In vivo evaluation of anionic thiolated polymers as oral delivery systems for efflux pump inhibition

2015 ◽  
Vol 491 (1-2) ◽  
pp. 318-322 ◽  
Author(s):  
Thomas F. Palmberger ◽  
Flavia Laffleur ◽  
Melanie Greindl ◽  
Andreas Bernkop-Schnürch
2017 ◽  
Vol 166 ◽  
pp. 73-82 ◽  
Author(s):  
Delia Mandracchia ◽  
Adriana Trapani ◽  
Giuseppe Tripodo ◽  
Maria Grazia Perrone ◽  
Gaetano Giammona ◽  
...  

Author(s):  
Venu Madhav K ◽  
Somnath De ◽  
Chandra Shekar Bonagiri ◽  
Sridhar Babu Gummadi

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.


2014 ◽  
Vol 10 (2) ◽  
pp. 263-270 ◽  
Author(s):  
Maulick Chopra ◽  
Usha Y. Nayak ◽  
Aravind Kumar Gurram ◽  
M. Sreenivasa Reddy ◽  
K.B. Koteshwara

2020 ◽  
Vol 10 ◽  
Author(s):  
Aditya Nath Pandey ◽  
Kuldeep Rajpoot ◽  
Sunil K. Jain

Background:: Several studies have suggested potential aptitude of polylactic-co-glycolic acid (PLGA)-derived nanoparticles (NPs) to improve the antitumor efficacy of anticancer drugs against colon cancer. Further, conjugation of lectins over the surface of the NPs may ameliorate interaction and thus enhance attachment of NPs with receptors. Objective:: The main goal of the study was to prepare and evaluate targeting potential (in vivo) of the optimized NPs against colorectal cancer. Methods:: The 5-fluorouracil (5-FU) loaded and wheat germ agglutinin (WGA)-conjugated PLGA-NPs (WFUNPs) were prepared and then they were evaluated in vivo for targeting aptitude of formulation using gamma scintigraphy after oral delivery. The WGA-conjugated and non-conjugated optimized NPs were compared for any significant results. Further, optimized formulations were also assessed for different parameters such as radiolabeling efficiency, sodium pertechnetate uptake, stability of NPs, and organ distribution study. Results:: Findings suggested prolonged retention of 99mTc-tagged WFUNPs in the colonic region after 24 h study. Eventually, the outcome from conjugated formulation revealed enhanced bioavailability of the drug in blood plasma for up to 24 h. Conclusion:: In conclusion, WGA-conjugation to NPs could improve the performance of the PLGA-NPs in the treatment of colorectal cancer.


Coatings ◽  
2021 ◽  
Vol 11 (7) ◽  
pp. 781
Author(s):  
Sadaf Jamal Gilani ◽  
May Nasser Bin-Jumah ◽  
Syed Sarim Imam ◽  
Sultan Alshehri ◽  
Mohammed Asadullah Jahangir ◽  
...  

The authors wish to make the following corrections to this paper [...]


2008 ◽  
Vol 41 (2) ◽  
pp. 106-110 ◽  
Author(s):  
Hiromu Yoshiura ◽  
Yoshiro Tahara ◽  
Masakazu Hashida ◽  
Noriho Kamiya ◽  
Akihiko Hirata ◽  
...  

1995 ◽  
Vol 18 (1) ◽  
pp. 5-22 ◽  
Author(s):  
E.C. Lavelle ◽  
S. Sharif ◽  
N.W. Thomas ◽  
J. Holland ◽  
S.S. Davis

2016 ◽  
Vol 513 (1-2) ◽  
pp. 211-217 ◽  
Author(s):  
Nrupa Borkar ◽  
René Holm ◽  
Mingshi Yang ◽  
Anette Müllertz ◽  
Huiling Mu

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