Kazi Mohsin, Almarri Fahad, Shahba Ahmad Abdul-Wahhab, Ahmad Ajaz, Albraiki Salem, Alanazi Fars Kaed
Department of Pharmaceutics, College of Pharmacy, POBOX- 2457, King Saud University, Riyadh, 11451, Kingdom of Saudi Arabia.
Department of Pharmaceutics, College of Pharmacy, POBOX- 2457, King Saud University, Riyadh, 11451, Kingdom of Saudi Arabia.
Biochem Biophys Res Commun. 2024 May 21;709:149852. doi: 10.1016/j.bbrc.2024.149852. Epub 2024 Mar 28.
Vitamin D3 (VD3) deficiency among children in Saudi Arabia remains a pressing concern due to its poor bioavailability and the limitations of current pediatric formulations. To address this challenge, we developed a groundbreaking pediatric self-nanoemulsifying drug delivery system (Bio-SNEDDS) for VD3, fortified with black seed oil and moringa seed oil for dual therapeutic benefits. Through meticulous formulation optimization using ternary phase diagrams and comprehensive testing, our Bio-SNEDDS demonstrated exceptional performance.
Bio-SNEDDS were manufactured by incorporating Black seed oil and moringa seed oil as bioactive nutraceutical excipients along with various cosurfactant and surfactants. Bio-SNEDDS were systematically optimized through ternary phase diagrams, visual tests, droplet size analysis, drug solubilization studies, dispersion assessments, and pharmacokinetic testing in rats compared to Vi-De 3®.
Pseudoternary phase diagrams identified oil blends producing large nanoemulsion regions optimal for SNEDDS formation. The optimized F1 Bio-SNEDDS showed a mean droplet diameter of 33.7 nm, solubilized 154.46 mg/g VD3 with no metabolite formation, and maintained >88% VD3 in solution during 24 h dispersion testing. Notably, in vivo pharmacokinetic evaluation at a high VD3 dose demonstrated an approximately two-fold greater relative bioavailability over Vi-De 3®, validating the superb oral delivery performance of Bio-SNEDDS even under challenging high-dose conditions.
The Bio-SNEDDS provides an effective VD3 delivery strategy with established in vivo superiority over marketed products, along with offering additional health benefits from the natural oils.
由于维生素D3（VD3）生物利用度低以及现有儿科制剂存在局限性，沙特阿拉伯儿童中VD3缺乏仍然是一个紧迫问题。为应对这一挑战，我们开发了一种开创性的用于VD3的儿科自纳米乳化药物递送系统（Bio-SNEDDS），添加了黑种草籽油和辣木籽油以获得双重治疗益处。通过使用三元相图进行精心的制剂优化和全面测试，我们的Bio-SNEDDS表现出卓越性能。
通过将黑种草籽油和辣木籽油作为生物活性营养辅料与各种助表面活性剂和表面活性剂相结合来制造Bio-SNEDDS。与Vi-De 3®相比，通过三元相图、视觉测试、液滴尺寸分析、药物溶解研究、分散评估和大鼠药代动力学测试对Bio-SNEDDS进行系统优化。
伪三元相图确定了产生大纳米乳液区域的油混合物，这些区域最适合形成SNEDDS。优化后的F1 Bio-SNEDDS平均液滴直径为33.7 nm，溶解了154.46 mg/g VD3且无代谢物形成，在24小时分散测试期间溶液中VD3含量保持>88%。值得注意的是，在高VD3剂量下的体内药代动力学评估表明，其相对生物利用度比Vi-De 3®高约两倍，证实了即使在具有挑战性的高剂量条件下Bio-SNEDDS也具有出色的口服递送性能。
Bio-SNEDDS提供了一种有效的VD3递送策略，在体内表现出优于市售产品的优势，同时天然油还带来额外的健康益处。
