An Evolving Role of Aqueous Piperazine to Improve the Solubility of Non-Steroidal Anti-Inflammatory Drugs

Fang, Zhengyu; Zhang, Baoxi; Xing, Wenhui; Yu, Hongmei; Cheng, Xing; Gong, Ningbo; Lü, Yang; Du, Guanhua

doi:10.1016/j.xphs.2022.05.009

Cited by 4 publications

(5 citation statements)

References 33 publications

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“…SMX tends to transform into a protonated species (H 2 N → H 3 N + ) at lower pH, and at higher pH, it transforms into a deprotonated species (HN → N – ) . Notably, the ionization of SMX also gets influenced by PIP, which influences the solubility behavior of SMX …”

Section: Resultsmentioning

confidence: 99%

“… The complete phase transition observed for samples could be related to the metastable salt, which translates back to the stable crystalline form of SMX–H 2 O upon complete solubilization of the PIP (Figure ). The hypothesis behind the increase in the equilibrium solubility of the salt is the basic nature of PIP, which influences the ionization of SMX, which is correlated with the microenvironmental pH and effect on speciation …”

Section: Resultsmentioning

confidence: 99%

“…46 Notably, the ionization of SMX also gets influenced by PIP, which influences the solubility behavior of SMX. 47 It was observed that the SMX−PIP exhibits significantly higher solubilities in neutral and basic pH media than in acidic media (Figure 8). 46 The complete phase transition observed for samples could be related to the metastable salt, which translates back to the stable crystalline form of SMX−H 2 O upon complete solubilization of the PIP (Figure 9).…”

Section: Determination Of Plasma Concentration Of Smx Using Lc/ms/msmentioning

confidence: 95%

“…48 The hypothesis behind the increase in the equilibrium solubility of the salt is the basic nature of PIP, which influences the ionization of SMX, which is correlated with the microenvironmental pH and effect on speciation. 47 3.6. Intrinsic Dissolution Rate.…”

Section: Determination Of Plasma Concentration Of Smx Using Lc/ms/msmentioning

confidence: 99%

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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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Section: Resultsmentioning

confidence: 99%

Section: Resultsmentioning

confidence: 99%

Section: Determination Of Plasma Concentration Of Smx Using Lc/ms/msmentioning

confidence: 95%

Section: Determination Of Plasma Concentration Of Smx Using Lc/ms/msmentioning

confidence: 99%

See 2 more Smart Citations

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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show abstract

“…Although DMNs exhibit several advantages, some unmet needs for precision medicine remain. Specifically, most of the materials used in DMNs show strong hydrophilicity, such as hyaluronic acid (HA) [ 18 ], polyvinyl alcohol (PVA) [ 38 ], and povidone K30 (PVP K30) [ 39 ], while about 75% of marketed products and 90% of drugs in development pipelines are hydrophobic [ 40 ]. Therefore, hydrophobic drugs display low solubility in hydrophilic microneedle materials [ 41 ], which is attributed to a poor drug loading capacity.…”

Section: Nanoparticle-loaded Dmns: a Better Choice For Precision Medi...mentioning

confidence: 99%

The Necessity to Investigate In Vivo Fate of Nanoparticle-Loaded Dissolving Microneedles

Chang,

Wu,

et al. 2024

Pharmaceutics

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Transdermal drug delivery systems are rapidly gaining prominence and have found widespread application in the treatment of numerous diseases. However, they encounter the challenge of a low transdermal absorption rate. Microneedles can overcome the stratum corneum barrier to enhance the transdermal absorption rate. Among various types of microneedles, nanoparticle-loaded dissolving microneedles (DMNs) present a unique combination of advantages, leveraging the strengths of DMNs (high payload, good mechanical properties, and easy fabrication) and nanocarriers (satisfactory solubilization capacity and a controlled release profile). Consequently, they hold considerable clinical application potential in the precision medicine era. Despite this promise, no nanoparticle-loaded DMN products have been approved thus far. The lack of understanding regarding their in vivo fate represents a critical bottleneck impeding the clinical translation of relevant products. This review aims to elucidate the current research status of the in vivo fate of nanoparticle-loaded DMNs and elaborate the necessity to investigate the in vivo fate of nanoparticle-loaded DMNs from diverse aspects. Furthermore, it offers insights into potential entry points for research into the in vivo fate of nanoparticle-loaded DMNs, aiming to foster further advancements in this field.

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Novel aloe emodin–hydroxyethyl piperazine hybrid dihydrochloride induces oral cancer CAL-27 cells apoptosis through ROS production, DNA damage and mitochondrial pathways

Long,

Yang,

Chen

et al. 2023

Med Chem Res

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An Evolving Role of Aqueous Piperazine to Improve the Solubility of Non-Steroidal Anti-Inflammatory Drugs

Cited by 4 publications

References 33 publications

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

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

The Necessity to Investigate In Vivo Fate of Nanoparticle-Loaded Dissolving Microneedles

Novel aloe emodin–hydroxyethyl piperazine hybrid dihydrochloride induces oral cancer CAL-27 cells apoptosis through ROS production, DNA damage and mitochondrial pathways

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