Omer Safaa, Nagy Nándor, Pinke Balázs, Mészáros László, Kazsoki Adrienn, Zelkó Romána
Center of Pharmacology and Drug Research & Development, University Pharmacy Department of Pharmacy Administration, Semmelweis University, Hőgyes Endre Street 7-9, H-1092 Budapest, Hungary.
Department of Anatomy, Histology and Embryology, Semmelweis University, Tűzoltó Street 58, H-1094 Budapest, Hungary.
Pharmaceutics. 2024 Aug 9;16(8):1052. doi: 10.3390/pharmaceutics16081052.
Nanofibers can be utilized to overcome the challenges faced by conventional ophthalmic formulations. This study aimed to develop and characterize cysteamine (Cys)-loaded nanofiber-based ophthalmic inserts (OIs) as a potential candidate for the treatment of ophthalmic cystinosis using water-soluble polyvinyl alcohol (PVA)/poloxamer 407 (PO-407) and water-insoluble tetraethoxysilane (TEOS)/PVA nanofibers. Plain and Cys-loaded fibers in different proportions were prepared by the electrospinning method and studied for their morphological, physicochemical, release study, cytocompatibility effects, and stability study. The fiber formation was confirmed by scanning electron microscopy, while Fourier transform infrared spectra showed the most critical peaks for the Cys and the excipients. The release of the Cys was fast from the two polymeric matrices (≤20 min). The release from TEOS/PVA nanofibers is characterized by Case II transport (0.75 < β < 1), while the release from PVA/PO-407 nanofibers follows Fickian diffusion (β < 0.75). The cytocompatibility of compositions was confirmed by hen eggs tested on the chorioallantoic membrane (HET-CAM) of chick embryos. All formulations remained stable under stress conditions (40 ± 2 °C, 75 ± 5% relative humidity) regarding morphology and physicochemical characteristics. The developed nanofibrous mats could be an excellent alternative to available Cys drops, with better stability and convenience of self-administration as OIs.
纳米纤维可用于克服传统眼科制剂所面临的挑战。本研究旨在开发并表征载有半胱胺（Cys）的纳米纤维基眼科插入剂（OIs），以作为治疗眼科胱氨酸病的潜在候选药物，采用水溶性聚乙烯醇（PVA）/泊洛沙姆407（PO - 407）和水不溶性四乙氧基硅烷（TEOS）/PVA纳米纤维。通过静电纺丝法制备了不同比例的空白和载有Cys的纤维，并对其进行了形态学、物理化学、释放研究、细胞相容性效应和稳定性研究。通过扫描电子显微镜确认了纤维的形成，而傅里叶变换红外光谱显示了Cys和辅料的最关键峰。Cys从两种聚合物基质中的释放很快（≤20分钟）。从TEOS/PVA纳米纤维的释放以第二类转运为特征（0.75 < β < 1），而从PVA/PO - 407纳米纤维的释放遵循菲克扩散（β < 0.75）。通过在鸡胚绒毛尿囊膜（HET - CAM）上进行的鸡蛋测试证实了组合物的细胞相容性。所有制剂在应力条件（40 ± 2°C，75 ± 5%相对湿度）下在形态和物理化学特性方面保持稳定。所开发的纳米纤维垫可能是现有Cys滴眼液的极佳替代品，作为OIs具有更好的稳定性和自我给药便利性。
