scholarly journals Influence of Sodium Alginate on Hypoglycemic Activity of Metformin Hydrochloride in the Microspheres Obtained by the Spray Drying

2016 ◽  
Vol 2016 ◽  
pp. 1-12 ◽  
Author(s):  
Marta Szekalska ◽  
Magdalena Wróblewska ◽  
Katarzyna Sosnowska ◽  
Katarzyna Winnicka
Keyword(s):  
Sodium Alginate ◽  
Spray Drying ◽  
Drug Loading ◽  
Release Profile ◽  
Hypoglycemic Activity ◽  
Metformin Hydrochloride ◽  
Drying Method ◽  
Alginate Concentration ◽  
Polymer Ratio

Alginate microspheres with metformin hydrochloride were prepared by the spray drying method in order to improve residence time of drug in the stomach. Nine formulations (F1–F9) with various drug : polymer ratio (1 : 2, 1 : 1, and 2 : 1) and different sodium alginate concentration (1%, 2%, and 3%) were evaluated for size, morphology, drug loading, Zeta potential, and swelling degree.In vitrodrug release, mathematical release profile, and physical state of microspheres were also evaluated. Optimal formulation characterized by the highest drug loading was formulation F6 (drug : polymer ratio 2 : 1 and 2% alginate solution). Based on glucose uptake inSaccharomyces cerevisiaecells andα-amylase inhibition tests, it could be concluded that alginate microspheres enhance hypoglycemic activity of metformin hydrochloride evaluatedin vitro. Designed microspheres are promising as alternative, multicompartment dosage form for metformin hydrochloride delivery.

scholarly journals Preparation and Evaluation of Gastroretentive Floating Pellets of Metronidazole

2013 ◽  
Vol 16 (1) ◽  
pp. 107-115 ◽  
Author(s):  
Shahriar Nowshad ◽  
Md Saiful Islam Pathan
Keyword(s):  
Drug Release ◽  
Bulk Density ◽  
Sodium Alginate ◽  
Drug Loading ◽  
Simulated Gastric Fluid ◽  
Gi Tract ◽  
Enhanced Absorption ◽  
Psyllium Husk ◽  
Alginate Concentration

Traditionally metronidazole is used in the treatment of bacterial vaginosis, trichomoniasis, amoebiasis and is also used in combination with other drugs to treat Helicobacter pylori (H. pylori) that causes stomach or intestinal ulcers. The main aim of this study was to develop a gastroretentive floating pellets for the treatment of above pathological conditions. Such kind of dosage form may provide an extension of drug presence in the upper GI tract resulting enhanced absorption and improved bioavailability for the treatment against protozoa and bacteria. Nine formulations of metronidazole floating pellets such as F1, F2, F3, F4, F5, F6, F7, F8 and F9 were prepared by ionic gelation method using different quantities of sodium alginate and psyllium husk. The drug and polymer ratio were 1:1.4, 1:1.5, 1:1.6, 1:1.6; 1:1.7, 1:1.8, 1:1.8, 1:1.9 and 1:2.0, respectively. The in vitro drug release study was carried out in 900 ml phosphate buffer (pH 7.4) at 37±0.50C and 50 rpm for 12 hours using USP XXIV paddle method and the content of drug release was determined by UV spectrometer at 277nm. Maximum and minimum drug release were found in F1 (88.63%) and in F6 (73.21%), respectively. It indicates that increase in sodium alginate concentration decreases drug release. All the formulations were buoyant for more than 12 hours in simulated gastric fluid at 370C. The maximum and minimum bulk density tapped were 0.57 and 0.52 in F1 and F9, respectively where drug loading were 14.07% in F1 and 12.56% in F9 which indicates that bulk density of the pellets is directly proportional to drug loading. The maximum and minimum swelling were in F3 (75%) and F7 (59%), respectively which demonstrate that swelling of pellets were inversely proportional to the sodium alginate concentration but it is directly proportional to psyllium husk content. In addition, the psyllium husk keeps the GI tract healthy by scavenging toxins and residues of digestive systems. Therefore, it can be concluded that combination of sodium alginate and biodegradable psyllium husk can be prospectively used for the preparation of gastroretentive floating pellets. DOI: http://dx.doi.org/10.3329/bpj.v16i1.14504 Bangladesh Pharmaceutical Journal 16(1): 107-115, 2013

scholarly journals Formulation and development of metformin-loaded microspheres using Khaya senegalensis (Meliaceae) gum as co-polymer

2020 ◽  
Vol 6 (1) ◽  
Author(s):  
Chukwuebuka H. Ozoude ◽  
Chukwuemeka P. Azubuike ◽  
Modupe O. Ologunagba ◽  
Sejoro S. Tonuewa ◽  
Cecilia I. Igwilo
Keyword(s):  
Controlled Release ◽  
Sodium Alginate ◽  
Release Kinetics ◽  
Drug Carrier ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Metformin Hydrochloride ◽  
Scanning Calorimetry ◽  
Khaya Senegalensis

Abstract Background Khaya gum is a bark exudate from Khaya senegalensis (Maliaecae) that has drug carrier potential. This study aimed to formulate and comparatively evaluate metformin-loaded microspheres using blends of khaya gum and sodium alginate. Khaya gum was extracted and subjected to preformulation studies using established protocols while three formulations (FA; FB and FC) of metformin (1% w/v)-loaded microspheres were prepared by the ionic gelation method using 5% zinc chloride solution as the cross-linker. The formulations contained 2% w/v blends of khaya gum and sodium alginate in the ratios of 2:3, 9:11, and 1:1, respectively. The microspheres were evaluated by scanning electron microscopy, Fourier transform-infrared spectroscopy, differential scanning calorimetry, entrapment efficiency, swelling index, and in vitro release studies. Results Yield of 28.48%, pH of 4.00 ± 0.05, moisture content (14.59% ± 0.50), and fair flow properties (Carr’s index 23.68 ± 1.91 and Hausner’s ratio 1.31 ± 0.03) of the khaya gum were obtained. FTIR analyses showed no significant interaction between pure metformin hydrochloride with excipients. Discrete spherical microspheres with sizes ranging from 1200 to 1420 μm were obtained. Drug entrapment efficiency of the microspheres ranged from 65.6 to 81.5%. The release of the drug from microspheres was sustained for the 9 h of the study as the cumulative release was 62% (FA), 73% (FB), and 80% (FC). The release kinetics followed Korsmeyer-Peppas model with super case-II transport mechanism. Conclusion Blends of Khaya senegalensis gum and sodium alginate are promising polymer combination for the preparation of controlled-release formulations. The blend of the khaya gum and sodium alginate produced microspheres with controlled release properties. However, the formulation containing 2:3 ratio of khaya gum and sodium alginate respectively produced microspheres with comparable controlled release profiles to the commercial brand metformin tablet.

scholarly journals Eudragit S-100 coated sodium alginate microspheres of naproxen sodium: Formulation, optimization and in vitro evaluation / Alginatne mikrosfere naproksen natrija obložene Eudragitom S-100: Priprava, optimizacija i in vitro vrednovanje

2012 ◽  
Vol 62 (4) ◽  
pp. 529-545 ◽  
Author(s):  
Anuj Chawla ◽  
Pooja Sharma ◽  
Pravin Pawar
Keyword(s):  
Drug Release ◽  
Sodium Alginate ◽  
Naproxen Sodium ◽  
Drug Loading ◽  
Size Analysis ◽  
Scanning Calorimetry ◽  
Sem Images ◽  
S 100 ◽  
Eudragit S 100

The aim of the study was to prepare site specific drug delivery of naproxen sodium using sodium alginate and Eudragit S-100 as a mucoadhesive and pH-sensitive polymer, respectively. Core microspheres of alginate were prepared by a modified emulsification method followed by cross-linking with CaCl2, which was further coated with the pH dependent polymer Eudragit S-100 (2.5 or 5 %) to prevent drug release in the upper gastrointestinal environment. Microspheres were characterized by FT-IR spectroscopy, X-ray diffraction, differential scanning calorimetry and evaluated by scanning electron microscopy, particle size analysis, drug loading efficiency, in vitro mucoadhesive time study and in vitro drug release study in different simulated gastric fluids. Stability studies of the optimized formulation were carried out for 6 months. SEM images revealed that the surface morphology was rough and smooth for core and coated microspheres, respectively. Core microspheres showed better mucoadhesion compared to coated microspheres when applied to the mucosal surface of freshly excised goat colon. The optimized batch of core microspheres and coated microspheres exhibited 98.42 ± 0.96 and 95.58 ± 0.74 % drug release, respectively. Drug release from all sodium alginate microsphere formulations followed Higuchi kinetics. Moreover, drug release from Eudragit S-100 coated microspheres followed the Korsmeyer-Peppas equation with a Fickian kinetics mechanism. Stability study suggested that the degradation rate constant of microspheres was minimal, indicating 2 years shelf life of the formulation.

scholarly journals FORMULATION AND EVALUATION OF MUCOADHESIVE MICROSPHERES OF AN ANTI-MIGRAINE DRUG

2018 ◽  
Vol 8 (5) ◽  
pp. 465-474
Author(s):  
S PADMA PRIYA ◽  
AN Rajalakshmi ◽  
P Ilaveni
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Sodium Alginate ◽  
Release Kinetics ◽  
Drug Loading ◽  
Research Work ◽  
Entrapment Efficiency ◽  
Polyvinyl Pyrrolidone ◽  
Anti Migraine Drug

Objective: The objective of this research work is to develop and evaluate mucoadhesive microspheres of an anti-migraine drug for sustained release. Materials and Methods:  Mucoadhesive microspheres were prepared by emulsification method using Sodium alginate (SA), polyvinyl pyrrolidone (PVP) and Chitosan in the various drug-polymer ratios of 1:1, 1:2 and 1:3. Nine  formulations were formulated and  evaluated for  possible drug polymer interactions, percentage yield, micromeritic properties, particle size, drug content, drug entrapment efficiency, drug loading, swelling index, In-vitro wash off test, in vitro  drug release, surface morphology and release kinetics. Results: The results showed that no significant drug polymer interaction in FTIR studies. Among all the formulations SF3 containing sodium alginate showed 77.18% drug release in 6hrs. Conclusion: Amongst the developed mucoadhesive microspheres, SF3 formulation containing sodium alginate exhibited slow and sustained release in a controlled manner and it is a promising formulation for sustained release of Sumatriptan succinate. Keywords: Mucoadhesive microspheres, Sodium alginate, polyvinyl pyrrolidone, Chitosan, sustained release.

scholarly journals Sodium Alginate Nanoparticles of Isoniazid: Preparation and Evaluation

2019 ◽  
Vol 11 (06) ◽  
Author(s):  
Sumit Kumar ◽  
Dinesh Chandra Bhatt
Keyword(s):  
Particle Size ◽  
Sodium Alginate ◽  
Encapsulation Efficiency ◽  
Drug Loading ◽  
Average Particle Size ◽  
Average Particle ◽  
In Vitro Drug Release ◽  
Ionotropic Gelation ◽  
Preparation And Evaluation

Fabrication and evaluation of the Isoniazid loaded sodium alginate nanoparticles (NPs) was main objective of current investigation. These NPs were engineered using ionotropic gelation technique. The NPs fabricated, were evaluated for average particle size, encapsulation efficiency, drug loading, and FTIR spectroscopy along with in vitro drug release. The particle size, drug loading and encapsulation efficiency of fabricated nanoparticles were ranging from 230.7 to 532.1 nm, 5.88% to 11.37% and 30.29% to 59.70% respectively. Amongst all batches studied formulation F-8 showed the best sustained release of drug at the end of 24 hours.

scholarly journals Controlled Release of 5-FU from Chi–DHA Nanoparticles Synthetized with Ionic Gelation Technique: Evaluation of Release Profile Kinetics and Cytotoxicity Effect

2020 ◽  
Vol 11 (3) ◽  
pp. 48
Author(s):  
Mariarosa Ruffo ◽  
Ortensia Ilaria Parisi ◽  
Francesco Patitucci ◽  
Marco Dattilo ◽  
Rocco Malivindi ◽  
...  
Keyword(s):  
Docosahexaenoic Acid ◽  
High Efficiency ◽  
Drug Loading ◽  
In Vitro Release ◽  
Release Profile ◽  
Order Kinetic ◽  
Ionic Gelation ◽  
Cytotoxicity Studies ◽  
Order Kinetic Model

The ionic gelation technique allows us to obtain nanoparticles able to function as carriers for hydrophobic anticancer drugs, such as 5-fluoruracil (5-FU). In this study, reticulated chitosan– docosahexaenoic acid (Chi–DHAr) nanoparticles were synthesized by using a chemical reaction between amine groups of chitosan (Chi) and carboxylic acids of docosahexaenoic acid (DHA) and the presence of a link between Chi and DHA was confirmed by FT-IR, while the size and morphology of the obtained Chi-DHAr nanoparticles was evaluated with dynamic light scattering (DLS) and scanning electron microscopy (SEM), respectively. Drug-loading content (DLC) and drug-loading efficiency (DLE) of 5-FU in Chi-DHAr nanoparticles were 33.74 ± 0.19% and 7.9 ± 0.26%, respectively, while in the non-functionalized nanoparticles (Chir + 5FU), DLC, and DLE were in the ranges of 23.73 ± 0.14%, 5.62%, and 0.23%, respectively. The in vitro release profile, performed in phosphate buffer saline (PBS, pH 7.4) at 37 °C, indicated that the synthetized Chi–DHAr nanoparticles provided a sustained release of 5-FU. Based on the obtained regression coefficient value (R2), the first order kinetic model provided the best fit for both Chir and Chi-DHAr nanoparticles. Finally, cytotoxicity studies of chitosan, 5-FU, Chir, Chir + 5-FU, Chi-DHAr, and Chi-DHAr + 5-FU nanoparticles were conducted. Overall, Chi-DHAr nanoparticles proved to be much more biocompatible than Chir nanoparticles while retaining the ability to release the drug with high efficiency, especially towards specific types of cancerous cells.

In vitro release of metformin hydrochloride from sodium alginate/polyvinyl alcohol hydrogels

2017 ◽  
Vol 155 ◽  
pp. 182-191 ◽  
Author(s):  
Fabián Martínez-Gómez ◽  
Juan Guerrero ◽  
Betty Matsuhiro ◽  
Jorge Pavez
Keyword(s):  
Polyvinyl Alcohol ◽  
Sodium Alginate ◽  
In Vitro Release ◽  
Metformin Hydrochloride ◽  
Vitro Release

scholarly journals In vitro and in vivo evaluation of sustained release ketoprofen-loaded nanoparticles

2013 ◽  
Vol 16 (1) ◽  
pp. 15-25
Author(s):  
Tuyen Thi Phuong Dao ◽  
Nhan Ngoc Thanh Le ◽  
Anh Tuan Nguyen ◽  
Khai Tan Tran ◽  
Dam Duy Le ◽  
...  
Keyword(s):  
Spray Drying ◽  
In Vitro Dissolution ◽  
Drying Method ◽  
In Vivo Evaluation ◽  
The Matrix ◽  
Nanoparticle Formulation ◽  
Electron Microscopes ◽  
Size And Morphology

The purpose of this study is to i) fabricate a biodegradable nanoparticle formulation of Ketoprofen, ii) evaluate its characteristics, iii) investigate its in vitro dissolution and in vivo pharmaceutical property. The nanoparticle formulation was prepared by spray drying method using Eudragit L100 as the matrix polymer. Size and morphology of drug-loaded nanoparticles were characterized with the electron microscopes (TEM, SEM). These successfully prepared nanoparticles by spray drying method are spherical in shape and quite homologous with diameter size of 100 – 200 nm. The in vitro dissolution studies were conducted at pH 1.2 and 7.4. The results indicated that there is a significant increase in Keto concentration at pH 7.4 compared to pH 1.2. For the in vivo assessment, our Keto-loaded nanoparticles and referential Profenid were administered by oral gavages to rabbits. The results implied that Keto-loadednanoparticles remarkably increased AUC compared to Profenid.

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