scholarly journals A new nanosuspension prepared with wet milling method for oral delivery of highly variable drug Cyclosporine A: Development, optimization and in vivo evaluation

2022 ◽  
pp. 106123
Author(s):  
Sıla Gülbağ Pınar ◽  
Hande Canpınar ◽  
Çağman Tan ◽  
Nevin Çelebi
Keyword(s):  
Cyclosporine A ◽  
Oral Delivery ◽  
Wet Milling ◽  
In Vivo Evaluation ◽  
Milling Method

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.

Formulation, Characterization and In Vivo Evaluation of Self-Nanoemulsifying Drug Delivery System for Oral Delivery of Valsartan

2014 ◽  
Vol 10 (2) ◽  
pp. 263-270 ◽  
Author(s):  
Maulick Chopra ◽  
Usha Y. Nayak ◽  
Aravind Kumar Gurram ◽  
M. Sreenivasa Reddy ◽  
K.B. Koteshwara
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Oral Delivery ◽  
In Vivo Evaluation

5-Fluorouracil Loaded Orally Administered WGA-decorated Poly(lactic-co-glycolic acid) Nanoparticles for Treatment of Colorectal Cancer: In Vivo Evaluation

2020 ◽  
Vol 10 ◽  
Author(s):  
Aditya Nath Pandey ◽  
Kuldeep Rajpoot ◽  
Sunil K. Jain
Keyword(s):  
Colorectal Cancer ◽  
Colon Cancer ◽  
Oral Delivery ◽  
Wheat Germ ◽  
Glycolic Acid ◽  
Organ Distribution ◽  
In Vivo Evaluation ◽  
Distribution Study ◽  
Prolonged Retention

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.

Design and in vivo evaluation of solid-in-oil suspension for oral delivery of human growth hormone

2008 ◽  
Vol 41 (2) ◽  
pp. 106-110 ◽  
Author(s):  
Hiromu Yoshiura ◽  
Yoshiro Tahara ◽  
Masakazu Hashida ◽  
Noriho Kamiya ◽  
Akihiko Hirata ◽  
...  
Keyword(s):  
Growth Hormone ◽  
Human Growth Hormone ◽  
Oral Delivery ◽  
Human Growth ◽  
In Vivo Evaluation

In vivo evaluation of lipid-based formulations for oral delivery of apomorphine and its diester prodrugs

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

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 DEVELOPMENT AND OPTIMIZATION OF ZALEPLON LOADED EUDRAGIT® NANOPARTICLES FOR ORAL DELIVERY: IN-VITRO AND IN-VIVO EVALUATION

2019 ◽  
Vol 10 (7) ◽  
pp. 154-162
Author(s):  
Sanaa A El-Gizawy ◽  
Ebtessam A Essa ◽  
Ahmed Kh Abosalha
Keyword(s):  
Oral Delivery ◽  
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.

Gastrointestinal Responsive Polymeric Nanoparticles for Oral Delivery of Insulin: Optimized Preparation, Characterization, and In Vivo Evaluation

2019 ◽  
Vol 108 (9) ◽  
pp. 2994-3002 ◽  
Author(s):  
Yan Fang ◽  
Qi Wang ◽  
Xiaojie Lin ◽  
Xuechao Jin ◽  
Dongjuan Yang ◽  
...  
Keyword(s):  
Oral Delivery ◽  
Polymeric Nanoparticles ◽  
In Vivo Evaluation

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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