Bilosomes as a promising nanoplatform for oral delivery of an alkaloid nutraceutical: improved pharmacokinetic profile and snowballed hypoglycemic effect in diabetic rats.
Bilosomes as a promising nanoplatform for oral delivery of an alkaloid nutraceutical: improved pharmacokinetic profile and snowballed hypoglycemic effect in diabetic rats.
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DOI：
10.1080/10717544.2022.2110997
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发表时间：
2022-12
期刊：
影响因子：
6
通讯作者：
中科院分区：
文献类型：
--
作者：
糖尿病是一种危及生命的代谢性疾病。本研究的目的是开发小檗碱载药的生物体（BER-BLS），以提高天然抗糖尿病药物小檗碱的口服生物利用度和疗效。BER-BLS使用薄膜水合策略制造，并使用中心复合设计（面心）进行优化。优化的BER-BLS制剂的平均囊泡尺寸、包封率和表面电荷分别为196.5 nm、89.7%、（-）36.4 mV。与盐酸小檗碱溶液（BER-SOL）相比，盐酸小檗碱缓释片具有更高的稳定性和更好的缓释效果。将BER-BLS和BER-SOL给予链脲佐菌素诱导的糖尿病大鼠。优化的BER-BLS制剂具有显著的降血糖作用，最大血糖降低41%，而BER-SOL仅降低血糖19%。此外，与皮下注射胰岛素（1 IU）相比，口服BER-BLS和BER-SOL的药理作用分别为99.3%和31.7%。药代动力学分析发现，与BER-SOL相比，BER-BLS中小檗碱的相对生物利用度在100 mg/kg体重的剂量下增加了6.4倍。组织学研究表明，BER-BLS适合口服给药。我们的数据表明，BLS是一个潜在的纳米载体黄连素管理，提高其口服生物利用度和抗糖尿病活性。
Diabetes mellitus is a life-threatening metabolic disease. At the moment, there is no effective treatment available to combat it. In this study, we aimed to develop berberine-loaded bilosomes (BER-BLS) to boost the oral bioavailability and therapeutic efficacy of berberine, a natural antidiabetic medication. The BER-BLS was fabricated using a thin-film hydration strategy and optimized using a central composite design (face-centered). The average vesicle size, entrapment efficiency, and surface charge of the optimized BER-BLS preparation were 196.5 nm, 89.7%, (−) 36.4 mV, respectively. In addition, it exhibited higher stability and better-sustained release of berberine than the berberine solution (BER-SOL). BER-BLS and BER-SOL were administered to streptozocin-induced diabetic rats. The optimized BER-BLS formulation had a significant hypoglycemic impact, with a maximum blood glucose decrease of 41%, whereas BER-SOL only reduced blood glucose by 19%. Furthermore, the pharmacological effect of oral BER-BLS and BER-SOL corresponded to 99.3% and 31.7%, respectively, when compared to subcutaneous insulin (1 IU). A pharmacokinetic analysis found a 6.4-fold rise in the relative bioavailability of berberine in BER-BLS when compared to BER-SOL at a dosage of 100 mg/kg body weight. Histopathological investigation revealed that BER-BLS is suitable for oral administration. Our data demonstrate that BLS is a potential nanocarrier for berberine administration, enhancing its oral bioavailability and antidiabetic activity.
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DOI：
10.3390/ph15030281
发表时间：
2022-02-24
期刊：
Pharmaceuticals (Basel, Switzerland)
影响因子：
--
作者：
Abo El-Enin HA;Elkomy MH;Naguib IA;Ahmed MF;Alsaidan OA;Alsalahat I;Ghoneim MM;Eid HM
通讯作者：
Eid HM
影响因子：
5.4
作者：
Elkomy MH;Alruwaili NK;Elmowafy M;Shalaby K;Zafar A;Ahmad N;Alsalahat I;Ghoneim MM;Eissa EM;Eid HM
通讯作者：
Eid HM
影响因子：
3.4
作者：
Elkomy, Mohammed H.;El Menshawe, Shahira F.;Ali, Ahmed M. A.
通讯作者：
Ali, Ahmed M. A.
影响因子：
5.4
作者：
Eissa, Essam M.;Elkomy, Mohammed H.;Eid, Hussein M.;Ali, Adel A.;Abourehab, Mohammed A. S.;Alsubaiyel, Amal M.;Naguib, Ibrahim A.;Alsalahat, Izzeddin;Hassan, Amira H.
通讯作者：
Hassan, Amira H.
影响因子：
4.4
作者：
Ahmed, Tarek A.
通讯作者：
Ahmed, Tarek A.