Influence of the formulation components on the properties of the system SLN-dextran hydrogel for the modified release of drugs

Paolicelli, Patrizia; Cerreto, F.; Cesa, Stefania; Feeney, Michelle; Corrente, Federica; Marianecci, Carlotta; Casadei, Maria Antonietta

doi:10.1080/02652040802372899

Cited by 19 publications

(12 citation statements)

References 19 publications

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“…It is well known and also shown by DSC measurements that the melting point of colloidal structures is lower than that of the bulk due to the influence of surface energy [44]. A difference in release profiles caused by a difference in lipid melting points was also suggested by Paolicelli et al [49]. The release of QSI was more prolonged in SLF showing < 20 % burst in all SLNs, Fig.…”

Section: In Vitro Release Of Qsisupporting

confidence: 60%

Antibiotic-free nanotherapeutics: Ultra-small, mucus-penetrating solid lipid nanoparticles enhance the pulmonary delivery and anti-virulence efficacy of novel quorum sensing inhibitors

Nafee

Husari

Maurer

et al. 2014

Journal of Controlled Release

175

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Cystic fibrosis (CF) is a genetic disease mainly manifested in the respiratory tract. Pseudomonas aeruginosa (P. aeruginosa) is the most common pathogen identified in cultures of the CF airways, however, its eradication with antibiotics remains challenging as it grows in biofilms that counterwork human immune response and dramatically decrease susceptibility to antibiotics. P. aeruginosa regulates pathogenicity via a cell-to-cell communication system known as quorum sensing (QS) involving the virulence factor (pyocyanin), thus representing an attractive target for coping with bacterial pathogenicity. The first in vivo potent QS inhibitor (QSI) was recently developed. Nevertheless, its lipophilic nature might hamper its penetration of non-cellular barriers such as mucus and bacterial biofilms, which limits its biomedical application. Successful anti-infective inhalation therapy necessitates proper design of a biodegradable nanocarrier allowing: 1) high loading and prolonged release, 2) mucus penetration, 3) effective pulmonary delivery, and 4) maintenance of the anti-virulence activity of the QSI. In this context, various pharmaceutical lipids were used to prepare ultra-small solid lipid nanoparticles (us-SLNs) by hot melt homogenization. Plain and QSI-loaded SLNs were characterized in terms of colloidal properties, drug loading, in vitro release and acute toxicity on Calu-3 cells. Mucus penetration was studied using a newly-developed confocal microscopy technique based on 3D-time-lapse imaging. For pulmonary application, nebulization efficiency of SLNs and lung deposition using next generation impactor (NGI) were performed. The anti-virulence efficacy was investigated by pyocyanin formation in P. aeruginosa cultures. Ultra-small SLNs (<100nm diameter) provided high encapsulation efficiency (68-95%) according to SLN composition, high burst in phosphate buffer saline compared to prolonged release of the payload over >8h in simulated lung fluid with minor burst. All types and concentrations of plain and QSI-loaded SLNs maintained the viability of Calu-3 cells. 3D time-lapse confocal imaging proved the ability of SLNs to penetrate into artificial sputum model. SLNs were efficiently nebulized; NGI experiments revealed their deposition in the bronchial region. Overall, nanoencapsulated QSI showed up to sevenfold superior anti-virulence activity to the free compound. Most interestingly, the plain SLNs exhibited anti-virulence properties themselves, which was shown to be related to anti-virulence effects of the emulsifiers used. These startling findings represent a new perspective of ultimate significance in the area of nano-based delivery of novel anti-infectives.

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Section: In Vitro Release Of Qsisupporting

confidence: 60%

Antibiotic-free nanotherapeutics: Ultra-small, mucus-penetrating solid lipid nanoparticles enhance the pulmonary delivery and anti-virulence efficacy of novel quorum sensing inhibitors

Nafee

Husari

Maurer

et al. 2014

Journal of Controlled Release

175

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“…It is well known that the melting point of colloidal structures may be lower than that of the bulk due to the influence of surface energy (Mader, 2006). A difference in release profiles caused by a difference in lipid melting points was also suggested by Paolicelli et al (2008) in a study with ibuprofen and acylglycerols differing in melting points. The higher amount released from trimyristate particles may also reflect the smaller size of these particles.…”

Section: Release Profiles Of Betamethasone-17-valerate Loaded Sln Depmentioning

confidence: 91%

Corticosteroid solubility and lipid polarity control release from solid lipid nanoparticles

Jensen

Magnussson

Gunnarsson

et al. 2010

International Journal of Pharmaceutics

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“…Moreover, the decreased drug mobility at the experimental release temperature is a result of a higher melting point of Compritol. Paolicelli et al (34) reported a variation in the release profiles of ibuprofen and acylglycerols with different melting points and suggested that the reason for this variation was the difference in lipid melting points.…”

Section: In Vitro Release Study Of Slnsmentioning

confidence: 99%

Development, Optimization, and Evaluation of Carvedilol-Loaded Solid Lipid Nanoparticles for Intranasal Drug Delivery

et al. 2016

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Abstract. Carvedilol, a beta-adrenergic blocker, suffers from poor systemic availability (25%) due to firstpass metabolism. The aim of this work was to improve carvedilol bioavailability through developing carvedilol-loaded solid lipid nanoparticles (SLNs) for nasal administration. SLNs were prepared by emulsion/solvent evaporation method. A 2 3 factorial design was employed with lipid type (Compritol or Precirol), surfactant (1 or 2% w/v poloxamer 188), and co-surfactant (0.25 or 0.5% w/v lecithin) concentrations as independent variables, while entrapment efficiency (EE%), particle size, and amount of carvedilol permeated/unit area in 24 h (Q 24 ) were the dependent variables. Regression analysis was performed to identify the optimum formulation conditions. The in vivo behavior was evaluated in rabbits comparing the bioavailability of carvedilol after intravenous, nasal, and oral administration. The results revealed high drug EE% ranging from 68 to 87.62%. Carvedilol-loaded SLNs showed a spherical shape with an enriched core drug loading pattern having a particle size in the range of 66 to 352 nm. The developed SLNs exhibited significant high amounts of carvedilol permeated through the nasal mucosa as confirmed by confocal laser scanning microscopy. The in vivo pharmacokinetic study revealed that the absolute bioavailability of the optimized intranasal SLNs (50.63%) was significantly higher than oral carvedilol formulation (24.11%). Hence, we conclude that our developed SLNs represent a promising carrier for the nasal delivery of carvedilol.

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Influence of the formulation components on the properties of the system SLN-dextran hydrogel for the modified release of drugs

Cited by 19 publications

References 19 publications

Antibiotic-free nanotherapeutics: Ultra-small, mucus-penetrating solid lipid nanoparticles enhance the pulmonary delivery and anti-virulence efficacy of novel quorum sensing inhibitors

Antibiotic-free nanotherapeutics: Ultra-small, mucus-penetrating solid lipid nanoparticles enhance the pulmonary delivery and anti-virulence efficacy of novel quorum sensing inhibitors

Corticosteroid solubility and lipid polarity control release from solid lipid nanoparticles

Development, Optimization, and Evaluation of Carvedilol-Loaded Solid Lipid Nanoparticles for Intranasal Drug Delivery

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