AIMC Topic: Permeability

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Mechanics of small intestine motility for oral macromolecular delivery: modelling segmentation versus peristalsis.

Drug delivery
Intestinal motility, including peristalsis and segmentation, drives complex fluid movements critical for the oral delivery of biologics and other macromolecules. Despite advances, oral delivery remains commercially limited by low bioavailability, oft...

Enhancing the Predictive Power of Macrocyclic Drug Permeability by Knowledge Distillation from Analogous Pretraining Data.

Journal of medicinal chemistry
Macrocyclic drugs offer powerful opportunities for modulating protein-protein interactions, yet their development is limited by poor and unpredictable membrane permeability. Experimental testing is slow, and 3D modeling of macrocycles is computationa...

Enhancing Permeability Prediction of Heterobifunctional Degraders Using Machine Learning and Metadynamics-Informed 3D Molecular Descriptors.

Journal of chemical information and modeling
Heterobifunctional degraders, a class of targeted protein degraders (TPDs), often occupy beyond-rule-of-five (bRo5) chemical space, where traditional passive permeability models─calibrated on drug-like molecules or peptides and based on topological d...

Manifold Embedding of Quantum Information as Molecule Representation to Predict Blood-Brain Barrier Permeability by Deep Learning.

Molecular pharmaceutics
Neurological disorders continue to be a leading global health challenge, with the blood-brain barrier (BBB) presenting considerable obstacles to effective drug delivery for central nervous system (CNS) therapies. Accurately predicting BBB permeabilit...

Integrated evaluation and optimization of acid fracturing effectiveness in carbonate reservoirs: Experimental insights and field validation.

PloS one
The development of carbonate reservoirs is confronted with significant challenges, including pronounced heterogeneity and suboptimal porosity-permeability characteristics. These challenges are particularly acute in low-porosity, low-permeability comp...

Advances in brain-targeted delivery strategies and natural product-mediated enhancement of blood-brain barrier permeability.

Journal of nanobiotechnology
The blood-brain barrier (BBB) represents a formidable challenge in the treatment of neurological disorders, as it restricts the passage of most therapeutic agents into the central nervous system (CNS). Research in brain-targeted delivery strategies a...

Intestinal permeability of N-acetylcysteine is driven by gut microbiota-dependent cysteine palmitoylation.

Nature communications
Trillions of intestinal microbiota are essential to the permeability of orally administered drugs. However, identifying microbial-drug interactions remains challenging due to the highly variable composition of intestinal flora among individuals. Usin...

Modelling of intrinsic membrane permeability of drug molecules by explainable ML-based q-RASPR approach towards better pharmacokinetics and toxicokinetics properties.

SAR and QSAR in environmental research
Drug discovery's success lies in potent inhibition against a target and optimum pharmacokinetic and toxicokinetic properties of drug molecules. Membrane permeability is a crucial factor in determining the absorption, distribution, metabolism, and exc...

GCN-BBB: Deep Learning Blood-Brain Barrier (BBB) Permeability PharmacoAnalytics with Graph Convolutional Neural (GCN) Network.

The AAPS journal
The Blood-Brain Barrier (BBB) is a selective barrier between the Central Nervous System (CNS) and the peripheral system, regulating the distribution of molecules. BBB permeability has been crucial in CNS-targeting drug development, such as glioblasto...

Seeking Correlation Among Porin Permeabilities and Minimum Inhibitory Concentrations Through Machine Learning: A Promising Route to the Essential Molecular Descriptors.

Molecules (Basel, Switzerland)
Developing effective antibiotics against Gram-negative bacteria remains challenging due to their protective outer membrane. With this study, we investigated the relationship between antibiotic permeation through the OmpF porin of and antimicrobial e...