Dextran-b-poly(lactide-co-glycolide) polymersome for oral delivery of insulin: In vitro and in vivo evaluation

2016 ◽  
Vol 227 ◽  
pp. 58-70 ◽  
Author(s):  
Mona Alibolandi ◽  
Fatemeh Alabdollah ◽  
Fatemeh Sadeghi ◽  
Marzieh Mohammadi ◽  
Khalil Abnous ◽  
...  
Keyword(s):  
Oral Delivery ◽  
In Vivo Evaluation

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 Preparation and in vitro and in vivo evaluation of quercetin-loaded mixed micelles for oral delivery

2018 ◽  
Vol 82 (2) ◽  
pp. 238-246 ◽  
Author(s):  
Zhen Lu ◽  
Cuiping Bu ◽  
Weicheng Hu ◽  
Hui Zhang ◽  
Mengrui Liu ◽  
...  
Keyword(s):  
Oral Delivery ◽  
Mixed Micelles ◽  
In Vivo Evaluation

scholarly journals In Vitro, Ex Vivo and In Vivo Evaluation of Microcontainers for Oral Delivery of Insulin

Pharmaceutics ◽  
2020 ◽  
Vol 12 (1) ◽  
pp. 48 ◽  
Author(s):  
Jacob Rune Jørgensen ◽  
Feiyang Yu ◽  
Ramakrishnan Venkatasubramanian ◽  
Line Hagner Nielsen ◽  
Hanne Mørck Nielsen ◽  
...  
Keyword(s):  
Oral Delivery ◽  
Ex Vivo ◽  
Sodium Dodecyl ◽  
Insulin Absorption ◽  
Oral Gavage ◽  
In Vivo Evaluation ◽  
Sodium Caprate ◽  
Intestinal Membrane

Enhancing the oral bioavailability of peptides has received a lot of attention for decades but remains challenging, partly due to low intestinal membrane permeability. Combining a permeation enhancer (PE) with unidirectionally releasing microcontainers (MCs) has previously been shown to increase insulin permeation across Caco-2 cell monolayers. In the present work, this setup was further employed to compare three common PEs—sodium caprate (C10), sodium dodecyl sulfate (SDS), and lauroyl carnitine. The concept was also studied using porcine intestinal tissue with the inclusion of 70 kDa fluorescein isothiocyanate-dextran (FD70) as a pathogen marker. Moreover, a combined proteolysis and Caco-2 cell permeation setup was developed to investigate the effect of soybean trypsin inhibitor (STI) in the MCs. Lastly, in vivo performance of the MCs was tested in an oral gavage study in rats by monitoring blood glucose and insulin absorption. SDS proved to be the most potent PE without increasing the ex vivo uptake of FD70, while the implementation of STI further improved insulin permeation in the combined proteolysis Caco-2 cell setup. However, no insulin absorption in rats was observed upon oral gavage of MCs loaded with insulin, PE and STI. Post-mortem microscopic examination of their gastrointestinal tract indicated lack of intestinal retention and optimal orientation by the MCs, possibly precluding the potential advantage of unidirectional release.

Oral Delivery of Teriparatide Using a Nanoemulsion System: Design, in Vitro and in Vivo Evaluation

2020 ◽  
Vol 37 (4) ◽  
Author(s):  
Bashar M Altaani ◽  
Ammar M Almaaytah ◽  
Suha Dadou ◽  
Khouloud Alkhamis ◽  
Mousa H Daradka ◽  
...  
Keyword(s):  
System Design ◽  
Oral Delivery ◽  
In Vivo Evaluation

scholarly journals In Vitro-In Vivo Evaluation of Novel Co-spray Dried Rifampicin Phospholipid Lipospheres for Oral Delivery

2016 ◽  
Vol 18 (1) ◽  
pp. 138-146 ◽  
Author(s):  
Charan Singh ◽  
L. V. Seshu Kumar Koduri ◽  
Tara Datt Bhatt ◽  
Sarbjit Singh Jhamb ◽  
Vijay Mishra ◽  
...  
Keyword(s):  
Oral Delivery ◽  
In Vivo Evaluation ◽  
Spray Dried

Development of an α-linolenic acid containing soft nanocarrier for oral delivery: in vitro and in vivo evaluation

RSC Advances ◽  
2016 ◽  
Vol 6 (81) ◽  
pp. 77590-77602 ◽  
Author(s):  
Mahendra Singh ◽  
Jovita Kanoujia ◽  
Pooja Singh ◽  
Chandra B. Tripathi ◽  
Malti Arya ◽  
...  
Keyword(s):  
Synergistic Effect ◽  
Linolenic Acid ◽  
Oral Delivery ◽  
Lipid Levels ◽  
In Vivo Evaluation

Use of α-linolenic acid as an oil phase for microemulsion preparation with synergistic effect of oil in lowering of lipid levels in combination with simvastatin.

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