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Appl. Sci. 2018, 8(8), 1291; https://doi.org/10.3390/app8081291

Sildenafil Citrate Liposomes for Pulmonary Delivery by Ultrasonic Nebulization

1
Department of Pharmaceutical Sciences, Faculty of Pharmacy, University of Salamanca, 37007 Salamanca, Spain
2
Institute of Biopharmaceutical Sciences of the University of Salamanca (IBSAL), 37007 Salamanca, Spain
3
CPIRN-IPG-Center of Potential and Innovation of Natural Resources, Polytechnic Institute of Guarda, 6300-035 Guarda, Portugal
4
CICS-UBI-Health Sciences Research Centre, University of Beira Interior, 6201-001 Covilha, Portugal
5
Department of Chemical Sciences, Laboratory of Applied Chemistry, Faculty of Pharmacy, Porto University, 4050-313 Porto, Portugal
*
Author to whom correspondence should be addressed.
Received: 26 June 2018 / Revised: 12 July 2018 / Accepted: 19 July 2018 / Published: 2 August 2018
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Abstract

Technological advances in lipid vesicles facilitate optimization of their properties to achieve therapeutic goals and promote alternative drug administration routes. Sildenafil citrate (SC) is orally administered for the treatment of pulmonary hypertension, but local release would be advantageous in terms of efficacy and safety. In the present study, liposomes from egg phosphatidylcholine and cholesterol loaded with SC, with and without d-α-tocopheryl polyethylene glycol 1000 succinate (Vit E TPGS), were prepared by sonication of the components. A transmembrane pH gradient was applied for active loading of liposomes, and the size, zeta potential, and entrapment efficiency (EE%) were determined. The liposomes were lyophilized and then nebulized. The nebulized samples were collected and the EE% was determined. The transmembrane pH gradient produced a significant increase in the EE% (from 17.68 ± 4.25% to 89.77 ± 7.64%) and, after lyophilization, the EE% remained the same as that of the originals, but the size and zeta potential were modified. EE% of liposomes decreased upon nebulization, particularly for those with Vit E TPGS. Thus, the additives used for lyoprotection reduced the impact of nebulization. Additional studies are essential, but according to these results, SC-loaded liposomes can be considered as suitable and safe carriers for the local release of sildenafil in the pulmonary system. View Full-Text
Keywords: liposomes; pulmonary delivery; sildenafil; local drug release; transmembrane pH gradient; solvent-free pharmaceutical procedures liposomes; pulmonary delivery; sildenafil; local drug release; transmembrane pH gradient; solvent-free pharmaceutical procedures
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).
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de Jesús Valle, M.J.; Gil González, P.; Prata Ribeiro, M.; Araujo Pereira, A.R.T.S.; Sánchez Navarro, A. Sildenafil Citrate Liposomes for Pulmonary Delivery by Ultrasonic Nebulization. Appl. Sci. 2018, 8, 1291.

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