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Updated: Sep 19, 2025

Transport Properties of Ibuprofen Encapsulated in Cyclodextrin Nanosponge Hydrogels: A Proton HR-MAS NMR Spectroscopy Study
Published on: August 15, 2016
Ibuprofen lysine salt complexed with β-cyclodextrin oral suspension: an innovative pediatric formulation with
Giorgio Ciprandi1, Raffaele Badolato2, Susanna Esposito3
1Allergy Clinic, Casa di Cura Villa Montallegro, Genoa, Italy - gio.cip@libero.it.
Insights
Ibuprofen lysine salt complexed with β-cyclodextrin (ILS-β-CD) offers rapid and prolonged pain and fever relief in children. This formulation enhances absorption and tolerability, making it a beneficial option for pediatric acute conditions.
Area of Science:
- Pediatric Pharmacology
- Drug Delivery Systems
- Pain Management
Background:
- Fever and acute pain are common in children, necessitating effective and rapid relief.
- Standard ibuprofen formulations have poor solubility, leading to delayed absorption and action onset.
- Salification with lysine and complexation with β-cyclodextrin (β-CD) improve ibuprofen's solubility, absorption, and pharmacokinetic profile.
Purpose of the Study:
- To review and discuss the pharmacological profile of ibuprofen lysine salt complexed with β-cyclodextrin (ILS-β-CD).
- To evaluate the suitability of ILS-β-CD for managing fever and pain in pediatric patients.
Main Methods:
- Pharmacological profile review of ILS-β-CD.
- Analysis of clinical studies investigating the product's efficacy and safety.
Main Results:
- ILS-β-CD demonstrates rapid absorption, leading to high and prolonged plasma concentrations.
- The safety profile of ILS-β-CD is comparable to other NSAIDs.
- Two clinical studies support the efficacy of this formulation.
Conclusions:
- ILS-β-CD is a promising option for managing acute fever and pain in children and adolescents.
- The formulation provides rapid onset of action and sustained therapeutic concentrations.
- Optimal tolerability and a favorable safety profile are key benefits.
Background:
Fever and acute pain are frequent symptoms in pediatric age requiring prompt relief when necessary. International guidelines recommend a standard treatment including ibuprofen and acetaminophen. Ibuprofen is an analgesic and antipyretic agent with anti-inflammatory activity. Since the ibuprofen standard formulation is acid and lipophilic, the solubility in an aqueous environment (typically the gastrointestinal mucosa) is poor. As a result, the absorption and action onset are consequently negatively affected. To solve this drawback, salifying with lysine hastens gastrointestinal absorption and increases gastrointestinal tolerability. In addition, complexation with β-cyclodextrin (β-CD) improves hydro-solubility, increasing and prolonging plasmatic concentrations.
Methods:
This compound is presently available as oral suspension indicated in children and adolescents. Thus, the present article reviews and discusses the pharmacological profile of this product.
Results:
Although ibuprofen lysine salt complexed with β-cyclodextrin (ILS-β-CD) has a similar safety profile to other NSAIDs, its quick absorption and high and prolonged plasmatic concentrations make it ideal for managing acute conditions. Two clinical studies investigated this product.
Conclusions:
Based on this evidence, ILS-β-CD may represent a beneficial option for managing fever and pain in children and adolescents. This formulation may provide a rapid onset of action and prolonged concentrations, assuring adequate therapeutic concentrations, optimal tolerability, and a valuable safety profile.
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