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Cyclodextrins as a potential carrier in drug nebulization
B Evrard1, P Bertholet, M Gueders
1Department of Pharmacy, University of Liège, CHU-Tour 4, Bât B36, Avenue de l' Hôpital 1, 4000, Liège 1, Belgium. B.Evrad@ulg.ac.be
Summary
Cyclodextrins (CDs) enhance hydrophobic drug solubility for inhalation therapy. Short-term inhalation of HP-beta-CD, gamma-CD, and RAMEB solutions showed no significant toxicity in mice.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
- Inhalation Therapy
Background:
- The inhalation route is a key delivery method for local and systemic drug distribution.
- Solubilizing hydrophobic drugs for inhalation formulations presents a significant challenge.
Purpose of the Study:
- To evaluate the feasibility of using cyclodextrins (CDs) for formulating hydrophobic drugs for inhalation.
- To assess the short-term toxicity of inhaled cyclodextrin solutions in a mouse model.
Main Methods:
- Aerosolization of Hydroxypropyl-beta-cyclodextrin (HP-beta-CD), gamma-cyclodextrin (gamma-CD), and RAMEB solutions.
- Assessment of droplet size for pulmonary deposition compatibility.
- In vivo toxicity testing in C57BL/6 mice, including bronchoalveolar lavage (BAL), histology, and physiological measurements.
Main Results:
- HP-beta-CD, gamma-CD, and RAMEB solutions were successfully aerosolized with suitable droplet sizes for lung deposition.
- Short-term inhalation exposure to these CD solutions demonstrated no significant toxicity.
- A minor increase in lymphocyte count in BAL fluid was observed post-HP-beta-CD and gamma-CD inhalation.
Conclusions:
- Cyclodextrins are effective in enhancing the solubility of apolar drugs for inhalation therapy.
- Inhaled HP-beta-CD, gamma-CD, and RAMEB show a favorable short-term safety profile.
- Further investigation is warranted regarding the observed increase in BAL lymphocytes.