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A Microstirring Pill Enhances Bioavailability of Orally Administered Drugs
Advanced Science ( IF 14.3 ) Pub Date : 2021-05-18 , DOI: 10.1002/advs.202100389 Rodolfo Mundaca-Uribe 1 , Emil Karshalev 1 , Berta Esteban-Fernández de Ávila 1 , Xiaoli Wei 1 , Bryan Nguyen 1 , Irene Litvan 2 , Ronnie H Fang 1 , Liangfang Zhang 1 , Joseph Wang 1
Advanced Science ( IF 14.3 ) Pub Date : 2021-05-18 , DOI: 10.1002/advs.202100389 Rodolfo Mundaca-Uribe 1 , Emil Karshalev 1 , Berta Esteban-Fernández de Ávila 1 , Xiaoli Wei 1 , Bryan Nguyen 1 , Irene Litvan 2 , Ronnie H Fang 1 , Liangfang Zhang 1 , Joseph Wang 1
Affiliation
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Majority of drugs are administered orally, yet their efficient absorption is often difficult to achieve, with a low dose fraction reaching the blood compartment. Here, a microstirring pill technology is reported with built-in mixing capability for oral drug delivery that greatly enhances bioavailability of its therapeutic payload. Embedding microscopic stirrers into a pill matrix enables faster disintegration and dissolution, leading to improved release profiles of three widely used model drugs, aspirin, levodopa, and acetaminophen, without compromising their loading. Unlike recently developed drug-carrying nanomotors, drug molecules are not associated with the microstirrers, and hence there is no limitation on the loading capacity. These embedded microstirrers are fabricated through the asymmetric coating of titanium dioxide thin film onto magnesium microparticles. In vitro tests illustrate that the embedded microstirrers lead to substantial enhancement of local fluid transport. In vivo studies using murine and porcine models demonstrate that the localized stirring capability of microstirrers leads to enhanced bioavailability of drug payloads. Such improvements are of considerable importance in clinical scenarios where fast absorption and high bioavailability of therapeutics are critical. The encouraging results obtained in porcine model suggest that the microstirring pill technology has translational potential and can be developed toward practical biomedical applications.
中文翻译：
微搅拌药丸增强口服药物的生物利用度
大多数药物都是口服给药，但它们的有效吸收通常很难实现，只有低剂量部分到达血液室。据报道，微搅拌药丸技术具有用于口服药物输送的内置混合功能，可大大提高其治疗有效负载的生物利用度。将微型搅拌器嵌入药丸基质中可以更快地崩解和溶解，从而改善阿司匹林、左旋多巴和对乙酰氨基酚这三种广泛使用的模型药物的释放曲线，而不会影响其载量。与最近开发的载药纳米电机不同，药物分子不与微搅拌器结合，因此负载能力没有限制。这些嵌入式微搅拌器是通过在镁微粒上不对称涂覆二氧化钛薄膜而制成的。体外测试表明，嵌入式微搅拌器可显着增强局部液体输送。使用小鼠和猪模型的体内研究表明，微搅拌器的局部搅拌能力可提高药物有效负载的生物利用度。这种改进在治疗药物的快速吸收和高生物利用度至关重要的临床场景中具有相当重要的意义。在猪模型中获得的令人鼓舞的结果表明，微搅拌丸技术具有转化潜力，可以发展到实际的生物医学应用。
更新日期：2021-06-24
中文翻译：
微搅拌药丸增强口服药物的生物利用度
大多数药物都是口服给药，但它们的有效吸收通常很难实现，只有低剂量部分到达血液室。据报道，微搅拌药丸技术具有用于口服药物输送的内置混合功能，可大大提高其治疗有效负载的生物利用度。将微型搅拌器嵌入药丸基质中可以更快地崩解和溶解，从而改善阿司匹林、左旋多巴和对乙酰氨基酚这三种广泛使用的模型药物的释放曲线，而不会影响其载量。与最近开发的载药纳米电机不同，药物分子不与微搅拌器结合，因此负载能力没有限制。这些嵌入式微搅拌器是通过在镁微粒上不对称涂覆二氧化钛薄膜而制成的。体外测试表明，嵌入式微搅拌器可显着增强局部液体输送。使用小鼠和猪模型的体内研究表明，微搅拌器的局部搅拌能力可提高药物有效负载的生物利用度。这种改进在治疗药物的快速吸收和高生物利用度至关重要的临床场景中具有相当重要的意义。在猪模型中获得的令人鼓舞的结果表明，微搅拌丸技术具有转化潜力，可以发展到实际的生物医学应用。
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