Nebulized solid lipid nanoparticles for the potential treatment of pulmonary hypertension via targeted delivery of phosphodiesterase-5-inhibitor

Makled, Shaimaa; Nafee, Noha; Boraie, Nabila

doi:10.1016/j.ijpharm.2016.12.026

Cited by 70 publications

(45 citation statements)

References 52 publications

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“…The samples were scanned from 30 to 3008C, at 108C min 21 of flow rate. Nitrogen gas was used as purge gas, at 40 ml min 21 . The melting point ( peak maximum), was calculated using the (NETZSCH Proteus w Software-Thermal Analysis-Version 6.1) software provided for the DSC equipment.…”

Section: Differential Scanning Calorimetrymentioning

confidence: 99%

Overcoming clofazimine intrinsic toxicity: statistical modelling and characterization of solid lipid nanoparticles

Chaves

Lima

Vieira

et al. 2018

J. R. Soc. Interface.

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The aim of this work was to develop solid lipid nanoparticles (SLNs) loaded with clofazimine (CLZ) (SLNs-CLZ) to overcome its intrinsic toxicity and low water solubility, for oral drug delivery. A Box-Behnken design was constructed to unravel the relations between the independent variables in the selected responses. The optimized SLNs-CLZ exhibited the following properties: particle size 230 nm, zeta potential of -34.28 mV, association efficiency of 72% and drug loading of 2.4%, which are suitable for oral delivery. Further characterization included Fourier transformed infrared spectroscopy that confirmed the presence of the drug and the absence of chemical interactions. By differential scanning calorimetry was verified the amorphous state of CLZ. The storage stability studies ensured the stability of the systems over a period of 12 weeks at 4°C. cytotoxicity studies evidenced no effect of both drug-loaded and unloaded SLNs on MKN-28 gastric cells and on intestinal cells, namely Caco-2 and HT29-MTX cells up to 25 µg ml in CLZ. Free CLZ solutions exhibited IC values of 16 and 20 µg ml for Caco-2 and HT29-MTX cells, respectively. It can be concluded that the optimized system, designed considering important variables for the formulation of poorly soluble drugs, represents a promising platform for oral CLZ delivery.

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Section: Differential Scanning Calorimetrymentioning

confidence: 99%

Overcoming clofazimine intrinsic toxicity: statistical modelling and characterization of solid lipid nanoparticles

Chaves

Lima

Vieira

et al. 2018

J. R. Soc. Interface.

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“…All the spectra present similar vibration modes with few notorious differences, which can be justified by the common chemical moieties encountered either in the lipidic constituents of the nanosystems [39][40][41][42][43][44][45] or in the bioactive omega-3 [42] or even in the textile substrate [43]. The presence of the bioactive RSV, normally detected by the presence of trans olefinic bands at 986 and 964 cm −1 [44], was also not possible to assign.…”

Section: Functionalization Of Textile Substratesmentioning

confidence: 99%

“…Although textile substrate possesses CH 2 groups in its composition, these groups appear in higher number in the long aliphatic tails of fatty acids constituents of lipids (e.g. Precirol® ATO 5) [39] or omega-3 [42], therefore originating more intense bands. The second difference noticed is a band at 1732 cm −1 characteristic of C=O bonds that are also part of the ester region of both Precirol® ATO 5 and omega-3 [39,42].…”

Section: Functionalization Of Textile Substratesmentioning

confidence: 99%

“…Precirol® ATO 5) [39] or omega-3 [42], therefore originating more intense bands. The second difference noticed is a band at 1732 cm −1 characteristic of C=O bonds that are also part of the ester region of both Precirol® ATO 5 and omega-3 [39,42]. The vibration modes characteristic of NLCs spectra are evident in both methods of functionalization, but are less intense in the impregnation method ( Fig.…”

Section: Functionalization Of Textile Substratesmentioning

confidence: 99%

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Incorporation of lipid nanosystems containing omega-3 fatty acids and resveratrol in textile substrates for wound healing and anti-inflammatory applications

et al. 2019

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In the present work, lipid nanosystems containing omega-3 fatty acid (nanostructured lipid carriers, NLCs) or omega-3 fatty acid and resveratrol (liposomes) were developed to improve cotton textile substrates as dressings with anti-inflammatory properties for wound healing applications. Lipid nanosystems were incorporated into woven, non-woven and knitted cotton substrates by exhaustion and impregnation. Based on physical-chemical characterization of the textile substrates, the textile structure and type of lipid nanosystems dictated the adsorption efficiency. In the case of NLCs, the woven substrate functionalized by exhaustion had a higher omega-3 release being the most promising for wound dressing application. Whereas for liposomes, the most adequate textile was the cationized knitted fabric functionalized by impregnation, that showed a more prolonged release profile of resveratrol.

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“…Accordingly, the inhalation of drugs entrapped in liposomes is likely to produce safer and more efficacious kinetic profiles than the inhalation of free drugs. Sildenafil formulations based on solid lipid nanoparticles [19,20] and polymeric biodegradable nanoparticles [21][22][23][24][25] have been recently developed and are currently being assessed as potential pulmonary delivery systems. However, liposomal formulations of sildenafil have only been proposed for vaginal delivery [26].…”

Section: Introductionmentioning

confidence: 99%

Sildenafil Citrate Liposomes for Pulmonary Delivery by Ultrasonic Nebulization

et al. 2018

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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.

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Nebulized solid lipid nanoparticles for the potential treatment of pulmonary hypertension via targeted delivery of phosphodiesterase-5-inhibitor

Cited by 70 publications

References 52 publications

Overcoming clofazimine intrinsic toxicity: statistical modelling and characterization of solid lipid nanoparticles

Overcoming clofazimine intrinsic toxicity: statistical modelling and characterization of solid lipid nanoparticles

Incorporation of lipid nanosystems containing omega-3 fatty acids and resveratrol in textile substrates for wound healing and anti-inflammatory applications

Sildenafil Citrate Liposomes for Pulmonary Delivery by Ultrasonic Nebulization

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