Pharmaceutical Co-crystal of Antiviral Agent Efavirenz with Nicotinamide for the Enhancement of Solubility, Physicochemical Stability, and Oral Bioavailability

Yadav, Dattatray; Savjani, Jignasa; Savjani, Ketan; Kumar, Aakash; Patel, Snehal

doi:10.1208/s12249-022-02467-7

Cited by 5 publications

(4 citation statements)

References 59 publications

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“… Amantadine Hydrochloride with Resveratrol Inhibit the M2 ion channel protein, disrupting the uncoating process and Prevents virus fusion with host cells Co-Crystal Enhance effectiveness [ 51 ] 15. Efavirenz Class: Reverse transcriptase inhibitor Mechanism of action: Prevents virus DNA synthesis Co-Crystal Enhance solubility, stability and bioavailability [ 52 ] 16. Ritonavir and efavirenz Protease inhibitor and reverse transcriptase inhibitor Solid dispersion Enhance solubility [ 13 ] 17.…”

Section: Methodsmentioning

confidence: 99%

Revolutionizing Antiviral Therapeutics: Unveiling Innovative Approaches for Enhanced Drug Efficacy

Megantara,

Rusdin,

Budiman

et al. 2024

IJN

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Since the beginning of the coronavirus pandemic in late 2019, viral infections have become one of the top three causes of mortality worldwide. Immunization and the use of immunomodulatory drugs are effective ways to prevent and treat viral infections. However, the primary therapy for managing viral infections remains antiviral and antiretroviral medication. Unfortunately, these drugs are often limited by physicochemical constraints such as low target selectivity and poor aqueous solubility. Although several modifications have been made to enhance the physicochemical characteristics and efficacy of these drugs, there are few published studies that summarize and compare these modifications. Our review systematically synthesized and discussed antiviral drug modification reports from publications indexed in Scopus, PubMed, and Google Scholar databases. We examined various approaches that were investigated to address physicochemical issues and increase activity, including liposomes, cocrystals, solid dispersions, salt modifications, and nanoparticle drug delivery systems. We were impressed by how well each strategy addressed physicochemical issues and improved antiviral activity. In conclusion, these modifications represent a promising way to improve the physicochemical characteristics, functionality, and effectiveness of antivirals in clinical therapy.

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Section: Methodsmentioning

confidence: 99%

Revolutionizing Antiviral Therapeutics: Unveiling Innovative Approaches for Enhanced Drug Efficacy

Megantara,

Rusdin,

Budiman

et al. 2024

IJN

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“…Characterization techniques like X-ray crystallography, differential scanning calorimetry (DSC), X-ray diffraction (XRD), Fourier-transform infrared spectroscopy (FTIR) and solid-state nuclear magnetic resonance (NMR) can be used to confirm the presence of co-crystals and their structure, while in vitro and in vivo evaluations assess the co-crystallization effect on drug performance. It is interesting to note that co-crystal formation may generate new intellectual property rights, as the composition and properties of the co-crystal can be patented to protect the innovation [ 9 , 51 , 52 ].…”

Section: Current Techniques To Improve Drug Solubility For Drug Desig...mentioning

confidence: 99%

Advancing Drug Delivery Paradigms: Polyvinyl Pyrolidone (PVP)-Based Amorphous Solid Dispersion for Enhanced Physicochemical Properties and Therapeutic Efficacy

Rusdin,

Mohd Gazzali,

Ain Thomas

et al. 2024

Polymers

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Background: The current challenge in drug development lies in addressing the physicochemical issues that lead to low drug effectiveness. Solubility, a crucial physicochemical parameter, greatly influences various biopharmaceutical aspects of a drug, including dissolution rate, absorption, and bioavailability. Amorphous solid dispersion (ASD) has emerged as a widely explored approach to enhance drug solubility. Objective: The objective of this review is to discuss and summarize the development of polyvinylpyrrolidone (PVP)-based amorphous solid dispersion in improving the physicochemical properties of drugs, with a focus on the use of PVP as a novel approach. Methodology: This review was conducted by examining relevant journals obtained from databases such as Scopus, PubMed, and Google Scholar, since 2018. The inclusion and exclusion criteria were applied to select suitable articles. Results: This study demonstrated the versatility and efficacy of PVP in enhancing the solubility and bioavailability of poorly soluble drugs. Diverse preparation methods, including solvent evaporation, melt quenching, electrospinning, coprecipitation, and ball milling are discussed for the production of ASDs with tailored characteristics. Conclusion: PVP-based ASDs could offer significant advantages in the formulation strategies, stability, and performance of poorly soluble drugs to enhance their overall bioavailability. The diverse methodologies and findings presented in this review will pave the way for further advancements in the development of effective and tailored amorphous solid dispersions.

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“…28 Furthermore, there is a documented shift from rod-shaped to needle-shaped crystals in the efavirenz-nicotinamide cocrystal. 29 Theophylline transforms from an acicular form to a flake-like structure in its cocrystal with urea, while irregular structures occur in its cocrystals with nicotinamide and saccharin. 30 Despite these findings, the systematic use of cocrystallization to enhance the crystal morphology remains underutilized.…”

Section: ■ Introductionmentioning

confidence: 99%

“…For instance, the carbamazepine cocrystal with nicotinamide is reported to show a significant change in morphology compared with its individual components . Furthermore, there is a documented shift from rod-shaped to needle-shaped crystals in the efavirenz-nicotinamide cocrystal . Theophylline transforms from an acicular form to a flake-like structure in its cocrystal with urea, while irregular structures occur in its cocrystals with nicotinamide and saccharin .…”

Section: Introductionmentioning

confidence: 99%

Improving Crystal Morphology through Cocrystallization: A Case Study of Rufinamide-Trimesic Acid Cocrystal

Ahmadi,

Spingler,

Rohani

2024

Crystal Growth & Design

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Crystal morphology plays a pivotal role in the production process of pharmaceutical compounds and influences the properties of the final product. Achieving control over crystal morphology, especially for thin and needle-like crystals, presents significant challenges to the industry. In this study, we investigate the crystal morphology of rufinamide (RUF) as a model compound with a notorious thread-like morphology. RUF polymorphs crystallize with markedly poor aspect ratios, with the most stable form (form A) exhibiting the thinnest morphology among all. Our initial attempts to modulate RUF crystal morphologies using solvent screening and habit-modifying additives proved unsuccessful. We explored cocrystals as a novel approach to enhance crystal morphology, given their wide application in improving various physicochemical properties of pharmaceutical solids. We employed trimesic acid (TMA) as the auxiliary compound for cocrystallization, resulting in the synthesis of RUF-TMA. The cocrystal was then subjected to solvent screening in pursuit of crystals with isometric morphology. We successfully obtained RUF-TMA cocrystals with an improved morphology using 3-pentanone as the solvent. This study offers a detailed exploration of five crystal structures, encompassing three polymorphs of RUF and two polymorphs of RUF-TMA. The elucidation of crystal structures is accompanied by a comprehensive characterization, including SCXRD, powder X-ray diffraction, thermogravimetric analysis, and differential scanning calorimetry. This study provides valuable insights into controlling crystal morphology and highlights the potential of cocrystals in enhancing morphology when conventional techniques such as solvent and additive screening of pure active pharmaceutical ingredients fall short.

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Pharmaceutical Co-crystal of Antiviral Agent Efavirenz with Nicotinamide for the Enhancement of Solubility, Physicochemical Stability, and Oral Bioavailability

Cited by 5 publications

References 59 publications

Revolutionizing Antiviral Therapeutics: Unveiling Innovative Approaches for Enhanced Drug Efficacy

Revolutionizing Antiviral Therapeutics: Unveiling Innovative Approaches for Enhanced Drug Efficacy

Advancing Drug Delivery Paradigms: Polyvinyl Pyrolidone (PVP)-Based Amorphous Solid Dispersion for Enhanced Physicochemical Properties and Therapeutic Efficacy

Improving Crystal Morphology through Cocrystallization: A Case Study of Rufinamide-Trimesic Acid Cocrystal

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