Interaction of mTHPC liposomal formulations with serum proteins
Bibliographic record
Abstract
The use of liposomes as drug delivery systems is an accepted approach to improve the photosensitizer efficacy. Because of their characteristic small size (between 50 and 200 nm) and good solubility and stability, liposomes represent an ideal delivery system for nonpolar photodrugs. In this perspective, a clinically approved photosensitizer, meta-tetra(hydroxyphenyl)chlorin (mTHPC) has been loaded into liposomes with or without addition of PEGylated lipid. The present study addresses the distribution pattern of liposomal mTHPC (Foslip(R) and Fospeg(R)) in blood serum assessed by gel-filtration chromatography It was found that the affinity of pure and liposome-based mTHPC towards different plasma proteins is almost identical. The major part of the photosensitizer localizes in the high density lipoproteins fractions, while a minor fraction passes through the column with low-density lipoproteins. Only a small part of mTHPC molecules is found in the albumin fraction. As opposed to conventional liposomes with a very rapid disruption of the lipid vesicles and fast release of the drugs, mTHPC loaded DPPC/DPPG liposomes show a very slow release of the active component. After 30 min of Foslip(R) incubation with serum only a small percentage of mTHPC redistributes from the liposomes. Increasing incubation time to 6 h results in a significant reduction of the mTHPC fluorescence signal associated with mTHPC embedded into liposomes and concomitant increase of the signal associated with the protein- based bands. After 24 h incubation the distribution pattern was similar to the elution profile of serum containing free mTHPC. In contrast to Foslip(R), short incubation of PEGylated liposomes containing mTHPC (Fospeg(R)) with serum results in a release of approximately half of mTHPC from the lipid carriers. The kinetics of release is clearly two-phased: rapid release followed by slow redistribution. The slow phase is decelerated compared to Foslip(R).
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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 | 0.000 | 0.000 |
| Meta-epidemiology (narrow) | 0.000 | 0.000 |
| Meta-epidemiology (broad) | 0.000 | 0.000 |
| Bibliometrics | 0.000 | 0.000 |
| Science and technology studies | 0.000 | 0.000 |
| Scholarly communication | 0.000 | 0.000 |
| Open science | 0.000 | 0.000 |
| Research integrity | 0.000 | 0.000 |
| 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".