Physicochemical characterization of sildenafil-loaded solid lipid nanoparticle dispersions (SLN) for pulmonary application

Paranjpe, Mukta; Finke, Jan Henrik; Richter, Claudia; Gothsch, T.; Kwade, Arno; Büttgenbach, S.; Müller‐Goymann, Christel C.

doi:10.1016/j.ijpharm.2014.09.031

Cited by 31 publications

(8 citation statements)

References 26 publications

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“…Although definitive guidelines on dosage regimens have not yet been established, conservative doses are currently recommended given the serious side effects observed with high doses [ 23 ]. Some studies have focused on sildenafil formulations based on polymeric and lipid solid nanoparticles for sustained pulmonary delivery [ 24 , 25 , 26 , 27 , 28 , 29 , 30 ], but liposome-based formulations have not been proposed yet. According to the above considerations, the aim of this work was to investigate the stabilizing effects of additives approved for pulmonary drug administration (mannitol and lactose) when used for the lyophilization of liposomes loaded with SC.…”

Section: Introductionmentioning

confidence: 99%

Lyoprotective Effects of Mannitol and Lactose Compared to Sucrose and Trehalose: Sildenafil Citrate Liposomes as a Case Study

et al. 2021

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The lyoprotective effects of mannitol and lactose have been evaluated in the production of sildenafil citrate liposomes. Liposomes were prepared by mixing the components under ultrasonic agitation, followed by a transmembrane pH gradient for remote drug loading. Mannitol and lactose, as compared to sucrose and trehalose, were used as the stabilizing agents, and different freeze-drying cycles were assayed. The remaining moisture and the thermal characteristics of the lyophilized samples were analyzed. Size, entrapment efficiency, biocompatibility, and cell internalization of original and rehydrated liposomes were compared. The type of additive did not affect the biocompatibility or cell internalization, but did influence other liposome attributes, including the thermal characteristics and the remaining moisture of the lyophilized samples. A cut-off of 5% (w/w) remaining moisture was an indicator of primary drying completion—information useful for scaling up and transfer from laboratory to large-scale production. Lactose increased the glass transition temperature to over 70 °C, producing lyoprotective effects similar to those obtained with sucrose. Based on these results, formulations containing liposomes lyophilized with lactose meet the FDA’s requirements and can be used as a biocompatible and biodegradable vehicle for the pulmonary delivery of therapeutic doses of sildenafil citrate.

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Section: Introductionmentioning

confidence: 99%

Lyoprotective Effects of Mannitol and Lactose Compared to Sucrose and Trehalose: Sildenafil Citrate Liposomes as a Case Study

et al. 2021

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“…Results of the study (LD 50 values) showed that sildenafil-loaded SLN could be used for PAH treatment via inhalation route. In a subsequent study [132], sildenafil-loaded SLNs were characterized for physiochemical properties for possible applications in PAH treatment following pulmonary administration. Analysis of nebulization performance was characterized using next generation impactor (NGI) whereas TEM was used to observe the morphology of nebulized particles.…”

Section: (Iv) Solid Lipid Nanoparticles (Slns)mentioning

confidence: 99%

Novel therapeutic approaches for pulmonary arterial hypertension: Unique molecular targets to site-specific drug delivery

Vaidya

Gupta

2015

Journal of Controlled Release

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“…19,20 Then, it was cooled down to room temperature to obtain the urbiprofen-loaded SLNs dispersion. 19,20 Then, it was cooled down to room temperature to obtain the urbiprofen-loaded SLNs dispersion.…”

Section: Preparation Of Urbiprofen-loaded Drtnmentioning

confidence: 99%

Development of a novel solid lipid nanoparticles-loaded dual-reverse thermosensitive nanomicelle for intramuscular administration with sustained release and reduced toxicity

et al. 2015

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To develop a novel solid lipid nanoparticles (SLNs)-loaded dual-reverse thermosensitive nanomicelle (DRTN) for intramuscular administration of flurbiprofen with sustained release and reduced toxicity, the DRTN was prepared with flurbiprofen-loaded SLNs, poloxamer 407 (P 407), poloxamer 188 (P 188) andwater. Its rheological characterization, release, stability, pharmacokinetics and morphology were evaluated after intramuscular administration to rats. These SLNs were solid at 25 C and transformed into liquid form at physiological temperature due to their melting point of about 32 C. Furthermore, the DRTN retained a liquid state at 25 C and gelled inside the body owing to its gelation temperature of about 34.7 C, leading to an opposite reversible property of the SLNs. When compared to the hydrogel, it significantly decreased the drug release and exhibited a reduced initial fast release. It sustained a high plasma concentration for 60 h, which was significantly higher when compared to the suspension, indicating enhanced bioavailability. However, it showed a lower plasma concentration, AUC, and C max values than that found for the hydrogel, suggesting the retarded release and decreased side effects of the drug. Unlike the hydrogel, it induced no injury to rat muscle as a result of no direct contact of the drug. It was stable for four months. Therefore, this novel DRTN system could be a strong candidate for the intramuscular administration of flurbiprofen.

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Physicochemical characterization of sildenafil-loaded solid lipid nanoparticle dispersions (SLN) for pulmonary application

Cited by 31 publications

References 26 publications

Lyoprotective Effects of Mannitol and Lactose Compared to Sucrose and Trehalose: Sildenafil Citrate Liposomes as a Case Study

Lyoprotective Effects of Mannitol and Lactose Compared to Sucrose and Trehalose: Sildenafil Citrate Liposomes as a Case Study

Novel therapeutic approaches for pulmonary arterial hypertension: Unique molecular targets to site-specific drug delivery

Development of a novel solid lipid nanoparticles-loaded dual-reverse thermosensitive nanomicelle for intramuscular administration with sustained release and reduced toxicity

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