Lipid carrier-based intranasal delivery of calcium channel blockers for Alzheimer’s disease
Bibliographic record
Abstract
BACKGROUND: Felodipine (FLD) is an L-type calcium channel blocker with pronounced neuroprotection against Alzheimer's disease (AD). Unfortunately, the efficacy of FLD has been impeded by limited solubility, poor bioavailability, and sub-optimal accumulation. Thus, the current study unfolds the potential of nanostructured lipid carriers based on in-situ gel of FLD (FLD-NLCs gel) to ameliorate dementia. METHODS: The FLD-contained NLCs were prepared using the microemulsion-sonication method and further integrated into thermosensitive gel comprised poloxamer 407 and HPMC K4M. The formulation was evaluated by ex-vivo permeation study, cell culture studies, and in-vivo efficacy study. The toxicity of formulation was assessed by HET-CAM assay, and nasal cilitoxicity study. RESULTS: The optimized FLD-NLCs had nanoscaled dimension, spherical shape, and augmented %EE (~96%). The FLD-NLCs gel displayed biphasic release, with ~1.3-fold higher permeation as relative to free FLD. The HET-CAM assay and cell culture study revealed compatible nature of formulation. The in-vivo biochemical, neurotransmitter, and inflammatory marker determination revealed neuroprotective and restorative potential of the FLD-NLCs gel. CONCLUSIONS: The repurposing tactic of FLD presents a viable concept to combat AD. Also, the NLC-based temperature responsive intranasal gel exemplifies a practical approach to augment the efficacy of FLD.
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How this classification was reachedexpand
Full frame distilled prediction
Teacher imitationNot calibrated prevalence, not ground truth. Human validation pending. Learned from the 10,348 direct Codex labels and 10,348 direct Gemma labels. Candidate is the union of thresholded teacher heads; consensus is their intersection. These outputs are machine_predicted_unvalidated and are not human labels or direct frontier model labels.
Codex and Gemma teacher scores by category
| Category | Codex | Gemma |
|---|---|---|
| Metaresearch | 0.001 | 0.000 |
| Meta-epidemiology (narrow) | 0.001 | 0.001 |
| Meta-epidemiology (broad) | 0.001 | 0.000 |
| Bibliometrics | 0.001 | 0.000 |
| Science and technology studies | 0.000 | 0.000 |
| Scholarly communication | 0.000 | 0.000 |
| Open science | 0.001 | 0.000 |
| Research integrity | 0.000 | 0.001 |
| Insufficient payload (model declined to judge) | 0.000 | 0.000 |
Machine scores (provisional)
The two teacher heads of the student model, read on this work. A score orders the frame for review; it never asserts a category, and the validation status ships verbatim with every row.
Baseline scores from an immature model (maturity gate not passed, 7 training rounds). Scores rank; they never assert a category.
score_only:v0-immature-baseline · verbatim from the scoring run: score_only means the number may rank works, and no category label ships from itClassification
machine, unvalidatedMachine predicted; a candidate call from one teacher head, not a consensus.
How this classification was reached, model by model and score by score, is at the end of the page under "How this classification was reached".