scholarly journals Entrapment of Hydrophilic and Hydrophobic Molecules in Beads Prepared from Isolated Denatured Whey Protein

Pharmaceutics ◽  
2021 ◽  
Vol 13 (7) ◽  
pp. 1001
Author(s):  
Joanne Heade ◽  
Robert Kent ◽  
Sinead B. Bleiel ◽  
David J. Brayden
Keyword(s):  
Whey Protein ◽  
Delivery System ◽  
Oral Delivery ◽  
Gastric Fluid ◽  
Oral Route ◽  
Protein Isolate ◽  
Water Soluble ◽  
Simulated Gastric Fluid ◽  
Sodium Fluorescein ◽  
Fast Green

The oral route of administration is by far the most convenient route, especially in the treatment of chronic conditions. However, many therapeutics present formulation difficulties which make them unsuitable for oral delivery. Recently, we synthesized a denatured whey protein isolate (dWPI) bead entrapped with insulin. Our present goal was to assess the suitability of this delivery system to the delivery of other potential molecules, both hydrophilic and hydrophobic. Beads of 1.2–1.5 mm in diameter were entrapped with four payloads representing a range of solubilities. The water-soluble payloads were sodium fluorescein (SF) and FITC dextran 4000 Da (FD4), while the hydrophobic ones were Fast Green and curcumin. Encapsulation efficiency (EE) was 73%, 84%, 70%, and 83% for SF, FD4, Fast Green, and curcumin-loaded beads, respectively. The corresponding loading capacity for each bead was 0.07%, 1.1%, 0.75%, and 1.1%, respectively. Each payload produced different release profiles in simulated gastric fluid (SGF) and simulated intestinal fluids (SIF). SF released steadily in both SGF and SIF. FD4 and curcumin release was not substantial in any buffers, while Fast Green release was low in SGF and high in SIF. The differences in release behaviour were likely due to the varying properties of the payloads. The effect of proteolysis on beads suggested that enzymatic degradation of the whey bead may promote payload release. The beads swelled rapidly in SGF compared to SIF, which likely contributed to the release from the beads, which was largely governed by solvent diffusion and polymer relaxation. Our results offer a systematic examination of the behaviour of hydrophilic and hydrophobic payloads in a dWPI delivery system. These beads may be further designed to orally deliver poorly permeable macromolecules and poorly soluble small molecules of pharmaceutical interest.

Floating Alginate Beads as Carriers for Self-Emulsifying System Containing Tetrahydrocurcumin

2012 ◽  
Vol 506 ◽  
pp. 517-520 ◽  
Author(s):  
S. Sriraksa ◽  
N. Sermkaew ◽  
S. Setthacheewakul ◽  
R. Wiwattanapatapee
Keyword(s):  
Oral Delivery ◽  
Aqueous Suspension ◽  
Aqueous Solubility ◽  
Gastric Fluid ◽  
Alginate Beads ◽  
Water Soluble ◽  
Simulated Gastric Fluid ◽  
Pore Former ◽  
Gastric Residence Time

Tetrahydrocurcumin (THC), one of the curcumin metabolites, exhibits pharmacological activities such as antioxidant, anti-inflammatory and anti-carcinogenic properties. However, the pharmacological effect of THC is limited due to its low aqueous solubility. Floating alginate beads containing self-emulsifying drug delivery system (SEDDS) of THC were developed to increase drug solubility and prolong gastric residence time. Use of different weight proportions of sodium alginate (Na-alg.), calcium chloride (CaCl2) and water soluble pore former (Polyvinylalcohol-polyethylene glycol copolymer; Kollicoat® IR) in bead formulations had different effects on the floating abilities and in vitro rate of THC release. The release profile of the optimized THC-SEDDS floating alginate beads (D3) indicated a significant increase in the dissolution rate of THC and provided a controlled release of THC over an 8 h period in a simulated gastric fluid. The release of about 80% of THC from the optimized beads as an o/w microemulsion with a particle size of less than 50 nm, compared to only 30 % by an aqueous suspension from the unformulated THC could be considerable greater absorbed. The self-emulsifying floating alginate beads may provide a useful solid dosage form for oral delivery of THC and other hydrophobic compounds.

Microsponges: An Overview

2017 ◽  
Vol 4 (4) ◽  
Author(s):  
Hamid Hussain ◽  
Divya Juyal ◽  
Archana Dhyani
Keyword(s):  
Controlled Release ◽  
Delivery System ◽  
Oral Delivery ◽  
Active Agent ◽  
Topical Delivery ◽  
Water Soluble ◽  
Wide Range ◽  
Porous Beads

Microsponge and Nanosponge delivery System was originally developed for topical delivery of drugs can also be used for controlled oral delivery of drugs using water soluble and bioerodible polymers. Microsponge delivery system (MDS) can entrap wide range of drugs and then release them onto the skin over a time by difussion mechanism to the skin. It is a unique technology for the controlled release of topical agents and consists of nano or micro porous beads loaded with active agent and also use for oral delivery of drugs using bioerodible polymers.

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 Formulation and Characterization of Eplerenone Nanoemulsion Liquisolids, An Oral Delivery System with Higher Release Rate and Improved Bioavailability

Pharmaceutics ◽  
2019 ◽  
Vol 11 (1) ◽  
pp. 40 ◽  
Author(s):  
Ahmed Khames
Keyword(s):  
Drug Release ◽  
Delivery System ◽  
Release Rate ◽  
Oral Delivery ◽  
Oral Route ◽  
Drug Release Rate ◽  
Enhanced Absorption ◽  
Oral Delivery System ◽  
Characterization Studies

Because Eplerenone (EPL) is a Biopharmaceutical Classification System (BCS) class-II drug and is prone to extensive liver degradation, it suffers from poor bioavailability after oral administration. This work aimed to prepare liquisolids loaded with EPL-nanoemulsions (EPL-NEs) that have a higher drug release rate and improved bioavailability by the oral route. Based on solubility studies, mixtures of Triacetin (oil) and Kolliphor EL/PEG 400 surfactant/co-surfactant (Smix) in different ratios were used to prepare EPL-NE systems, which were characterized and optimized for droplet size, zeta potential, polydispersity index (PDI), and drug content. Systems were then loaded onto liquisolid formulations and fully evaluated. A liquisolid formulation with better drug release and tableting properties was selected and compared to EPL-NEs and conventional EPL oral tablets in solid-state characterization studies and bioavailability studies in rabbits. Only five NEs prepared at 1:3, 1:2, and 3:1 Smix met the specified optimization criteria. The drug release rate from liquisolids was significantly increased (90% within 45 minutes). EPL-NE also showed significantly improved drug release but with a sustained pattern for four hours. Liquisolid bioavailability reached 2.1 and 1.2 relative to conventional tablets and EPL-NE. This suggests that the EPL-NE liquisolid is a promising oral delivery system with a higher drug release rate, enhanced absorption, decreased liver degradation, and improved bioavailability.

Maillard conjugation of whey protein isolate with water-soluble fraction of almond gum or flaxseed mucilage by dry heat treatment

2020 ◽  
Vol 128 ◽  
pp. 108779 ◽  
Author(s):  
Ali Sedaghat Doost ◽  
Maryam Nikbakht Nasrabadi ◽  
Sayed Amir Hossein Goli ◽  
Marleen van Troys ◽  
Peter Dubruel ◽  
...  
Keyword(s):  
Heat Treatment ◽  
Whey Protein ◽  
Soluble Fraction ◽  
Whey Protein Isolate ◽  
Protein Isolate ◽  
Water Soluble ◽  
Water Soluble Fraction ◽  
Dry Heat ◽  
Dry Heat Treatment

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.

Recent Advances in Nanosponges as Drug Delivery System

2013 ◽  
Vol 6 (1) ◽  
pp. 1934-1944 ◽  
Author(s):  
Uday B Bolmal ◽  
F V Manvi ◽  
Rajkumar Kotha ◽  
Sai Sowjanya Palla ◽  
Anusha Paladugu ◽  
...  
Keyword(s):  
Delivery System ◽  
Oral Delivery ◽  
Aqueous Solubility ◽  
The Body ◽  
Target Site ◽  
Water Soluble ◽  
Specific Target ◽  
Poor Solubility ◽  
Water Soluble Drugs ◽  
Important Character

Major problem of many newly developed chemical entities is their poor solubility in water and pharmacokinetic issues. These poorly-water soluble drugs show many problems in formulating them in conventional dosage forms and the critical problem associated is its very low bio-availability. Nanotechnology has attracted increasing attention during recent years and it can resolve the problems associated with solubility and bio-availability. Nanosponges are a part of nanotechnology. Nanosponges delivery system, which was originally developed for topical delivery of drugs, can also be used for controlled oral delivery of drugs using water soluble and bioerodible polymers. Nanosponges are tiny sponges with a size of about a virus, which can be filled with wide variety of drugs. These tiny sponges can circulate around the body until they encounter the specific target site and stick on the surface and begin to release the drug in a controlled and predictable manner. Because the drug can be released at the specific target site instead of circulating throughout the body it will be more effective for specific disease targeted treatment. Another important character of these sponges is their aqueous solubility; this allows the use of these systems effectively for drugs with poor solubility. 

Bilayer Floating Tablets for Gastroretentive Drug Delivery System

2013 ◽  
Vol 6 (3) ◽  
pp. 2097-2112
Author(s):  
Sai Sowjanya Palla ◽  
Rajkumar Kotha ◽  
Anusha Paladugu ◽  
E. Rajesh Kumar Reddy ◽  
Suryasri Lavanya Adavi ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Oral Delivery ◽  
Immediate Release ◽  
Gastric Fluid ◽  
New Era ◽  
Floating Tablets ◽  
Colloidal Gel ◽  
Floating Tablet

Oral delivery of the drug is by far the most preferable route of drug delivery due to the ease of administration, patient compliance and flexibility in the formulations but has a drawback of non-site specificity and short gastric resident time. In recent years, scientific and technological advancements have been made in the development of novel drug delivery systems by overcoming physiological troubles such as short gastric residence times and unpredictable gastric emptying times. Among Several approaches of floating systems, Bilayer floating technology is considered as promising approach. It combines the principle of bilayer technology and floating mechanism. The combined principle of bilayer floating tablet helps to release initial dose from the immediate release layer to reach the plasma concentration and then the floating layer absorbs gastric fluid forming an impermeable colloidal gel barrier on its surface, maintains a bulk density less than unity and thereby remains buoyant in stomach providing steady state concentration of drug in system. This review focuses on bilayer floating tablet technology a new era of gastro retentive drug delivery system, its advantages over conventional tablets and it also summarizes the bilayer tablet presses used in the industry, formulation design and evaluation parameters of bilayer floating tablets.  

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