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Record W4388520006 · doi:10.21203/rs.3.rs-3547278/v1

Antidepressant and Pharmacokinetic Evaluation of Self-Nanoemulsifying Drug Delivery Systems (SNEDDS) of Escitalopram

2023· preprint· en· W4388520006 on OpenAlexaff
M. Asaad, Abdul Majeed, Ghulam Abbas, Farhan Siddique, Furqan Muhammad Iqbal, Syed Nisar Hussain Shah, Muhammad Fawad Rasool, Sidra Muhammad Ali, Naveed Nisar, Maryam Bashir, Yousef A. Bin Jardan, Hiba‐Allah Nafidi, Mohammed Bourhia

Bibliographic record

VenueResearch Square · 2023
Typepreprint
Languageen
FieldPharmacology, Toxicology and Pharmaceutics
TopicDrug Solubulity and Delivery Systems
Canadian institutionsUniversité Laval
Fundersnot available
KeywordsBioavailabilityPulmonary surfactantChromatographyChemistrySolubilityDifferential scanning calorimetryDrug deliveryPolyethylene glycolPharmacologyOrganic chemistryMedicineBiochemistry

Abstract

fetched live from OpenAlex

Abstract Escitalopram (ETP) has poor oral bioavailability due to its low water solubility, hence the goal of this work was to design and optimize a self-nano-emulsifying drug delivery system (SNEDDS). Using the results of the investigations on solubility and emulsification, a pseudo-ternary phase diagram was produced. The three main ingredients chosen for the formulation were polyethylene glycol 400 (co-surfactant), tween 80 (surfactant), and geranium oil (lipid). ETP-SNEDDS was evaluated for the size of particles and surface charge. Fourier transforms infrared spectroscopy (FTIR), differential scanning calorimetry (DSC) and thermogravimetric analysis (TGA) were used to evaluate the chemical compatibility and thermal stability. Ex-vivo permeability, in vitro digestion, and in vitro dissolution investigations were carried out and compared with reference tablets. The bioavailability of ETP-loaded SNEDDS was evaluated in comparison to the control in Wistar rats (n = 6). With a droplet size of 145 nm, a polydispersity index of 0.120, and an emulsification period of almost one minute, the synthesized SNEDDS were thermodynamically stable. The ETP-loaded SNEDDS displayed 96% dissolution in FSSIF. The permeation investigation revealed that, in comparison to the ETP powder and reference tablet, respectively, the SNEDDS increased drug penetration by 4.2 and 3.1-folds. The enhancement of in vitro dissolution, in vitro digestion, and ex-vivo permeability was found significant (p < 0.05). In comparison to the reference, SNEDDS had C max and AUC increases of 5.34 and 4.71 fold, respectively. These findings suggested that the SNEDDS formulation would be a promising method for increasing the oral bioavailability and absorption of ETP.

Fetched live from OpenAlex and de-inverted. Abstracts are not stored in this database: the inverted indexes are 8.6 GB of the frame’s 9.3 GB of text, and the host has 13 GB free.

How this classification was reachedexpand

Full frame distilled prediction

Teacher imitation

Not 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.

metaresearch head score (Codex)0.021
metaresearch head score (Gemma)0.001
Version: codex-gemma-dda1882f352aValidation status: machine_predicted_unvalidated
Candidate categoriesMeta-epidemiology (narrow), Research integrity
Consensus categoriesnone
DomainCandidate signal: none · Consensus signal: none
Study designCandidate signal: Simulation or modeling · Consensus signal: Simulation or modeling
GenreCandidate signal: Empirical · Consensus signal: Empirical
Teacher disagreement score0.538
Threshold uncertainty score1.000

Codex and Gemma teacher scores by category

CategoryCodexGemma
Metaresearch0.0210.001
Meta-epidemiology (narrow)0.0000.000
Meta-epidemiology (broad)0.0010.000
Bibliometrics0.0010.001
Science and technology studies0.0000.001
Scholarly communication0.0000.000
Open science0.0010.002
Research integrity0.0010.003
Insufficient payload (model declined to judge)0.0000.000

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.

Opus teacher head0.362
GPT teacher head0.531
Teacher spread0.170 · how far apart the two teachers sit on this one work
Validation statusscore_only:v0-immature-baseline · verbatim from the scoring run: score_only means the number may rank works, and no category label ships from it

Classification

machine, unvalidated

Machine predicted; a candidate call from one teacher head, not a consensus.

Study designSimulation or modeling
Domainnot available
GenreEmpirical

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".

Quick stats

Citations1
Published2023
Admission routes1
Has abstractyes

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