Curcumin cocrystals using supercritical fluid technology

Ribas, Marcela M.; Sakata, Guilherme S.B.; Santos, Aline Elias dos; Magro, Camila Dal; Aguiar, Gean Pablo S.; Lanza, Marcelo; Oliveira, J. Vladimir

doi:10.1016/j.supflu.2019.104564

Cited by 29 publications

(13 citation statements)

References 38 publications

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“…Trial batches of etodolac cocrystal were prepared using coformers; p-hydroxybenzoic acid and glutaric acid which have the ability for the formation of hydrogen bonding (good proton donor and acceptor). But cocrystal formulation batches of glutaric acid results in increased aqueous solubility and dissolution rate of etodolac 22 . Hence glutaric acid is considered to be a more appropriate coformer for etodolac cocrystal formulation.…”

Section: Synthesis Of Etodolac Cocrystalsmentioning

confidence: 99%

“…Hence cocrystal formation is considered to be a convenient and novel crystal engineering technique in the arena of solubility enhancement. Co-crystals are formulated by various techniques such as slowly evaporation at room temperature 13,14 , reaction cocrystallization 15,16 , cooling co-crystallization 17,18 , grinding method 19,20 , and supercritical fluid technique 21,22 . By considering the pharmaceutical application of crystal engineering, it can be concluded that co-crystal may be a useful and successful strategy in improving the apparent solubility (combination of dissolution and solubility) of BCS Class II and class IV drugs which is the major problem in the expansion of optimized formulations of new chemical entities (NCEs) discovered in pharmaceutical industries 23,24 .…”

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confidence: 99%

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Cocrystal Formulation: A Novel Approach to Enhance Solubility and Dissolution of Etodolac

Ahirrao¹,

Sonawane²,

Bhambere³

et al. 2022

Biosci., Biotech. Res. Asia

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Etodolac (ETD) is a non-steroidal anti-inflammatory drug (NSAID) given in rheumatoid arthritis treatment. As it comes under BCS class II drug hence it exhibits low water solubility. Also, its dissolution rate-limited oral absorption results in delayed onset of action. The Novel approach in the solubility enhancement field; crystal engineering was preferred to prepare pharmaceutical cocrystals of etodolac with GRAS (generally recognized as safe) molecules. Pharmaceutical cocrystals of etodolac were prepared with p-hydroxybenzoic acid and glutaric acid with the drug: coformer ratio 1:1 and 1:2. Cooling cocrystallization was used to prepare etodolac cocrystals. Cocrystal formulations were characterized by saturation solubility study, in-vitro dissolution studies, and stability study. Cocrystal was also characterized by analytical parameters like Fourier transform infrared spectroscopy (FTIR), powder X-ray diffraction (PXRD), and differential scanning calorimetry (DSC). Optimized Cocrystal formulation dissolved more rapidly and their equilibrium solubility is greater than the plain drug.

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Section: Synthesis Of Etodolac Cocrystalsmentioning

confidence: 99%

mentioning

confidence: 99%

Cocrystal Formulation: A Novel Approach to Enhance Solubility and Dissolution of Etodolac

Ahirrao¹,

Sonawane²,

Bhambere³

et al. 2022

Biosci., Biotech. Res. Asia

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“…Also, the curcumin-Nacetylcysteine co-crystals developed by using acetone exhibited the highest dissolution in 180 min. 92 Goud et al formulated curcumin co-crystals using different coformers, namely, ferulic acid, p-hydroxybenzoic acid, nicotinamide, hydroquinone, and tartaric acid. Co-crystals were produced using the mechanochemical grinding method with an aim to improve the solubility of curcumin.…”

Section: Solvent Evaporationmentioning

confidence: 99%

A Review on Co-crystals of Herbal Bioactives for Solubility Enhancement: Preparation Methods and Characterization Techniques

Rathi

Kaur

Singh

2022

Crystal Growth & Design

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Co-crystallization is a promising approach for improving physical and pharmacological properties of API, viz., solubility, dissolution rate, stability, hygroscopicity, tablet ability, mechanical properties, bioavailability, and therapeutic efficacy. Different methods for the preparation of pharmaceutical co-crystals have been discussed. Instrumental and physicochemical characterization methods have also been included. Herbal bioactives are potential candidates for co-crystallization to improve solubility, mask taste, and improve bioavailability. Literature on the development of co-crystals of herbal bioactives like curcumin, quercetin, berberine, resveratrol, naringenin, and miscellaneous herbal compounds has been reported systematically in the present review. In conclusion, co-crystallization of herbal bioactives is a promising method for enhancing their physical properties. However, toxicological, stability, regulatory, and scaleup issues must be adequately addressed before commercial viability can be expected.

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“…Co-crystallization in SCF is not only applicable to typical pharmaceuticals, but also natural products. Recently, Ribas et al produced co-crystals of a natural product, curcumin, with two co-formers. , Co-crystallized curcumin by CSS gave improved solubility over neat curcumin. In their work, particles ranged from about 25–35 μm diameter, and the dissolution rate was anticorrelated to the size.…”

Section: Co-crystallization In Supercritical Fluidsmentioning

confidence: 99%

“…A number of studies have shown that reduction of co-crystal particle size improves overall dissolution. ,, Curiously, in one example, the initial dissolution (first 15 min) of larger particles was actually the same or greater than the smaller particles . This could arise from powder inhomogeneity or the presence of fines in a sample.…”

Section: Current Status and The Path Forwardmentioning

confidence: 99%

Supercritical Carbon Dioxide for Pharmaceutical Co-Crystal Production

MacEachern

Kermanshahi-pour

Mirmehrabi³

2020

Crystal Growth & Design

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Pharmaceuticals in Biopharmaceutics ClassificationSystem (BCS) Class II (low solubility, high permeability) are often modified to improve kinetic solubility. Co-crystallization and micronization are common methods for improving kinetic solubility. The basis of understanding co-crystallization processes is solubility and phase stability. In the majority of cocrystallizations, conventional solvents are utilized. Co-crystallization using supercritical carbon dioxide as a co-solvent and antisolvent can offer advantages over conventional co-crystallization including a greener solvent choice and the production of small, uniform particles without additional micronization. Gas antisolvent is the most widely reported supercritical fluid (SCF) co-crystallization process possibly due to its versatility in solvent selection and similarities to conventional antisolvent processes. This review focused on exploring critical co-crystallization parameters and feasibility of SCF techniques. In this review, it was identified that solvent choice proves to be one of the most critical parameters, impacting morphology, yield, phase purity, or polymorph to different extents. It was also identified that a systematic study of solubility to design co-crystallization processes is needed to optimize SCF co-crystallization yield and throughput. Furthermore, a focus on solubility and modeling of multicomponent systems and development of ternary phase diagrams can lead to robust, tailored co-crystallization processes in SCF systems, transitioning this technology to become more common in industry.

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Curcumin cocrystals using supercritical fluid technology

Cited by 29 publications

References 38 publications

Cocrystal Formulation: A Novel Approach to Enhance Solubility and Dissolution of Etodolac

Cocrystal Formulation: A Novel Approach to Enhance Solubility and Dissolution of Etodolac

A Review on Co-crystals of Herbal Bioactives for Solubility Enhancement: Preparation Methods and Characterization Techniques

Supercritical Carbon Dioxide for Pharmaceutical Co-Crystal Production

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