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Article

Improvement of Butamben Anesthetic Efficacy by the Development of Deformable Liposomes Bearing the Drug as Cyclodextrin Complex

1
Department of Chemistry, University of Florence, via Schiff 6, Sesto Fiorentino, 50019 Florence, Italy
2
Department of Neuroscience, Psychology, Drug Research and Child Health (NEUROFARBA), Pharmacology and Toxicology Section, University of Florence, 50139 Florence, Italy
*
Author to whom correspondence should be addressed.
Academic Editor: Christian Celia
Pharmaceutics 2021, 13(6), 872; https://doi.org/10.3390/pharmaceutics13060872
Received: 13 May 2021 / Revised: 7 June 2021 / Accepted: 9 June 2021 / Published: 12 June 2021
(This article belongs to the Special Issue Cyclodextrins in Drug Delivery)
This work was aimed at enhancing butamben (BTB) anesthetic efficacy by the “drug-in cyclodextrin (CD)-in deformable liposomes” strategy. In the study, phase-solubility studies with natural (α-, β-, γ-) and derivative (hydroxypropyl-α-and β-, sulfobutylether-β, methyl-β) CDs evidenced the highest BTB affinity for βCD and its derivatives and indicated methyl-βCD (RAMEB) as the best carrier. Drug-RAMEB complexes were prepared by different techniques and were characterized for solid-state and dissolution properties. The best BTB–RAMEB product was chosen for entrapment in the aqueous core of deformable liposomes containing stearylamine, either alone or with sodium cholate, as edge activators. Double-loaded (DL) liposomes, bearing the lipophilic drug (0.5% w/v) in the bilayer and its hydrophilic RAMEB complex (0.5% w/v) in the aqueous core, were compared to single-loaded (SL) liposomes bearing 1% w/v plain drug in the bilayer. All vesicles showed homogeneous dimensions (i.e., below 300 nm), high deformability, and excellent entrapment efficiency. DL-liposomes were more effective than SL ones in limiting drug leakage (<5% vs. >10% after a 3 months storage at 4 °C). In vivo experiments in rabbits proved that all liposomal formulations significantly (p < 0.05) increased the intensity and duration of drug anesthetic action compared to its hydroalcoholic solution; however, DL liposomes were significantly (p < 0.05) more effective than SL ones in prolonging BTB anesthetic effect, owing to the presence of the drug-RAMEB complex in the vesicle core, acting as a reservoir. DL liposomes containing both edge activators were found to have the best performance. View Full-Text
Keywords: butamben; deformable liposomes; stearylamine; sodium cholate; double-loading; in vivo anesthetic effect butamben; deformable liposomes; stearylamine; sodium cholate; double-loading; in vivo anesthetic effect
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MDPI and ACS Style

Mura, P.; Maestrelli, F.; Cirri, M.; Nerli, G.; Di Cesare Mannelli, L.; Ghelardini, C.; Mennini, N. Improvement of Butamben Anesthetic Efficacy by the Development of Deformable Liposomes Bearing the Drug as Cyclodextrin Complex. Pharmaceutics 2021, 13, 872. https://doi.org/10.3390/pharmaceutics13060872

AMA Style

Mura P, Maestrelli F, Cirri M, Nerli G, Di Cesare Mannelli L, Ghelardini C, Mennini N. Improvement of Butamben Anesthetic Efficacy by the Development of Deformable Liposomes Bearing the Drug as Cyclodextrin Complex. Pharmaceutics. 2021; 13(6):872. https://doi.org/10.3390/pharmaceutics13060872

Chicago/Turabian Style

Mura, Paola, Francesca Maestrelli, Marzia Cirri, Giulia Nerli, Lorenzo Di Cesare Mannelli, Carla Ghelardini, and Natascia Mennini. 2021. "Improvement of Butamben Anesthetic Efficacy by the Development of Deformable Liposomes Bearing the Drug as Cyclodextrin Complex" Pharmaceutics 13, no. 6: 872. https://doi.org/10.3390/pharmaceutics13060872

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