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Transport Properties of Ibuprofen Encapsulated in Cyclodextrin Nanosponge Hydrogels: A Proton HR-MAS NMR Spectroscopy Study
Published on: August 15, 2016
Characterisation of an inclusion complex between cladribine and 2-hydroxypropyl-beta-cyclodextrin
Valeria Van Axel Castelli1, Giovanni Trivieri, Ilaria Zucchelli
1Merck Serono SpA, Tiburtina Site, via L Einaudi 11, 00012 Guidonia Montecelio, Roma, Italy. valeria.vanaxel@merckserono.net
Journal of Pharmaceutical Sciences
|January 18, 2008
Summary
An oral formulation of cladribine (2-chloro-2'-deoxyadenosine) was developed using 2-hydroxypropyl-beta-cyclodextrin (2-HP-beta-CD). Chemical characterization confirmed a stable inclusion complex, suitable for treating multiple sclerosis (MS).
Area of Science:
- Pharmaceutical Chemistry
- Drug Delivery Systems
- Multiple Sclerosis Therapeutics
Background:
- Parenteral cladribine (2-chloro-2 -deoxyadenosine) shows efficacy in multiple sclerosis (MS) treatment.
- An oral formulation offers a more convenient therapeutic option for MS patients.
- Drug carrier molecules can improve the properties of active pharmaceutical ingredients.
Purpose of the Study:
- To chemically characterize the inclusion complex formed between cladribine and 2-hydroxypropyl-beta-cyclodextrin (2-HP-beta-CD).
- To assess the stability and manufacturability of a tablet formulation containing the cladribine-2-HP-beta-CD complex.
- To provide a foundation for the clinical investigation of oral cladribine for MS.
Main Methods:
- Formation of an inclusion complex between cladribine and 2-HP-beta-CD.
- Analysis of the complex in solution and solid states using various chemical characterization techniques.
- Nuclear magnetic resonance (NMR) spectroscopy to confirm complex formation.
- Evaluation of tablet formulation stability and manufacturing impact.
Main Results:
- Evidence confirmed the formation of a cladribine-2-HP-beta-CD inclusion complex, distinct from a physical mixture.
- Solution NMR spectroscopy verified the existence of the inclusion complex.
- The tablet formulation process did not alter the complex's chemical characteristics.
- The inclusion complex demonstrated stability during storage.
Conclusions:
- A stable oral formulation of cladribine has been successfully developed using 2-HP-beta-CD.
- The characterized inclusion complex is suitable for manufacturing into a stable tablet form.
- This oral formulation represents a promising advancement for multiple sclerosis treatment.
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