scholarly journals Hydrolyzed Karaya Gum: Gelatin Complex Coacervates for Microencapsulation of Soybean Oil and Curcumin

2021 ◽  
Vol 2021 ◽  
pp. 1-10
Author(s):  
My Lan Nguyen Le ◽  
Hang Nga Le Thi ◽  
Vinh Tien Nguyen
Keyword(s):  
Soybean Oil ◽  
Freeze Drying ◽  
Maximum Yield ◽  
In Vitro Release ◽  
Tween 80 ◽  
Linear Increase ◽  
Protective Effects ◽  
Pharmaceutical Industries ◽  
Karaya Gum

This is the first report on utilizing hydrolyzed karaya gum (HKG) as a novel polyanion material for complex coacervation with gelatin A. With negative zeta potentials at pH > 2.5, HKG formed the complex coacervate with a maximum yield at pH 3.75 and 1 : 1 HKG:gelatin ratio. The optimal complex coacervates were used to encapsulate soybean oil containing curcumin using different shell:core ratios, homogenization speeds, concentrations of emulsifier, and drying techniques. Optical microscopy showed that increasing homogenization speed and Tween 80 concentration produced smaller and more uniform coacervate particles. Increasing the shell:core mass ratio from 1 to 4 resulted in a linear increase in encapsulation efficiencies for both soybean oil and curcumin. Accelerated peroxidation tests on the microcapsules showed enhanced protective effects against oil peroxidation when increasing shell:core ratios and using freeze-drying instead of oven-drying at 50 oC. In vitro release of curcumin in simulated gastric and intestinal fluids was faster when using freeze-drying and decreasing shell:core ratio. This study shows perspective novel applications of HKG in microencapsulating active ingredients for food and pharmaceutical industries.

scholarly journals Optimization of sunflower head pectin extraction by ammonium oxalate and the effect of drying conditions on properties

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Xuemei Ma ◽  
Jiayi Yu ◽  
Jing Jing ◽  
Qian Zhao ◽  
Liyong Ren ◽  
...  
Keyword(s):  
High Performance ◽  
Freeze Drying ◽  
Antioxidant Activities ◽  
Structural Characteristics ◽  
Radical Scavenging ◽  
Ammonium Oxalate ◽  
Extraction Process ◽  
Size Exclusion ◽  
Pharmaceutical Industries

AbstractPectin is a kind of natural and complex carbohydrates which is extensively used in food, chemical, cosmetic, and pharmaceutical industries. Fresh sunflower (Helianthus annuus L.) heads were utilized as a novel source of pectin extracted by ammonium oxalate. The conditions of the extraction process were optimized implementing the response surface methodology. Under optimal extraction parameters (extraction time 1.34 h, liquid–solid ratio 15:1 mL/g, ammonium oxalate concentration 0.76% (w/v)), the maximum experimental yield was 7.36%. The effect of spray-drying and freeze-drying on the physiochemical properties, structural characteristics, and antioxidant activities was investigated by FT-IR spectroscopy, high performance size exclusion chromatography, and X-ray diffraction. The results showed freeze-drying lead to decrease in galacturonic acid (GalA) content (76.2%), molecular weight (Mw 316 kDa), and crystallinity. The antioxidant activities of pectin were investigated utilizing the in-vitro DPPH and ABTS radical-scavenging systems. This study provided a novel and efficient extraction method of sunflower pectin, and confirmed that different drying processes had an effect on the structure and properties of pectin.

scholarly journals Preparation and Characterization of PEG-PLA Genistein Micelles Using a Modified Emulsion-Evaporation Method

2020 ◽  
Vol 2020 ◽  
pp. 1-15
Author(s):  
Qiuchen Cheng ◽  
Wen Qin ◽  
Yanhong Yu ◽  
Guojian Li ◽  
Jizhou Wu ◽  
...  
Keyword(s):  
Smooth Muscle Actin ◽  
Drug Loading ◽  
In Vitro Release ◽  
Tween 80 ◽  
Original Method ◽  
Scanning Calorimetry ◽  
Experimental Conditions ◽  
Evaporation Method ◽  
Genistein Treatment

The objective of this study is to improve the bioavailability of genistein by encapsulation with polyethylene glycol-polylactic acid (PEG-PLA) copolymers. Genistein micelles (GMs) prepared using a modified emulsion-evaporation method were more stable than those made with the original method. The effect of polyvinyl alcohol, Tween 80, sonication time, PEG-PLA/genistein ratio, and organic phase (acetone)/H2O ratio on the size, polydispersity index, encapsulation efficiency, and drug loading efficiency of GMs was investigated. GMs were obtained and characterized under optimal experimental conditions. For long-term storage, GMs were lyophilized by freeze drying with trehalose to produce genistein lyophilized powder (GLP). The analysis of GLP by Fourier-transform infrared spectroscopy and differential scanning calorimetry showed that genistein was successfully incorporated into the micellar structure. In vitro release experiments revealed that the incorporation of genistein into PEG-PLA copolymers significantly improved its solubility and bioavailability. GLP was more potent in inhibiting the proliferation of HSC-T6 cells than genistein. Treatment with GLP at 10–20 μg/mL for 48 h significantly inhibited the protein expression of α-smooth muscle actin and collagen I in HSC-T6 cells compared with the control. These data demonstrated that the improved solubility and bioavailability of genistein in the form of GLP enhanced its antifibrotic effect in vitro.

NOVEL PHARMACEUTICAL COCRYSTAL OF TELMISARTAN AND HYDROCHLOROTHIAZIDE

2020 ◽  
pp. 104-112
Author(s):  
ALPANA KULKARNI ◽  
SWAPNIL SHETE ◽  
VISHAL HOL ◽  
RITESH BACHHAV
Keyword(s):  
Maximum Yield ◽  
In Vitro Release ◽  
Active Pharmaceutical Ingredient ◽  
Flow Properties ◽  
Acidic Group ◽  
X Ray ◽  
Poorly Soluble ◽  
Pharmaceutical Cocrystal ◽  
Vitro Release

Objective: Telmisartan (TEL), commonly used antihypertensive, is poorly soluble in water and has limited and variable bioavailability. Commercially, TEL is available as a single drug and in combination with hydrochlorothiazide (HYZ). Researchers have developed cocrystals of TEL with coformers, namely, oxalic acid, glutaric acid, and saccharin. An attempt was made to prepare the cocrystals of TEL with HYZ, an active pharmaceutical ingredient (API) itself so that both the APIs are available in a single tablet. The present study was aimed at enhancement in solubility of TEL by formation of its cocrystals. Methods: The cocrystals of TEL with HYZ, in different stoichiometric ratios (1:0.5, 1:1, and 1:2), were prepared by solvent coevaporation and liquid-assisted grinding methods. The cocrystals, consisting of TEL:HYZ (in 1:0.5 ratio and 1:1 ratio), depicted maximum yield, drug content, saturation solubility, and flow properties. These cocrystals were characterized by X-ray analysis, infrared spectroscopy, and thermal analysis. Results: The crystal structure of TEL-HYX revealed that it was a cocrystal, since no proton was transferred between the TEL and HYZ molecules. It was predicted that two molecules are associated through a hydrogen bond between an acidic group of TEL and sulfonamido group of HYZ. The cocrystallization improved the solubility of TEL 7 times. In vitro release rate of tablets of cocrystals was higher than that of marketed TEL tablets. HYZ has a potential to form the cocrystals of TEL. Conclusion: The objective of improvement in the solubility of TEL was successfully achieved by the formation of cocrystals of TEL: HYZ.

scholarly journals Evaluation of the antifungal activity by plant extracts against Colletotrichum gloeosporioides Penz

2008 ◽  
Vol 32 (2) ◽  
pp. 420-428 ◽  
Author(s):  
Polyanna Alves Silva ◽  
Denilson Ferreira Oliveira ◽  
Ney Robson Taironi do Prado ◽  
Douglas Antônio de Carvalho ◽  
Gilvane Aparecida de Carvalho
Keyword(s):  
Antifungal Activity ◽  
Freeze Drying ◽  
Colletotrichum Gloeosporioides ◽  
Plantago Lanceolata ◽  
Stevia Rebaudiana ◽  
Tween 80 ◽  
In Vitro Assays ◽  
Bioactive Substances ◽  
Stevia Rebaudiana Bertoni

Aiming to develop more efficient and environmental friendly methods than those available to control Colletotrichum gloeosporioides Penz, which causes blister spot in coffee trees, a search for plants able to produce substances active against such pathogen was carried out. Thus, extracts of 48 plant species, collected at Alto Rio Grande region, in Minas Gerais, were prepared and submitted to in vitro assays with that fungus. The best results were obtained with the extracts prepared from Digitalis lanata Ehrh, Origanum manjorona L., Plantago lanceolata Hook. and Stevia rebaudiana (Bertoni) Bertoni, which inhibited C. gloeosporioides spores germination. After dilution of some active extracts with aqueous 1 % Tween 80 solution in a 1:2 or 1:3 ratio (extract:aqueous solution), their antifungal activity vanished. Some of the active extracts were also submitted to freeze drying and none of them presented any alteration in their antifungal activity. Concluding, several plants presented potential to be used in the search for new bioactive substances to control C. gloeosporioides, especially O. manjorona L., which inhibited 96 % of the fungus spores germination.

scholarly journals FLUCONAZOLE NANOGEL: FABRICATION AND IN VITRO EVALUATION FOR TOPICAL APPLICATION

2021 ◽  
pp. 272-277
Author(s):  
DIVYA ◽  
INDERBIR SINGH ◽  
UPENDRA NAGAICH
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Release Kinetics ◽  
Seborrheic Dermatitis ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Tween 80 ◽  
Flow Index ◽  
In Vitro Evaluation

Objective: The aim of this study is to develop and in vitro evaluation of prepared fluconazole nanogel for seborrheic dermatitis Methods: Fluconazole nanogel was formulated to act against seborrheic dermatitis. The fluconazole nanoparticles were prepared by a simplified evaporation method and evaluated for particle size, entrapment efficiency, and percent in vitro drug release. The nanogel was also characterized based on parameters like particle size, percent entrapment efficiency, shape surface morphology, rheological properties, in vitro release R² = 0.9046, and release kinetics. Results: The nanoparticle with a combination of Eudragit RS and Tween 80 showed the best result with particle size in the range of 119.0 nm to 149.5 nm, with a cumulative percent drug release of 95 % up to 18 h. The formulated nanogel with optimum concentration of HPMC authenticate with particle size 149.50±0.5 with maximum drug release (92.13±0.32) %. Conclusion: Different percentages of polymers (ethyl-cellulose, eudragit, and tween 80) are used as variable components in the formulation of nanogel. The optimized batch showed good physical properties (flow index, spreadability, and viscosity) along with rapid drug release. Therefore, it can be concluded that nanogel containing fluconazole has potential application in topical delivery.

scholarly journals In Vitro Evaluation of Eudragit Matrices for Oral Delivery of BCG Vaccine to Animals

2019 ◽  
Author(s):  
Imran Saleem ◽  
Allan Coombes ◽  
Mark Chambers
Keyword(s):  
Oral Delivery ◽  
Freeze Drying ◽  
Tween 80 ◽  
Gastric Fluid ◽  
Powder Compaction ◽  
Bcg Vaccine ◽  
Simulated Gastric Fluid ◽  
Physical Damage ◽  
Freeze Dried

Bacillus Calmette-Guérin (BCG) vaccine is the only licensed vaccine against tuberculosis (TB) in humans and animals. It is most commonly administered parenterally but oral delivery is highly advantageous for immunisation of cattle and wildlife hosts of TB in particular. Since BCG is susceptible to inactivation in the gut, vaccine formulations were prepared from suspensions of Eudragit L100 copolymer powder and BCG in PBS, containing Tween 80, with and without the addition of mannitol or trehalose. Samples were frozen at -20oC, freeze-dried and the lyophilised powders were compressed to produce BCG-Eudragit matrices. Production of the dried powders resulted in a reduction in BCG viability. Substantial losses in viability occurred at the initial formulation stage and at the stage of powder compaction. Data indicated that the Eudragit matrix protected BCG against simulated gastric fluid (SGF). The matrices remained intact in SGF and dissolved completely in SIF within three hours. The inclusion of mannitol or trehalose in the matrix provided additional protection to BCG during freeze-drying. Control needs to be exercised over BCG aggregation, freeze-drying and powder compaction conditions to minimise physical damage of the bacterial cell wall and maximise the viability of oral BCG vaccines prepared by dry powder compaction.

scholarly journals EFFECTS OF DIFFERENT SURFACTANTS ON INDOMETHACIN MICROSPHERES FORMULATIONS

2015 ◽  
Vol 11 (4) ◽  
pp. 3453-3462
Author(s):  
Paolo Yammine ◽  
Therese Maarawi ◽  
Dima Moussa ◽  
Roula Abdel-Massih ◽  
Rima Kassab ◽  
...  
Keyword(s):  
Polyvinyl Alcohol ◽  
Release Rate ◽  
Drug Loading ◽  
In Vitro Release ◽  
Tween 80 ◽  
Polymeric Microspheres ◽  
Drug Content ◽  
Evaporation Technique ◽  
Drug Polymer Interaction

Microencapsulation by the solvent evaporation technique was used to formulate Indomethacin-loaded poly(DL-lactide-co-caprolactone) microspheres with three different surfactants: Tween 80, Span 80, and Polyvinyl alcohol. Different formulations were prepared by changing drug masses, while keeping the quantities of the polymer and of the surfactant constant. The prepared microspheres were evaluated for drug content, particle size, morphology, drug-polymer interaction, stability, in vitro release, and cytotoxicity assays. Comparison was done to study the effects of the surfactant type on their characteristics. Microspheres presented a spherical and porous profile and were characterized by the stable character of the encapsulated drug. The usage of the Polyvinyl alcohol revealed the highest percent drug entrapment and drug loading, the biggest particles sizes, and the lowest drug release rate. It was the opposite in the case of Tween 80. A negligible cytotoxic effect was noted on Polyvinyl alcohol formulations having the highest drug content. Polymeric microspheres were used efficiently as a delivery system for Indomethacin. Changing the surfactant type had many advantages on drug encapsulation and release rate.

scholarly journals THERAPEUTIC MICROEMULSION OF CURCUMIN FOR THE MANAGEMENT OF OSTEOARTHRITIS

2018 ◽  
Vol 8 (5-s) ◽  
pp. 341-347
Author(s):  
Shreyasi Sharma ◽  
Eisha Ganju ◽  
Neeraj Upmanyu ◽  
Prabhat Jain
Keyword(s):  
Oleic Acid ◽  
Zeta Potential ◽  
Antioxidant Activities ◽  
In Vitro Release ◽  
Tween 80 ◽  
Drug Content ◽  
In Vitro Diffusion ◽  
Span 80 ◽  
Microemulsion Gel

Curcumin (diferuloylmethane) is a natural polyphenolic compound with potent anti-inflammatory, anticancer and antioxidant activities. However, its bioavailability is low as it is poorly absorbed in the gastrointestinal tract. Microemulsions offer the potential to improve the solubility and bioavailability of bioactive compounds; the present work investigated the topical delivery potential of microemulsion gel loaded with curcumas. Curcumin microemulsion was prepared by spontaneous emul­sification method using oil (Oleic acid), surfactant:cosurfactant (Smix) (Ethanol and Tween 80, Span 80 and n Butanol) and water. The optimized formulations of microemulsions were subjected to thermodynamic stability tests. After stability study, stable formulation was characterized for droplet size, pH determination, centrifugation, % drug content in microemulsion, zeta potential and vesicle size measurement and then microemulsion gel were prepared and characterized for spreadability, measurement of viscosity, drug content, In-vitro diffusion, in-vitro release data. Tween 80, Span 80 was selected as surfactant, ethanol, n Butanol as co surfactant and Oleic acid as oil component based on solubility study. The optimized formulation contained Curcumin (10 mg). The in vitro drug release from curcumin microemulsion gel was found to be considerably higher in comparison to that of the pure drug. The in-vitro diffusion of microemulsion gel was significantly good. Based on this study, it can be concluded the solubility and permeability of curcumin can be increased by formulating into microemulsion gel. Keyword: Curcumin, Microemulsion, In-vitro diffusion, Spreadability, Zeta potential, Stability, span 40

scholarly journals Articaine in functional NLC show improved anesthesia and anti-inflammatory activity in zebrafish

2020 ◽  
Vol 10 (1) ◽  
Author(s):  
Gustavo H. Rodrigues da Silva ◽  
Gabriela Geronimo ◽  
Juan P. García-López ◽  
Lígia N. M. Ribeiro ◽  
Ludmilla D. de Moura ◽  
...  
Keyword(s):  
Release Kinetics ◽  
In Vitro Release ◽  
Tween 80 ◽  
Inflammatory Activity ◽  
Formulation Development ◽  
Anesthetic Effect ◽  
Copaiba Oil ◽  
Anti Inflammatory

AbstractAnesthetic failure is common in dental inflammation processes, even when modern agents, such as articaine, are used. Nanostructured lipid carriers (NLC) are systems with the potential to improve anesthetic efficacy, in which active excipients can provide desirable properties, such as anti-inflammatory. Coupling factorial design (FD) for in vitro formulation development with in vivo zebrafish tests, six different NLC formulations, composed of synthetic (cetyl palmitate/triglycerides) or natural (avocado butter/olive oil/copaiba oil) lipids were evaluated for loading articaine. The formulations selected by FD were physicochemically characterized, tested for shelf stability and in vitro release kinetics and had their in vivo effect (anti-inflammatory and anesthetic effect) screened in zebrafish. The optimized NLC formulation composed of avocado butter, copaiba oil, Tween 80 and 2% articaine showed adequate physicochemical properties (size = 217.7 ± 0.8 nm, PDI = 0.174 ± 0.004, zeta potential = − 40.2 ± 1.1 mV, %EE = 70.6 ± 1.8) and exhibited anti-inflammatory activity. The anesthetic effect on touch reaction and heart rate of zebrafish was improved to 100 and 60%, respectively, in comparison to free articaine. The combined FD/zebrafish approach was very effective to reveal the best articaine-in-NLC formulation, aiming the control of pain at inflamed tissues.

scholarly journals ENHANCING THE SUNSCREEN EFFICACY OF BEMOTRIZINOL MICROPIGMENT BY USING O/W NANOEMULSION TOPICAL PREPARATIONS

2019 ◽  
pp. 47-56
Author(s):  
Dina Medhat Hashim ◽  
Nermin Mohamed Sheta ◽  
Vivian Samir Elwazzan ◽  
Wedad Saed Sakran
Keyword(s):  
Ex Vivo ◽  
In Vitro Release ◽  
Tween 80 ◽  
Size Analysis ◽  
Isopropyl Myristate ◽  
Tape Stripping ◽  
Protection Factor ◽  
Potential Measurement ◽  
Optimum Formula

Objective: Bemotrizinol (BEMT) is the most efficient broad-spectrum UV-absorber having a dual mechanism of action in absorbing and reflecting photons. The main objective of this work was to develop successful oil in water (o/w) nanoemulsion for improving the solubility of BEMT and its protective characteristics. Methods: Pseudo-ternary phase diagrams were constructed using labrafac PG and isopropyl myristate as oil phase, tween 80 as surfactant (S) and cremophor EL as cosurfactant (CoS) the ratio of S/CoS was determined according to highest percent of water incorporation to the system. Full factorial study design (24) using Design-Expert® software was adopted to study the effect of four independent variables namely: oil type, oil concentration, S/CoSmix (3:1) concentrations and BEMT concentration on the particle size and the in vitro release at 2 h (Q2h) of the prepared nanoemulsion formulae. Two systems each of eight formulae were developed and evaluated through droplet size analysis, zeta potential measurement, refractive index, in vitro drug release and according to the desirability value two formulae (F6 and F14) were used for further evaluations including in vitro sun protection factor (SPF), ex-vivo deposition by tape stripping technique, permeation test and photostability study. Results: Formula (F14) was chosen as the optimum formula having an in vitro SPF of 16.08±0.39, lowest permeation of 140±0.06 μg/cm2after six h and highest photostability (t90% = 168.02) after 120 min. Conclusion: Despite the poor solubility of bemotrizinol, it could be enhanced by novel drug delivery systems with good SPF value while maintaining its photostability.

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