Improvement and characterization of oral absorption behavior of clofazimine by SNEDDS: Quantitative evaluation of extensive lymphatic transport

Yamanouchi, Keita; Ishimaru, Tomoki; Kakuno, Takuya; Takemoto, Yumi; Kawatsu, Sho; Kondö, Keiji; Maruyama, Masato; Higaki, Kazutaka

doi:10.1016/j.ejpb.2023.04.009

Cited by 10 publications

(2 citation statements)

References 52 publications

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“…Nevertheless, given the high content in Capryol 90:Imwitor 948, the studied NE might have the potential to provide a means to obtain a high concentration of lipophilic substances with a good solubility profile in this oil mixture. When compared to other oils, Capryol 90, in higher proportion in our formula, has shown to be the better solubilizer (among those tested) for very lipophilic drugs such as simvastatin (105 mg/mL [ 29 ]), clofazimine (18 mg/mL, [ 30 ]), luliconazole [~75 mg/mL [ 31 ]), terconazole (116 mg/mL [ 32 ]), tolvaptan (11 mg/g [ 33 ]), and even novel drug candidates such as JIN-001 (41 mg/mL [ 34 ]) and AC1497 (45 to 50 mg/mL [ 35 ]), to mention just a few examples. Precipitation upon dilution is not expected to occur since no water-miscible co-solvents account for the initial drug solubilization, and droplet size does not reduce upon dilution and is shown to provide a slow release of phenytoin used as the model drug.…”

Section: Discussionmentioning

confidence: 99%

“…Immediately before the experiment, the medium was replaced by 50 µL of complete fresh medium plus 50 µL of NE preconcentrates diluted in fresh medium at twice the concentration selected for treating the cells. Cells were then incubated for 30 The fluorescence intensity of plate wells was measured using an excitation wavelength of 570 nm and emission wavelength of 590 nm in a microplate fluorophotometer (Spectramax GeminiTM EM, Molecular Devices, LLC, San Jose, CA, USA). After subtracting background fluorescence (wells with blank resazurin solution), cell viability data were expressed as a percentage of the negative control of non-treated cells.…”

Section: Cell Culture and Cytotoxicity Evaluationmentioning

confidence: 99%

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Innovative Aqueous Nanoemulsion Prepared by Phase Inversion Emulsification with Exceptional Homogeneity

Pires,

Fernandes,

Nina

et al. 2023

Pharmaceutics

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Formulating low-solubility or low-permeability drugs is a challenge, particularly with the low administration volumes required in intranasal drug delivery. Nanoemulsions (NE) can solve both issues, but their production and physical stability can be challenging, particularly when a high proportion of lipids is necessary. Hence, the aim of the present work was to develop a NE with good solubilization capacity for lipophilic drugs like simvastatin and able to promote the absorption of drugs with low permeability like fosphenytoin. Compositions with high proportion of two lipids were screened and characterized. Surprisingly, one of the compositions did not require high energy methods for high droplet size homogeneity. To better understand formulation factors important for this feature, several related compositions were evaluated, and their relative cytotoxicity was screened. Optimized compositions contained a high proportion of propylene glycol monocaprylate NF, formed very homogenous NE using a low-energy phase inversion method, solubilized simvastatin at high drug strength, and promoted a faster intranasal absorption of the hydrophilic prodrug fosphenytoin. Hence, a new highly homogeneous NE obtained by a simple low-energy method was successfully developed, which is a potential alternative for industrial application for the solubilization and protection of lipophilic actives, as well as (co-)administration of hydrophilic molecules.

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Section: Discussionmentioning

confidence: 99%

Section: Cell Culture and Cytotoxicity Evaluationmentioning

confidence: 99%

Innovative Aqueous Nanoemulsion Prepared by Phase Inversion Emulsification with Exceptional Homogeneity

Pires,

Fernandes,

Nina

et al. 2023

Pharmaceutics

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From Challenges to Solution: The Evolving Landscape of Leprosy Management

Moreira,

Oliveira,

Chaves

et al. 2024

Advanced Therapeutics

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Leprosy, caused by Mycobacterium leprae, despite being a curable disease when treated can induce peripheral neuropathy. However, the medicines used in polychemotherapy promote several side effects. Thus, research for the development of new administration systems is an alternative, but there is a lack of preclinical and clinical studies of the systems, where 90.90% have a level of technological maturity 3 and 9.09% level 4. The main issues are associated with deficiencies in vitro and in vivo cultivation methodologies, lack of financing, as well as the disinterest of the pharmaceutical industry in investing in neglected tropical diseases. In addition, with the emergence of resistant bacteria, there is urgency in the search for vaccines and, therefore, in the expansion of immunomodulation studies to define the molecular targets of the vaccine and future medications. In addition, future treatments for various diseases, including leprosy, will be directly influenced by the evolution of additive manufacturing and 3D printing, seeking personalized, flexible, and reproducible treatment.

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Human milk improves the oral bioavailability of the poorly water-soluble drug clofazimine

Ponsonby-Thomas,

Pham,

Huang

et al. 2025

European Journal of Pharmaceutics and Biopharmaceutics

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Improvement and characterization of oral absorption behavior of clofazimine by SNEDDS: Quantitative evaluation of extensive lymphatic transport

Cited by 10 publications

References 52 publications

Innovative Aqueous Nanoemulsion Prepared by Phase Inversion Emulsification with Exceptional Homogeneity

Innovative Aqueous Nanoemulsion Prepared by Phase Inversion Emulsification with Exceptional Homogeneity

From Challenges to Solution: The Evolving Landscape of Leprosy Management

Human milk improves the oral bioavailability of the poorly water-soluble drug clofazimine

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