A Novel Chitosan-coated Leciplex Loaded with Ambrisentan as a Possible Pulmonary Nanosystem: Optimization, Characterization, and Pharmacokinetics Assessments

Eid, Hussein M.; Turkia, Toqa H.; Ali, Adel A.; Aboud, Heba M.

doi:10.1016/j.xphs.2024.03.027

Journal of Pharmaceutical Sciences

2024

DOI: 10.1016/j.xphs.2024.03.027

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A Novel Chitosan-coated Leciplex Loaded with Ambrisentan as a Possible Pulmonary Nanosystem: Optimization, Characterization, and Pharmacokinetics Assessments

Hussein M. Eid,

Toqa H. Turkia,

Adel A. Ali

et al.

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2024

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Cited by 2 publications

References 48 publications

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Brain Targeting of Venlafaxine via Intranasal Transbilosomes Thermogel for Improved Management of Depressive Disorder

Alsaidan,

Elkomy,

Zaki

et al. 2024

Journal of Pharmaceutical Sciences

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Brain Targeting of Venlafaxine via Intranasal Transbilosomes Thermogel for Improved Management of Depressive Disorder

Alsaidan,

Elkomy,

Zaki

et al. 2024

Journal of Pharmaceutical Sciences

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Optimization and Appraisal of Nintedanib-Loaded Mixed Polymeric Micelles as a Potential Nanovector for Non-Invasive Pulmonary Fibrosis Mitigation

Aboud,

El Menshawe,

Mohammed

et al. 2024

Pharmaceuticals

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Background/Objectives: Nintedanib (NTD), a triple tyrosine kinase receptor inhibitor, is the recommended first-line tackling option for idiopathic pulmonary fibrosis (IPF). Nevertheless, the adequacy of NTD is curtailed by issues associated with its low solubility, first-pass effect, poor bioavailability, and liver toxicity. The objective of our work was to develop a non-invasive intratracheal (i.t.) nanoparadigm based on NTD-loaded polymeric mixed micelles (NTD-PMMs) that can effectively treat IPF by sustaining the release of NTD, and snowballing its bioavailability, solubility, and efficacy. Methods: Design-Expert® software was used to optimize various NTD-PMMs formulations via Box–Behnken design adopting the thin-film hydration technique. The optimum formulation was chosen and in vivo tested in a rat model to explore its comparative bioavailability and toxicity. Results: The formulation composition with 309.217 mg of Soluplus, 150 mg of Tween 80, and 40 mg of sodium deoxycholate was found to fulfill the requisites of an optimum NTD-PMMs formulation. The optimum NTD-PMMs formulation divulged 90.26% entrapment efficiency with a surface charge of −14.72 mV and a nanoscale diameter of 61.36 nm. Also, it substantially sustained the release of NTD by 66.84% after 24 h and manifested a pronounced stability. In vivo histopathology investigations verified the safety of NTD-PMMs delivered intratracheally. Moreover, pharmacokinetic analyses disclosed accentuated relative bioavailability of the optimized NTD-PMMs by 2.4- and 3.82-fold as compared with both the i.t. and oral crude NTD suspensions, respectively. Conclusions: Overall, the current results elicited the potential of PMMs to serve as a promising pulmonary nanovector for the targeted delivery of NTD.

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A Novel Chitosan-coated Leciplex Loaded with Ambrisentan as a Possible Pulmonary Nanosystem: Optimization, Characterization, and Pharmacokinetics Assessments

Cited by 2 publications

References 48 publications

Brain Targeting of Venlafaxine via Intranasal Transbilosomes Thermogel for Improved Management of Depressive Disorder

Brain Targeting of Venlafaxine via Intranasal Transbilosomes Thermogel for Improved Management of Depressive Disorder

Optimization and Appraisal of Nintedanib-Loaded Mixed Polymeric Micelles as a Potential Nanovector for Non-Invasive Pulmonary Fibrosis Mitigation

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