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.

Fenofibrate Solid Dispersion for Improving Oral Bioavailability: Preparation, and Characterization and in vivo Evaluation

2020 ◽  
Vol 13 (5) ◽  
pp. 5102-5109
Author(s):  
Venu Madhav K ◽  
Somnath De ◽  
Chandra Shekar Bonagiri ◽  
Sridhar Babu Gummadi
Keyword(s):  
Oral Bioavailability ◽  
Oral Delivery ◽  
Solid Dispersions ◽  
In Vitro Release ◽  
Aqueous Solubility ◽  
Water Soluble ◽  
Scanning Calorimetry ◽  
In Vivo Evaluation

Fenofibrate (FN) is used in the treatment of hypercholesterolemia. It shows poor dissolution and poor oral bioavailability after oral administration due to high liphophilicity and low aqueous solubility. Hence, solid dispersions (SDs) of FN (FN-SDs) were develop that might enhance the dissolution and subsequently oral bioavailability. FN-SDs were prepared by solvent casting method using different carriers (PEG 4000, PEG 6000, β cyclodextrin and HP β cyclodextrin) in different proportions (0.25%, 0.5%, 0.75% and 1% w/v). FN-SDs were evaluated solubility, assay and in vitro release studies for the optimization of SD formulation. Differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD) and scanning electron microscopy (SEM) analysis was performed for crystalline and morphology analysis, respectively. Further, optimized FN-SD formulation evaluated for pharmacokinetic performance in Wistar rats, in vivo in comparison with FN suspension.  From the results, FN-SD3 and FN-SD6 have showed 102.9 ±1.3% and 105.5±3.1% drug release, respectively in 2 h. DSC and PXRD studies revealed that conversion of crystalline to amorphous nature of FN from FT-SD formulation. SEM studies revealed the change in the orientation of FN when incorporated in SDs. The oral bioavailability FN-SD3 and FN-SD6 formulations exhibited 2.5-folds and 3.1-folds improvement when compared to FN suspension as control. Overall, SD of FN could be considered as an alternative dosage form for the enhancement of oral delivery of poorly water-soluble FN.

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 Microemulsion Drug Delivery System: For Bioavailability Enhancement of Ampelopsin

2012 ◽  
Vol 2012 ◽  
pp. 1-4 ◽  
Author(s):  
Shailendra Singh Solanki ◽  
Brajesh Sarkar ◽  
Rakesh Kumar Dhanwani
Keyword(s):  
Drug Release ◽  
Delivery System ◽  
Oral Delivery ◽  
Aqueous Solubility ◽  
Water Soluble ◽  
Cremophor El ◽  
Bioavailability Enhancement ◽  
Capmul Mcm ◽  
Drug Solution

Ampelopsin, one of the most common flavonoids, reported to possess numerous pharmacological activities and shows poor aqueous solubility. The purpose of this study was to enhance the dissolution rate and bioavailability of this drug by developing a novel delivery system that is microemulsion (ME) and to study the effect of microemulsion (ME) on the oral bioavailability of ampelopsin. Capmul MCM-based ME formulation with Cremophor EL as surfactant and Transcutol as cosurfactant was developed for oral delivery of ampelopsin. Optimised ME was evaluated for its transparency, viscosity, percentage assay and so forth. Solubilisation capacity of the ME system was also determined. The prepared ME was compared with the pure drug solution and commercially available tablet for in vitro drug release. The optimised ME formulation containing ampelopsin, Capmul MCM (5.5%), Cremophor EL (25%), Transcutol P (8.5%), and distilled water showed higher in vitro drug release, as compared to plain drug suspension and the suspension of commercially available tablet. These results demonstrate the potential use of ME for improving the bioavailability of poor water soluble compounds, such as ampelopsin.

scholarly journals In Vitro Dissolution Evidence for Delivering Multiple Vitamin-Mineral Ingredients past the Stomach by Novel Capsule Delivery System (P24-009-19)

2019 ◽  
Vol 3 (Supplement_1) ◽  
Author(s):  
Luke Bucci ◽  
Mastaneh Sharafi ◽  
Nima Alamdari
Keyword(s):  
Absorption Spectrometry ◽  
Gastric Fluid ◽  
Water Soluble ◽  
In Vitro Dissolution ◽  
Magnesium Concentration ◽  
Simulated Gastric Fluid ◽  
Lauryl Sulfate ◽  
Simulated Intestinal Fluid ◽  
Tablet Disintegration

Abstract Objectives The ability of a novel beadlet-in-oil, gastric-resistant, vegetarian capsule containing a multiple vitamin-mineral (MVM) composition to deliver capsule contents past the stomach was tested by standard in vitro tablet disintegration procedures using magnesium as the marker of capsule contents dissolution. Methods A novel capsule design using a gastric-resistant vegetarian hypromellose/gellan gum capsule (DRcaps®, Capsugel®) was tested for disintegration in a standard tablet disintegration apparatus according to compendial United States Pharmacopeia methods, as per Good Manufacturing Practices for dietary supplements. The MVM ingredients were encapsulated into size 0 Vcaps® (hypromellose with no gastric acid resistance) and DRcaps®. Individual capsules were placed into chambers containing simulated gastric fluid (0.1 M HCl) for 120 minutes then changed to simulated intestinal fluid (buffered 2% sodium lauryl sulfate, pH 6.0) for an additional 300 minutes. Aliquots were tested for magnesium concentration at ten time points by atomic absorption spectrometry. Results Magnesium was contained inside coated beadlets along with ferrous bisglycinate, methylcobalamin, 5-methyltetrahydrofolate, calcium fructoborate and cellulose. Vcaps® released 50% of the magnesium between 30–45 minutes and all by 60 minutes in the acid phase. DRcaps® released 25% of the magnesium at 45 minutes, and 43% at 120 minutes, followed by slow, steady release of the remaining magnesium by 420 minutes. Conclusions These dissolution profiles reproduce the known, rapid disintegration profile of Vcaps® when wetted. DRcaps® released the majority of their contents after the pH was changed to intestinal conditions, and then the beadlets released the water-soluble ingredients (magnesium) in a linear manner over a two hour period. Since normal stomach emptying of DRcaps® without a meal is less than 20–30 minutes (previously shown), DRcap® MVMs bypass the stomach almost completely to release ingredients in the small intestine. Thus, a novel, beadlet-in-oil, gastric-resistant capsule delivered its contents past the stomach. These properties have the ability to improve tolerability and thus, compliance with users. Funding Sources Capsugel®, Greenwood, SC, conducted this study for Ritual. Supporting Tables, Images and/or Graphs

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.

scholarly journals FORMULATION AND EVALUATION OF SOLID SELF-EMULSIFYING DRUG DELIVERY SYSTEM OF GLICLAZIDE

2016 ◽  
Vol 8 (11) ◽  
pp. 144
Author(s):  
Suwarna R. Deshmukh ◽  
Suparna S. Bakhle ◽  
Kanchan P. Upadhye ◽  
Gouri R. Dixit
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Oral Delivery ◽  
Tween 80 ◽  
Aqueous Solubility ◽  
Water Soluble ◽  
In Vitro Dissolution ◽  
Water Soluble Drug

Objective: Gliclazide (GCZ) is a widely prescribed anti-diabetic drug belongs to class IΙ under BCS and exhibit low and variable oral bioavailability due to its poor aqueous solubility. The present investigations highlight the development of solid self-emulsifying drug delivery system (solid-SEDDS) for improved oral delivery of the poorly water-soluble drug, GCZ.Methods: Various oils, surfactant and co-surfactant, were screened for their emulsification ability. Ternary phase diagrams were plotted to identify the zone of micro-emulsification. Liquid SEDDS of the drug were formulated using lemon oil as the oil phase, tween 80, as the surfactant, and labrasol, as the co-surfactant. The optimized liquid SEDDS was transformed into free-flowing powder using florite R as the adsorbent. Results: Self-emulsifying powder retained the self-emulsifying property of the liquid SEDDS. The morphology of solid-SEDDS from scanning electron microscopy studies demonstrated the presence of spherical, granular particles indicating good flowing ability. X-ray powder diffraction studies confirmed solubilization of the drug in the lipid excipients and/or transformation of a crystalline form of the drug to amorphous form. In vitro dissolution studies revealed enhanced release of the drug from solid-SEDDS as compared to plain drug and marketed formulation.Conclusion: Thus it can be concluded that solid-SEDDS, amenable for the development of solid dosage form, can be successfully developed using florite R with the potential of enhancing the solubility, dissolution rate, and bioavailability of the drug.

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.

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.

scholarly journals Prediction of Permeation and Cellular Transport of Silybum marianum Extract Formulated in a Nanoemulsion by Using PAMPA and Caco-2 Cell Models

Planta Medica ◽  
2017 ◽  
Vol 83 (14/15) ◽  
pp. 1184-1193 ◽  
Author(s):  
Vieri Piazzini ◽  
Chiara Rosseti ◽  
Elisabetta Bigagli ◽  
Cristina Luceri ◽  
Anna Bilia ◽  
...  
Keyword(s):  
Membrane Permeability ◽  
Oral Delivery ◽  
Oral Absorption ◽  
Gastric Fluid ◽  
Simulated Gastric Fluid ◽  
Cellular Transport ◽  
Artificial Membrane ◽  
Silybum Marianum ◽  
Permeability Assay

AbstractThe present study explores the potential of nanoemulsion, a lipid drug delivery system, to improve solubility and oral absorption of Silybum marianum extract. The optimized formulation contained 40 mg/mL of commercial extract (4 % w/w) and it was composed of 2.5 g labrasol (20 %) as the oil phase, 1.5 g cremophor EL as the surfactant, and 1 g labrafil as the cosurfactant (mixture surfactant/cosurfactant, 20 %).The system was characterized by dynamic light scattering, transmission electron microscopy, and HPLC-DAD analyses in order to evaluate size, homogeneity, morphology, and encapsulation efficiency. Physical and chemical stabilities were assessed during 40 days at 4 °C and 3 months at 25 °C. Stability in simulated gastric fluid followed by simulated intestinal conditions was also considered. In vitro permeation studies were performed to determine the suitability of the prepared nanoemulsion for oral delivery. Different models such as the parallel artificial membrane permeability assay and Caco-2 cell lines were applied.The nanoemulsion showed a good solubilizing effect of the extract, with a pronounced action also on its permeability, in respect to a saturated aqueous solution. The Caco-2 test confirmed the parallel artificial membrane permeability assay results and they revealed the suitability of the prepared nanoemulsion for oral delivery.

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