Bashyal Santosh, Seo Jo-Eun, Keum Taekwang, Noh Gyubin, Lamichhane Shrawani, Lee Sangkil
College of Pharmacy, Keimyung University, 1095 Dalgubeol-daero, Dalseo-gu, Daegu 42601, Korea.
Center for Forensic Pharmaceutical Sciences, Keimyung University, 1095 Dalgubeol-daero, Dalseo-gu, Daegu 42601, Korea.
Pharmaceutics. 2021 Apr 16;13(4):565. doi: 10.3390/pharmaceutics13040565.
Buccal drug delivery is a suitable alternative to invasive routes of drug administration. The buccal administration of insulin for the management of diabetes has received substantial attention worldwide. The main aim of this study was to develop and characterize elastic liposomes and assess their permeability across porcine buccal tissues. Sodium-cholate-incorporated elastic liposomes (SC-EL) and sodium-glycodeoxycholate-incorporated elastic liposomes (SGDC-EL) were prepared using the thin-film hydration method. The prepared liposomes were characterized and their ex vivo permeability attributes were investigated. The distribution of the SC-EL and SGDC-EL across porcine buccal tissues was evaluated using confocal laser scanning microscopy (CLSM). The SGDC-EL were the most superior nanocarriers since they significantly enhanced the permeation of insulin across porcine buccal tissues, displaying a 4.33-fold increase in the permeability coefficient compared with the insulin solution. Compared with the SC-EL, the SGDC-EL were better at facilitating insulin permeability, with a 3.70-fold increase in the permeability coefficient across porcine buccal tissue. These findings were further corroborated based on bioimaging analysis using CLSM. SGDC-ELs showed the greatest fluorescence intensity in buccal tissues, as evidenced by the greater shift of fluorescence intensity toward the inner buccal tissue over time. The fluorescence intensity ranked as follows: SGDC-EL > SC-EL > FITC-insulin solution. Conclusively, this study highlighted the potential nanocarriers for enhancing the buccal permeability of insulin.
口腔给药是侵入性给药途径的一种合适替代方法。用于糖尿病管理的胰岛素口腔给药已在全球范围内受到广泛关注。本研究的主要目的是开发和表征弹性脂质体，并评估其在猪口腔组织中的渗透性。采用薄膜水化法制备了含胆酸钠的弹性脂质体（SC-EL）和含甘氨脱氧胆酸钠的弹性脂质体（SGDC-EL）。对制备的脂质体进行了表征，并研究了其体外渗透特性。使用共聚焦激光扫描显微镜（CLSM）评估了SC-EL和SGDC-EL在猪口腔组织中的分布。SGDC-EL是最优异的纳米载体，因为它们显著增强了胰岛素在猪口腔组织中的渗透，与胰岛素溶液相比，渗透系数增加了4.33倍。与SC-EL相比，SGDC-EL在促进胰岛素渗透方面表现更好，在猪口腔组织中的渗透系数增加了3.70倍。基于CLSM的生物成像分析进一步证实了这些发现。SGDC-EL在口腔组织中显示出最大的荧光强度，随着时间的推移，荧光强度向口腔内侧组织的更大偏移证明了这一点。荧光强度排序如下：SGDC-EL＞SC-EL＞FITC-胰岛素溶液。总之，本研究突出了用于增强胰岛素口腔渗透性的潜在纳米载体。
