ArticleMolecular pharmaceutics2016
Tools for Early Prediction of Drug Loading in Lipid-Based Formulations.
Article in Molecular pharmaceutics, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 32 papers.
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Who cites it
32 citing papers in PubMed.
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- Foamable pluroleosomes system loaded with amlodipine as a repurposed antibacterial topical formulation against MRSA-induced infection; optimization,International journal of pharmaceutics: X · 2025Article
- Machine Learning-Based Prediction of Drug Solubility in Lipidic Environments: The Sol_ME Tool for Optimizing Lipid-Based Formulations with a Preliminary Apalutamide Case Study.AAPS PharmSciTech · 2025Article
- Advancements in nanoscale delivery systems: optimizing intermolecular interactions for superior drug encapsulation and precision release.Drug delivery and translational research · 2025Review
- Comparative Analysis of Chemical Descriptors by Machine Learning Reveals Atomistic Insights into Solute-Lipid Interactions.Molecular pharmaceutics · 2024Article
- Solubility of Poorly Soluble Drugs in Phosphatidylcholine-Based Drug Delivery Systems: Comparison of the Loading Capacity in the Bulk Formulation and Its Dispersed State.Pharmaceuticals (Basel, Switzerland) · 2024Article
- Enhancing Solubility and Bioefficacy of Stilbenes by Liposomal Encapsulation-The Case of Macasiamenene F.ACS omega · 2024Article
- Nanostructured Lipid Carriers Mediated Drug Delivery to Posterior Segment of Eye and theirCurrent pharmaceutical biotechnology · 2024Review
- Solid Self Nano-Emulsifying Drug Delivery System of Dasatinib: Optimization,Therapeutic delivery · 2024Article
- Intrinsic lipolysis rate for systematic design of lipid-based formulations.Drug delivery and translational research · 2023Article
- IntegratedActa pharmaceutica Sinica. B · 2021Article
- In Vitro Evaluation of a Solid Supersaturated Self Nanoemulsifying Drug Delivery System (Super-SNEDDS) of Aprepitant for Enhanced Solubility.Pharmaceuticals (Basel, Switzerland) · 2021Article
- Premix Membrane Emulsification: Preparation and Stability of Medium-Chain Triglyceride Emulsions with Droplet Sizes below 100 nm.Molecules (Basel, Switzerland) · 2021Article
- Artificial Neural Networks to Predict the Apparent Degree of Supersaturation in Supersaturated Lipid-Based Formulations: A Pilot Study.Pharmaceutics · 2021Article
- Investigation of Self-Emulsifying Drug-Delivery System Interaction with a Biomimetic Membrane under Conditions Relevant to the Small Intestine.Langmuir : the ACS journal of surfaces and colloids · 2021Article
- Targeted drug delivery strategies for precision medicines.Nature reviews. Materials · 2021Article
- Formulation of Cannabidiol in Colloidal Lipid Carriers.Molecules (Basel, Switzerland) · 2021Article
- In-Silico Screening of Lipid-Based Drug Delivery Systems.Pharmaceutical research · 2020Article
Corrections and comments
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Authors and funding
3 authors.
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Abstract
Identification of the usefulness of lipid-based formulations (LBFs) for delivery of poorly water-soluble drugs is at date mainly experimentally based. In this work we used a diverse drug data set, and more than 2,000 solubility measurements to develop experimental and computational tools to predict the loading capacity of LBFs. Computational models were developed to enable in silico prediction of solubility, and hence drug loading capacity, in the LBFs. Drug solubility in mixed mono-, di-, triglycerides (Maisine 35-1 and Capmul MCM EP) correlated (R(2) 0.89) as well as the drug solubility in Carbitol and other ethoxylated excipients (PEG400, R(2) 0.85; Polysorbate 80, R(2) 0.90; Cremophor EL, R(2) 0.93). A melting point below 150 °C was observed to result in a reasonable solubility in the glycerides. The loading capacity in LBFs was accurately calculated from solubility data in single excipients (R(2) 0.91). In silico models, without the demand of experimentally determined solubility, also gave good predictions of the loading capacity in these complex formulations (R(2) 0.79). The framework established here gives a better understanding of drug solubility in single excipients and of LBF loading capacity. The large data set studied revealed that experimental screening efforts can be rationalized by solubility measurements in key excipients or from solid state information. For the first time it was shown that loading capacity in complex formulations can be accurately predicted using molecular information extracted from calculated descriptors and thermal properties of the crystalline drug.
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