Enhancement of itraconazole solubility and release by hot-melt extrusion with Soluplus®

Darwich, May; Mohylyuk, Valentyn; Kolter, Karl; Bodmeier, Roland; Dashevskiy, Andriy

doi:10.1016/j.jddst.2023.104280

Cited by 5 publications

(2 citation statements)

References 42 publications

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“…Polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol (Soluplus) is an amphiphilic copolymer composed of hydrophilic and lipophilic segments. This structure allows Soluplus to form micelles or colloidal structures when dispersed in water [ 42 ] increasing the solubility of various compounds like curcumin [ 43 ], hesperidin [ 44 ], pterostilbene [ 45 ], or itraconazole [ 46 ]. Magnesium aluminometasilicate (Neusilin US2) is an amorphous, porous material with a high surface area and adsorption capacity.…”

Section: Introductionmentioning

confidence: 99%

Co-Dispersion Delivery Systems with Solubilizing Carriers Improving the Solubility and Permeability of Cannabinoids (Cannabidiol, Cannabidiolic Acid, and Cannabichromene) from Cannabis sativa (Henola Variety) Inflorescences

Stasiłowicz-Krzemień,

Szulc,

Cielecka-Piontek

2023

Pharmaceutics

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Cannabinoids: cannabidiol (CBD), cannabidiolic acid (CBDA), and cannabichromene (CBC) are lipophilic compounds with limited water solubility, resulting in challenges related to their bioavailability and therapeutic efficacy upon oral administration. To overcome these limitations, we developed co-dispersion cannabinoid delivery systems with the biopolymer polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol (Soluplus) and magnesium aluminometasilicate (Neusilin US2) to improve solubility and permeability. Recognizing the potential therapeutic benefits arising from the entourage effect, we decided to work with an extract instead of isolated cannabinoids. Cannabis sativa inflorescences (Henola variety) with a confirming neuroprotective activity were subjected to dynamic supercritical CO2 (scCO2) extraction and next they were combined with carriers (1:1 mass ratio) to prepare the co-dispersion cannabinoid delivery systems (HiE). In vitro dissolution studies were conducted to evaluate the solubility of CBD, CBDA, and CBC in various media (pH 1.2, 6.8, fasted, and fed state simulated intestinal fluid). The HiE-Soluplus delivery systems consistently demonstrated the highest dissolution rate of cannabinoids. Additionally, HiE-Soluplus exhibited the highest permeability coefficients for cannabinoids in gastrointestinal tract conditions than it was during the permeability studies using model PAMPA GIT. All three cannabinoids exhibited promising blood-brain barrier (BBB) permeability (Papp higher than 4.0 × 10−6 cm/s), suggesting their potential to effectively cross into the central nervous system. The improved solubility and permeability of cannabinoids from the HiE-Soluplus delivery system hold promise for enhancement in their bioavailability.

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Section: Introductionmentioning

confidence: 99%

Co-Dispersion Delivery Systems with Solubilizing Carriers Improving the Solubility and Permeability of Cannabinoids (Cannabidiol, Cannabidiolic Acid, and Cannabichromene) from Cannabis sativa (Henola Variety) Inflorescences

Stasiłowicz-Krzemień,

Szulc,

Cielecka-Piontek

2023

Pharmaceutics

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“…To overcome this challenge, scientists have extensively investigated diverse strategies aimed at augmenting the solubility and dissolution rate of Itraconazole. [27][28][29] This study investigates the solubility enhancement of Itraconazole (ITZ) through CMS, a solid-state processing technique. The objective is to improve ITZ's solubility and dissolution rate by transforming its crystalline structure to an amorphous state.…”

Section: Introductionmentioning

confidence: 99%

Solubility Enhancement of Itraconazole by Centrifugal Melt Spinning Technique

PJ,

2023

IJDDT

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Itraconazole is an antifungal drug with poor water solubility and limited bioavailability, presenting difficulties in achieving effective therapeutic applications. This study aimed to employ centrifugal melt spinning, an innovative method, to improve the solubility of itraconazole. In this process, itraconazole was subjected to centrifugal forces while melting, forming amorphous solid dispersions. Microfibers loaded with 10% w/w itraconazole were prepared through centrifugal melt spinning, employing sucrose as a carrier. ITZ-sucrose microfibers with uniform morphology and an average diameter of 14.27 ± 2.90 μm were successfully fabricated, as evidenced by the scanning electron microscopy results. XRD and DSC measurements confirmed the amorphous nature of the spun microfibers. The solubility of Itraconazole sucrose microfibers was significantly enhanced by 17-fold compared to plain itraconazole. The dissolution experiments demonstrated that sucrose microfibers loaded with ITZ achieved a significant release of 94.96 ± 1.47% within 10 minutes, representing a substantial enhancement compared to plain drugs. The study indicated that utilizing the centrifugal melt spinning technique successfully generated amorphous solid dispersions of itraconazole, leading to a considerable improvement in the drug’s solubility.

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Amorphous solid dispersions of amphiphilic polymer excipients and indomethacin prepared by hot melt extrusion

Keßler,

Mishra,

Hietala

et al. 2025

European Journal of Pharmaceutical Sciences

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Enhancement of itraconazole solubility and release by hot-melt extrusion with Soluplus®

Cited by 5 publications

References 42 publications

Co-Dispersion Delivery Systems with Solubilizing Carriers Improving the Solubility and Permeability of Cannabinoids (Cannabidiol, Cannabidiolic Acid, and Cannabichromene) from Cannabis sativa (Henola Variety) Inflorescences

Co-Dispersion Delivery Systems with Solubilizing Carriers Improving the Solubility and Permeability of Cannabinoids (Cannabidiol, Cannabidiolic Acid, and Cannabichromene) from Cannabis sativa (Henola Variety) Inflorescences

Solubility Enhancement of Itraconazole by Centrifugal Melt Spinning Technique

Amorphous solid dispersions of amphiphilic polymer excipients and indomethacin prepared by hot melt extrusion

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