Enhanced NSAIDs Solubility in Drug–Drug Formulations with Ciprofloxacin

Acebedo-Martínez, Francisco Javier; Domínguez‐Martín, Alicia; Alarcón-Payer, Carolina; Sevillano-Páez, Alejandro; Verdugo‐Escamilla, Cristóbal; González‐Pérez, Josefa María; Barrero, Fernando; Choquesillo-Lazarte, Duane

doi:10.3390/ijms24043305

Cited by 2 publications

(20 citation statements)

References 67 publications

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“…The solid-state arrangement may improve a wide range of APIs' physicochemical properties, including their solubility, stability, flowability, and permeability. Many also enhance activities and performances, as recently reported [30,[51][52][53][54][55]. However, the first benefit is solubility enhancement, which is stated to be the most crucial characteristic of the particles.…”

Section: Antibiotic Multi-component Structure Developmentmentioning

confidence: 99%

“…For example, pymetrozine multi-component systems showed a four-fold improvement in these parameters [54], and nicorandil multicomponent crystals showed a 1.9-5.2-fold improvement [55]. Meanwhile, the solubility of NSAIDs after salt formation with fluoroquinolones reaches values tens to hundreds of times higher than their parent compound [30].…”

Section: Antibiotic Multi-component Structure Developmentmentioning

confidence: 99%

“…This structural derivation has been applied for a long time, significantly increasing drug solubility and stability, physically and chemically. In addition, the changes observed in antibiotics' physicochemical properties after salt formation can improve in terms of antibacterial potency, as shown by levofloxacin in combination with antioxidants, citric acid [6], and dihydroxybenzoic acids [7], as well as by ciprofloxacin in combination with NSAIDs [30,31].…”

Section: Salt/ionic Multi-component Structurementioning

confidence: 99%

“…However, even though the crystal structure data are easier to interpret, the spatial properties of a single crystal may not represent the bulk solid, or appropriately describe the bulk properties of interest for a given application [72]. In this case, the structure's image is commonly supported by software, such as SHELXL, SHELXT, and Mercury, in order to match the structure based on diffraction data, as measured by the goniometer [30,69,70].…”

Section: X-ray Diffractometrymentioning

confidence: 99%

“…On the other side, NSAIDs are insoluble, and some are unstable, such as indomethacin and diclofenac acid [8]. Hence, in another section, we describe combinations with NSAIDs, since they are commonly used to treat infected patients [30][31][32], completing the paper with considerations regarding the activity and toxicity caused by drug-drug interactions [31][32][33].…”

Section: Introductionmentioning

confidence: 99%

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The Benefits and Challenges of Antibiotics–Non-Steroidal Anti-Inflammatory Drugs Non-Covalent Reaction

2023

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Recently, non-covalent reactions have emerged as approaches to improve the physicochemical properties of active pharmaceutical ingredients (API), including antibiotics and non-steroidal anti-inflammatory drugs (NSAIDs). This review aimed to present and discuss the non-covalent reaction products of antibiotics, including salt and neutral multi-component solid forms, by framing their substituents and molar ratios, manufacturing techniques, characterization methods, benefits, potency changes, and toxicity, and is completed with an analysis of the development of computational models used in this field. Based on the data, NSAIDs are the most-developed drugs in multi-component system preparations, followed by antibiotics, i.e., antituberculosis and fluoroquinolones. They have reacted with inorganic elements, excipients, nutraceuticals, natural products, and other drugs. However, in terms of treatments for common infections, fluoroquinolones are more frequently used. Generally, NSAIDs are acquired on an over-the-counter basis, causing inappropriate medication. In addition, the pKa differences between the two groups of medicine offer the potential for them to react non-covalently. Hence, this review highlights fluoroquinolone–NSAID multi-component solid systems, which offer some benefits. These systems can increase patient compliance and promote the appropriate monitoring of drug usage; the dual drug multi-component solids have been proven to improve the physicochemical properties of one or both components, especially in terms of solubility and stability. In addition, some reports show an enhancement of the antibiotic activity of the products. However, it is important to consider the possibility of activity changes, interaction, and toxicity when using drug combinations. Hence, these aspects also are discussed in this review. Finally, we present computational modeling, which has been utilized broadly to support multi-component system designs, including coformer screening, preparation methods, and structural modeling, as well as to predict physicochemical properties, potency, and toxicity. This integrated review is expected to be useful for further antibiotic–NSAID multi-component system development.

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Section: Antibiotic Multi-component Structure Developmentmentioning

confidence: 99%

Section: Antibiotic Multi-component Structure Developmentmentioning

confidence: 99%

Section: Salt/ionic Multi-component Structurementioning

confidence: 99%

Section: X-ray Diffractometrymentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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The Benefits and Challenges of Antibiotics–Non-Steroidal Anti-Inflammatory Drugs Non-Covalent Reaction

2023

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Study on Sulfamethoxazole–Piperazine Salt: A Mechanistic Insight into Simultaneous Improvement of Physicochemical Properties

Roy,

Chakraborty,

Pandey

et al. 2023

Mol. Pharmaceutics

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Multidrug salts represent more than one drug in a crystal lattice and thus could be used to deliver multiple drugs in a single dose. It showcases unique physicochemical properties in comparison to individual components, which could lead to improved efficacy and therapeutic synergism. This study presents the preparation and scale-up of sulfamethoxazole−piperazine salt, which has been thoroughly characterized by X-ray diffraction and thermal and spectroscopic analyses. A detailed mechanistic study investigates the impact of piperazine on the microenvironmental pH of the salt and its effect on the speciation profile, solubility, dissolution, and diffusion profile. Also, the improvement in the physicochemical properties of sulfamethoxazole due to the formation of salt was explored with lattice energy contributions. A greater ionization of sulfamethoxazole (due to pH changes contributed by piperazine) and lesser lattice energy of sulfamethoxazole−piperazine contributed to improved solubility, dissolution, and permeability. Moreover, the prepared salt addresses the stability issues of piperazine and exhibits good stability behavior under accelerated stability conditions. Due to the improvement of physicochemical properties, the sulfamethoxazole−piperazine salt demonstrates better pharmacokinetic parameters in comparison to sulfamethoxazole and provides a strong suggestion for the reduction of dose. The following study suggests that multidrug salts can concurrently enhance the physicochemical properties of drugs and present themselves as improved fixed-dose combinations.

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Enhanced NSAIDs Solubility in Drug–Drug Formulations with Ciprofloxacin

Cited by 2 publications

References 67 publications

The Benefits and Challenges of Antibiotics–Non-Steroidal Anti-Inflammatory Drugs Non-Covalent Reaction

The Benefits and Challenges of Antibiotics–Non-Steroidal Anti-Inflammatory Drugs Non-Covalent Reaction

Study on Sulfamethoxazole–Piperazine Salt: A Mechanistic Insight into Simultaneous Improvement of Physicochemical Properties

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