubescensBenth. (FHPp) was microencapsulated in polymeric systems. These systems were developed using a complex coacervation method and consisted of alginate/medium-molecular-weight chitosan (F1-MC), alginate/chitosan with greater than 75% deacetylation (F2-MC), and alginate/low-molecular-weight chitosan (F3-MC). These developed systems have the potential to both mask the taste of the extract, and to protect its constituents against possible chemical degradation. The influence of the formulation parameters and process were determined by chemical profiling and measurement of the microencapsulation efficiency of the oleaginous fraction, and by assessment of microcapsule morphology. The obtained formulations were slightly yellow, odorless, and had a pleasant taste. The average diameters of the microcapsules were 0.4679 µm (F2-MC), 0.5885 µm (F3-MC), and 0.9033 µm (F1-MC). The best formulation was F3-MC, with FHPp microencapsulation efficiency of 61.01 ± 2.00% and an in vitro release profile of 75.88 ± 0.45%; the content of vouacapans 3-4 was 99.49 ± 2.80%. The best model to describe the release kinetics for F1-MC and F3-MC was that proposed by Higuchi; however, F2-MC release displayed first-order kinetics; the release mechanism was of the supercase II type for all formulations.

scholarly journals Kinetic studies of the release profiles of antiepileptic drug released from a nanostructured TiO2 matrix.

2016 ◽  
Vol 12 (4) ◽  
pp. 4365-4373
Author(s):  
M. González Hurtado ◽  
J. Rieumont Briones ◽  
Laura. M. Castro González ◽  
E. Ortiz- Islas ◽  
Inti Zumeta- Dube
Keyword(s):  
Sol Gel ◽  
In Vitro Release ◽  
Kinetic Studies ◽  
The United States ◽  
Release Mechanism ◽  
Release Kinetic ◽  
Constant Diffusion ◽  
The Matrix ◽  
Vitro Release

In this paper is reported the “in vitro” release kinetic studies of antiepileptic drugs released from an inorganic, titanium oxide (TiO2) porous matrix. In order to determine the drug release mechanism, the experimental values were fitted to different mathematical models: zero-order, firs-order, Higuchi, Hixson-Crowel and Peppas. TiO2 was prepared by the sol-gel method adding valproic acid (VPA) or phenytoine (DHP) during the titanium n-butoxide hydrolysis step. The drug-TiO2 systems were observed by scanning electron microscopy. The “in vitro” release experiments were performed at laboratory scale following the United States Pharmacopeia (USP) standards. The obtained materials have a morphology of nanoparticle agglomerates. The particles have different sizes with some roughness and spherical shape. Peppas model suggests for both systems, that the release mechanism is controlled by two parallel processes. The first one is by diffusion of the drug through the matrix and the second is related to a gradient of constant diffusion by ingress of the solvent in the matrix.

scholarly journals Development and Evaluation of Salbutamol Sulphate Loaded Ethyl Cellulose Microcapsules using Emulsion Solvent Evaporation Technique

2015 ◽  
Vol 18 (2) ◽  
pp. 132-136 ◽  
Author(s):  
Md Shamsul Alam ◽  
Jakir Ahmed Chowdhury ◽  
Sams Mohammad Anowar Sadat ◽  
Md Selim Reza
Keyword(s):  
Ethyl Cellulose ◽  
In Vitro Release ◽  
Solvent Evaporation ◽  
Matrix Tablets ◽  
In Vitro Dissolution ◽  
Release Mechanism ◽  
Salbutamol Sulphate ◽  
Evaporation Technique ◽  
Vitro Release

Ethyl cellulose (EC) microcapsules containing Salbutamol sulphate (SS) were prepared through emulsion-solvent evaporation technique. Microcapsules were compressed and in-vitro release profiles were studied from both microcapsules and their compressed matrix tablets. Different amounts of drug were added in order to obtain various drugs to polymer ratios and it was found that the size of microcapsules reduced with the increase in core loading. In the preparation of formulations, Tween 80 was used as an emulsifying or dispersing agent and light liquid paraffin (LLP) was used as oil phase. The in-vitro release of EC microcapsules was studied in distilled water at 37º ± 0.5°C. A biphasic release behavior of SS from microcapsules was observed. In case of microcapsules, an immediate release was observed but for their compressed tablet form, initially a burst effect and then slow release were observed which was extended for 8 hours. In order to further investigate the type of drug release mechanism, the dissolution data were plotted according to the different kinetic models. In-vitro dissolution studies showed that zero-order and square-root of time (Higuchi model) release characteristics were exhibited.Bangladesh Pharmaceutical Journal 18(2): 132-136, 2015

scholarly journals PHYSICO-MECHANICAL AND RELEASE PROPERTIES OF SUSTAINED RELEASE ARTESUNATE TABLETS IN HYDROXYPROPYL METHYLCELLULOSE MATRIX

2018 ◽  
Vol 10 (1) ◽  
pp. 103 ◽  
Author(s):  
Musiliu Adedokun ◽  
Benjamin Onah ◽  
Anthony Attama
Keyword(s):  
Sustained Release ◽  
Hydroxypropyl Methylcellulose ◽  
In Vitro Release ◽  
Angle Of Repose ◽  
Simulated Gastric Fluid ◽  
Release Mechanism ◽  
Average Weight ◽  
Significant Difference ◽  
Vitro Release

Objective: This work was aimed at formulating artesunate tablets with hydroxypropyl methylcellulose (HPMC)-a hydrophilic polymer for the purpose of achieving a sustained release profile of the drug and evaluating their properties.Methods: The solubility profile of artesunate was determined in water, methanol, ethanol, ethanol/water mixtures (50/50, 40/60 v/v), simulated intestinal fluid (SIF) without enzymes (pH 7, 7.2 and 8), simulated gastric fluid (SGF) without enzymes (pH 1.2), 0.1N hydrochloric acid (HCI), 0.1N sodium hydroxide (NaOH), 0.1N acetic acid and phosphate buffer solution, PBS (pH 7, 7.2 and 8). Four batches of oral sustained release artesunate tablets intended for once-daily dosing were formulated with 10%, 20%, 25% and 30% w/w concentrations of HPMC using wet granulation method. Evaluation of granule properties was done by determining the angle of repose, flow rate, bulk density, tapped density, Carr’s index and Hausner’s quotient. The compressed tablets were also evaluated using official and non-official parameters. Absolute drug contents were determined in 0.1N NaOH, ethanol and methanol. In vitro release was studied in different media and release kinetics mechanism elucidated. In vivo studies were carried out using healthy Wistar rats.Results: Artesunate was observed to exhibit solubility at varying degrees depending on solvents or media employed as well as the pH of the media. All the granule batches have Hausner’s quotient value of approximately 1.2. The values for Carr’s index for all the batches ranged between 30 and 40. The angle of repose, Carr’s index and Hausner’s quotient values indicate good flow properties of the granules for all the batches. All the tablet batches conformed to official standard in terms of weight uniformity as no single tablet deviated beyond 5% from the average weight in each batch with no significant difference in the values (p>0.05). Values of hardness increased insignificantly from batches A to D (p>0.05). Friability values were very low and follows no specific pattern among the batches but the difference in the values was significant (p<0.05). Absolute drug content reduced while in vitro release times increased as hardness increased, indicating the probable progressive reduction in the tendency of the matrix to release the drug as the concentration of HPMC increased from batches A to D. n values obtained from analysis of release mechanism were above 0.89 for each batch.Conclusion: The release mechanism was shown to be complex and the release involved zero order, first order, and Higuchi model kinetics. The biological half-life of artesunate was shown to be 1.05 hr, and metabolites which bear resemblance to artesunate in absorbance seem to be encountered. In this work, HPMC matrix yielded high-quality tablets indicating its usefulness in sustained released product development.

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