scholarly journals Zein Beta-Cyclodextrin Micropowders for Iron Bisglycinate Delivery

Pharmaceutics ◽  
2020 ◽  
Vol 12 (1) ◽  
pp. 60 ◽  
Author(s):  
Diletta Esposito ◽  
Giovanni Dal Poggetto ◽  
Aurélie Demont ◽  
Nicolai Kraut ◽  
Agnese Miro ◽  
...  
Keyword(s):  
Oral Delivery ◽  
Raw Materials ◽  
Gastric Fluid ◽  
Simulated Gastric Fluid ◽  
Scanning Calorimetry ◽  
Simulated Intestinal Fluid ◽  
Food Ingredients ◽  
Rational Combination ◽  
Novel Strategy ◽  
Micro Technology

Given the limited number of materials available to design delivery platforms for nutrients, the rational combination of raw materials already approved as food ingredients and their processing through nano-micro technology can offer a unique tool for innovation. Here, we propose a nano-in-micro strategy to produce powders based on the hydrophobic protein zein, useful for the oral delivery of a hydrophilic iron source (iron bisglycinate) in anaemic patients. Iron-loaded powders were prepared through a two-step strategy consisting in the formation of a zein pseudolatex followed by a spray-drying step. To extend the manipulation space for zein and entrap iron bisglycinate, β-cyclodextrin (βCD) was selected as helping excipient. Addition of βCD allowed iron loading in the pseudolatex and greatly increased product yields after the drying process as compared to zein alone. Iron-loaded micro-sized powders were characterised by attenuated total reflectance–Fourier transform infrared (ATR-FTIR) spectra, thermogravimetric analysis (TGA), and differential scanning calorimetry (DSC) to elucidate the role of βCD as a compatibilizer for the zein–iron system. Remarkably, micropowders released only 20% of FeBIS in a simulated gastric fluid, whereas release in a simulated intestinal fluid was almost completed in 7 h. In summary, βCD association to zein is a novel strategy to expand applications in the oral delivery of iron bisglycinate and, prospectively, to micronutrient chelates.

scholarly journals Microencapsulation of Bacteriophage Felix O1 into Chitosan-Alginate Microspheres for Oral Delivery

2008 ◽  
Vol 74 (15) ◽  
pp. 4799-4805 ◽  
Author(s):  
Yongsheng Ma ◽  
Jennifer C. Pacan ◽  
Qi Wang ◽  
Yongping Xu ◽  
Xiaoqing Huang ◽  
...  
Keyword(s):  
Oral Delivery ◽  
Gastric Fluid ◽  
Viable Count ◽  
Simulated Gastric Fluid ◽  
Intestinal Fluid ◽  
Simulated Intestinal Fluid ◽  
Testing Period ◽  
Acidic Environments ◽  
Free Phage

ABSTRACT This paper reports the development of microencapsulated bacteriophage Felix O1 for oral delivery using a chitosan-alginate-CaCl2 system. In vitro studies were used to determine the effects of simulated gastric fluid (SGF) and bile salts on the viability of free and encapsulated phage. Free phage Felix O1 was found to be extremely sensitive to acidic environments and was not detectable after a 5-min exposure to pHs below 3.7. In contrast, the number of microencapsulated phage decreased by 0.67 log units only, even at pH 2.4, for the same period of incubation. The viable count of microencapsulated phage decreased only 2.58 log units during a 1-h exposure to SGF with pepsin at pH 2.4. After 3 h of incubation in 1 and 2% bile solutions, the free phage count decreased by 1.29 and 1.67 log units, respectively, while the viability of encapsulated phage was fully maintained. Encapsulated phage was completely released from the microspheres upon exposure to simulated intestinal fluid (pH 6.8) within 6 h. The encapsulated phage in wet microspheres retained full viability when stored at 4°C for the duration of the testing period (6 weeks). With the use of trehalose as a stabilizing agent, the microencapsulated phage in dried form had a 12.6% survival rate after storage for 6 weeks. The current encapsulation technique enables a large proportion of bacteriophage Felix O1 to remain bioactive in a simulated gastrointestinal tract environment, which indicates that these microspheres may facilitate delivery of therapeutic phage to the gut.

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

Pharmaceutics ◽  
2019 ◽  
Vol 11 (6) ◽  
pp. 270
Author(s):  
Imran Saleem ◽  
Allan G. A. Coombes ◽  
Mark A. Chambers
Keyword(s):  
Oral Delivery ◽  
Freeze Drying ◽  
Gastric Fluid ◽  
Powder Compaction ◽  
Bcg Vaccine ◽  
Simulated Gastric Fluid ◽  
Physical Damage ◽  
Simulated Intestinal Fluid ◽  
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 the 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 phosphate-buffered saline (PBS), containing Tween® 80, with and without the addition of mannitol or trehalose. Samples were frozen at −20 °C, 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 simulated intestinal fluid (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.

Characterization and Drug Release Control Ability of Chitosan/Lovastatin Particles Coated by Alginate

2020 ◽  
Vol 20 (12) ◽  
pp. 7347-7355
Author(s):  
Dam Xuan Thang ◽  
Nguyen Thuy Chinh ◽  
Bach Long Giang ◽  
Hoang Tran Dung ◽  
C. I. Sathish ◽  
...  
Keyword(s):  
Drug Release ◽  
Liquid Solution ◽  
Gastric Fluid ◽  
Simulated Gastric Fluid ◽  
Drug Release Profile ◽  
Scanning Calorimetry ◽  
Simulated Intestinal Fluid ◽  
Coated Particles ◽  
Structure Morphology ◽  
3D Printing Technique

We report on the coating of chitosan/lovastatin particles with a liquid solution of alginate using a 3D printing technique. The prepared particles are characterized by Scanning Electronic Microscopy, Infrared Spectroscopy, Dynamic Light Scattering, Differential Scanning Calorimetry, and Ultraviolet-Visible Spectroscopy. Characterization results reveal that the coating of alginate makes a considerable difference in the structure, morphology, size distribution and zeta potential of the chitosan/lovastatin particles, and the size of the coated particles is increased after the coating. We also demonstrate the drug release ability of the chitosan/lovastatin particles in simulated gastric fluid and controlled in simulated intestinal fluid. Drug release study reveals that the drug release profile of the coated particles varies significantly with the pH of the solution and the coating process significantly reduces the rate of release of the drug. We also report that the bioavailability of lovastatin particles can be improved by coating with the biopolymer layers.

scholarly journals Chitosan-Carrageenan Polyelectrolyte Complex for the Delivery of Protein Drugs

2013 ◽  
Vol 2013 ◽  
pp. 1-6 ◽  
Author(s):  
Cunben Li ◽  
San Hein ◽  
Kean Wang
Keyword(s):  
Oral Delivery ◽  
Digestive Enzymes ◽  
Polyelectrolyte Complex ◽  
Ph Value ◽  
Release Kinetics ◽  
Gastric Fluid ◽  
Simulated Gastric Fluid ◽  
Protein Drugs ◽  
Simulated Intestinal Fluid ◽  
Speed Up

A chitosan-carrageenan polyelectrolyte complex (PEC) was prepared by salt induced impeding of polyplex formation method and was encapsulated with bovine serum albumin (BSA) to study the potential to be tailored to the pH responsive oral delivery of protein drugs. The FTIR spectra showed the successful formation of the PEC under the experimental condition. The release kinetics of BSA from the PEC was studied in the simulated gastrointestinal fluids with and without digestive enzymes. The prepared PEC showed the nature of pH-sensitivity. A typical controlled release of BSA from the PEC (180 μg of BSA from 3 mg of PEC) was obtained in the simulated intestinal fluid (SIF, pH 7.5), which was due to the significant swelling and disintegration of PEC, but little amount of BSA was released (11 μg of BSA from 3 mg of PEC) in the simulated gastric fluid (SGF, pH 1.2), confirming acidic stability of the prepared PEC. The presence of digestive enzymes was found not to affect the response of PEC to ambient pH value, but to speed up the release of BSA from carriers.

scholarly journals Fabrication of Multi-Layered Microspheres Based on Phase Separation for Drug Delivery

Micromachines ◽  
2021 ◽  
Vol 12 (6) ◽  
pp. 723
Author(s):  
He Xia ◽  
Ang Li ◽  
Jia Man ◽  
Jianyong Li ◽  
Jianfeng Li
Keyword(s):  
Aqueous Solution ◽  
Phase Separation ◽  
Gastric Fluid ◽  
Simulated Gastric Fluid ◽  
Sustained Drug Release ◽  
Simulated Intestinal Fluid ◽  
Glycol Diacrylate ◽  
Emulsion Droplets ◽  
Collection Tube ◽  
Poly Ethylene

In this work, we used a co-flow microfluidic device with an injection and a collection tube to generate droplets with different layers due to phase separation. The phase separation system consisted of poly(ethylene glycol) diacrylate 700 (PEGDA 700), PEGDA 250, and sodium alginate aqueous solution. When the mixture droplets formed in the outer phase, PEGDA 700 in the droplets would transfer into the outer aqueous solution, while PEGDA 250 still stayed in the initial droplet, breaking the miscibility equilibrium of the mixture and triggering the phase separation. As the phase separation proceeded, new cores emerged in the droplets, gradually forming the second and third layers. Emulsion droplets with different layers were polymerized under ultraviolet (UV) irradiation at different stages of phase separation to obtain microspheres. Microspheres with different layers showed various release behaviors in simulated gastric fluid (SGF) and simulated intestinal fluid (SIF). The release rate decreased with the increase in the number of layers, which showed a potential application in sustained drug release.

Preparation and Characterization of Cefradine/Montmorillionite Composites

2012 ◽  
Vol 560-561 ◽  
pp. 434-437 ◽  
Author(s):  
Lan Wang ◽  
Wen Ji Guo ◽  
Yan Zhao Zhao
Keyword(s):  
Gastric Fluid ◽  
Simulated Gastric Fluid ◽  
X Ray Diffraction ◽  
Simulated Intestinal Fluid ◽  
Solution Intercalation ◽  
Method Of Solution ◽  
Ft Ir ◽  
In The Beginning ◽  
Ft Ir Spectroscopy

The objective of this paper was to prepare the composite of crefradine/montmorillionite in the method of solution intercalation. The drug load and intercalation rate varied with the drug concentration. X-ray diffraction (XRD), Fourier transformed infrared (FT-IR) Spectroscopy, and thermal analysis (TG-DSC) were applied to characterize composite mentioned above. Together with drug release tests, results indicate cefradine intercalated into montmorillionite.The release profiles of cefradine/MMT in simulated gastric fluid (pH 1.2) and simulated intestinal fluid (pH 7.4) at 37°Cduring 10h are shown in Fig. 4. The amount of cefradine in the beginning 2h came up to 35% and 50%, and in the following time, cefradine released slowly. The release behaviors met the requirements of sustained release.

Fusion as an Approach to Enhance Dissolution Rate of a Poorly Water-Soluble Drug (Curcurmin)

2011 ◽  
Vol 393-395 ◽  
pp. 119-122
Author(s):  
Dong Hua Wan ◽  
Fen Lin ◽  
Qu Xiang Liao
Keyword(s):  
Dissolution Rate ◽  
Drug Loading ◽  
Solid Dispersions ◽  
Gastric Fluid ◽  
Molecular State ◽  
Water Soluble ◽  
Drug Dissolution ◽  
Simulated Gastric Fluid ◽  
Scanning Calorimetry ◽  
Rate Improvement

It’s well known that curcumin is practically insoluble in water. Therefore, to improve the drug dissolution rate, fusion approach was employed to prepare curcumin solid dispersions (SDs) in the carrier Pluronic F68 with three different drug loads. The dissolution rate of curcumin from the SDs was measured at simulated gastric fluid. The concentration of the dissolved drug in the medium was determined by HPLC. The dissolution rates of the formulations were dependent on the drug loading in SDs. 92.2% CUR was dissolved in 10 min from the SDs with 8.97% drug load, whereas the amounts of drug released were 65.8% and 84.2% within 120 min from the SDs with 18.9% and 29.0% drug loads, respectively. The Fourier transform infrared spectra indicated hydrogen bond between the drug and carrier. Furthermore, their physicochemical properties were well investigated using differential scanning calorimetry and X-ray diffraction. In the dispersions containing 8.97% CUR, the drug was in the molecular state. At a composition of approximately 18.9%, CUR was dispersed as micro-fine crystals. These interesting results indicate that the physical states of the drug in the carrier, which are governed by the drug loading, can affect the dissolution rate improvement.

scholarly journals THE USE OF CLINOPTILOLITES AS CARRIER OF METFORMIN HYDROCHLORIDE IN DRUG DELIVERY SYSTEM: IN VITRO DRUG RELEASE STUDY

2018 ◽  
Vol 11 (11) ◽  
pp. 285
Author(s):  
Putra Imwa ◽  
Kusumawati Igaw
Keyword(s):  
Drug Release ◽  
Gastric Fluid ◽  
Simulated Gastric Fluid ◽  
Metformin Hydrochloride ◽  
Simulated Intestinal Fluid ◽  
In Vitro Drug Release ◽  
Encapsulation Process ◽  
N2 Sorption ◽  
Metformin Hcl

Objective: As an antidiabetic drug, metformin hydrochloride (HCl) has been well known to possess low oral bioavailability and short half-life. In this study, we prepared the drug delivery system (DDS) of metformin HCl and clinoptilolite as its carrier. The in vitro drug release profile was further investigated.Methods: DDS was made by encapsulating metformin HCl on clinoptilolite using the wet impregnation method at various pH and initial concentration of metformin HCl. Fourier transform infrared spectrometer (FTIR), X-ray diffractometer (XRD), and N2 Sorption Analyzer were used to characterize the as-synthesized DDS. Drug release study was conducted by stirring the DDS in simulated gastric fluid and simulated intestinal fluid over 12 h.Results: The encapsulation process was achieved optimally at pH 7.0 and initial concentration of metformin HCl of 300 mg/l (CLI2-300 denoted DDS). The results of FTIR and N2 sorption analyzer confirmed the existence of metformin HCl on clinoptilolites. Meanwhile, the XRD result showed that the crystallinity of clinoptilolites remained unchanged after the encapsulation process. The cumulative drug release in the simulated gastric fluid was found to be higher than that in the simulated intestinal fluid, which indicated the potent influence of pH on the release properties of the drugs. The drug release kinetics of metformin HCl from clinoptilolite was best fitted into the Korsmeyer-Peppas model with non-Fickian transport mechanism.Conclusion: We found that clinoptilolite was suitable for DDS application, particularly as a carrier of metformin HCl.

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 Release Activity of Encapsulated Lactobacillus plantarum NBRC 3070 in Optimum Alginate - Aloe vera Matrices during Simulated Gastric Fluid (SGF) and Simulated Intestinal Fluid (SIF) Exposure

2017 ◽  
Vol 5 (2) ◽  
Author(s):  
Nur Syahirah Sallehudin ◽  
Khalilah Abdul Khalil ◽  
Maslinda Musa ◽  
Hifa Nazirah Mohd Yazid ◽  
Anida Yusof
Keyword(s):  
Aloe Vera ◽  
Clinical Results ◽  
Gastric Fluid ◽  
Alginate Beads ◽  
Simulated Gastric Fluid ◽  
Intestinal Fluid ◽  
Simulated Intestinal Fluid ◽  
Encapsulated Cells ◽  
Aloe Vera Gel ◽  
Encapsulation Process

Probiotic encapsulation approach has the potential to protect microorganisms and to deliver them into the gut. Because of the promising preclinical and clinical results, probiotics have been incorporated into a range of products. However, there are still many challenges to overcome with respect to the encapsulation process and the conditions prevailing in the gut. Thus in this study, the release activity of encapsulated L. plantarum NBRC 3070 and Aloe vera gel within alginate coated chitosan matrices during simulated gastric fluid (SGF) and simulated intestinal fluid (SIF) exposure were investigated. There were four groups of beads prepared in this study: 1) Encapsulated probiotic and Aloe vera within alginate beads (chitosan coated), 2) Encapsulated probiotic within alginate beads (chitosan coated), 3) Encapsulated probiotic and Aloe vera within alginate beads (uncoated) and 4) Encapsulated probiotic alone within alginate beads (uncoated). Encapsulation process was carried out using extrusion method. The optimized composition of alginate matrix (1.34% w/v) and Aloe vera gel (1.99% w/v) were used.  In order to investigate their release activity, all beads were exposed in Simulated Gastric (SGF) at pH 2.5 and Simulated Intestinal Fluids (SIF) at pH 6.5 for 120 min and 270 min, respectively. Based on the findings, alginate-Aloe vera beads with chitosan coated was able to protect L. plantarum NBRC 3070 during SGF exposure with only 1 log10 cfu/mL reduction. The presence of Aloe vera gel in the beads improved the survivability of the cells. Encapsulated cells were observed successfully slow released of cells from the beads after exposure in SIF. Scan Electron Microscope (SEM) result had shown that cross link activity of the optimum alginate-Aloe vera with chitosan coating resulted in better survival of cells after simulated gastro and able to deliver sufficient probiotic dose to intestinal region. The combinations were able to improve encapsulated cells survivability during low acidic environment passage and release activity into the intestinal target region.   

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