Sildenafil Citrate Liposomes for Pulmonary Delivery by Ultrasonic Nebulization
Abstract
:1. Introduction
2. Materials and Methods
2.1. Reagents
2.2. Preparation of Liposomes
2.3. Lyophilization
2.4. Nebulization
2.5. Characterization of Liposomes
2.6. Statistical Analysis
3. Results
4. Discussion
5. Conclusions
Author Contributions
Funding
Conflicts of Interest
References
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Influence of the Transmembrane pH Gradient on the Characteristics of the Liposomes | ||||||
---|---|---|---|---|---|---|
Liposomes | Dh (nm) | PDI | Zeta Potential (mV) | EE (%) | DL (mg/g lipid) | |
Without Vit E TPGS | pH = 6.7 | - | - | - | <18% | <11 |
pH = 3.2 | 304.3 | 0.413 | −2.10 | 49.47 ± 9.78 | 29.71 ± 5.87 | |
pH gradient | 209.7 | 0.537 | −20.90 | 89.77 ± 7.64 | 53.92 ± 4.59 | |
With Vit E TPGS | pH = 6.7 | - | - | - | <15% | <9 |
pH = 3.2 | 303.2 | 0.452 | −2.05 | 22.67 ± 11.32 | 13.62 ± 11.00 | |
pH gradient | 219.8 | 0.534 | −21.30 | 80.30 ± 11.03 | 48.23 ± 6.62 |
Influence of Lyophilization on the Characteristics of the Liposomes | ||||||
---|---|---|---|---|---|---|
Liposomes | Dh (nm) | PDI | Zeta Potential (mV) | EE% | DL (mg/g Lipid) | |
Without Vit E TPGS | Fresh | 209.7 | 0.537 | −20.90 | 89.77 ± 7.64 | 53.32 ± 4.59 |
S | 408.4 | 0.572 | −21.0 | 89.65 ± 1.02 | 53.84 ± 0.61 | |
T | 433.1 | 0.577 | −46.6 | 89.95 ± 2.15 | 54.02 ± 1.29 | |
S + T | 471.7 | 0.701 | −38.9 | 88.95 ± 0.30 | 53.42 ± 0.18 | |
Liposomes | Dh (nm) | PDI | Zeta Potential (mV) | EE% | DL (mg/g Lipid) | |
With Vit E TPGS | Fresh | 219.8 | 0.534 | −21.30 | 80.30 ± 11.03 | 48.23 ± 0.13 |
S | 367.5 | 0.642 | −34.0 | 88.77 ± 0.22 | 53.32 ± 0.35 | |
T | 826.9 | 0.642 | −36.6 | 88.57 ± 0.59 | 53.20 ± 0.35 | |
S + T | 688.4 | 0.682 | −31.2 | 88.39 ± 0.25 | 53.09 ± 0.15 | |
Influence of Nebulization on the Liposomes Stability (EE%) | |||||
---|---|---|---|---|---|
Liposomes | 0 min | 5 min | 10 min | 15 min | |
Without Vit E TPGS | Fresh | 89.77 ± 7.64 | 85.10 ± 0.64 | 83.56 ± 3.04 | 77.78 ± 0.89 |
S | 89.65 ± 1.02 | 87.35 ± 0.88 | 82.73 ± 1.28 | 79.47 ± 1.02 | |
T | 89.95 ± 2.15 | 86.90 ± 0.50 | 81.23 ± 4.29 | 78.15 ± 1.91 | |
S + T | 88.95 ± 0.30 | 87.06 ± 0.39 | 83.04 ± 0.88 | 79.89 ± 1.79 | |
With Vit E TPGS | Fresh | 80.30 ± 11.03 | 76.76 ± 0.52 | 69.34 ± 1.16 | 59.24 ± 1.61 |
S | 88.77 ± 0.22 | 85.84 ± 0.92 | 84.06 ± 0.97 | 82.20 ± 1.13 | |
T | 88.57 ± 0.59 | 85.94 ± 0.43 | 82.86 ± 0.53 | 81.12 ± 1.43 | |
S + T | 88.39 ± 0.25 | 86.05 ± 1.05 | 84.15 ± 1.04 | 81.82 ± 0.89 |
Nebulizer Performance | |||||
---|---|---|---|---|---|
Liposomes | DR (mL/min) | NE (%) | η (mm2/s) | ρ (g/mL) | |
Without Vit E TPGS | Fresh | 0.21 ± 0.01 | 50.51 ± 2.47 | 1.13 ± 0.04 | 1.01 ± 0.01 |
S | 0.17 ± 0.01 | 65.19 ± 2.98 | 1.27 ± 0.03 | 1.02 ± 0.01 | |
T | 0.19 ± 0.02 | 75.22 ± 6.08 | 1.24 ± 0.01 | 1.01 ± 0.01 | |
S + T | 0.19 ± 0.02 | 68.00 ± 2.48 | 1.27 ± 0.01 | 1.02 ± 0.01 | |
With Vit E TPGS | Fresh | 0.20 ± 0.01 | 50.87 ± 1.90 | 1.18 ± 0.06 | 1.01 ± 0.01 |
S | 0.16 ± 0.02 | 76.99 ± 2.69 | 1.30 ± 0.04 | 1.02 ± 0.01 | |
T | 0.18 ± 0.01 | 78.41 ± 0.22 | 1.28 ± 0.03 | 1.00 ± 0.00 | |
S + T | 0.16 ± 0.01 | 81.24 ± 2.12 | 1.26 ± 0.04 | 1.02 ± 0.01 |
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De Jesús Valle, M.J.; Gil González, P.; Prata Ribeiro, M.; Araujo, A.R.T.S.; Sánchez Navarro, A. Sildenafil Citrate Liposomes for Pulmonary Delivery by Ultrasonic Nebulization. Appl. Sci. 2018, 8, 1291. https://doi.org/10.3390/app8081291
De Jesús Valle MJ, Gil González P, Prata Ribeiro M, Araujo ARTS, Sánchez Navarro A. Sildenafil Citrate Liposomes for Pulmonary Delivery by Ultrasonic Nebulization. Applied Sciences. 2018; 8(8):1291. https://doi.org/10.3390/app8081291
Chicago/Turabian StyleDe Jesús Valle, María José, Pablo Gil González, Maximiano Prata Ribeiro, André R. T. S. Araujo, and Amparo Sánchez Navarro. 2018. "Sildenafil Citrate Liposomes for Pulmonary Delivery by Ultrasonic Nebulization" Applied Sciences 8, no. 8: 1291. https://doi.org/10.3390/app8081291