Enhanced Solubility and Oral Bioavailability of Hydrophobic Drugs Using Pluronic Nanomicelles: An In‐Vitro Evaluation

2021 ◽  
Vol 6 (28) ◽  
pp. 7040-7048
Author(s):  
Sofiya J. Shaikh ◽  
Hemil S. Patel ◽  
Debes Ray ◽  
Vinod K. Aswal ◽  
Sushmita Singh ◽  
...  
Keyword(s):  
Oral Bioavailability ◽  
Hydrophobic Drugs ◽  
In Vitro Evaluation ◽  
Enhanced Solubility

In Vitro and In Vivo Evaluation of Olmesartan Medoxomil Microcrystals and Nanocrystals: Preparation, Characterization, and Pharmacokinetic Comparison in Beagle Dogs

2019 ◽  
Vol 16 (6) ◽  
pp. 500-510
Author(s):  
Rong Chai ◽  
Hailing Gao ◽  
Zhihui Ma ◽  
Meng Guo ◽  
Qiang Fu ◽  
...  
Keyword(s):  
Particle Size ◽  
Oral Bioavailability ◽  
Olmesartan Medoxomil ◽  
Water Soluble ◽  
Size Reduction ◽  
Drug Dissolution ◽  
Beagle Dogs ◽  
Enhanced Solubility

Background: Olmesartan medoxomil (OLM) is a promising prodrug hydrolyzed to olmesartan (OL) during absorption from the gastrointestinal tract. OL is a selective angiotensin II receptor antagonist, with high drug resistance and low drug interaction. However, OLM has low solubility and low bioavailability. Therefore, it is extremely urgent to reduce the drug particle size to improve its biological bioavailability. Objective: The aim of the study was to improve the oral bioavailability of poorly water-soluble olmesartan medoxomil (OLM) by using different particle size-reduction strategies. Method: Raw drug material was micronized or nanosized by either jet or wet milling processes, respectively. The particle sizes of the prepared nanocrystals (100-300 nm) and microcrystals (0.5-16 μm) were characterized by DLS, SEM, and TEM techniques. Solid state characterization by XPRD and DSC was used to confirm the crystalline state of OLM after the milling processes. Results: We demonstrated that OLM nanocrystals enhanced solubility and dissolution in the non-sink condition in which high sensitivity was found in purified water. After 1 h, 65.4% of OLM was dissolved from nanocrystals, while microcrystals and OLMETEC® only showed 37.8% and 31.9% of drug dissolution, respectively. In the pharmacokinetic study using Beagle dogs, an increase in Cmax (～2 fold) and AUC (～1.6 fold) was observed after oral administration of OLM nanocrystals when compared to microcrystals and reference tablets, OLMETEC®. In contrast, OLM microcrystals failed to improve the oral bioavailability of the drugs. Conclusion: Particles size reduction to nano-scale by means of nanocrystals technology significantly increased in vitro dissolution rate and in vivo oral bioavailability of OLM.

ChemInform Abstract: Synthesis, Oral Bioavailability Determination, and in vitro Evaluation of Prodrugs of the Antiviral Agent 9-(2-(Phosphonomethoxy)ethyl) adenine (PMEA).

ChemInform ◽  
2010 ◽  
Vol 25 (44) ◽  
pp. no-no
Author(s):  
J. E. JUN. STARRETT ◽  
D. R. TORTOLANI ◽  
J. RUSSELL ◽  
M. J. M. HITCHCOCK ◽  
V. WHITEROCK ◽  
...  
Keyword(s):  
Oral Bioavailability ◽  
Antiviral Agent ◽  
In Vitro Evaluation

scholarly journals The oral bioavailability, excretion and cytochrome P450 inhibition properties of epiberberine: an in vivo and in vitro evaluation

2017 ◽  
Vol Volume 12 ◽  
pp. 57-65 ◽  
Author(s):  
Ning Chen ◽  
Xiao-yan Yang ◽  
Chang-e Guo ◽  
Xin-ning Bi ◽  
Jian-hua Chen ◽  
...  
Keyword(s):  
Cytochrome P450 ◽  
Oral Bioavailability ◽  
In Vitro Evaluation

scholarly journals Fabrication, characterization and in vitro evaluation of silibinin nanoparticles: an attempt to enhance its oral bioavailability

2017 ◽  
Vol Volume 11 ◽  
pp. 1453-1464 ◽  
Author(s):  
Muhammad Umar Khayam Sahibzada ◽  
Abdul Sadiq ◽  
Shahzeb Khan ◽  
Hani S Faidah ◽  
Naseem Ullah ◽  
...  
Keyword(s):  
Oral Bioavailability ◽  
In Vitro Evaluation

Synthesis, Oral Bioavailability Determination, and in vitro Evaluation of Prodrugs of the Antiviral Agent 9-[2-(Phosphonomethoxy)ethyl]adenine (PMEA)

1994 ◽  
Vol 37 (12) ◽  
pp. 1857-1864 ◽  
Author(s):  
John E. Jr. Starrett ◽  
David R. Tortolani ◽  
John Russell ◽  
Michael J. M. Hitchcock ◽  
Valerie Whiterock ◽  
...  
Keyword(s):  
Oral Bioavailability ◽  
Antiviral Agent ◽  
In Vitro Evaluation

In vitro evaluation of IL-18 effects in Crohn's disease

2001 ◽  
Vol 120 (5) ◽  
pp. A316-A317
Author(s):  
P MAERTEN ◽  
S COLPAERT ◽  
Z LIU ◽  
K GEBOES ◽  
J CEUPPENS ◽  
...  
Keyword(s):  
Crohn’S Disease ◽  
Crohn's Disease ◽  
In Vitro Evaluation

52: In Vitro Evaluation of Ureteral Stent Compression

2006 ◽  
Vol 175 (4S) ◽  
pp. 18-18
Author(s):  
Kari Hendlin ◽  
Krishna Vedula ◽  
Christina Horn ◽  
Manoj Monga
Keyword(s):  
Ureteral Stent ◽  
In Vitro Evaluation
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