Preparation and Optimization of Moxifloxacin Microspheres for Colon Targeted Delivery Using Quality by Design Approach: In Vitro and In Vivo Study

2016 ◽  
Vol 13 (7) ◽  
pp. 1021-1033 ◽  
Author(s):  
Bhumika Prajapati ◽  
Prasant Kumar Jena ◽  
Tejal Mehta ◽  
Sriram Seshadri
Keyword(s):  
Targeted Delivery ◽  
Quality By Design ◽  
Design Approach ◽  
In Vivo Study ◽  
Quality By Design Approach

scholarly journals Development and in vitro/in vivo  evaluation of a novel benznidazole liquid dosage form using a quality-by-design approach

2017 ◽  
Vol 22 (12) ◽  
pp. 1514-1522 ◽  
Author(s):  
Higo Fernando Santos Souza ◽  
Daniel Real ◽  
Darío Leonardi ◽  
Sandra Carla Rocha ◽  
Victoria Alonso ◽  
...  
Keyword(s):  
Dosage Form ◽  
Quality By Design ◽  
Design Approach ◽  
In Vivo Evaluation ◽  
Quality By Design Approach ◽  
Liquid Dosage Form

scholarly journals Modelling the Effect of Process Parameters on the Wet Extrusion and Spheronisation of High-Loaded Nicotinamide Pellets Using a Quality by Design Approach

Pharmaceutics ◽  
2019 ◽  
Vol 11 (4) ◽  
pp. 154 ◽  
Author(s):  
Eva-Maria Theismann ◽  
Julia K. Keppler ◽  
Martin Owen ◽  
Karin Schwarz ◽  
Walkiria Schlindwein
Keyword(s):  
Process Parameters ◽  
Quality By Design ◽  
Spherical Shape ◽  
Release Profile ◽  
Design Approach ◽  
Quality By Design Approach ◽  
Solid Feed Rate ◽  
Wet Extrusion ◽  
Spray Granulation

The aim of the present study was to develop an alternative process to spray granulation in order to prepare high loaded spherical nicotinamide (NAM) pellets by wet extrusion and spheronisation. Therefore, a quality by design approach was implemented to model the effect of the process parameters of the extrusion-spheronisation process on the roundness, roughness and useable yield of the obtained pellets. The obtained results were compared to spray granulated NAM particles regarding their characteristics and their release profile in vitro after the application of an ileocolon targeted shellac coating. The wet extrusion-spheronisation process was able to form highly loaded NAM pellets (80%) with a spherical shape and a high useable yield of about 90%. However, the water content range was rather narrow between 24.7% and 21.3%. The design of experiments (DoE), showed that the spheronisation conditions speed, time and load had a greater impact on the quality attributes of the pellets than the extrusion conditions screw design, screw speed and solid feed rate (hopper speed). The best results were obtained using a low load (15 g) combined with a high rotation speed (900 m/min) and a low time (3–3.5 min). In comparison to spray granulated NAM pellets, the extruded NAM pellets resulted in a higher roughness and a higher useable yield (63% vs. 92%). Finally, the coating and dissolution test showed that the extruded and spheronised pellets are also suitable for a protective coating with an ileocolonic release profile. Due to its lower specific surface area, the required shellac concentration could be reduced while maintaining the release profile.

Development of Atovaquone Nanosuspension: Quality by Design Approach

2020 ◽  
Vol 17 (2) ◽  
pp. 112-125
Author(s):  
Pratik Kakade ◽  
Sandip Gite ◽  
Vandana Patravale
Keyword(s):  
Particle Size ◽  
Quality By Design ◽  
Green Technology ◽  
In Vitro Dissolution ◽  
Pharmacokinetic Studies ◽  
Physicochemical Interaction ◽  
Nano Crystalline ◽  
Quality By Design Approach

Objective: The present study reports the use of MicrofluidizerTM technology to form a stable nanosuspension of atovaquone (ATQ) using quality by design (QbD) approach. Methods: The patient-centric quality target product profile and critical quality attributes (CQAs) were identified. A Box-Behnken design was employed for the optimization of dependent variables, while CQAs like particle size and PDI were evaluated as response variables. Effective optimization of ATQ nanosuspension preparation using Microfluidizer processor as a novel green technology was achieved using QbD approach. Result: The prepared nanosuspension had a mean particle size of 865 nm ± 5%, PDI of 0.261 ± 3%, and zeta potential of -1.79 ± 5 mV. The characterization of the prepared nanosuspension by SEM, DSC, and XRD revealed its nano-crystalline nature whereas FTIR spectroscopic analysis confirmed the absence of any physicochemical interaction because of process parameters between the drug and excipients. Conclusion: In vitro dissolution studies of the nanosuspension using USP-IV exhibited a 100% cumulative drug release over 90 minutes, which is significantly better than that of ATQ pure API. In vivo pharmacokinetic studies revealed bioequivalence of ATQ nanosuspensions by Microfluidizer homogenization process to the marketed formulation1.

scholarly journals Exploring the Interplay between Drug Release and Targeting of Lipid-Like Polymer Nanoparticles Loaded with Doxorubicin

Molecules ◽  
2021 ◽  
Vol 26 (4) ◽  
pp. 831
Author(s):  
Tatyana Kovshova ◽  
Nadezhda Osipova ◽  
Anna Alekseeva ◽  
Julia Malinovskaya ◽  
Alexey Belov ◽  
...  
Keyword(s):  
Drug Release ◽  
Targeted Delivery ◽  
Compartmental Analysis ◽  
Formulation Development ◽  
Surface Design ◽  
Significant Difference ◽  
Quality By Design Approach ◽  
The One

Targeted delivery of doxorubicin still poses a challenge with regards to the quantities reaching the target site as well as the specificity of the uptake. In the present approach, two colloidal nanocarrier systems, NanoCore-6.4 and NanoCore-7.4, loaded with doxorubicin and characterized by different drug release behaviors were evaluated in vitro and in vivo. The nanoparticles utilize a specific surface design to modulate the lipid corona by attracting blood-borne apolipoproteins involved in the endogenous transport of chylomicrons across the blood–brain barrier. When applying this strategy, the fine balance between drug release and carrier accumulation is responsible for targeted delivery. Drug release experiments in an aqueous medium resulted in a difference in drug release of approximately 20%, while a 10% difference was found in human serum. This difference affected the partitioning of doxorubicin in human blood and was reflected by the outcome of the pharmacokinetic study in rats. For the fast-releasing formulation NanoCore-6.4, the AUC0→1h was significantly lower (2999.1 ng × h/mL) than the one of NanoCore-7.4 (3589.5 ng × h/mL). A compartmental analysis using the physiologically-based nanocarrier biopharmaceutics model indicated a significant difference in the release behavior and targeting capability. A fraction of approximately 7.310–7.615% of NanoCore-7.4 was available for drug targeting, while for NanoCore-6.4 only 5.740–6.057% of the injected doxorubicin was accumulated. Although the targeting capabilities indicate bioequivalent behavior, they provide evidence for the quality-by-design approach followed in formulation development.

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