Edge activators and a polycationic polymer enhance the formulation of porous voriconazole nanoagglomerate for the use as a dry powder inhaler

Salem, Heba F.; Kharshoum, Rasha M; Hakim, Lekaa F Abdel; Abdelrahim, Mohamed

doi:10.3109/08982104.2016.1140182

Cited by 14 publications

(8 citation statements)

References 27 publications

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“…The optimized TBN-NVS formulation exhibited a highly negative ζ potential (−31.17 ± 2.58 mV) indicating quality of dispersion. The negative charge on the surface of NVS might be owed to the presence of stearic acid that increased NVS stability in the aqueous phase (Salem et al., 2016 ).…”

Section: Resultsmentioning

confidence: 99%

“…The total emitted dosage described as the entire amount of medication ejected from the mouthpiece and expressed based on the nominal emitted dosage that represents the initial amount of medication introduced in the device (Salem et al., 2016 ). The medication delivery mechanism was constructed in such manner analogous to that of a rat receiving the TBN-NVS suspension via endotracheal tube.…”

Section: Characterization Of Tbn-nvsmentioning

confidence: 99%

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Innovative pulmonary targeting of terbutaline sulfate-laded novasomes for non-invasive tackling of asthma: statistical optimization and comparative in vitro/in vivo evaluation

et al. 2022

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Asthma represents a globally serious non-communicable ailment with significant public health outcomes for both pediatrics and adults triggering vast morbidity and fatality in critical cases. The β 2 -adrenoceptor agonist, terbutaline sulfate (TBN), is harnessed as a bronchodilator for monitoring asthma noising symptoms. Nevertheless, the hepatic first-pass metabolism correlated with TBN oral administration mitigates its clinical performance. Likewise, the regimens of inhaled TBN dosage forms restrict its exploitation. Consequently, this work is concerned with the assimilation of TBN into a novel non-phospholipid nanovesicular paradigm termed novasomes (NVS) for direct and effective TBN pulmonary targeting. TBN-NVS were tailored based on the thin film hydration method and Box-Behnken design was applied to statistically optimize the formulation variables. Also, the aerodynamic pattern of the optimal TBN-NVS was explored via cascade impaction. Moreover, comparative pharmacokinetic studies were conducted using a rat model. TBN elicited encapsulation efficiency as high as 70%. The optimized TBN-NVS formulation disclosed an average nano-size of 223.89 nm, ζ potential of −31.17 mV and a sustained drug release up to 24 h. Additionally, it manifested snowballed in vitro lung deposition behavior in cascade impactor with a fine particle fraction of 86.44%. In vivo histopathological studies verified safety of intratracheally-administered TBN-NVS. The pharmacokinetic studies divulged 3.88-fold accentuation in TBN bioavailability from the optimum TBN-NVS versus the oral TBN solution. Concisely, the results proposed that NVS are an auspicious nanovector for TBN pulmonary delivery with integral curbing of the disease owing to target specificity.

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Section: Resultsmentioning

confidence: 99%

Section: Characterization Of Tbn-nvsmentioning

confidence: 99%

Innovative pulmonary targeting of terbutaline sulfate-laded novasomes for non-invasive tackling of asthma: statistical optimization and comparative in vitro/in vivo evaluation

et al. 2022

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“…69 This smaller MMAD of improved SD/ P4 compared to improved SD/P6 (3.18 ± 0.29 µm) might guarantee deposition in the alveolar region. 70 It could be concluded that the use of curcumin-loaded proliposomes aerosol 71,72 might result in better lung deposition over the use of the pure powder suggestive for a future clinical bioequivalence test to consolidate this finding.…”

Section: Aerodynamic Particle Size Characterizationmentioning

confidence: 99%

Design and Characterization of Spray-Dried Proliposomes for the Pulmonary Delivery of Curcumin

Adel

ElMeligy

Abdelrahim

et al. 2021

IJN

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Purpose The goal was to directly deliver curcumin, a natural polyphenolic anticancer and anti-inflammatory compound, to the lung tissues with minimal systemic exposure through the fabrication of proliposomes, overcoming its poor aqueous solubility and oral bioavailability. Methods Nano-spray drying was employed to prepare proliposomes using hydroxypropyl beta-cyclodextrin as a carrier. Lecithin and cholesterol were used as lipids, stearylamine and Poloxamer 188 were added as positive charge inducer and a surfactant, respectively. Different characterization parameters were evaluated like percentage yield, entrapment efficiency, drug loading, aerodynamic particle size, in vitro release besides morphological examination. Cytotoxicity studies on cell line A549 lung tumor cells as well as in vivo lung pharmacokinetic studies were also carried. Results The optimized formulations showed superior aerosolization properties coupled their enhanced ability to reach deep lung tissues with a high % of fine particle fraction. Cytotoxicity studies using MTT assay demonstrated enhanced growth inhibitory effect on lung tumor cells A549 and significant reduction of proinflammatory cytokines such as tumor necrosis factor-α, interleukin-6 and interleukin-10 compared to the pure drug. Results of lung pharmacokinetic tests confirmed the superiority of proliposomal curcumin over curcumin powder in both, the rate and extent of lung tissue absorption, as well as the mean residence time within the lung tissues. Conclusion The pulmonary delivery of curcumin-loaded proliposomes as dry powder provides a direct approach to lung tissues targeting while avoiding the limitations of the oral route and offering a non-invasive alternative to the parenteral one.

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“…In addition to the possibility of sustained-release, which facilitates patient adherence to fungal infection treatments, one of the goals of using nanotechnology is also related to improving the solubility of voriconazole in aqueous media, or allowing new routes of administration [212,213]. In order to provide new routes of administration for voriconazole besides the oral one, nanotechnology has been explored for ocular [54,214,215,216], pulmonary [53,217,218,219], and nail [220] distribution routes.…”

Section: Voriconazolementioning

confidence: 99%

“…Nanostructured systems have been used to increase flucytosine permeability in different tissues. Salem et al [217] incorporated flucytosine into gold nanoparticles to increase intraocular penetration and to evaluate the therapeutic efficacy of this topically applied formulation. In addition to intraocular permeation, Salem et al [240] used glutathione to increase flucytosine permeation through the blood-brain barrier, achieving a system with an average size of 100 nm and 70% drug release.…”

Section: Flucytosinementioning

confidence: 99%

Nanoparticles as a Tool for Broadening Antifungal Activities

Renzi

Campos

Miranda

et al. 2021

CMC

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: The Fungal infections are diseases that are considered neglected although their infection rates have increased worldwide in the last decades. Thus, since the antifungal arsenal is restricted and many strains have shown resistance new therapeutic alternatives are necessary. Nanoparticles are considered important alternatives to promote drug delivery. In this sense, the objective of the present study was to evaluate the contributions of newly developed nanoparticles to the treatment of fungal infections. Studies have shown that nanoparticles generally improve the biopharmaceutical and pharmacokinetic characteristics of antifungals, which is reflected in a greater pharmacodynamic potential and lower toxicity, as well as the possibility of prolonged action. It also offers the proposition of new routes of administration. Nanotechnology is known to contribute to a new drug delivery system, not only for the control of infectious diseases, but for various other diseases as well. In recent years, several studies have emphasized its application in infectious diseases, presenting better alternatives for the treatment of fungal infections.

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Edge activators and a polycationic polymer enhance the formulation of porous voriconazole nanoagglomerate for the use as a dry powder inhaler

Cited by 14 publications

References 27 publications

Innovative pulmonary targeting of terbutaline sulfate-laded novasomes for non-invasive tackling of asthma: statistical optimization and comparative in vitro/in vivo evaluation

Innovative pulmonary targeting of terbutaline sulfate-laded novasomes for non-invasive tackling of asthma: statistical optimization and comparative in vitro/in vivo evaluation

Design and Characterization of Spray-Dried Proliposomes for the Pulmonary Delivery of Curcumin

Nanoparticles as a Tool for Broadening Antifungal Activities

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