Improved oral bioavailability of docetaxel by nanostructured lipid carriers: in vitro characteristics, in vivo evaluation and intestinal transport studies

RSC Advances ◽  
2015 ◽  
Vol 5 (117) ◽  
pp. 96437-96447 ◽  
Author(s):  
Guihua Fang ◽  
Bo Tang ◽  
Yanhui Chao ◽  
Yu Zhang ◽  
Hui Xu ◽  
...  
Keyword(s):  
Oral Bioavailability ◽  
Oral Delivery ◽  
Intestinal Transport ◽  
Nanostructured Lipid Carriers ◽  
Absorption Mechanism ◽  
In Vivo Evaluation ◽  
Transport Studies

The objective of the current study was to explore the potential of nanostructured lipid carriers (NLC) for oral delivery of docetaxel (DTX) and investigate the absorption mechanismin vivo.

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.

Lacidipine Loaded Solid Lipid Nanoparticles for Oral Delivery: Preparation, Characterization and In vivo Evaluation

2016 ◽  
Vol 9 (6) ◽  
pp. 3524-3530 ◽  
Author(s):  
Kishan V. ◽  
Sandeep V ◽  
Narendar D ◽  
Arjun N
Keyword(s):  
Solid Lipid Nanoparticles ◽  
Oral Bioavailability ◽  
Oral Delivery ◽  
Lipid Nanoparticles ◽  
Pharmacokinetic Studies ◽  
Electron Microscopic ◽  
In Vivo Evaluation ◽  
Solid Lipid

The objective of this study was to develop and evaluate lacidipine (LD) loaded solid lipid nanoparticles (LD-SLNs) for improving the oral bioavailability. LD-SLNs were prepared in two steps. First step was hot homogenization and next by ultrasonication method, using triglycerides (tripalmitin and tristearin), monoglyceride and surfactants (Poloxamer 188 and egg lecithin E80). The prepared LD-SLNs were characterized for particle size, PDI, zeta potential, drug content, entrapment efficiency (EE %).         In vitro drug release studies using a dialysis bag method in 0.1N HCl and pH 6.8 phosphate buffer were conducted. In addition, long-term physical stability of the optimized SLNs was investigated at refrigerated and room temperature for 60 days. FTIR and DSC studies revealed that no interaction between the drug and lipids. LD-SLNs prepared with Dynasan-116 (F3), having the size of 141.86nm, PDI of 0.293, ZP of -22.3 m with 94.75% of EE was optimized and was stable for 60days. Scanning electron microscopic studies showed nearly spherical shaped particles. Further, pharmacokinetic studies were conducted in wistar rats. The relative bioavailability of LD in SLNs was 2.03 times when compared with that of the LD suspension. The results are indicative of SLNs as suitable lipid based carrier system for improving the oral bioavailability of LD. 

Freeze-Dried Clopidogrel Loaded Lyotropic Liquid Crystal: Box-Behnken Optimization, In-Vitro and In-Vivo Evaluation

2020 ◽  
Vol 17 (3) ◽  
pp. 207-217
Author(s):  
Eman A. Hakeem ◽  
Galal M. El-Mahrouk ◽  
Ghada Abdelbary ◽  
Mahmoud H. Teaima
Keyword(s):  
Statistical Analysis ◽  
Oral Bioavailability ◽  
Quadratic Model ◽  
Lipid Phase ◽  
Individual Response ◽  
In Vivo Evaluation ◽  
Freeze Dried ◽  
Suggested Formula

Background: Clopidogrel (CLP) suffers from extensive first pass metabolism results in a negative impact on its oral systemic bioavailability. Cubosomes are Lyotropic Liquid Crystalline (LLC) nano-systems comprising monoolein, a steric stabilizer and an aqueous system, it considered a promising carrier for different pharmaceutical compounds. Box-Behnken Design (BBD) is an efficient tool for process analysis and optimization skipping forceful treatment combinations. Objective: The study was designed to develop freeze-dried clopidogrel loaded LLC (cubosomes) for enhancement of its oral bioavailability. Methods: A 33 BBD was adopted, the studied independent factors were glyceryl monooleate (GMO lipid phase), Pluronic F127 (PL F127steric stabilizer) and polyvinyl alcohol powder (stabilizer). Particle Size (PS), Polydispersity Index (PDI) and Zeta Potential (ZP) were set as independent response variables. Seventeen formulae were prepared in accordance with the bottom up approach and in-vitro evaluated regarding PS, PDI and ZP. Statistical analysis and optimization were achieved using design expert software®, then the optimum suggested formula was prepared, in-vitro revaluated, freeze-dried with 3% mannitol (cryoprotectant), solid state characterized and finally packed in hard gelatin capsule for comparative in-vitro release and in-vivo evaluation to Plavix®. Results: Results of statistical analysis of each individual response revealed a quadratic model for PS and PDI where a linear model for ZP. The optimum suggested formula with desirability factor equal 0.990 consisting of (200 mg GMO, 78.15 mg PL F127 and 2% PVA). LC/MS/MS study confirmed significant higher C>max, AUC>0-24h and AUC>0-∞ than that of Plavix®. Conclusion: The results confirm the capability of developed carrier to overcome the low oral bioavailability.

In vitro and in vivo evaluation of folate-mediated PEGylated nanostructured lipid carriers for the efficient delivery of furanodiene

2017 ◽  
Vol 43 (10) ◽  
pp. 1610-1618 ◽  
Author(s):  
Jianmei Zhang ◽  
Yunpeng He ◽  
Jianqi Jiang ◽  
Meng Li ◽  
Chenhao Jin ◽  
...  
Keyword(s):  
Nanostructured Lipid Carriers ◽  
In Vivo Evaluation ◽  
Efficient Delivery

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
Sign in / Sign up

Export Citation Format

Share Document