scholarly journals Application of the quality-by-design (QbD) approach to improve the nose-to-brain delivery of diazepam-loaded nanostructured lipid carriers (NLC)

2020 ◽  
Author(s):  
Cláudia Costa ◽  
Sara Cunha ◽  
Andreia Peixoto ◽  
João Moreira ◽  
José Sousa Lobo ◽  
...  
Keyword(s):  
Quality By Design ◽  
Nanostructured Lipid Carriers ◽  
Brain Delivery

scholarly journals Double Optimization of Rivastigmine-Loaded Nanostructured Lipid Carriers (NLC) for Nose-to-Brain Delivery Using the Quality by Design (QbD) Approach: Formulation Variables and Instrumental Parameters

Pharmaceutics ◽  
2020 ◽  
Vol 12 (7) ◽  
pp. 599 ◽  
Author(s):  
Sara Cunha ◽  
Cláudia Pina Costa ◽  
Joana A. Loureiro ◽  
Jorge Alves ◽  
Andreia F. Peixoto ◽  
...  
Keyword(s):  
Particle Size ◽  
High Pressure ◽  
Drug Release ◽  
Quality By Design ◽  
Nanostructured Lipid Carriers ◽  
Brain Delivery ◽  
High Pressure Homogenization ◽  
Ultrasound Technique ◽  
Formulation Variables

Rivastigmine is a drug commonly used in the management of Alzheimer’s disease that shows bioavailability problems. To overcome this, the use of nanosystems, such as nanostructured lipid carriers (NLC), administered through alternative routes seems promising. In this work, we performed a double optimization of a rivastigmine-loaded NLC formulation for direct drug delivery from the nose to the brain using the quality by design (QbD) approach, whereby the quality target product profile (QTPP) was the requisite for nose to brain delivery. The experiments started with the optimization of the formulation variables (or critical material attributes—CMAs) using a central composite design. The rivastigmine-loaded NLC formulations with the best critical quality attributes (CQAs) of particle size, polydispersity index (PDI), zeta potential (ZP), and encapsulation efficiency (EE) were selected for the second optimization, which was related to the production methods (ultrasound technique and high-pressure homogenization). The most suitable instrumental parameters for the production of NLC were analyzed through a Box–Behnken design, with the same CQAs being evaluated for the first optimization. For the second part of the optimization studies, were selected two rivastigmine-loaded NLC formulations: one produced by ultrasound technique and the other by the high-pressure homogenization (HPH) method. Afterwards, the pH and osmolarity of these formulations were adjusted to the physiological nasal mucosa values and in vitro drug release studies were performed. The results of the first part of the optimization showed that the most adequate ratios of lipids and surfactants were 7.49:1.94 and 4.5:0.5 (%, w/w), respectively. From the second part of the optimization, the results for the particle size, PDI, ZP, and EE of the rivastigmine-loaded NLC formulations produced by ultrasound technique and HPH method were, respectively, 114.0 ± 1.9 nm and 109.0 ± 0.9 nm; 0.221 ± 0.003 and 0.196 ± 0.007; −30.6 ± 0.3 mV and −30.5 ± 0.3 mV; 97.0 ± 0.5% and 97.2 ± 0.3%. Herein, the HPH was selected as the most suitable production method, although the ultrasound technique has also shown effectiveness. In addition, no significant changes in CQAs were observed after 90 days of storage of the formulations at different temperatures. In vitro studies showed that the release of rivastigmine followed a non-Fickian mechanism, with an initial fast drug release followed by a prolonged release over 48 h. This study has optimized a rivastigmine-loaded NLC formulation produced by the HPH method for nose-to-brain delivery of rivastigmine. The next step is for in vitro and in vivo experiments to demonstrate preclinical efficacy and safety. QbD was demonstrated to be a useful approach for the optimization of NLC formulations for which specific physicochemical requisites can be identified.

Clozapine loaded nanostructured lipid carriers engineered for brain targeting via nose-to-brain delivery: Optimization and in vivo pharmacokinetic studies

2021 ◽  
pp. 102533
Author(s):  
Hetal P. Patel ◽  
Priyanshi A. Gandhi ◽  
Priyanka S. Chaudhari ◽  
Bhargavi V. Desai ◽  
Ditixa T. Desai ◽  
...  
Keyword(s):  
Nanostructured Lipid Carriers ◽  
Brain Targeting ◽  
Pharmacokinetic Studies ◽  
Brain Delivery

scholarly journals Nanostructured lipid carriers employing polyphenols as promising anticancer agents: Quality by design (QbD) approach

2017 ◽  
Vol 526 (1-2) ◽  
pp. 506-515 ◽  
Author(s):  
Ketki Bhise ◽  
Sushil Kumar Kashaw ◽  
Samaresh Sau ◽  
Arun K. Iyer
Keyword(s):  
Anticancer Agents ◽  
Quality By Design ◽  
Nanostructured Lipid Carriers

Glycol chitosan functionalized asenapine nanostructured lipid carriers for targeted brain delivery: Pharmacokinetic and teratogenic assessment

2018 ◽  
Vol 108 ◽  
pp. 1092-1100 ◽  
Author(s):  
Sanjay Kumar Singh ◽  
Mahendra Kumar Hidau ◽  
Shrikant Gautam ◽  
Kiran Gupta ◽  
Krishna Pal Singh ◽  
...  
Keyword(s):  
Nanostructured Lipid Carriers ◽  
Brain Delivery ◽  
Glycol Chitosan
Sign in / Sign up

Export Citation Format

Share Document