Influence of Sodium Alginate Concentration on Microcapsules Properties Foreseeing the Protection and Controlled Release of Bioactive Substances

To understand the abilities of Ca-alginate microcapsules and their specific applications in different fields, it is necessary to determine the physicochemical and structural properties of those formulated microcapsules. In this work, we aimed to study the effect of alginate concentration in the improvement of the encapsulation efficiency (EE) and on the release of phenolic and flavonoid substances. The relationship between the structure of the encapsulated bioactive substance and Ca-alginate network and their effect on the EE and release kinetics have been investigated. The incorporation, structure, morphology, and phase properties of all elaborated materials were characterized by UV-spectroscopy, Fourier transform infrared (ATR-FTIR), scanning electron microscope (SEM), and X-ray diffraction (DRX). The results indicate that increasing the polymer concentration increases the EE and decreases the loading capacity (LC), whereas the effect of alginate polymer concentration on the release was not observed. The release study of bioactive substances showed that the release kinetics is relatively dependent on the structure and the physicochemical characteristics of the bioactive substance, which became clear when the encapsulated compounds were released from the core of calcium alginate microcapsules. Thus, it could be concluded that the pores size of the Ca-alginate network is smaller than the volume of the crocin molecule (2794.926 Å3) and higher than the volume of the gallic acid molecule (527.659 Å3). For the same microcapsules system, the release mechanism is affected by the structure and physicochemical properties of the encapsulated molecules.

Download Full-text

Development and evaluation of sustained release losartan potassium matrix tablet using kollidon SR as release retardant

Brazilian Journal of Pharmaceutical Sciences ◽

10.1590/s1984-82502012000400005 ◽

2012 ◽

Vol 48 (4) ◽

pp. 621-628 ◽

Cited By ~ 2

Author(s):

Shahid Sarwar ◽

Mohammad Salim Hossain

Keyword(s):

Drug Release ◽

Sustained Release ◽

Release Kinetics ◽

Polymer Concentration ◽

In Vitro Release ◽

Matrix Tablets ◽

Losartan Potassium ◽

Dissolution Time ◽

Release Mechanism ◽

Matrix Tablet

The present study was undertaken to develop sustained release (SR) matrix tablets of losartan potassium, an angiotensin-II antagonist for the treatment of hypertension. The tablets were prepared by direct compression method, along with Kollidon SR as release retardant polymer. The amount of losartan potassium remains fixed (100 mg) for all the three formulations whereas the amounts of Kollidon SR were 250 mg, 225 mg, and 200 mg for F-1, F-2, and F-3 respectively. The evaluation involves three stages: the micromeritic properties evaluation of granules, physical property studies of tablets, and in-vitro release kinetics studies. The USP apparatus type II was selected to perform the dissolution test, and the dissolution medium was 900 mL phosphate buffer pH 6.8. The test was carried out at 75 rpm, and the temperature was maintained at 37 ºC ± 0.5 ºC. The release kinetics was analyzed using several kinetics models. Higher polymeric content in the matrix decreased the release rate of drug. At lower polymeric level, the rate and extent of drug release were enhanced. All the formulations followed Higuchi release kinetics where the Regression co-efficient (R²) values are 0.958, 0.944, and 0.920 for F-1, F-2, and F-3 respectively, and they exhibited diffusion dominated drug release. Statistically significant (P<0.05) differences were found among the drug release profile from different level of polymeric matrices. The release mechanism changed from non-fickian (n=0.489 for F-1) to fickian (n=0.439 and 0.429 for F-2, and F-3 respectively) as a function of decreasing the polymer concentration. The Mean Dissolution Time (MDT) values were increased with the increase in polymer concentration.

Download Full-text

In Vitro Dissolution of Aceclofenac Loaded Hydrophilic Polymer Based Matrix Tablets and its Release Mechanism

Bangladesh Journal of Scientific and Industrial Research ◽

10.3329/bjsir.v45i2.5712 ◽

1970 ◽

Vol 45 (2) ◽

pp. 141-150

Author(s):

M Mesbah Uddin Talukder ◽

Nadia Ahmed ◽

Tasnuva Haque ◽

Sadia Afreen Chowdhury

Keyword(s):

Release Rate ◽

Phosphate Buffer ◽

Release Kinetics ◽

Polymer Concentration ◽

Hydroxypropyl Methylcellulose ◽

Matrix Tablets ◽

Hydrophilic Polymers ◽

Release Mechanism ◽

Physical Parameters ◽

Erosion Index

Hydrophilic polymers are widely used to prepare sustained release matrix tablets. These polymers showed their sustained action by forming a barrier of thick gel layer around the matrix. Here swelling of the polymer and erosion of matrix plays a major role to control the release of the drug. In this present study the swelling and erosion properties of some hydrophilic polymers were correlated to their sustaining and rate controlling behavior. Matrix tablets containing hydroxypropyl methylcellulose (HPMC K100cps), carboxymethyl cellulose (CMC 50,000 cps) and methocel K15M CR polymers were prepared. The powder mixture was evaluated for their flow properties and the prepared tablets for their physical parameters. Swelling and erosion index of the tablets were carried out in pH 6.8 phosphate buffer and dissolution in 0.1N HCl (2 hours) followed by pH 6.8 phosphate buffer (8 hours) using USP apparatus II (paddle method) at 50 r.p.m. HPMC K100 cps was found to be not as rate retarding as the other two. From the all results it was observed that F-6 (containing 43.243% methocel K15M CR) showed highest swelling and erosion index (740.589% and 12.017% respectively), slowest release rate (24.491% at 8 hours) and highest MDT value (55.401 hours). Finally it can be concluded that increasing the polymer concentration or polymer's viscosity grade, swelling and erosion index increases, release rate decreases and MDT value increases. Key words: Aceclofenac; Matrix tablets; HPMC; CMC; Physical parameters; Release kinetics. DOI: 10.3329/bjsir.v45i2.5712Bangladesh J. Sci. Ind. Res. 45(2), 141-150, 2010

Download Full-text

The Layered Encapsulation of Vitamin B2 and β-Carotene in Multilayer Alginate/Chitosan Gel Microspheres: Improving the Bioaccessibility of Vitamin B2 and β-Carotene

Foods ◽

10.3390/foods11010020 ◽

2021 ◽

Vol 11 (1) ◽

pp. 20

Author(s):

Peilong Liao ◽

Shicheng Dai ◽

Ziteng Lian ◽

Xiaohong Tong ◽

Sai Yang ◽

...

Keyword(s):

Multilayered Structure ◽

Vitamin B2 ◽

X Ray Diffraction ◽

Bioactive Substances ◽

Excellent Thermal Stability ◽

Ph Response ◽

Alginate Concentration ◽

The Stability ◽

Β Carotene ◽

Simultaneous Delivery

This research underlines the potential of alginate multilayered gel microspheres for the layered encapsulation and the simultaneous delivery of vitamin B2 (VB) and β-carotene (BC). Chitosan was used to improve the stability and controlled release ability of alginate-based gel microspheres. It was shown that a clear multilayered structure possessed the characteristics of pH response, and excellent thermal stability. The sodium alginate concentration and the number of layers had notable effects on mechanical properties and particle size of gel microspheres. Fourier-transform infrared spectroscopy and X-ray diffraction analyses further proved that VB and BC were encapsulated within the gel microspheres. Compared with the three-layer VB-loaded gel microspheres, the total release of VB from the three-layer VB and BC-loaded gel decreased from 93.23 to 85.58%. The total release of BC from the three-layer VB and BC-loaded gel increased from 66.11 to 69.24% compared with three-layer BC-loaded gel. The simultaneous encapsulation of VB and BC in multilayered gel microspheres can markedly improve their bioaccessibility and bioavailability. These results showed the multilayer gel microspheres synthesized herein have potential for applications in the layered encapsulation and simultaneous delivery of various bioactive substances to the intestinal tract.

Download Full-text

Optimization, Characterization and Pharmacokinetic Study of Meso-Tetraphenylporphyrin Metal Complex-Loaded PLGA Nanoparticles

International Journal of Molecular Sciences ◽

10.3390/ijms222212261 ◽

2021 ◽

Vol 22 (22) ◽

pp. 12261

Author(s):

Mariia R. Mollaeva ◽

Nikita Yabbarov ◽

Maria Sokol ◽

Margarita Chirkina ◽

Murad D. Mollaev ◽

...

Keyword(s):

Spherical Shape ◽

Physicochemical Characteristics ◽

Plga Nanoparticles ◽

Release Mechanism ◽

X Ray Diffraction ◽

Technological Parameters ◽

Hemolysis Assay ◽

Optimized Model ◽

Nanoparticle Formulation

The selection of technological parameters for nanoparticle formulation represents a complicated development phase. Therefore, the statistical analysis based on Box–Behnken methodology is widely used to optimize technological processes, including poly(lactic-co-glycolic acid) nanoparticle formulation. In this study, we applied a two-level three-factor design to optimize the preparation of nanoparticles loaded with cobalt (CoTPP), manganese (MnClTPP), and nickel (NiTPP) metalloporphyrins (MeP). The resulting nanoparticles were examined by dynamic light scattering, X-ray diffraction, Fourier transform infrared spectroscopy, MTT test, and hemolytic activity assay. The optimized model of nanoparticle formulation was validated, and the obtained nanoparticles possessed a spherical shape and physicochemical characteristics enabling them to deliver MeP in cancer cells. In vitro hemolysis assay revealed high safety of the formulated MeP-loaded nanoparticles. The MeP release demonstrated a biphasic profile and release mechanism via Fick diffusion, according to release exponent values. Formulated MeP-loaded nanoparticles revealed significant antitumor activity and ability to generate reactive oxygen species. MnClTPP- and CoTPP-nanoparticles specifically accumulated in tissues, preventing wide tissue distribution caused by long-term circulation of the hydrophobic drug. Our results suggest that MnClTPP- and CoTPP-nanoparticles represent the greatest potential for utilization in in anticancer therapy due to their effectiveness and safety.

Download Full-text

Release kinetics of lime essential oil (Citrus aurantifolia) from beads microencapsulated through ion-gel method

The Journal of Agriculture and Development ◽

10.52997/jad.8.01.2021 ◽

2021 ◽

Vol 20 (1) ◽

pp. 58-66

Author(s):

Vinh Truong

Keyword(s):

Essential Oil ◽

Release Rate ◽

Release Kinetics ◽

Chitosan Beads ◽

Gel Method ◽

Citrus Aurantifolia ◽

Alginate Concentration ◽

Significant Difference ◽

Ion Gel ◽

Ca Alginate

Ca-Alginate beads for microencapsulation of lime oil (Citrus aurantifolia) by ion-gel method was manufactured and then soaked in Chitosan solution to obtain Ca-Alginate-Chitosan beads. Increased CaCl2 concentrations reduced lime essential oil release. The alginate concentration (2 to 3%) and water temperature significantly affected the release of oil (P < 0.05). The higher temperatures, the higher the release rate. The oil release at 75oC was twice as much as at 45oC. At 45oC, the difference in the release rate among the alginate concentrations of 2%, 2.5% and 3% was clear and statistically significant (P < 0.05). However, at 60oC and 75oC, there was no significant difference in release between the alginate concentration of 2.5% and 3% (P > 0.05). In the storage of beads in 1% CaCl2 solution at normal temperature, after the first 15 days, Ca Alginate-Chitosan system released about 3% slower than Ca-Alginate system, but there was no difference between the two systems after 45 days. This shows that if prolonged for a long time, the ion-gelation of Ca-Alginate prevails over the Alginate-Chitosan cross-link.

Download Full-text

Novel Hydrogels of Chitosan and Poly (vinyl alcohol) Reinforced with Inorganic Particles of Bioactive Glass

Polymers ◽

10.3390/polym13050691 ◽

2021 ◽

Vol 13 (5) ◽

pp. 691

Author(s):

O. Sánchez-Aguinagalde ◽

Ainhoa Lejardi ◽

Emilio Meaurio ◽

Rebeca Hernández ◽

Carmen Mijangos ◽

...

Keyword(s):

Mechanical Properties ◽

Drug Release ◽

Bioactive Glass ◽

Vinyl Alcohol ◽

Release Kinetics ◽

The Body ◽

Poly Vinyl Alcohol ◽

X Ray Diffraction ◽

Inorganic Particles ◽

Release Studies

Chitosan (CS) and poly (vinyl alcohol) (PVA) hydrogels, a polymeric system that shows a broad potential in biomedical applications, were developed. Despite the advantages they present, their mechanical properties are insufficient to support the loads that appear on the body. Thus, it was proposed to reinforce these gels with inorganic glass particles (BG) in order to improve mechanical properties and bioactivity and to see how this reinforcement affects levofloxacin drug release kinetics. Scanning electron microscopy (SEM), X-ray diffraction (XRD), swelling tests, rheology and drug release studies characterized the resulting hydrogels. The experimental results verified the bioactivity of these gels, showed an improvement of the mechanical properties and proved that the added bioactive glass does affect the release kinetics.

Download Full-text

Clinoptilolite Microparticles as Carriers of Catechin-Rich Acacia Catechu Extracts: Microencapsulation and In Vitro Release Study

Molecules ◽

10.3390/molecules26061655 ◽

2021 ◽

Vol 26 (6) ◽

pp. 1655

Author(s):

Zvezdelina Yaneva ◽

Donika Ivanova ◽

Nikolay Popov

Keyword(s):

Composite System ◽

Release Kinetics ◽

Spectral Characteristics ◽

In Vitro Release ◽

Medium Ph ◽

Release Capacity ◽

Bioactive Substance ◽

Acacia Catechu ◽

Vitro Release

The main goal of the present study was to investigate the microencapsulation, in vitro release capacity and efficiency of catechin-rich Acacia catechu extract by Clinosorbent-5 (CLS-5) microparticles by in-depth detailed analyses and mathematical modelling of the encapsulation and in vitro release kinetics behaviour of the polyphenol-mineral composite system. The bioflavanol encapsulation and release efficiency on/from the mineral matrix were assessed by sorption experiments and interpretative modelling of the experimental data. The surface and spectral characteristics of the natural bioactive substance and the inorganic microcarrier were determined by Fourier Transform Infrared Spectroscopy (FTIR) and Ultraviolet/Visible (UV/Vis) spectrophotometric analyses. The maximum extent of catechin microencapsulation in acidic medium was 32%. The in vitro release kinetics study in simulated enzyme-free gastric medium (pH = 1.2) approved 88% maximum release efficiency achieved after 24 h. The in vitro release profile displayed that the developed bioflavanol/clinoptilolite microcarrier system provided sustained catechin in vitro release behaviour without an initial burst effect. Thus, the results from the present study are essential for the design and development of innovative catechin-CLS-5 microcarrier systems for application in human and veterinary medicine.

Download Full-text

Biodiesel Production on Monometallic Pt, Pd, Ru, and Ag Catalysts Supported on Natural Zeolite

Materials ◽

10.3390/ma14010048 ◽

2020 ◽

Vol 14 (1) ◽

pp. 48

Author(s):

Pawel Mierczynski ◽

Magdalena Mosińska ◽

Lukasz Szkudlarek ◽

Karolina Chalupka ◽

Misa Tatsuzawa ◽

...

Keyword(s):

Photoelectron Spectroscopy ◽

Natural Zeolite ◽

Noble Metals ◽

Methyl Esters ◽

Physicochemical Characteristics ◽

Biodiesel Production ◽

X Ray Diffraction ◽

X Ray ◽

Yield Values ◽

Temperature Programmed

Biodiesel production from rapeseed oil and methanol via transesterification reaction facilitated by various monometallic catalyst supported on natural zeolite (NZ) was investigated. The physicochemical characteristics of the synthesized catalysts were studied by X-ray diffraction (XRD), Brunauer–Emmett–Teller method (BET), temperature-programmed-reduction in hydrogen (H2-TPR), temperature-programmed-desorption of ammonia (NH3-TPD), Scanning Electron Microscope equipped with EDX detector (SEM-EDS), and X-ray photoelectron spectroscopy (XPS) methods. The highest activity and methyl ester yields were obtained for the Pt/NZ catalyst. This catalyst showed the highest triglycerides conversion of 98.9% and fatty acids methyl esters yields of 94.6%. The activity results also confirmed the high activity of the carrier material (NZ) itself in the investigated reaction. Support material exhibited 90.5% of TG conversion and the Fatty Acid Methyl Esters yield (FAME) of 67.2%. Introduction of noble metals improves the TG conversion and FAME yield values. Increasing of the metal loading from 0.5 to 2 wt.% improves the reactivity properties of the investigated catalysts.

Download Full-text

Formulation and evaluation of proniosome loaded sertaconazole nitrate for topical application

International Journal of Life Science Research Archive ◽

10.53771/ijlsra.2021.1.2.0060 ◽

2021 ◽

Vol 1 (2) ◽

pp. 023-037

Author(s):

Shailaja D ◽

Latha K ◽

Manasa D ◽

Shirisha A ◽

Padmavathi R ◽

...

Keyword(s):

Ex Vivo ◽

Release Kinetics ◽

Skin Irritation ◽

Water Soluble ◽

Ionic Surfactants ◽

Release Mechanism ◽

Stability Studies ◽

Zero Order Release ◽

Poorly Soluble

Proniosomal technology is a novel solution for poorly soluble drugs. Proniosomes are water-soluble carrier particles which are coated with non-ionic surfactants. Proniosomal gels were prepared by coacervation phase separation method using non-ionic surfactants, lipid carriers and cholesterol as a membrane stabilizer. FTIR compatibility studies revealed that the drug and excipients were compatible. All formulations were evaluated for pH, drug content, extrudability, spreadability, viscosity, in-vitro, ex-vivo, skin irritation and stability studies. Among formulations prepared, F80H1 has shown higher % EE (83.02) and least diffusion through dialysis membrane i.e., 17.68%. With ex-vivo studies, F80H1 formulation has shown highest skin deposition and lower flux of sertaconazole nitrate through the rat skin. F80H1 was selected as final optimized formulation. F80H1 exhibited good stability and SEM studies revealed that the vesicles were spherical in shape. The optimized formulation was found to follow zero order release kinetics and korsmeyer-peppas release mechanism. F80H1 found to be non-irritant and stable from skin irritation and stability studies.

Download Full-text

Preparation of Sodium Paeonolsilate Intercalated into Layered Double Hydroxides and its Release Properties

Advanced Materials Research ◽

10.4028/www.scientific.net/amr.1095.349 ◽

2015 ◽

Vol 1095 ◽

pp. 349-354 ◽

Cited By ~ 1

Author(s):

Liang Hua Gu ◽

Hong Qing Song ◽

Zhi Yong Sun ◽

Ji Yong Zheng ◽

Jin Wei Zhang ◽

...

Keyword(s):

Controlled Release ◽

Release Kinetics ◽

Molar Ratio ◽

Burst Release ◽

X Ray Diffraction ◽

Release Process ◽

Rate Determining Step ◽

Release Ratio ◽

Double Hydroxide ◽

Double Hydroxides

A controlled release composite has been prepared by intercalation of sodium paeonolsilate (PAS) into Mg/Al layered double hydroxide (LDH) with the molar ratio (M2+/M3+) of 2:1. The powder X-ray diffraction (XRD) and Fourier transform infrared spectroscopy (FT-IR) confirm the intercalation of PAS into the galleries of LDH. The chemical composites of PAS-LDH were revealed by elemental analysis. Release tests of the PAS-LDH composite showed that no burst release phenomenon occurred at the beginning stage and a high release ratio of PAS (89.8%) was obtained, exhibiting controlled release behavior. Furthermore, the parabolic diffusion model was used to simulate the release kinetics of PAS from the LDH carrier, indicating that the intraparticle diffusion via ion-exchange is the rate-determining step in the release process. It is significance in this work for introducing the PAS-LDH composite to develop antifouling materials with long-term activity.

Download Full-text