Homogenization of Amorphous Solid Dispersions Prepared by Electrospinning in Low-Dose Tablet Formulation

Fülöp, Gergő; Balogh, Attila; Farkas, Balázs; Farkas, Attila; Szabó, Bence; Démuth, Balázs; Borbás, Enikő; Nagy, Zsombor Kristóf; Marosi, György

doi:10.3390/pharmaceutics10030114

Cited by 15 publications

(3 citation statements)

References 44 publications

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“…a) Crystal engineering: Through the utilization of Crystal engineering, scientists are researching techniques to wisely design and synthesize crystalline solids which contain a specific combination of ions and molecules. This method capitalizes on non-covalent interactions among ionic or molecular components allowing for solid structures with remarkable optical, magnetic and electrical properties 44,45 . b) Hydrates/solvates: Solvates are advanced molecules that form a crystal lattice with solvent molecules at their core.…”

Section: Modification Of the Crystal Habitmentioning

confidence: 99%

Contemporary Review on Solubility Enhancement Techniques

NARMADA¹

2023

J. Drug Delivery Ther.

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The limited water solubility of pharmacoactive molecules hinders their ability to be used as pharmacological agents, yet the indispensability of a certain solubility parameter precludes any compromises. To overcome this challenge, various methods are employed in order to increase their bioavailability. Pharmaceutical molecules with lower solubility present an elevated risk of failure for drug development and innovation. Their solubility affects important processes such as pharmacokinetics, pharmacodynamics, distribution, protein binding, and absorption. As a result these parameters are greatly impacted by the dissolution rate of a particular molecule. Out of all pharmaceutical dosage forms, more than half are oral. For the drug molecule to reach its target site and be effective therapeutically, solubility and bioavailability must be taken into consideration. Unfortunately, during screening programs conducted by the pharmaceutical industry it became evident that nearly 40% of new chemical entities (NCEs) face various roadblocks when transitioning from formulation to development due to their poor solubility and bioavailability. The pharmaceutical industry is constantly confronted with the difficulty of improving drug bioavailability and solubility in formulations. This article covers a range of technological advancements to boost the solubility of insoluble drugs, such as complexation, emulsions and micelles production, microemulsion generation with cosolvents, polymeric micelle preparation methods, particle size decrease techniques, pharmaceutical salts application, prodrugs usage, solid-state alteration practices, soft gel technology implementation crystal engineering approaches and nanomorphology. Through this review, we will discuss a variety of more complex methods for improving solubility and bioavailability such as crystal engineering, micronization, solid dispersions, nano sizing, and use of cyclodextrins, solid lipid nanoparticles (SLNPs), colloidal drug delivery systems and drug conjugates. We'll also provide references to studies that have been conducted in connection with these topics. Keywords: Solubility, permeability, bioavailability, nano particles drug delivery systems, microemulsions, low water solubility

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Section: Modification Of the Crystal Habitmentioning

confidence: 99%

Contemporary Review on Solubility Enhancement Techniques

NARMADA¹

2023

J. Drug Delivery Ther.

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“…Two recent studies have focussed on the mixing step in the conversion of electrospun drug-loaded fibre mats into tablets. Fülöp et al [ 23 ] showed that it is possible to prepare low-dose tablets with acceptable content uniformity from electrospun drug-loaded fibre mats after high-shear dry mixing with conventional tabletting excipients on a reasonable development lab scale (500 g) and compression on a rotary tablet press. Szabó et al [ 24 ] successfully applied continuous manufacturing processing techniques (mixing, compression) with inline analysis to prepare tablets from electrospun drug-loaded microfibre mats; in this case, the milled fibres were treated as a starting material.…”

Section: Introductionmentioning

confidence: 99%

Development of Robust Tablet Formulations with Enhanced Drug Dissolution Profiles from Centrifugally-Spun Micro-Fibrous Solid Dispersions of Itraconazole, a BCS Class II Drug

et al. 2023

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Fibre-based oral drug delivery systems are an attractive approach to addressing low drug solubility, although clear strategies for incorporating such systems into viable dosage forms have not yet been demonstrated. The present study extends our previous work on drug-loaded sucrose microfibres produced by centrifugal melt spinning to examine systems with high drug loading and investigates their incorporation into realistic tablet formulations. Itraconazole, a model BCS Class II hydrophobic drug, was incorporated into sucrose microfibres at 10, 20, 30, and 50% w/w. Microfibres were exposed to high relative humidity conditions (25 °C/75% RH) for 30 days to deliberately induce sucrose recrystallisation and collapse of the fibrous structure into powdery particles. The collapsed particles were successfully processed into pharmaceutically acceptable tablets using a dry mixing and direct compression approach. The dissolution advantage of the fresh microfibres was maintained and even enhanced after humidity treatment for drug loadings up to 30% w/w and, importantly, retained after compression into tablets. Variations in excipient content and compression force allowed manipulation of the disintegration rate and drug content of the tablets. This then permitted control of the rate of supersaturation generation, allowing the optimisation of the formulation in terms of its dissolution profile. In conclusion, the microfibre-tablet approach has been shown to be a viable method for formulating poorly soluble BCS Class II drugs with improved dissolution performance.

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“…Electrospinning is based on the application of a high electric field to a polymeric solution to generate ultrathin fibrous structures. The rapid evaporation rate of the solvent during the process leads to rapid entrapment of the drug within the polymeric matrix, leaving little possibility for the API to reorganize itself and crystalize [ 16 , 17 ]. Furthermore, the resultant fibrous materials have a high specific area, tunable pore size and controlled mechanical properties, making them attractive in drug delivery applications [ 18 ].…”

Section: Introductionmentioning

confidence: 99%

Development of Multilayer Ciprofloxacin Hydrochloride Electrospun Patches for Buccal Drug Delivery

Teno¹,

Pardo-Figuerez

Figueroa-López

et al. 2022

JFB

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Bacterial infections in the oral cavity can become a serious problem causing pain, sores and swelling for several weeks. This type of infection could be alleviated using mucoadhesive delivery systems, allowing local administration of the antibiotic to inhibit bacterial spreading. This work reports the development of a multilayer antibiotic patch containing ciprofloxacin hydrochloride (CPX)-loaded electrospun fibers for the treatment of such infections. For this, the release kinetics of the CPX-loaded fibers was modulated using different ratios of polyester blends. The selected reservoir layer was analyzed by scanning electron microscopy (SEM), Fourier transform infrared spectroscopy (FTIR), wide angle X-ray scattering (WAXS) and differential scanning calorimetry (DSC). These analyses confirmed the presence and good distribution of the drug in the fibers and that the drug is in an amorphous state within the reservoir layer. To enhance mucoadhesion whilst ensuring drug directionality, the reservoir layer was assembled to a backing and an adhesive layer. This multilayer patch was assessed in terms of in vitro drug release, adhesion and antimicrobial properties. The multilayer strategy showed excellent antimicrobial properties over time and also a strong adhesion patch time in the volunteers for an average of 7 h. These results highlight the capabilities of multilayer electrospun patches as platforms to treat oral infections.

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Homogenization of Amorphous Solid Dispersions Prepared by Electrospinning in Low-Dose Tablet Formulation

Cited by 15 publications

References 44 publications

Contemporary Review on Solubility Enhancement Techniques

Contemporary Review on Solubility Enhancement Techniques

Development of Robust Tablet Formulations with Enhanced Drug Dissolution Profiles from Centrifugally-Spun Micro-Fibrous Solid Dispersions of Itraconazole, a BCS Class II Drug

Development of Multilayer Ciprofloxacin Hydrochloride Electrospun Patches for Buccal Drug Delivery

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