Designing highly porous amorphous celecoxib particles by spray freeze drying leads to accelerated drug absorption in-vivo

Lucas, Dominic; Kožák, Jan; Rautenberg, Annika; Chrétien, Chloé; Pellequer, Yann; Lamprecht, Alf

doi:10.1016/j.ejpb.2022.03.007

Cited by 6 publications

(1 citation statement)

References 23 publications

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“…SFD has been used to prepare particles of poorly water-soluble therapeutic ingredients, such as ciclosporin, in combination with dissolution-enhanced carriers like mannitol [ 114 ]. SFD has also been employed to produce nanoparticle aggregates (or nano-aggregates) for inhaled delivery, with the choice of excipients and the nanoparticle-to-excipient ratio affecting the characteristics of the nano-aggregates [ 115 ]. SFD has been recognized as a technology that can achieve continuous pharmaceutical manufacturing and has been applied in the development of lyophilization as a downstream operation [ 110 ].…”

Section: Approaches For Particle Engineeringmentioning

confidence: 99%

Engineering Inhalable Therapeutic Particles: Conventional and Emerging Approaches

Negi,

Nimbkar,

Moses

2023

Pharmaceutics

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Respirable particles are integral to effective inhalable therapeutic ingredient delivery, demanding precise engineering for optimal lung deposition and therapeutic efficacy. This review describes different physicochemical properties and their role in determining the aerodynamic performance and therapeutic efficacy of dry powder formulations. Furthermore, advances in top-down and bottom-up techniques in particle preparation, highlighting their roles in tailoring particle properties and optimizing therapeutic outcomes, are also presented. Practices adopted for particle engineering during the past 100 years indicate a significant transition in research and commercial interest in the strategies used, with several innovative concepts coming into play in the past decade. Accordingly, this article highlights futuristic particle engineering approaches such as electrospraying, inkjet printing, thin film freeze drying, and supercritical processes, including their prospects and associated challenges. With such technologies, it is possible to reshape inhaled therapeutic ingredient delivery, optimizing therapeutic benefits and improving the quality of life for patients with respiratory diseases and beyond.

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Section: Approaches For Particle Engineeringmentioning

confidence: 99%

Engineering Inhalable Therapeutic Particles: Conventional and Emerging Approaches

Negi,

Nimbkar,

Moses

2023

Pharmaceutics

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Synergistic Effect of Synthetic Magnesium Aluminometasilicate and Dual Polymer in Celecoxib Solubilization by Solid Dispersion Method

Sohn,

Choi

2024

J Pharm Innov

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Microfluidics-on-a-chip for designing celecoxib-based amorphous solid dispersions: when the process shapes the product

Figueiredo,

Mendes,

Pais

et al. 2024

Drug Deliv. and Transl. Res.

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The fundamental idea underlying the use of amorphous solid dispersions (ASDs) is to make the most of the solubility advantage of the amorphous form of a drug. However, the drug stability becomes compromised due to the higher free energy and disorder of molecular packing in the amorphous phase, leading to crystallization. Polymers are used as a matrix to form a stable homogeneous amorphous system to overcome the stability concern. The present work aims to design ASD-based formulations under the umbrella of quality by design principles for improving oral drug bioavailability, using celecoxib (CXB) as a model drug. ASDs were prepared from selected polymers and tested both individually and in combinations, using various manufacturing techniques: high-shear homogenization, high-pressure homogenization, microfluidics-on-a-chip, and spray drying. The resulting dispersions were further optimized, resorting to a 32 full-factorial design, considering the drug:polymers ratio and the total solid content as variables. The formulated products were evaluated regarding analytical centrifugation and the influence of the different polymers on the intrinsic dissolution rate of the CXB-ASDs. Microfluidics-on-a-chip led to the amorphous status of the formulation. The in vitro evaluation demonstrated a remarkable 26-fold enhancement in the intrinsic dissolution rate, and the translation of this formulation into tablets as the final dosage form is consistent with the observed performance enhancement. These findings are supported by ex vivo assays, which exhibited a two-fold increase in permeability compared to pure CXB. This study tackles the bioavailability hurdles encountered with diverse active compounds, offering insights into the development of more effective drug delivery platforms. Graphical Abstract

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Designing highly porous amorphous celecoxib particles by spray freeze drying leads to accelerated drug absorption in-vivo

Cited by 6 publications

References 23 publications

Engineering Inhalable Therapeutic Particles: Conventional and Emerging Approaches

Engineering Inhalable Therapeutic Particles: Conventional and Emerging Approaches

Synergistic Effect of Synthetic Magnesium Aluminometasilicate and Dual Polymer in Celecoxib Solubilization by Solid Dispersion Method

Microfluidics-on-a-chip for designing celecoxib-based amorphous solid dispersions: when the process shapes the product

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