Current study was aimed to design and develop muco-adhesive self-nano emulsifying drug delivery system (SNEDDs) for improved pharmacokinetics of Cefixime (CFX) in rabbits. The components of SNEDDs formulation i.e., cinnamon oil, Tween® 80, and PEG 200 as oil, surfactant, and co-surfactant respectively were selected based on their high solubilizing capability of the drug. SNEDDs formulation was optimized using Design of experiments (D-optimal design) in terms of droplet size, poly dispersity index and zeta potential. The optimized SNEDDs formulation was studied for various parameters like droplet size, morphology, zeta potential, emulsification, optical clarity, thermodynamic stability, GIT stability, and robustness to dilution. CFX was loaded to optimized formulation to form CFX-SNEDDs. Furthermore, acyl-chitosan, a muco-adhesive agent, was added to CFX-SNEDDS to prepare CHT-CFX-SNEDDS. In vitro drug release showed the controlled release behavior reached a maximum value of 70 % at pH 6.8 within 24 h. The droplet size, atomic force microscopy, and optical clarity analysis revealed the formation of nanosized emulsion (156 ± 25 nm) with spherical morphology. Also in vivo pharmacokinetic studies on rabbits showed an increased drug plasma concentration for CHT-CFX-SNEDDs (15 ± 3 μg/mL) and CFX-SNEDDs (9 ± 2 μg/mL) in comparison with control CFX (4 ± 1 μg/mL). The results indicated that the developed CHT-CFX-SNEDDs with an increased degree of solubilization, permeation, and nanosized range emulsion enhance the oral performance of CFX.

目前的研究旨在设计和开发黏液粘附自纳米乳化给药系统 (SNEDDs)，以改善兔头孢克肟 (CFX) 的药代动力学。SNEDDs 制剂的成分，即肉桂油、Tween® 80 和 PEG 200 分别作为油、表面活性剂和助表面活性剂，是根据它们对药物的高增溶能力来选择的。SNEDDs 配方使用实验设计（D 最优设计）在液滴尺寸、多分散指数和 zeta 电位方面进行了优化。研究了优化的 SNEDDs 配方的各种参数，如液滴大小、形态、zeta 电位、乳化、光学透明度、热力学稳定性、GIT 稳定性和稀释稳定性。CFX 被加载到优化的配方中以形成 CFX-SNEDD。此外，酰基壳聚糖，一种粘液粘合剂，体外药物释放显示控释行为在 pH 6.8 下 24 小时内达到最大值 70%。液滴尺寸、原子力显微镜和光学透明度分析表明形成了具有球形形态的纳米级乳液 (156 ± 25 nm)。此外，兔体内药代动力学研究表明，与对照 CFX (4 ± 1 μg/mL) 相比，CHT-CFX-SNEDDs (15 ± 3 μg/mL) 和 CFX-SNEDDs (9 ± 2 μg/mL) 的药物血浆浓度增加。毫升）。结果表明，开发的 CHT-CFX-SNEDDs 具有更高的增溶度、渗透性和纳米级乳液，可提高 CFX 的口服性能。