scholarly journals Formulation Optimization and Evaluation of Probiotic Lactobacillus sporogenes-Loaded Sodium Alginate with Carboxymethyl Cellulose Mucoadhesive Beads Using Design Expert Software

2016 ◽  
Vol 2016 ◽  
pp. 1-14 ◽  
Author(s):  
Himanshu K. Solanki ◽  
Dushyant A. Shah
Keyword(s):  
Carboxymethyl Cellulose ◽  
Room Temperature ◽  
Entrapment Efficiency ◽  
Gastric Fluid ◽  
Pharmaceutical Products ◽  
Sodium Carboxymethyl Cellulose ◽  
Simulated Gastric Fluid ◽  
Formulation Optimization ◽  
Design Expert ◽  
Alginate Concentration

The present study deals with the formulation optimization of sodium carboxymethyl cellulose-alginate mucoadhesive beads containing probiotic Lactobacillus sporogenes through ionotropic gelation using 32 factorial design. The effect of sodium carboxymethyl cellulose-alginate concentration on the probiotic entrapment efficiency (PEE, %), viability in simulated gastric fluid (log CFU/g), and mucoadhesion over 8 hr (%) was optimized. The optimized beads containing probiotic Lactobacillus sporogenes showed entrapment efficiency of 93.7±1.97%, viability of probiotic in simulated gastric fluid (log CFU/g) of 9.34, mucoadhesion of 71.75±1.38%, and mean diameter of 1.21±0.11 mm. The beads were also characterized by SEM, FTIR, and XRD. The swelling and degradation of these beads were influenced by pH of the test medium. Finally, stability tests performed at room temperature (25~28°C) highlighted a bacterial viability of about 91% and 86% after 1 and 2 months, respectively. The advantageous properties of probiotic Lactobacillus sporogenes-loaded mucoadhesive beads make them suitable for incorporation in functional food and/or pharmaceutical products.

scholarly journals Investigation of Crystallization and Salt Formation of Poorly Water-Soluble Telmisartan for Enhanced Solubility

Pharmaceutics ◽  
2019 ◽  
Vol 11 (3) ◽  
pp. 102 ◽  
Author(s):  
Chulhun Park ◽  
Nileshkumar Meghani ◽  
Yongkwan Shin ◽  
Euichaul Oh ◽  
Jun-Bom Park ◽  
...  
Keyword(s):  
Room Temperature ◽  
Gastric Fluid ◽  
Water Soluble ◽  
Simulated Gastric Fluid ◽  
Distilled Water ◽  
Salt Formation ◽  
Intestinal Fluid ◽  
Salt Form ◽  
Enhanced Solubility ◽  
Poorly Water Soluble

The crystal changes and salt formation of poorly water-soluble telmisartan (TEL) in various solvents were investigated for enhanced solubility, stability and crystallinity. Polymorphic behaviors of TEL were characterized by dispersing in distilled water, acetone, acetonitrile, DMSO, or ethanol using Method I: without heat and then dried under vacuum at room temperature; and Method II: with heat below boiling temperature, cooled at 5 °C, and then dried under vacuum at 40 °C. For salt formation (Method III), the following four powdered mixtures were prepared by dispersing in solution of hydrochloric acid (HCl) (pH 1.2), TEL/HCl; in simulated gastric fluid (pH 1.2 buffer), TEL/simulated gastric fluid (SGF); in intestinal fluid (pH 6.8 buffer), TEL/simulated intestinal fluid (SIF); or in NaOH (pH 6.8), TEL/NaOH, respectively, and then dried under a vacuum at room temperature. The structures of powdered mixtures were then studied using a field emission scanning electron microscope (FESEM), differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD), FTIR, 1H nuclear magnetic resonance (1H-NMR), and LC–MS. The solubility of TEL in powdered forms was performed in pH 6.8, pH 1.2, and distilled water. No polymorphic behaviors of TEL were observed in various solvents as characterized by FESEM, DSC, PXRD, and FTIR. However, the structural changes of powdered mixtures obtained from Method III were observed due to the formation of salt form. Moreover, the solubility of salt form (TEL/HCl) was highly increased as compared with pure TEL. There were no significant changes of TEL/HCl compared with TEL in the content assay, PXRD, DSC, and FTIR during stressed storage conditions at 40 °C/75% relative humidity (RH) for 4 weeks under the closed package condition. Therefore, the present study suggests the new approach for the enhanced stability and solubility of a poorly water-soluble drug via salt form.

scholarly journals Physico-chemical evaluation of Gastroretentive Ranitidine Hydrochloride: An Anti-Ulcer Drug

2016 ◽  
Vol 3 (2) ◽  
pp. 4-12
Author(s):  
RK Yadav ◽  
Satyam Prakash ◽  
K Yadav ◽  
NK Yadav ◽  
M Mostafa
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Entrapment Efficiency ◽  
Lag Time ◽  
Gastric Fluid ◽  
Simulated Gastric Fluid ◽  
Drug Content ◽  
Drug Entrapment Efficiency ◽  
Gastro Retentive

Background  and  Objectives:  The  prevention  and  treatment  of  peptic  ulcers  has  become  an important challenge in the current medicine  world.   Modern progress in novel drug delivery system aims to improve the efficacy of the drug molecule by formulating a dosage form of RHCL. One of the most feasible approaches for achieving a prolonged and predictable drug delivery profile in GI tract is to control the gastric residence time.  Therefore, a multi-unit gastro retentive dosage form of RHCL capable of floating on simulated gastric fluid for more than 12 hours was formulated and evaluated.Materials  and  Methods:  Nine  batches  of  the  light  liquid  paraffin  entrapped  emulsion  gel  beads were  prepared  by  a  new  emulsion  gelation  technique  using  sodium  alginate  and  xanthan  gum  as polymers.  The  polymeric  solution  was  extruded  into  Calcium  chloride  solution  by  the  use  of  21G needles.  Morphology  of  beads,  drug  content,  drug  entrapment  efficiency,  floating  lag  time  and buoyancy were studied. Compatibility study of Ranitidine HCl with polymers used in the formulation was performed using DSC and FT-IR.Results:  Mean  surface  diameter  were  between  1.220  ±  2.259%  (F1)  to  1.230  ±  2.316%  (F9)  and floating lag time were between 6 minute (F9) to 11 minute (F1). All formulations were buoyant for more than 12 hours in simulated gastric  fluid  at  37ºC.  The  drug  content  and  drug  entrapment efficiency  among  the  formulations  were  between  17.48%~19.68%  and  71.06%  ~84.32% respectively. Formulation F1 showed lowest drug content and drug entrapment efficiency while F9 showed highest drug content and drug entrapment efficiency. F4 showed most acceptable sustained drug release profile.Conclusion:  The gastro retentive drug delivery system designed as floating beads was found to be satisfactory drug delivery system for Ranitidine HCl to improve the bioavailability of the drug. Janaki Medical College Journal of Medical Sciences (2015) Vol. 3 (2): 4-12

scholarly journals Improvement in Entrapment Efficiency and In Vitro Digestion Stability of Lutein by Zein Nanocarriers with Pepsin Hydrolysis

2020 ◽  
Vol 2020 ◽  
pp. 1-9 ◽  
Author(s):  
Yan Jiao ◽  
He Han ◽  
Ying Chang ◽  
Dajing Li ◽  
Asad Riaz
Keyword(s):  
Structural Characteristics ◽  
Average Particle Size ◽  
Entrapment Efficiency ◽  
In Vitro Digestion ◽  
Gastric Fluid ◽  
Simulated Gastric Fluid ◽  
Average Particle ◽  
Simulated Intestinal Fluid ◽  
Bioactive Ingredients

Zein is one of the popular bioactive carriers and play critical roles in the promotion of stability, absorption, and utilization of the nutrients and bioactive ingredients. The application of zein delivery systems for the encapsulation of bioactive ingredients has recently gained increasing interest. The aim of this work was to modify zein by pepsin and prepare the lutein-loaded zein nanoparticle (LZN) and the lutein-loaded zein hydrolysate nanoparticle (LZHN), respectively. The effects of zein hydrolysation on entrapment efficiency and in vitro digestion stability of lutein were also evaluated in this study. Hydrolysation of zein by the pepsin has important effects on lutein embedding. The optimal hydrolysis conditions, including the pepsin concentration (1.5%), temperature (55°C), and time (4 h), enhanced the entrapment efficiency (EE) of lutein by 93.82 ± 2.82% as compared to 85.18 ± 3.28% of the untreated zein, respectively. In contrast to LZN, LZHN had better structural characteristics, the average particle size decreases from 158.40 ± 3.22 nm to 112.2 ± 1.56 nm, and LZHN showed better dispersivity and zeta potential. The stability and release assays in simulated gastric fluid (SGF) and simulated intestinal fluid (SIF) showed that hydrolyzed zein nanocarriers by pepsin improved the digestion stability and promoted the release of lutein under gastrointestinal digestive conditions. These results suggest that hydrolyzed zein with pepsin may act as an effective carrier for lutein delivery and shows many potential advantages compared with the zein.

scholarly journals Influence of Chitosan-Alginate Microcapsules Containing Anti-Vibrio Harveyi IgY in the Gastrointestinal Tract Simulation

2015 ◽  
Vol 9 (12) ◽  
pp. 110 ◽  
Author(s):  
Kawin Punyokun ◽  
Ratchanee Hongprayoon ◽  
Prapansak Srisapoome ◽  
Theerapol Sirinarumitre
Keyword(s):  
Egg Yolk ◽  
Gastric Fluid ◽  
Simulated Gastric Fluid ◽  
Gastrointestinal Infections ◽  
Simulated Intestinal Fluid ◽  
Egg Yolk Immunoglobulin ◽  
Alginate Concentration ◽  
Cacl2 Concentration ◽  
The Stability ◽  
Processing Factors

<p class="zhengwen"><span lang="EN-GB">Egg yolk immunoglobulin (IgY) is an alternative treatment for the prevention of gastrointestinal infections in pigs, cows, chickens and fish. In our previous report, we preliminarily proved that anti-<em>V. harveyi</em> IgY had effective potential to control luminous disease in black tiger shrimp. However,</span><span lang="EN-GB">IgY activity may be reduced or destroyed by gastric conditions, particularly low pH and digestive enzymes. Therefore, it is necessary to find an effective method to preserve the therapeutic function of IgY antibodies during gastric passage. Chitosan-alginate microcapsules have been developed to protect IgY from gastric inactivation. The processing factors included different forms of chitosan and alginate, while a CaCl2 concentration and encapsulation medium was investigated. The optimum results were obtained under the following conditions: High Mw chitosan concentration 0.2% (w/v), medium viscosity alginate concentration 2% (w/v), CaCl2 concentration 0.5% (w/v). The stability of IgY in simulated gastric fluid (SGF, pH 1.2) was greatly improved by encapsulation in chitosan-alginate microcapsules, and retained greater than 90% activity after 2 h exposure to SGF. Less than 10% IgY was released upon the microcapsules’ exposure to SGF for 2 h, and more than 80% IgY was released upon the microcapsules’ exposure to simulated intestinal fluid (SIF, pH 6.8) for 16 h. </span></p>

scholarly journals Development and Characterization of Novel Site Specific Hollow Floating Microspheres Bearing 5-Fu for Stomach Targeting

2014 ◽  
Vol 2014 ◽  
pp. 1-11 ◽  
Author(s):  
Peeyush Bhardwaj ◽  
Deepti Chaurasia ◽  
Ranjit Singh ◽  
Anoop Swarup
Keyword(s):  
Drug Release ◽  
Entrapment Efficiency ◽  
Gastric Fluid ◽  
Simulated Gastric Fluid ◽  
Drug Bioavailability ◽  
Gastric Residence Time ◽  
Evaporation Technique ◽  
Multiple Unit

Multiple-unit-type oral floating hollow microspheres of 5-fluorouracil (5-Fu) were developed using modified solvent evaporation technique to prolong gastric residence time, to target stomach cancer, and to increase drug bioavailability. The prepared microspheres were characterized for micromeritic properties, floating behavior, entrapment efficiency, and scanning electron microscopy (SEM). Thein vitrodrug release and floating behavior were studied in simulated gastric fluid (SGF) at pH 1.2. The yield of microspheres was obtained up to84.46±6.47%. Microspheres showed passable flow properties. Based on optical microscopy, particle size was found to be ranging from158.65±12.02to198.67±17.45 μm. SEM confirmed spherical size, perforated smooth surface, and a hollow cavity inside the microspheres. Different kinetic models for drug release were also applied on selected batches.

Formulation and In vitro Characterization of Floating Gel Beads of Metformin Hydrochloride

2014 ◽  
Vol 7 (1) ◽  
pp. 2356-2362
Author(s):  
Yasir Mohd ◽  
A Bhattacharyya ◽  
M Bajpai ◽  
M Yasir ◽  
M Asif
Keyword(s):  
Sustained Release ◽  
Sodium Alginate ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Gastric Fluid ◽  
Simulated Gastric Fluid ◽  
Metformin Hydrochloride ◽  
Gel Beads ◽  
Formulation Parameters

A floating type dosage form, gel beads of metformin hydrochloride was prepared by emulsification gelation technique. The gel bead was formed by mixing the polymer in water, oil phase and it was extruded in the calcium chloride solution as curing agent. The formulation parameters optimized were polymer ratio, concentration of oil, curing time on drug content, floating lag time, morphology, swelling of beads and release kinetics.The scanning electron photomicrographs revealed morphology of beads. The size of beads was measured. Entrapment efficiency of drug loaded beads was found to be over 90%. In vitro release of metformin hydrochloride from alginate–pectin beads into simulated gastric fluid at 37 ºC showed no significant burst effect. The cumulative release reached above 74.71 ± 4.15% in about 12h. The use of sodium alginate and combinations of sodium alginate with pectin were used to study the effect on the sustained release of the drug from the formed beads. It was found that sodium alginate was not sufficient to sustain the drug release at gastric pH (fed condition). Appropriate combination of alginate and pectin could provide the sustained release of drug. Floating gel beads formulation provides an alternative delivery for metformin in diabetes treatment.

scholarly journals Characterization of alginate extracted from Sargassum latifolium and its use in Chlorella vulgaris growth promotion and riboflavin drug delivery

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Shimaa R. Dalal ◽  
Mervat H. Hussein ◽  
Noura El-Ahmady El-Naggar ◽  
Sahar I. Mostafa ◽  
Sami A. Shaaban-Dessuuki
Keyword(s):  
Chlorella Vulgaris ◽  
Growth Promotion ◽  
Crystallinity Index ◽  
Entrapment Efficiency ◽  
Gastric Fluid ◽  
Simulated Gastric Fluid ◽  
Guaiacol Peroxidase ◽  
Growth Promoter ◽  
Total Carbohydrates ◽  
Drug Entrapment Efficiency

AbstractAlginates derived from macroalgae have been widely used in a variety of applications due to their stability, biodegradability and biocompatibility. Alginate was extracted from Egyptian Sargassum latifolium thallus yielding 17.5% w/w. The chemical composition of S. latifolium is rich in total sugars (41.08%) and uronic acids (47.4%); while, proteins, lipids and sulfates contents are 4.61, 1.13 and 0.09%, respectively. NMR, FTIR and TGA analyses were also performed. Crystallinity index (0.334) indicates alginate semicrystalline nature. Sodium alginate hydrolysate was evaluated as Chlorella vulgaris growth promoter. The highest stimulation (0.7 g/L biomass) was achieved by using 0.3 g/L alginate hydrolysate supplementation. The highest total soluble proteins and total carbohydrates were 179.22 mg/g dry wt and 620.33 mg/g dry wt, respectively. The highest total phenolics content (27.697 mg/g dry wt.), guaiacol peroxidase activity (2.899 µmol min−1 g−1) were recorded also to 0.3 g/L alginate hydrolysate supplementation. Riboflavin-entrapped barium alginate-Arabic gum polymeric matrix (beads) was formulated to achieve 89.15% optimum drug entrapment efficiency (EE%). All formulations exhibited prolonged riboflavin release over 120 min in simulated gastric fluid, followed Higuchi model (R2 = 0.962–0.887) and Korsmeyer–Peppas model with Fickian release (n ranges from 0.204 to 0.3885).

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