scholarly journals Improvement of effect of water-in-oil microemulsion as an oral delivery system for fexofenadine: in vitro and in vivo studies

2011 ◽  
pp. 1631 ◽  
Author(s):  
Evren Gundogdu ◽  
isabel gonzalez alvarez ◽  
ercüment karasulu
Keyword(s):  
Delivery System ◽  
Oral Delivery ◽  
In Vivo Studies ◽  
Oral Delivery System ◽  
Effect Of Water

Preliminary evaluation of a novel oral delivery system for rhPTH1-34: In vitro and in vivo

2011 ◽  
Vol 420 (1) ◽  
pp. 172-179 ◽  
Author(s):  
Liting Guo ◽  
Erli Ma ◽  
Haiwei Zhao ◽  
Yingfang Long ◽  
Changxue Zheng ◽  
...  
Keyword(s):  
Delivery System ◽  
Oral Delivery ◽  
Preliminary Evaluation ◽  
Oral Delivery System

Biopharmaceutical and Preclinical Studies of Zaleplon as Semisolid Dispersions with Self-emulsifying Lipid Surfactants for Oral Delivery

1970 ◽  
Vol 9 (1) ◽  
pp. 3102-3111
Author(s):  
Narendar Dudhipala ◽  
Arjun Narala ◽  
Dinesh Suram ◽  
Karthik Yadav Janga
Keyword(s):  
Oral Delivery ◽  
Molecular State ◽  
In Vivo Studies ◽  
In Vitro Dissolution ◽  
Content Uniformity ◽  
Phase Solubility ◽  
Microscopic Studies ◽  
Pure Drug

The objective of this present study is to develop a semisolid dispersion (SSD) of zaleplon with the aid of self-emulsifying lipid based amphiphilic carriers (TPGS E or Gelucire 44/14) addressing the poor solubility of this drug. A linear relationship between the solubility of drug with respect to increase in the concentration of lipid surfactant in aqueous medium resulting in AL type phase diagram was observed from phase solubility studies. Fusion method was employed to obtain semisolid dispersions (SSD) of zaleplon which showed high content uniformity of drug. The absence of chemical interactions between the pure drug, excipients and formulations were conferred by Fourier transmission infrared spectroscopic examinations. The photographic images from polarized optical microscopic studies revealed the change in crystalline form of drug to amorphous or molecular state. The superior dissolution parameters of zaleplon from SSD over pure crystalline drug interpreted from in vitro dissolution studies envisage the ability of these lipid surfactants as solubility enhancers. Further, the caliber of TPGS E or Gelucire 44/14 in encouraging the GI absorption of drug was evident with the higher human effective permeability coefficient and fraction oral dose of drug absorbed from SSD in situ intestinal permeation study. In conclusion, in vivo studies in Wister rats demonstrated an improvement in the oral bioavailability of zaleplon from SSD over control pure drug suspension suggesting the competence of Gelucire 44/14 and TPGS E as conscientious carriers to augment the dissolution rate limited bioavailability of this active

Novel Self-Micro Emulsifying Drug Delivery System for safe intra muscular delivery with improved pharmacodynamics and pharmacokinetics

2021 ◽  
Vol 18 ◽  
Author(s):  
Subheet Kumar Jain ◽  
Neha Panchal ◽  
Amrinder Singh ◽  
Shubham Thakur ◽  
Navid Reza Shahtaghi ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Inflammatory Diseases ◽  
Diclofenac Sodium ◽  
Physical Stability ◽  
In Vivo Studies ◽  
High Concentration

Background: Diclofenac sodium (DS) injection is widely used in the management of acute or chronic pain and inflammatory diseases. It incorporates 20 % w/v Transcutol-P as a solubilizer to make the stable injectable formulation. However, the use of Transcutol-P in high concentration leads to adverse effects such as severe nephrotoxicity, etc. Some advancements resulted in the formulation of an aqueous based injectable but that too used benzyl alcohol reported to be toxic for human use. Objective: To develop an injectable self-micro emulsifying drug delivery system (SMEDDS) as a novel carrier of DS for prompt release with better safety and efficacy. Methods: A solubility study was performed with different surfactants and co-surfactants. The conventional stirring method was employed for the formulation of SMEDDS. Detailed in vitro characterization was done for different quality control parameters. In vivo studies were performed using Wistar rats for pharmacokinetic evaluation, toxicological analysis, and analgesic activity. Results: The optimized formulation exhibited good physical stability, ideal globule size (156±0.4 nm), quick release, better therapeutics, and safety, increase in LD50 (221.9 mg/kg) to that of the commercial counterpart (109.9 mg/kg). Further, pre-treatment with optimized formulation reduced the carrageenan-induced rat paw oedema by 88±1.2 % after 4 h, compared to 77±1.6 % inhibition with commercial DS formulation. Moreover, optimized formulation significantly (p<0.05) inhibited the pain sensation in the acetic-acid induced writhing test in mice compared to its commercial equivalent with a better pharmacokinetic profile. Conclusion: The above findings confirmed that liquid SMEDDS could be a successful carrier for the safe and effective delivery of DS

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 Fabrication of PLA-PEG Nanoparticles as Delivery Systems for Improved Stability and Controlled Release of Catechin

2017 ◽  
Vol 2017 ◽  
pp. 1-9 ◽  
Author(s):  
Neha Atulkumar Singh ◽  
Abul Kalam Azad Mandal ◽  
Zaved Ahmed Khan
Keyword(s):  
Controlled Release ◽  
Delivery System ◽  
Oral Delivery ◽  
Polymeric Nanoparticles ◽  
Double Emulsion ◽  
Hydrodynamic Diameter ◽  
Sem Image ◽  
Oral Delivery System ◽  
Improved Stability

The purpose of this study was to develop an oral delivery system for the controlled release of catechin and evaluate the antioxidant potential and stability of catechin loaded PLA/PEG nanoparticles (CATNP). Nanoparticles were synthesized using a double emulsion solvent evaporation method. The fabricated nanoparticles were relatively small with a hydrodynamic diameter of 300 nm and an encapsulation efficiency of 95%. SEM image analysis showed uniform sized and spherically shaped nanoparticles. In vitro release profiles indicated a slow and sustained release of catechin from the nanoparticle. Stability of the nanoparticle in simulated gastric and intestinal fluids is maintained due to the PEG coating on the nanoparticles, which effectively protected catechin against gastrointestinal enzyme activity. Enhanced inhibition action of free radicals and metal chelation potential was noted when catechin was encapsulated in these polymeric nanoparticles. The reports obtained from this study would provide an opportunity for designing an oral delivery system aimed at inhibiting oxidative stress in the human body.

Oil based nanocarrier for improved oral delivery of silymarin: In vitro and in vivo studies

2011 ◽  
Vol 413 (1-2) ◽  
pp. 245-253 ◽  
Author(s):  
Rabea Parveen ◽  
Sanjula Baboota ◽  
Javed Ali ◽  
Alka Ahuja ◽  
Suruchi S. Vasudev ◽  
...  
Keyword(s):  
Oral Delivery ◽  
In Vivo Studies

In vivo evaluation of an oral delivery system for P-gp substrates based on thiolated chitosan

Biomaterials ◽  
2006 ◽  
Vol 27 (23) ◽  
pp. 4250-4255 ◽  
Author(s):  
Florian Föger ◽  
Thierry Schmitz ◽  
Andreas Bernkop-Schnürch
Keyword(s):  
Delivery System ◽  
Oral Delivery ◽  
In Vivo Evaluation ◽  
Thiolated Chitosan ◽  
Oral Delivery System
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