Related Experiment Video
Updated: Jan 10, 2026
09:57
A Facile and Efficient Approach for the Production of Reversible Disulfide Cross-linked Micelles
Published on: December 23, 2016
9.2K
Cyclodextrin Complexes for Clinical Translatability: Applications for Cladribine and Retrometabolically Designed
Nicholas Bodor1, Peter Buchwald2,3
1Bodor Laboratories, Miami, FL 33137, USA.
International Journal of Molecular Sciences
|November 27, 2025
Summary
Cyclodextrin-based formulations enhance oral drug delivery. Modified cyclodextrins improve solubility and stability, enabling successful oral cladribine tablets for multiple sclerosis treatment.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery
- Medicinal Chemistry
Background:
- Cyclodextrins (CDs) are cyclic oligosaccharides forming inclusion complexes to enhance drug properties.
- Challenges exist in formulating poorly soluble and unstable drugs for oral administration.
- Retrometabolic chemical delivery systems (CDSs) aim for targeted drug delivery.
Purpose of the Study:
- To review cyclodextrin applications in oral drug formulation.
- To enhance the bioavailability of cladribine via oral tablets.
- To improve the solubility and stability of estredox (estradiol-CDS) and other CDSs.
Main Methods:
- Utilized modified cyclodextrins, specifically 2-hydroxypropyl-β-cyclodextrin (HPβCD).
- Developed dual CD-complex formulations for cladribine tablets.
- Investigated host-guest inclusion complex formation and stability.
Main Results:
- HPβCD significantly increased water solubility and oxidative stability of estredox.
- HPβCD facilitated the development of orally bioavailable cladribine tablets.
- Cladribine-HPβCD tablets (Mavenclad) achieved worldwide approval for multiple sclerosis.
Conclusions:
- Tailored cyclodextrin approaches overcome formulation barriers for challenging drugs.
- CD inclusion complexes demonstrate versatility and clinical impact in pharmaceutical development.
- HPβCD is crucial for developing effective oral drug formulations and targeted delivery systems.
Related Concept Videos
01:05Bioavailability Enhancement: Drug Stability Enhancement and GI Retention
185
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...
185
01:14Drug Metabolism: Phase II Reactions
4.8K
Phase II reactions are essential for the detoxification and elimination of drugs from the body. These reactions involve the conjugation of parent drugs or their phase I metabolites with endogenous molecules, resulting in more hydrophilic drug conjugates. The primary conjugation reactions in this phase are sulfation and glucuronidation. Both sulfation and glucuronidation typically produce biologically inactive metabolites. However, in some cases involving prodrugs, active metabolites may be...
4.8K
01:18β-Dicarbonyl Compounds via Crossed Claisen Condensations
3.8K
Crossed Claisen condensations are base-promoted reactions between two different ester molecules producing β-dicarbonyl compounds. The reaction involving esters, with both containing α hydrogen, results in a mixture of four different products that are difficult to isolate. This reduces the synthetic utility of the reaction.
3.8K
01:19Phase II Reactions: Miscellaneous Conjugation Reactions
340
Phase II biotransformations are detoxification mechanisms that conjugate xenobiotics with endogenous substances, neutralizing their toxicity.
A key example involves the conjugation of cyanide ions, which impair cellular respiration and alter hemoglobin into non-oxygen-carrying cyanmethemoglobin. To neutralize this threat, a sulfur atom from thiosulphate is transferred to the cyanide ion, catalyzed by the enzyme rhodanese, resulting in an inactive compound called thiocyanate. The production of...
A key example involves the conjugation of cyanide ions, which impair cellular respiration and alter hemoglobin into non-oxygen-carrying cyanmethemoglobin. To neutralize this threat, a sulfur atom from thiosulphate is transferred to the cyanide ion, catalyzed by the enzyme rhodanese, resulting in an inactive compound called thiocyanate. The production of...
340
01:16Drug Biotransformation: Overview
3.5K
Pharmaceutical substances known as xenobiotics are predominantly lipophilic and nonionized. This enables them to permeate lipid bilayers, such as cell membranes, and interact with intracellular target receptors. Lipophilic drugs have an advantage in crossing biological barriers and reaching their intended sites of action. However, lipophilic drugs often have a restricted capacity for renal expulsion or elimination from the body. When these drugs enter the kidneys and undergo glomerular...
3.5K