Januskaite Patricija, Goyanes Alvaro, Orlu Mine, Basit Abdul W
Department of Pharmaceutics, UCL School of Pharmacy, University College London, 29-39 Brunswick Square, London, WC1N 1AX, UK.
FABRX Ltd., Henwood House, Henwood, Ashford, Kent, TN24 8DH, UK.
Drug Deliv Transl Res. 2025 Apr 22. doi: 10.1007/s13346-025-01862-4.
Males and females are known to exhibit significant differences in drug pharmacokinetics and pharmacodynamics, which are still overlooked in pharmaceutical research and development. These disparities contribute to adverse effects and increased mortality in females, highlighting the critical need for sex-specific formulations. Extended-release formulations of doxazosin mesylate, an alpha blocker used to treat hypertension, have shown significant sex-based differences in pharmacokinetics, leading to heightened adverse effects in females and rendering current titration recommendations impractical. This study explored the potential of a 3D printing (3DP) technology, direct powder extrusion (DPE), for producing personalised, sex-specific doses of doxazosin mesylate. A simple three component formulation was made composed of hydroxypropyl cellulose (HPC) polymer Klucel JF, D-mannitol, and doxazosin mesylate. Extended-release printlets of varying doses (1, 2, and 3 mg) were manufactured from a single 1% w/w doxazosin pharma-ink batch, enabling easy dose personalisation by adjusting the printlet dimensions. The use of a single pharma-ink supports the technology's ease of use in a pharmacy setting, by eliminating frequent pharma-ink changes during the pharmaceutical compounding process. In vitro dissolution testing revealed an extended drug release profile, influenced by surface-area-to-volume (SA: V) ratios. Introducing channels in larger printlets standardized the SA: V ratios, enhancing release profile uniformity. Release kinetics followed the Hixson-Crowell and Korsmeyer-Peppas models, indicating diffusion and polymer swelling mechanisms. This work highlights the capability of DPE 3DP for creating personalized, extended-release oral dosage forms, supporting precise dose customization for patient-specific therapy. Graphical Abstract.
众所周知,男性和女性在药物药代动力学和药效学方面存在显著差异,而这些差异在药物研发中仍被忽视。这些差异导致女性出现不良反应并增加死亡率,凸显了针对性别制定药物制剂的迫切需求。甲磺酸多沙唑嗪是一种用于治疗高血压的α受体阻滞剂,其缓释制剂在药代动力学方面表现出显著的性别差异,导致女性的不良反应增加,使当前的滴定建议不切实际。本研究探讨了三维打印(3DP)技术——直接粉末挤出(DPE)用于生产个性化、针对性别的甲磺酸多沙唑嗪剂量的潜力。制备了一种简单的三元配方,由羟丙基纤维素(HPC)聚合物Klucel JF、D-甘露醇和甲磺酸多沙唑嗪组成。从单一的1%w/w多沙唑嗪药物油墨批次中制造出不同剂量(1、2和3毫克)的缓释打印片,通过调整打印片尺寸可轻松实现剂量个性化。使用单一的药物油墨消除了药物配制过程中频繁更换药物油墨的问题,支持了该技术在药房环境中的易用性。体外溶出试验显示药物释放曲线延长,受表面积与体积(SA:V)比的影响。在较大的打印片中引入通道可使SA:V比标准化,提高释放曲线的均匀性。释放动力学遵循希克森-克劳威尔和科尔斯梅尔-佩帕斯模型,表明存在扩散和聚合物溶胀机制。这项工作突出了DPE 3DP技术创建个性化缓释口服剂型的能力,支持为患者特异性治疗进行精确的剂量定制。图形摘要。