scholarly journals Bolalipid-Doped Liposomes: Can Bolalipids Increase the Integrity of Liposomes Exposed to Gastrointestinal Fluids?

Pharmaceutics ◽  
2019 ◽  
Vol 11 (12) ◽  
pp. 646 ◽  
Author(s):  
Sindy Müller ◽  
Kai Gruhle ◽  
Annette Meister ◽  
Gerd Hause ◽  
Simon Drescher
Keyword(s):  
Oral Drug Delivery ◽  
Lipid Vesicles ◽  
Gastric Fluid ◽  
Simulated Gastric Fluid ◽  
Oral Drug ◽  
Single Chain ◽  
Drug Delivery Vehicles ◽  
The Stability ◽  
Archaeal Lipids ◽  
Calcein Release

The use of archaeal lipids and their artificial analogues, also known as bolalipids, represents a promising approach for the stabilization of classical lipid vesicles for oral application. In a previous study, we investigated the mixing behavior of three single-chain alkyl-branched bolalipids PC-C32(1,32Cn)-PC (n = 3, 6, 9) with either saturated or unsaturated phosphatidyl-cholines. We proved, that the bolalipids PC-C32(1,32C6)-PC and PC-C32(1,32C9)-PC show miscibility with 1-palmitoyl-2-oleoyl-sn-glycero-3-phosphocholine (POPC) and 1,2-dioleoyl-sn-glycero-3-phosphocholine (DOPC). In the present work, we extended our vesicle system to natural lipid mixtures using phosphatidylcholine from soy beans, and we investigated the effect of incorporated bolalipids on the integrity of these mixed liposomes (bolasomes) in different gastrointestinal fluids using a dithionite assay and a calcein release assay in combination with particle size measurements. Finally, we also studied the retention of calcein within the bolasomes during freeze-drying. As a main result, we could show that in particular PC-C32(1,32C6)-PC is able to increase the stability of bolasomes in simulated gastric fluid—a prerequisite for the further use of liposomes as oral drug delivery vehicles.

Evaluation of Ibuprofen/Montmorillonite Nano-Clay Composites as an Oral Drug Delivery System and In-Vitro Drug Release Performance

2021 ◽  
Vol 21 (7) ◽  
pp. 3651-3655
Author(s):  
Woo Chang Kwon ◽  
Moonhee Choi ◽  
Kyung Chan Kang ◽  
Dong Hyun Kim
Keyword(s):  
Oral Drug Delivery ◽  
Gastric Fluid ◽  
Controlled Delivery ◽  
Simulated Gastric Fluid ◽  
Oral Drug ◽  
Simulated Intestinal Fluid ◽  
Oral Drug Delivery System ◽  
Nano Clay ◽  
Best Fitting

A formulation for controlled delivery of ibuprofen (IBU) involving montmorillonite (MMT) nanoclays has been proposed. The present work has investigated the beneficial effect of MMT in improving controlled delivery of IBU. The intercalation of IBU into the interlayer of MMT was studied under different processing conditions such as reaction time and initial concentration of IBU. To characterize the IBU/MMT composites, X-ray diffraction (XRD) and Fourier transform infrared spectra (FTIR) were performed. The release behavior of IBU from IBU/MMT composites have been investigated under vitro conditions using buffer media of simulated gastric fluid (pH 1.2) and simulated intestinal fluid (pH 7.4) at 37 °C. Controlled release of IBU from IBU/MMT composite has been observed during in vitro release experiments. Different mathematical models were used for fitting our experimental results, among them the best fitting was found for Higuchi equation based on the parabolic diffusion process.

Preparation and Charaterization of DAM-1 type Materials

2000 ◽  
Vol 662 ◽  
Author(s):  
Decio Coutinho ◽  
Ying Ma ◽  
Kenneth J. Balkus
Keyword(s):  
Vitamin E ◽  
Oral Delivery ◽  
Oral Drug Delivery ◽  
Gastric Fluid ◽  
Simulated Gastric Fluid ◽  
Oral Drug ◽  
Preliminary Evaluation ◽  
Structure Directing Agent ◽  
Vitamin E Tpgs ◽  
Gel Composition

AbstractVitamin E TPGS was found to be an effective structure-directing agent for the preparation of both hexagonal all silica DAM-1 and the alumina analog, Al-DAM-1. These free flowing powders offer many advantages in the handling and oral delivery of the sticky vitamin E TPGS. Upon exposure to simulated gastric fluid, the Al-DAM-1 host molecular sieve is dissolved releasing the vitamin E TPGS. As much as 0.6 grams of vitamin E TPGS can be immobilized into 1 gram of Al-DAM-1. Vitamin E TPGS also templates highly ordered mesoporous DAM-1 with tunable morphologies such as hexagons (various lengths), gyroids, rods, spheres and discoids depending upon the temperature and gel composition. Characterization of these composites as well as a preliminary evaluation of Al-DAM-1 as an oral drug delivery system under physiological conditions is presented.

scholarly journals Synthesis and Characterization of Thiolated Gum Ghatti as a Novel Excipient: Development of Compression Coated Mu-Coadhesive Tablets of Domperidone

2021 ◽  
Author(s):  
Vivek Puri ◽  
Ameya Sharma ◽  
Pradeep Kumar ◽  
Inderbir Singh ◽  
Kampanart Huanbutta
Keyword(s):  
Drug Delivery ◽  
Oral Drug Delivery ◽  
Ex Vivo ◽  
Gastric Fluid ◽  
Hydroxyl Group ◽  
Simulated Gastric Fluid ◽  
Oral Drug ◽  
Ester Formation ◽  
In Silico Studies ◽  
Gum Ghatti

Background: Mucoadhesive polymers represent a major part of site-specific and localized retention strategies in oral drug delivery. Present research was designed to synthesize and characterize a novel mucoadhesive carbohydrate polymer (thiolated gum ghatti; TGG) which was further employed to fabricate mucoadhesive tablets of domperidone using an industrially viable compression coating technique. Methods: Thiolation of gum ghatti was achieved by the ester formation (esterification) between hydroxyl group and carboxyl group of gum ghatti and thioglycolic acid. Results: TGG was characterized by various physico-chemical techniques such as FTIR, XRD, SEM and DSC techniques. In rheological studies, the observed viscosities of pure gum-mucin were 45.45 and 71.75 mPas and that of thiolated gum were 78.7 and 112.58 mPas respectively in water and simulated gastric fluid. Signifi-cant increase in viscosity for thiolated gum may be attributed to increased macromolecular interactions responsible for enhanced mucoadhesive potential of thiolated gum. In-silico studies corroborate the role of mucin gum interaction and energetic stabilization for en-hanced mucoadhesion properties of thiolated gum. Ex-vivo mucoadhesion strength of gum ghatti and thiolated gum ghatti coated tablets was found to be ranging between 4.67± 0.79 to 8.99± 0.75 g and 11.76± 1.34 to 18.83± 2.07 g respectively. Conclusion: Thiolated gum ghatti may be regarded as a promising polymer for developing different mucoadhesive drug delivery systems.

scholarly journals Synthesis and characterization of oral drug delivery, a pH – sensitive silver nanocomposite based on sodium alginate extracted from Sargassum asperifolium collected from Jazan coasts, KSA

2019 ◽  
Author(s):  
Fatimah. A. Agili ◽  
Sahera. F. Mohamed
Keyword(s):  
Electron Microscope ◽  
Drug Release ◽  
Sodium Alginate ◽  
Oral Drug Delivery ◽  
Drug Carrier ◽  
Gastric Fluid ◽  
Ph Sensitive ◽  
Oral Drug ◽  
Release Mechanism ◽  
X Ray

AbstractThe pH-sensitive nanocomposite composed of sodium alginate/ Pectin/ Tannic acid – silver SA/Pec/TA-Ag was prepared using microwave irradiation and employed as a carrier for Propranolol drug. Physico-chemical characteristics of the prepared systems using Fourier Transform Infrared Spectroscopy (FTIR), X-ray Diffraction (XRD), Field Emission Scanning Electron Microscope (FESEM), High-Resolution Transmission Electron Microscope (HRTEM), Dynamic light Scattering instrument (DLS), and Energy Dispersive X-Ray Analysis (EDX). The percentage drug release was 96% at pH 7.4 within 420 min. The drug release data was fitted into different kinetic models included zero order, First order, Higuchi and Ritger-Peppas model. The release mechanism is non-Fickian character where it controlled by diffusion and relaxation of polymer chains. It can be concluded that SA/Pec/TA-Ag nanocomposite is candidate for the oral drug carrier specific for intestinal system and has stability against gastric fluid.

scholarly journals Long-Term Stability of the Electronic Sensor Component of a Digital Pill System in Real-World Storage Settings

2021 ◽  
pp. 875512252098521
Author(s):  
Peter R. Chai ◽  
Georgia Goodman ◽  
Majo J. Bustamante ◽  
Yassir Mohamed ◽  
Jose Castillo-Mancilla ◽  
...  
Keyword(s):  
Clinical Trial ◽  
Gastric Fluid ◽  
Simulated Gastric Fluid ◽  
Once Daily ◽  
Long Term Stability ◽  
Long Term Storage ◽  
System Requirements ◽  
The Stability ◽  
Term Storage

Background: Digital pill systems comprise an ingestible sensor integrated into a gelatin capsule that overencapsulates medication allowing real-time measures of medication ingestion. These systems may improve the manner in which medication adherence can be assessed and supported. Objective: In this investigation, we tested the durability of the ingestible sensor as part of a clinical trial to measure the feasibility and acceptability of the system to measure adherence to once daily tenofovir disoproxil fumarate/emtricitabine (NCT03842436). Methods: Digital pills not dispensed during the study were stored in a pharmacy. Seventeen sensors were selected from digital pills stored for at least 12 months and activated in a simulated gastric environment. A radiofrequency spectrum analyzer and the reader device used in the clinical trial to capture ingestion events were used to measure activation of emitters. A passing evaluation was defined as an energized emitter within 30 minutes of immersion, ability to broadcast a signal for 10 minutes, and successful acquisition by the reader. Results: All ingestible sensors passed the stability test. Mean activation time in simulated gastric fluid was 3.33 minutes (SD = 1.47); emitters remained active for a mean of 47.72 minutes (SD = 1.78). These parameters matched guidelines defined in the ID-Cap system requirements for use in patients. Conclusions: Ingestible sensor components of the ID-Cap system were therefore stable after long-term storage.

scholarly journals Stability of Principal Hydrolysable Tannins from Trapa taiwanensis Hulls

Molecules ◽  
2019 ◽  
Vol 24 (2) ◽  
pp. 365 ◽  
Author(s):  
Ching-Chiung Wang ◽  
Hsyeh-Fang Chen ◽  
Jin-Yi Wu ◽  
Lih-Geeng Chen
Keyword(s):  
Protective Effect ◽  
Water Solution ◽  
Gastric Fluid ◽  
Simulated Gastric Fluid ◽  
Intestinal Fluid ◽  
Buffer Solution ◽  
Simulated Intestinal Fluid ◽  
Hydrolysable Tannins ◽  
The Stability ◽  
Tellimagrandin Ii

The fruit and hulls of the water caltrop (Trapa taiwanensis Nakai) are used as hepatoprotective herbal tea ingredients in Taiwan. The stability of hydrolysable tannins in herbal drinks has rarely been reported. In the present study, two hydrolysable tannins, tellimagrandin II (TGII) and 1,2,3,4,6-pentagalloylglucopyranose (PGG), were isolated from water caltrop hulls. The stability of the two compounds was evaluated by treatment with various pH buffer solutions, simulated gastric fluid and intestinal fluid, different temperatures, and photo-irradiation at 352 nm in different solvents. Results showed that TGII and PGG were more stable in a pH 2.0 buffer solution (with 91.88% remaining) and in a water solution with 352 nm irradiation (with 95% remaining). TGII and PGG were more stable in methanol or ethanol solutions (with >93.69% remaining) than in an aqueous solution (with <43.52% remaining) at 100 °C. In simulated gastric fluid, more than 96% of the hydrolysable tannins remained after incubation at 37 °C for 4 h. However, these hydrolysable tannins were unstable in simulated intestinal fluid, as after incubation at 37 °C for 9 h, the content of TGII had decreased to 31.40% and of PGG to 12.46%. The synthetic antioxidants, butyl hydroxy anisole (BHA), di-butyl hydroxy toluene (BHT), and propyl gallate, did not exhibit photoprotective effects on these hydrolysable tannins. However, catechin, a natural antioxidant, displayed a weak photoprotective effect. Ascorbic acid had a short-term thermal-protective effect but not a long-term protective effect. The different stability properties of hydrolysable tannins in solutions can be used in the development of related herbal teas in the future.

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>

Nanoemulsion as Oral Drug Delivery - A Review

2020 ◽  
Vol 12 (1) ◽  
pp. 4-15 ◽  
Author(s):  
Khaleel Basha Sabjan ◽  
Syed Muzammil Munawar ◽  
Dhandayuthabani Rajendiran ◽  
Sugantha Kumari Vinoji ◽  
Kaviyarasu Kasinathan
Keyword(s):  
Drug Delivery ◽  
Oral Drug Delivery ◽  
Drug Stability ◽  
Drug Carriers ◽  
Therapeutic Agents ◽  
Oral Drug ◽  
Advantages And Disadvantages ◽  
Insoluble Drugs ◽  
The Stability ◽  
Near Future

Background: Objective:: The stability and delivery of drugs remain one of the key hurdles in the present situation. The present study depends on the design of a novel nanoemulsion drugdelivery system that would encapsulate a drug and to improve drug stability. The charisma of nanotechnology is majorly due to the smallest particle size at the nanoscale. Methods: Nanoemulsions attention is focused on emphasizing formulation aspect, method of preparation characterization techniques, evaluation parameters and various application of the nanoemulsions, several techniques to be used for the preparation of nanoemulsions like microfluidization, high-pressure homogenization, low energy emulsification and solvent evaporation method and their parameters to be characterized. Results: The design of effective formulations for drugs is being applied to enhance the solubility and bioavailability of water-insoluble drugs. The nanosized droplets have led to considerable attraction for this formulation, for the delivery of hydrophilic as well as hydrophobic drugs as drug carriers because of their improved drug solubilization capacity, long shelf life, ease of preparation and improvement of bioavailability of drugs. Conclusion: The application of these nanoformulation preparations, limitations, their advantages and disadvantages as nanoemulsions will solve the various problems that current therapeutic agents face and has opened a new scenario to formulate nanoemulsions with various therapeutic agents with heightened competence along with oral drug delivery to treat diseases in the near future.

Engineering Silica Particles as Oral Drug Delivery Vehicles

2008 ◽  
Vol 14 (18) ◽  
pp. 1821-1831 ◽  
Author(s):  
S. Rigby ◽  
M. Fairhead ◽  
C. van der Walle
Keyword(s):  
Drug Delivery ◽  
Oral Drug Delivery ◽  
Silica Particles ◽  
Oral Drug ◽  
Drug Delivery Vehicles ◽  
Delivery Vehicles
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