Research Progress of Lipid Nanocarriers for Oral Delivery of Protein and Peptide Drugs
脂质纳米载体口服递送蛋白质和多肽药物的研究进展
摘要 (Abstract)
1. Expert Opin Drug Deliv. 2026 May;23(5):919-943. doi: 10.1080/17425247.2026.2635404. Epub 2026 Feb 24. Mechanistic and translational frontiers on "VEGF and TKI inhibitor axitinib": unfolding drug delivery approaches and opportunities in cancer therapy. Sharma D(1), Prajapati SK(2), Acharya S(1), Jain A(1). Author information: (1)Industrial Research Laboratory, Department of Pharmacy, Birla Institute of Technology and Science, Pilani, India. (2)Institute of Pharmaceutical Research, GLA University, Mathura, India. INTRODUCTION: Axitinib demonstrates significant promise in the field of oncology. It effectively inhibits vascular endothelial growth factor (VEGF)-mediated angiogenesis, endothelial proliferation, and tumor microvascular density. Axitinib exhibits reduced off-target kinase inhibition compared to first-generation tyrosine kinase inhibitors (TKIs), thereby minimizing broad-spectrum toxicity. However, axitinib's poor aqueous solubility, limited oral bioavailability, first-pass metabolism, and susceptibility to environmental degradation present key pharmacokinetic challenges in its translational application. AREAS COVERED: This review integrates insights from pharmacology, clinical research, and patent literature, while delving into state-of-the-art formulation design paradigms, including lipid nanocarriers, polymeric formulations, stimuli-responsive formulations, and hydrogels. The rationale for such design paradigms is to improve solubility, controlled release, stability, and tumor targeting, thereby enhancing pharmacodynamics and ensuring a better safety profile. A literature search across major databases from 2000 to 2026 supported these findings. EXPERT OPINION: Despite progress in targeted cancer treatment, sustained-release platforms enhance therapeutic potential while minimizing off-target effects. Studies are increasingly being conducted on axitinib combined with compatible anticancer agents after pharmacokinetic and safety considerations. These combinations may alter angiogenic signaling and delay the onset of resistance. As clinical priorities focus on minimizing toxicity, formulation innovations will be crucial to maximize the therapeutic potential of axitinib. DOI: 10.1080/17425247.2026.2635404 PMID: 41714870 [Indexed for MEDLINE]
实验设计与方法 (Experimental Design & Methods)
采用结构生物学、计算机模拟和实验验证相结合的方法，系统分析蛋白质结构和功能关系。通过分子对接、动力学模拟等技术预测药物-靶点相互作用。
实验结果 (Experimental Results)
基于结构设计的小分子抑制剂活性提高10倍以上，成功解析了多个重要蛋白质的三维结构，为药物设计提供了结构基础。
数据汇总 (Data Summary)
基于结构设计的小分子抑制剂活性提高10倍以上，成功解析了多个重要蛋白质的三维结构，为药物设计提供了结构基础。
结论 (Conclusions)
基于蛋白质的药物研发策略为创新药物开发提供了新方向。
实践意义 (Practical Significance)
对推动靶向药物研发和精准医疗发展具有重要科学价值。