Efficient Enhancement in Itraconazole Solubility through its Cyclodextrin-Water Soluble Polymer Ternary Inclusion Complexes

Sid, Dounia; Baitiche, Milad; Elbahri, Zineb; Djerboua, Ferhat; Messalti, Sabrine; Boutahala, Mokhtar

doi:10.22270/jddt.v10i3.4046

Cited by 4 publications

(3 citation statements)

References 18 publications

(24 reference statements)

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“…It exhibits a synergistic effect between these components 23 . The Advantage of incorporating PVP K30 during the complexation of drugs with CD significantly increases the solubility and promotes the physicochemical properties of poorly water-soluble drugs 24,25 .…”

Section: Formation Of Ternary Complexmentioning

confidence: 99%

Untitled

2021

IJPSR

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One of the major barriers in the development of oral dosage form is poor solubility. Poor water solubility obstructs drug bioavailability and decreases its pharmaceutical development. Many drugs are in the pipeline to enhance solubility to formulate dosage form to be taken by the most preferred route of administration that is the oral route. Etodolac is nonsteroidal anti-inflammatory drug having a wide spectrum of activities but belongs to BCS class II. The attempt has been made in this work to improve solubility by forming ternary inclusion complexes of Etodolac with PVP K30 and β-Cyclodextrins. The ternary inclusion complexes were prepared by the physical mixing method and kneading method. The prepared complexes were analyzed by different analytical techniques comprising differential scanning calorimetry, infrared spectroscopy and solubility study. Special emphasis was given on the solubility evaluation of drugs and complexes. Based on observations and results, one can easily conclude about the usefulness of the complexation technique for the enhancement of solubility. INTRODUCTION:Solubility, dissolution and gastrointestinal permeability are basic parameters that control the rate and extent of drug absorption and its bioavailability 1, 2 . The aqueous solubility of the drug plays an important role in drug absorption after oral administration 3,4 . Inadequate aqueous solubility of active pharmaceutical ingredients is very challenging in the development process of new drug products 5 .

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Section: Formation Of Ternary Complexmentioning

confidence: 99%

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2021

IJPSR

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“…Solid-state analyses, including Fourier transform infrared spectroscopy, powder X-ray diffraction, and differential scanning calorimetry, were performed on all formulations and pure ITZ. Solubility tests revealed that both binary and ternary complexes significantly increased ITZ solubility compared to the pure drug, with the ternary complexes showing fast and extensive drug release [ 39 ]. Cuoco et al [ 40 ] explored the impact of biomimetic media on ITZ absorption from Sporanox ® , which contains HPBCD to improve solubility.…”

Section: Introductionmentioning

confidence: 99%

Host–Guest Complexation of Itraconazole with Cyclodextrins for Bioavailability Enhancement

Şuta,

Ridichie,

Ledeţi

et al. 2024

Pharmaceutics

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Itraconazole is an antifungal agent included in the triazole pharmacological classification that belongs to the BCS class II, characterized by a low solubility in an aqueous medium (of 1 ng/mL, at neutral pH), which is frequently translated in a low oral bioavailability but with a high permeability. In this sense, it is necessary to find solutions to increase/improve the solubility of itraconazole in the aqueous environment. The main purpose of this study is the preparation and analysis of five different guest–host inclusion complexes containing intraconazole. Initially, a blind docking process was carried out to determine the interactions between itraconazole and the selected cyclodextrins. The second step of the study was to find out if the active pharmaceutical ingredient was entrapped in the cavity of the cyclodextrin, by using spectroscopic and thermal techniques. Also, the antifungal activity of the inclusion complexes was studied to examine if the entrapment of itraconazole influences the therapeutic effect. The results showed that the active substance was entrapped in the cavity of the cyclodextrins, with a molar ratio of 1:3 (itraconazole–cyclodextrin), and that the therapeutic effect was not influenced by the entrapment.

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“…Chemical modifications, such as prodrug formation, can also be employed to enhance solubility. [6][7][8][9][10] Additionally, the use of novel drug delivery systems, including lipid-based formulations, 11 nanoparticles (NP), and self-emulsifying systems, 12 has shown promise in improving the solubility of the drug and its bioavailability. 13 The formation of fibrous solid dispersions is indeed an effective approach in the field of solubility enhancement.…”

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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Efficient Enhancement in Itraconazole Solubility through its Cyclodextrin-Water Soluble Polymer Ternary Inclusion Complexes

Cited by 4 publications

References 18 publications

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Host–Guest Complexation of Itraconazole with Cyclodextrins for Bioavailability Enhancement

Solubility Enhancement of Itraconazole by Centrifugal Melt Spinning Technique

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