Akram Muhammad Abdullah, Khan Barkat Ali, Khan Muhammad Khalid, Alqahtani Ali, Alshahrani Sultan M, Hosny Khaled M
Drug Delivery and Cosmetics (DDC) Laboratory, Gomal Center of Pharmaceutical Sciences, Faculty of Pharmacy, Gomal University, Dera Ismail Khan 29050, Pakistan.
Department of Pharmacology, College of Pharmacy, King Khalid University, Abha 62529, Saudi Arabia.
Polymers (Basel). 2021 Nov 11;13(22):3904. doi: 10.3390/polym13223904.
() is the main cause of chronic dermatophytosis which is highly prevalent worldwide. This study was aimed to fabricate and characterize polymeric emulgel of eugenol and linalool for the treatment of infections. Using the slow emulsification method, the emulgel was prepared and characterized for thermodynamic stability, pH analysis, viscosity, spreadability, swelling behavior, %drug content, surface morphology, globules size, polydispersity index, surface charge (mV), thermal behavior, in vitro drug release and XRD studies. Biological activities of emulgel were conducted against in vitro and in vivo. Results indicated that emulgel formulations were thermodynamically stable. The pH of the formulations was within an acceptable range for skin. The viscosity and spreadability were optimum for the better patient compliance. The swelling behavior was 111.10 ± 1.25% after 90 min. The drug content was within the official pharmacopeia limit i.e., 100 ± 10%. The surface morphology revealed by scanning electron microscopy showed a spherical-shaped structure with characteristic larger cracks and wrinkles. The droplet size, PDI, and surface charge of the optimized emulgel were 888.45 ± 8.78 nm, 0.44 and -20.30 mV, respectively. The emulgel released 84.32% of eugenol and 76.93% of linalool after 12 h. There was complete disappearance of the diffraction peaks corresponding to the drugs after XRD analysis. In rabbits, the infection was safely and completely recovered after 12 days and the emulgel produced significant effects ( < 0.05) similar to the standard product Clotrim. It is concluded that the eugenol-linalool emulgel best described all its physical properties and can be applied topically for the treatment of infections.
（）是全球高度流行的慢性皮肤癣菌病的主要病因。本研究旨在制备并表征用于治疗感染的丁香酚和芳樟醇聚合物乳化凝胶。采用缓慢乳化法制备乳化凝胶，并对其进行热力学稳定性、pH分析、粘度、铺展性、溶胀行为、药物含量百分比、表面形态、球粒大小、多分散指数、表面电荷（mV）、热行为、体外药物释放和X射线衍射研究。对乳化凝胶进行了体外和体内的生物活性研究。结果表明，乳化凝胶制剂具有热力学稳定性。制剂的pH值在皮肤可接受范围内。粘度和铺展性最佳，有利于提高患者依从性。90分钟后溶胀行为为111.10±1.25%。药物含量在法定药典限度内，即100±10%。扫描电子显微镜显示的表面形态为具有特征性较大裂缝和皱纹的球形结构。优化后的乳化凝胶的液滴大小、多分散指数和表面电荷分别为888.45±8.78nm、0.44和-20.30mV。12小时后乳化凝胶释放了84.32%的丁香酚和76.93%的芳樟醇。X射线衍射分析后对应药物的衍射峰完全消失。在兔子身上，感染在12天后安全且完全恢复，乳化凝胶产生了与标准产品克霉唑相似且显著的效果（P<0.05）。结论是，丁香酚-芳樟醇乳化凝胶很好地描述了其所有物理性质，可局部应用于治疗感染
