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嵌入镁铝层状双氢氧化物中的苯妥英钠的溶解度、溶出度和生物利用度的改善

Improvement of solubility, dissolution, and bioavailability of phenytoin intercalated in Mg-Al layered double hydroxide.

作者信息

Anwar Bakr Rehab, Kotta Sabna, Aldawsari Hibah Mubarak, Ashri Lubna Y, Badr-Eldin Shaimaa M, Eltahir Heba, Ahmed Sameh A, Alahmadi Yaser M, Abouzied Mekky

机构信息

Department of Pharmaceutics, Faculty of Pharmacy, King Abdulaziz University, Jeddah, Saudi Arabia.

Center of Excellence for Drug Research and Pharmaceutical Industries, King Abdulaziz University, Jeddah, Saudi Arabia.

出版信息

Front Pharmacol. 2024 Aug 2;15:1440361. doi: 10.3389/fphar.2024.1440361. eCollection 2024.

DOI:10.3389/fphar.2024.1440361
PMID:39156110
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11327046/
Abstract

Layered double hydroxides (LDHs) are highly effective drug delivery systems, owing to their capacity to intercalate or adsorb biomaterials, flexible structure, swelling property, high stability, good biocompatibility, and ease of synthesis. Phenytoin (PHT) is an antiseizure BCS (Biopharmaceutics Classification System) class II drug, presenting low aqueous solubility. Therefore, the current study aimed at increasing its solubility, dissolution, and bioavailability. PHT was intercalated to the MgAl-LDH formed and successful intercalation to form MgAl-PHT-LDH was confirmed by FTIR, PXRD, DSC, and TGA. Examination of particle size and morphology (by photon correlation spectroscopy and electron microscopy, respectively) confirmed the formation and intercalation of nanostructured LDH. Intercalation enhanced the saturation solubility of PHT at 25°C in 0.1N HCl and phosphate buffer (pH 6.8) by 6.57 and 10.5 times respectively. The selected drug excipient powder blend for the formulation of MgAl-PHT-LDH tablets exhibited satisfactory properties in both pre-compression parameters (angle of repose, bulk density, tapped density, Carr's index, and Hausner ratio) and tablet characteristics (weight variation, thickness, hardness, friability, content uniformity, and disintegration time). MgAl-PHT-LDH tablets showed better dissolution of PHT compared to unprocessed PHT tablets at all time points. Oral bioavailability of MgAl-PHT-LDH tablets and unprocessed PHT tablets was tested in two groups of Sprague Dawley rats based on analysis of serum levels of both forms of PHT by UPLC-ESI-MS/MS serum. MgAl-PHT-LDH tablets demonstrated a relative bioavailability of 130.15% compared to unprocessed PHT tablets, confirming a significantly higher oral bioavailability of MgAl-PHT-LDH. In conclusion, MgAl-PHT-LDH could provide a strategy for enhancing solubility, dissolution, and thereby bioavailability of PHT, enabling the evaluation of theclinical efficacy of MgAl-PHT-LDH tablets for the treatment of seizures at lower PHT doses.

摘要

层状双氢氧化物（LDHs）是高效的药物递送系统，这归因于它们嵌入或吸附生物材料的能力、灵活的结构、膨胀特性、高稳定性、良好的生物相容性以及易于合成。苯妥英（PHT）是一种抗癫痫的BCS（生物药剂学分类系统）II类药物，水溶性较低。因此，本研究旨在提高其溶解度、溶出度和生物利用度。PHT被嵌入到形成的MgAl-LDH中，通过傅里叶变换红外光谱（FTIR）、粉末X射线衍射（PXRD）、差示扫描量热法（DSC）和热重分析（TGA）证实成功嵌入形成MgAl-PHT-LDH。分别通过光子相关光谱法和电子显微镜对粒径和形态的检测证实了纳米结构LDH的形成和嵌入。嵌入分别使PHT在25°C下于0.1N盐酸和磷酸盐缓冲液（pH 6.8）中的饱和溶解度提高了6.57倍和10.5倍。用于制备MgAl-PHT-LDH片剂的选定药物辅料粉末混合物在预压参数（休止角、堆密度、振实密度、卡尔指数和豪斯纳比）和片剂特性（重量差异、厚度、硬度、脆碎度、含量均匀度和崩解时间）方面均表现出令人满意的性能。在所有时间点，MgAl-PHT-LDH片剂的PHT溶出度均优于未处理的PHT片剂。基于通过超高效液相色谱-电喷雾串联质谱法（UPLC-ESI-MS/MS）分析血清中两种形式PHT的水平，在两组Sprague Dawley大鼠中测试了MgAl-PHT-LDH片剂和未处理的PHT片剂的口服生物利用度。与未处理的PHT片剂相比，MgAl-PHT-LDH片剂的相对生物利用度为130.15%，证实MgAl-PHT-LDH的口服生物利用度显著更高。总之，MgAl-PHT-LDH可为提高PHT的溶解度、溶出度以及生物利用度提供一种策略，从而能够在较低PHT剂量下评估MgAl-PHT-LDH片剂治疗癫痫的临床疗效。

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