Supersaturable self-microemulsifying delivery systems: an approach to enhance oral bioavailability of benzimidazole anticancer drugs

Rosso, Annalisa; Almouazen, Eyad; Pontes, Jorge F.; Andretto, Valentina; Leroux, Marine; Romasko, Etienne; Azzouz-Maache, Samira; Bordes, Claire; Coste, Isabelle; Renno, Touffic; Giraud, Stéphane; Briançon, Stéphanie; Lollo, Giovanna

doi:10.1007/s13346-021-00904-x

Cited by 8 publications

(5 citation statements)

References 46 publications

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“…The high hydroxyl group presence within the pegylated surfactants used can allow for a strong interaction/attraction force between the APIs resulting in a significantly smaller particle size. SNEDDS were able to be loaded with high amounts of both NFX and BNZ (2.5 and 10 mg g −1 almost double than previously reported [59,60]), and are concentrations that can be translated preclinically (allowing for 25 mg kg −1 and 50 mg kg −1 doses respectively).…”

Section: Discussionmentioning

confidence: 75%

Solid Nanomedicines of Nifurtimox and Benznidazole for the Oral Treatment of Chagas Disease

Rolón¹,

Hanna

Vega³

et al. 2022

Pharmaceutics

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Chagas disease (CD) is a parasitic zoonosis endemic in Central and South America affecting nearly 10 million people, with 100 million people at high risk of contracting the disease. Treatment is only effective when received at the early stages of the disease and it involved two drugs (nifurtimox (NFX) and benznidazole (BNZ)). Both treatments require multiple daily administrations of high doses, suffer from variable efficacy and insufficient efficacy in chronic CD, many side effects, and a very long duration of treatment that results in poor compliance, while combined available therapies that lead to reduced duration of treatment are not available and polypharmacy reduces compliance and increases the cost further. Here we present self-nanoemulsified drug delivery systems (SNEDDS) able to produce easily scalable combined formulations of NFX and BNZ that can allow for tailoring of the dose and can be easily converted to oral solid dosage form by impregnation on mesoporous silica particles. SNEDDS demonstrated an enhanced solubilisation capacity for both drugs as demonstrated by flow-through studies and in vitro lipolysis studies. High loading of SNEDDS to Syloid 244 and 3050 silicas (2:1 w/w) allowed clinically translatable amounts of both NFX and BNZ to be loaded. Tablets prepared from NFX-BNZ combined SNEDDS loaded on Syloid 3050 silicas demonstration near complete dissolution in the flow through cell apparatus compared to NFX and BNZ commercial tablets respectively (Lampit® and Rochagan®). NFX-BNZ-SNEDDS demonstrated nanomolar efficacy in epimastigotes and amastigotes of T. cruzi with acceptable selectivity indexes and demonstrated enhanced survival and reduced parasitaemia in acute murine experimental models of CD. Thus, the results presented here illustrate the ability for an easily scalable and personalised combination oral therapy prepared from GRAS excipients, enabling treatment access worldwide for the treatment of CD.

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Section: Discussionmentioning

confidence: 75%

Solid Nanomedicines of Nifurtimox and Benznidazole for the Oral Treatment of Chagas Disease

Rolón¹,

Hanna

Vega³

et al. 2022

Pharmaceutics

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“…The transport of β-carotene loaded into an NDS across Caco-2 cell monolayers was studied following the method of Rosso et al [19]. Caco-2 cells were seeded onto Transwell inserts (ThinCert™ Greiner Bio-One, Les Ulis, France) in 24-well tissue culture plates (Cellstar ® Greiner Bio-One, Les Ulis, France).…”

Section: In Vitro Safety and Absorption Assessmentmentioning

confidence: 99%

“…Thus, liquid emulsion delivery systems inevitably suffer from poor physical or chemical stability, and carriage, transportation, or storage inconvenience, which are commonly associated with liquid formulations in practical applications [16]. Although a solid self-emulsifying delivery system could make the delivery system solid [17], both the formulations and procedures of emulsion fabrication are pretty complicated [18,19].…”

Section: Introductionmentioning

confidence: 99%

Dry Nutrition Delivery System Based on Defatted Soybean Particles and Its Application with β-Carotene

Ouyang

Zhou

et al. 2023

Molecules

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Many nutrition delivery systems (NDSs) have been developed for the encapsulation, protection, and delivery of bioactive compounds, such as β-carotene. Most of those systems were prepared in solution, which is inconvenient for transportation and storage in the food industry. In the present work, we constructed an environmentally friendly dry NDS based on defatted soybean particles (DSPs) by milling a β-carotene-DSP mixture. The loading efficiency of the NDS reached 89.0%, and the cumulative release rate decreased from 15.1% (free β-carotene) to 6.0% within 8 h. The stability of β-carotene in the dry NDS was found to have increased in a thermogravimetric analysis. Stored for 14 days at 55 °C or under UV irradiation, the retaining rates of β-carotene in the NDS increased to 50.7% and 63.6%, respectively, while they were 24.2% and 54.6% for the free samples. The bioavailability of β-carotene was improved by the NDS too. The apparent permeability coefficient of the NDS reached 1.37 × 10−6 cm/s, which is 12 times that of free β-carotene (0.11 × 10−6 cm/s). Besides being environmentally friendly, the dry NDS can facilitate carriage, transportation, or storage in the food industry, and similar to other NDSs, it improves the stability and bioavailability of nutrients.

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“…Benzothiazole derivatives have a wide spectrum of biological applications, including anticancer, [106] anticonvulsant [107] and antidiabetic activity [108] …”

Section: Bicyclic Compoundsmentioning

confidence: 99%

SAR Analysis of Heterocyclic Compounds with Monocyclic and Bicyclic Structures as Antifungal Agents

Liu

Sun

et al. 2022

ChemMedChem

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Infections caused by eukaryotic organisms, such as fungi, are generally more difficult to treat than bacterial infections. With the widespread use of antifungal drugs in humans and plants, resistance and toxicity have emerged. Therefore, it is desirable to develop new antifungal drugs with low toxicity that are not susceptible to the development of resistance. This review presents a summary of the past few years (2017-2021) of research on heterocyclic compounds as antifungal agents for use in humans and plants, focusing on the structure-activity relationships (SAR) of these compounds. This review may provide ideas and information for designing and developing new antifungal drugs with fewer side effects compared with currently available drugs.

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Supersaturable self-microemulsifying delivery systems: an approach to enhance oral bioavailability of benzimidazole anticancer drugs

Cited by 8 publications

References 46 publications

Solid Nanomedicines of Nifurtimox and Benznidazole for the Oral Treatment of Chagas Disease

Solid Nanomedicines of Nifurtimox and Benznidazole for the Oral Treatment of Chagas Disease

Dry Nutrition Delivery System Based on Defatted Soybean Particles and Its Application with β-Carotene

SAR Analysis of Heterocyclic Compounds with Monocyclic and Bicyclic Structures as Antifungal Agents

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