scholarly journals Preparation andIn VitroRelease of Drug-Loaded Microparticles for Oral Delivery Using Wholegrain Sorghum Kafirin Protein

2015 ◽  
Vol 2015 ◽  
pp. 1-8 ◽  
Author(s):  
Esther T. L. Lau ◽  
Stuart K. Johnson ◽  
Roger A. Stanley ◽  
Deirdre Mikkelsen ◽  
Zhongxiang Fang ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Gastrointestinal Tract ◽  
Drug Delivery System ◽  
Delivery System ◽  
Targeted Delivery ◽  
Oral Delivery ◽  
Protein Digestibility ◽  
Target Area ◽  
Sorghum Grains

Kafirin microparticles have been proposed as an oral nutraceutical and drug delivery system. This study investigates microparticles formed with kafirin extracted from white and raw versus cooked red sorghum grains as an oral delivery system. Targeted delivery to the colon would be beneficial for medication such as prednisolone, which is used in the management of inflammatory bowel disease. Therefore, prednisolone was loaded into microparticles of kafirin from the different sources using phase separation. Differences were observed in the protein content,in vitroprotein digestibility, and protein electrophoretic profile of the various sources of sorghum grains, kafirin extracts, and kafirin microparticles. For all of the formulations, the majority of the loaded prednisolone was not released inin vitroconditions simulating the upper gastrointestinal tract, indicating that most of the encapsulated drug could reach the target area of the lower gastrointestinal tract. This suggests that these kafirin microparticles may have potential as a colon-targeted nutraceutical and drug delivery system.

scholarly journals Development of Piperine-Loaded Solid Self-Nanoemulsifying Drug Delivery System: Optimization, In-Vitro, Ex-Vivo, and In-Vivo Evaluation

Nanomaterials ◽  
2021 ◽  
Vol 11 (11) ◽  
pp. 2920
Author(s):  
Ameeduzzafar Zafar ◽  
Syed Sarim Imam ◽  
Nabil K. Alruwaili ◽  
Omar Awad Alsaidan ◽  
Mohammed H. Elkomy ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Oral Delivery ◽  
Ex Vivo ◽  
In Vitro Release ◽  
System Optimization ◽  
Globule Size

Hypertension is a cardiovascular disease that needs long-term medication. Oral delivery is the most common route for the administration of drugs. The present research is to develop piperine self-nanoemulsifying drug delivery system (PE-SNEDDS) using glyceryl monolinoleate (GML), poloxamer 188, and transcutol HP as oil, surfactant, and co-surfactant, respectively. The formulation was optimized by three-factor, three-level Box-Behnken design. PE-SNEDDs were characterized for globule size, emulsification time, stability, in-vitro release, and ex-vivo intestinal permeation study. The optimized PE-SNEDDS (OF3) showed the globule size of 70.34 ± 3.27 nm, percentage transmittance of 99.02 ± 2.02%, and emulsification time of 53 ± 2 s Finally, the formulation OF3 was transformed into solid PE-SNEDDS (S-PE-SNEDDS) using avicel PH-101 as adsorbent. The reconstituted SOF3 showed a globule size of 73.56 ± 3.54 nm, PDI of 0.35 ± 0.03, and zeta potential of −28.12 ± 2.54 mV. SEM image exhibited the PE-SNEDDS completely adsorbed on avicel. Thermal analysis showed the drug was solubilized in oil, surfactant, and co-surfactant. S-PE-SNEDDS formulation showed a more significant (p < 0.05) release (97.87 ± 4.89% in 1 h) than pure PE (27.87 ± 2.65% in 1 h). It also exhibited better antimicrobial activity against S. aureus and P. aeruginosa and antioxidant activity as compared to PE dispersion. The in vivo activity in rats exhibited better (p < 0.05) antihypertensive activity as well as 4.92-fold higher relative bioavailability than pure PE dispersion. Finally, from the results it can be concluded that S-PE-SNEDDS might be a better approach for the oral delivery to improve the absorption and therapeutic activity.

scholarly journals Quality-By-Design-Based Development of a Voxelotor Self-Nanoemulsifying Drug-Delivery System with Improved Biopharmaceutical Attributes

Pharmaceutics ◽  
2021 ◽  
Vol 13 (9) ◽  
pp. 1388
Author(s):  
Aristote B. Buya ◽  
Romano Terrasi ◽  
Jérémie K. Mbinze ◽  
Giulio G. Muccioli ◽  
Ana Beloqui ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Oral Bioavailability ◽  
Oral Delivery ◽  
Ternary Phase Diagram ◽  
Desirability Function ◽  
Limiting Factors ◽  
In Vitro Dissolution

Low aqueous solubility and poor oral bioavailability are limiting factors in the oral delivery of voxelotor, an antisickling agent. To overcome these limitations, a voxelotor self-nanoemulsifying drug delivery system was developed. Various oils, surfactants, and cosurfactants were screened for their solubilization potential for the drug. The area of nanoemulsification was identified using a ternary phase diagram. An experimental mixture design and a desirability function were applied to select SNEDDSs that contain a maximum amount of lipids and a minimum amount of surfactant, and that possess optimal emulsification properties (i.e., droplet sizes, polydispersity index (PDI), emulsification time, and transmittance percentage). The optimized SNEDDS formulation was evaluated for the self-emulsifying time (32 s), droplet size (35 nm), and zeta potential (−8 mV). In vitro dissolution studies indicated a 3.1-fold improvement in drug solubility from the optimized SNEDDS over pure drug powder. After 60 min of in vitro lipolysis, 88% of the voxelotor loaded in the SNEDDS remained in the aqueous phase. Cytotoxicity evaluation, using Caco-2 cells, indicated the safety of the formulation at 0.9 mg/mL. The transport of the voxelotor SNEDDS across Caco-2 monolayers was significantly enhanced compared to that of the free drug. Compared to the drug suspension, the developed SNEDDS enhanced the oral bioavailability (1.7-fold) of voxelotor in rats. The results suggest that further development of SNEDDSs for the oral delivery of voxelotor is needed.

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.

Improved Oral Delivery of Rosuvastatin by Using Self Nanoemulsifying Drug Delivery System

2013 ◽  
Vol 678 ◽  
pp. 286-290 ◽  
Author(s):  
N. Subramanian ◽  
P. Chandra Sekar ◽  
S. Abimanyu ◽  
S.P. Sharavanan ◽  
R. Gayathri ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Drug Delivery System ◽  
Delivery System ◽  
Oral Delivery ◽  
Oral Absorption ◽  
Ex Vivo ◽  
Lipid Lowering ◽  
Conventional Tablet

The aim of the present study was to develop a self nanoemulsifying drug delivery system (SNEDDS) for the improved oral delivery of Rosuvastatin, a lipid lowering agent. Captex 810D, based on the higher solubility of Rosuvastatin was selected as an oil phase. Mixture of permeation enhancers such as Solutol HS15 and Acconon MC8 was selected as surfactants for the formulation of SNEDDS. Formulated SNEDDS upon mixing with water, dispersed rapidly into fine droplets size ranging from 95-263nm. Further the SNEDDS was evaluated for self nanoemulsification time, precipitation, cloud point, morphology, in-vitro drug release and ex-vivo permeation. Formulation (F3) showed the globule size of 139nm, quick self nanoemulsifiation time (20 sec) and transparency (97%). Maximum drug release of 99.9% and higher drug permeation of 95% was observed with formulation F3 when compared with conventional tablet. The formulated SNEDDS can be used to improve the oral absorption and bioavailability of Rosuvastatin.

scholarly journals FLOATING DRUG DELIVERY SYSTEM OF NSAIDS TO INCREASE GASTRIC RETENTION TIME IN UPPER PART OF GASTROINTESTINAL TRACT

2021 ◽  
Vol 12 (1) ◽  
pp. 33-39
Author(s):  
Ankita Tripathi ◽  
Suraj Neupane ◽  
Khushboo Bhardwaj ◽  
Shiva Mishra ◽  
Meenakshi Gupta ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Gastrointestinal Tract ◽  
Drug Delivery System ◽  
Residence Time ◽  
Delivery System ◽  
Dosage Form ◽  
In Vitro Release ◽  
Floating Drug Delivery ◽  
Floating Drug Delivery System

The purpose of the present work is to prolong the gastric residence time of Lornoxicam by developing gastric floating drug delivery system. Lornoxicam is non-steroidal anti-inflammatory drugs. Its short half life 2 to 3 hrs and maximal absorption of upper part of gastrointestinal tract. The residence time of the dosage form in the stomach depends upon various factors like pH, size of the dosage form, food intake, and biological factors which include age, body weight gender, posture, and diseased states Floating tablet prepared by melt granulation techniques, using bees wax as a binder and the other polymers include HPMC 50cPs,15cPs,5cPs and Sodium Alginate. The Prepared granules were then evaluated for Precompression Properties. The best batches were then tabulated, and Evaluation was carried out for the following parameters with in vitro release, buoyancy, Floating Lag timed. Batch F12 and F13 Showed best Floating time of 12hrs and Floating Lag time of 60 second.

Sign in / Sign up

Export Citation Format

Share Document