Cetirizine from topical phosphatidylcholine liposomes: Evaluation of peripheral antihistaminic activity and systemic absorption in a rabbit model
Bibliographic record
Abstract
This study was performed to assess the peripheral H(1)-antihistaminic activity and extent of systemic absorption of cetirizine from liposomes applied to the skin. Cetirizine was incorporated into small unilamellar vesicles (SUV) and multilamellar vesicles (MLV) prepared using L-alpha-phosphatidylcholine, and into Glaxal Base (GB), used as the control. In a randomized, cross-over study, each formulation, containing 10 mg of cetirizine, was applied to depilated areas on the backs of six rabbits (3.08+/-0.05 kg). Histamine-induced wheal tests and blood sampling were performed before cetirizine application and at designated times for up to 24 h. Compared with the baseline, histamine-induced wheal formation was suppressed by cetirizine in SUV and MLV from 0.5-24 h and by cetirizine in GB from 0.5-8 h, p</=0.05. Maximum wheal suppression by cetirizine in SUV and MLV ranged from 90.6%+/-4.9% to 89.0%+/-3.8% and 98.0%+/-1.3% to 94.0%+/-2.3%, respectively, from 6 to 8 h. The plasma cetirizine AUC of 201+/-24.2 ng.h/ml from SUV was lower than from PC-MLV, 334.6+/-65.1 ng.h/ml and from GB, 248.3+/-34.6 ng.h/ml. After 24 h, the percent of the cetirizine dose remaining on the backs of the rabbits from SUV was lower than from both MLV and GB, p</=0.05. In this model, cetirizine from both SUV and MLV had excellent topical H(1)-antihistaminic effects, while systemic exposure to cetirizine from SUV was reduced.
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How this classification was reachedexpand
Full frame machine prediction
Teacher imitationNot calibrated prevalence, not ground truth. Human validation pending. The Gemma side is a direct model label for every work in the frame, read from the title-only record. The Codex side is a classifier learned from the 10,348 direct Codex labels and calibrated to design-weighted sample rates; fields without enough sample support carry no Codex call. Candidate is the union of the two sides; consensus is their intersection. These outputs are machine_predicted_unvalidated and are not human labels.
Distilled classifier scores by category (both heads)
| Category | Codex | Gemma |
|---|---|---|
| Metaresearch | 0.001 | 0.000 |
| Meta-epidemiology (narrow) | 0.001 | 0.000 |
| Meta-epidemiology (broad) | 0.001 | 0.000 |
| Bibliometrics | 0.000 | 0.000 |
| Science and technology studies | 0.000 | 0.000 |
| Scholarly communication | 0.000 | 0.001 |
| Open science | 0.000 | 0.000 |
| Research integrity | 0.001 | 0.001 |
| Insufficient payload (model declined to judge) | 0.001 | 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 source (direct Gemma or distilled Codex), 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".