Department of Pharmaceutics, Faculty of Pharmacy, Merit University, Sohag, Egypt.
Department of Cell and Tissues, Faculty of Veterinary Medicine, Assiut University, Assiut, Egypt.
Sci Rep. 2023 Apr 8;13(1):5790. doi: 10.1038/s41598-023-32545-0.
Simvastatin (SV) is a poorly soluble drug; its oral administration is associated with a significant problem: Myopathy. The present study aims to formulate SV microsponges that have the potential to minimize the myotoxicity accompanying the oral administration of the drug. SV microsponges were prepared by exploiting the emulsion solvent evaporation technique. The % entrapment efficiency (%EE) of the drug approached 82.54 ± 1.27%, the mean particle size of SV microsponges ranged from 53.80 ± 6.35 to 86.03 ± 4.79 µm in diameter, and the % cumulative drug release (%CDR) of SV from microsponges was significantly higher than that from free drug dispersion much more, the specific surface area of the optimized microsponges formulation was found to be 16.6 m/g revealed the porosity of prepared microsponges. Histological and glycogen histochemical studies in the skeletal muscles of male albino rats revealed that microsponges were safer than free SV in minimizing myotoxicity. These findings were proven by Gene expression of Mitochondrial fusion and fission (Mfn1) & (Fis1) and (Peroxisome proliferator-activated receptor gamma co-activator 1α) PGC-1α. Finally, our study ascertained that SV microsponges significantly decreased the myotoxicity of SV.
辛伐他汀（SV）是一种难溶性药物；其口服给药与一个重大问题相关：肌病。本研究旨在制备 SV 微孔海绵，以潜在地最小化药物口服给药伴随的肌毒性。SV 微孔海绵是通过利用乳化溶剂蒸发技术制备的。药物的%包封效率（%EE）接近 82.54±1.27%，SV 微孔海绵的平均粒径范围为 53.80±6.35 至 86.03±4.79μm，SV 从微海绵中的%累积药物释放（%CDR）显著高于自由药物分散体，优化的微海绵制剂的比表面积被发现为 16.6 m/g 揭示了所制备的微海绵的多孔性。雄性白化大鼠骨骼肌的组织学和糖原组织化学研究表明，微孔海绵在最小化肌毒性方面比游离 SV 更安全。这些发现通过线粒体融合和裂变（Mfn1）和（Fis1）和（过氧化物酶体增殖物激活受体γ共激活因子 1α）PGC-1α的基因表达得到证实。最后，我们的研究证实 SV 微孔海绵显著降低了 SV 的肌毒性。
