Related Experiment Video
Updated: Jan 9, 2026
16:26
Setting-up an In Vitro Model of Rat Blood-brain Barrier BBB: A Focus on BBB Impermeability and Receptor-mediated Transport
Published on: June 28, 2014
43.2K
Rationally engineered cyclodextrins: smart shuttles for neurological drug targeting and BBB modulation
Mokhtar Rejili1, Gaurav Gupta2, Sachin Kumar Singh3
1Department of Biology, College of Sciences, Imam Mohammad Ibn Saud Islamic University (IMSIU), Riyadh 11623, Saudi Arabia.
Bioorganic Chemistry
|December 9, 2025
Summary
Cyclodextrins (CDs) enhance drug delivery across the blood-brain barrier (BBB) for neurodegenerative disorders. These cyclic oligosaccharides improve drug solubility and neuroprotection by modulating cell membranes and mitochondrial function.
Area of Science:
- Neuroscience
- Pharmacology
- Biochemistry
Background:
- The blood-brain barrier (BBB) limits drug efficacy in treating neurodegenerative diseases due to its selective permeability.
- Conventional drugs often face challenges with solubility and accessing neural targets.
- Neurodegenerative disorders require innovative therapeutic strategies to overcome biological barriers.
Purpose of the Study:
- To review the mechanisms of cyclodextrin (CD)-based drug delivery systems for overcoming BBB limitations.
- To explore how CDs enhance drug solubility, biodistribution, and neuroprotection.
- To discuss the potential of CDs in treating neurodegenerative pathologies.
Main Methods:
- Review of contemporary literature on CD-based drug delivery systems.
- Analysis of CD supramolecular structure and inclusion complex formation.
- Examination of CD interactions with cell membranes, lipids, and transporters.
Main Results:
- CDs form inclusion complexes, enhancing solubility and pharmacokinetics of lipophilic drugs.
- CDs demonstrate neuroprotective effects by modulating membrane lipids, autophagy, and mitochondrial function.
- CDs show potential in traversing the BBB and modulating key pathological processes like neuroinflammation and protein aggregation.
Conclusions:
- CDs offer a promising therapeutic paradigm for neurodegenerative diseases by improving drug delivery and providing inherent neuroprotection.
- Understanding CD-drug conjugate mechanisms, membrane interactions, and transporter effects is crucial for optimizing their use.
- CDs represent a versatile platform for developing novel neurotherapeutics.
Related Concept Videos
00:49The Blood-brain Barrier
52.2K
Overview
52.2K
01:23Factors Affecting Drug Distribution: Physiological Barriers
659
Drug distribution in the body is intricately regulated by various physiological barriers that control the passage of substances. These include the capillary endothelial barrier, the blood-brain, blood-cerebrospinal fluid, blood-placental, and blood-testis barriers.
The capillary endothelial barrier allows only smaller molecules below 600 Da (Daltons) to pass through. It also restricts drugs like heparin that are bound to blood components, limiting their movement within the bloodstream.
The...
The capillary endothelial barrier allows only smaller molecules below 600 Da (Daltons) to pass through. It also restricts drugs like heparin that are bound to blood components, limiting their movement within the bloodstream.
The...
659
01:05Bioavailability Enhancement: Drug Stability Enhancement and GI Retention
184
Body:Improving a drug's stability in the gastrointestinal (GI) tract is paramount for enhancing its bioavailability and therapeutic effectiveness. Various strategies are employed to protect the drug from the harsh gastric milieu and to ensure its release and absorption at the desired site within the GI tract.Polymer coatings are one such method used to shield drugs from the stomach's acidic environment. By preventing premature drug release, these coatings improve the bioavailability of unstable...
184
01:22Biopharmaceutical Factors Influencing Drug Product Design: Overview
222
Rational drug product design integrates knowledge of the drug’s physicochemical properties, formulation components, manufacturing techniques, and intended route of administration. Each factor influences the drug’s performance, including how it is released, absorbed, and eliminated in the body.The physicochemical properties of a drug—such as solubility, stability, and particle size—affect its compatibility with excipients and the choice of dosage form. Excipients, though...
222
01:24Cellular Membranes and Drug Transport
1.4K
Drugs must traverse multiple biological barriers, such as multi-layered skin, single-layered intestinal epithelium, and the plasma membrane, to reach their target sites within the body. The plasma membrane, a highly structured composite of phospholipids, carbohydrates, and proteins, is the cell's protective boundary, facilitating selective substance exchange.
Phospholipids arrange themselves into a bilayer, with hydrophilic heads oriented outward and hydrophobic tails facing inward.
Phospholipids arrange themselves into a bilayer, with hydrophilic heads oriented outward and hydrophobic tails facing inward.
1.4K