Khan Abdul Shakur, Shah Kifayat Ullah, Mohaini Mohammed Al, Alsalman Abdulkhaliq J, Hawaj Maitham A Al, Alhashem Yousef N, Ghazanfar Shakira, Khan Kamran Ahmad, Niazi Zahid Rasul, Farid Arshad
Faculty of Pharmacy, Gomal University, Dera Ismail Khan 29050, Pakistan.
Basic Sciences Department, College of Applied Medical Sciences, King Saud bin Abdulaziz University for Health Sciences, Alahsa 31982, Saudi Arabia.
Gels. 2022 Feb 18;8(2):129. doi: 10.3390/gels8020129.
The currently available topical formulations of tacrolimus have minimal and variable absorption, elevated mean disposition half-life, and skin irritation effects resulting in patient noncompliance. In our study, we fabricated tacrolimus-loaded solid lipid nanoparticles (SLNs) that were converted into a gel for improved topical applications. The SLNs were prepared using a solvent evaporation method and characterized for their physicochemical properties. The particle size of the SLNs was in the range of 439 nm to 669 nm with a PDI of ≤0.4, indicating a monodispersed system. The Zeta potential of uncoated SLNs (F1-F5) ranged from -25.80 to -15.40 mV. Those values reverted to positive values for chitosan-decorated formulation (F6). The drug content and entrapment efficiency ranged between 0.86 ± 0.03 and 0.91 ± 0.03 mg/mL and 68.95 ± 0.03 and 83.68 ± 0.04%, respectively. The pH values of 5.45 to 5.53 depict their compatibility for skin application. The surface tension of the SLNs decreased with increasing surfactant concentration that could increase the adherence of the SLNs to the skin. The release of drug from gel formulations was significantly retarded in comparison to their corresponding SLN counterparts ( ≤ 0.05). Both SLNs and their corresponding gel achieved the same level of drug permeation, but the retention of the drug was significantly improved with the conversion of SLNs into their corresponding gel formulation ( ≤ 0.05) due to its higher bioadhesive properties.
目前可用的他克莫司局部制剂吸收极少且变化不定,平均处置半衰期延长,还会产生皮肤刺激效应,导致患者依从性差。在我们的研究中,我们制备了负载他克莫司的固体脂质纳米粒(SLNs),并将其转化为凝胶以改善局部应用。采用溶剂蒸发法制备了SLNs,并对其理化性质进行了表征。SLNs的粒径在439nm至669nm范围内,PDI≤0.4,表明为单分散体系。未包衣的SLNs(F1 - F5)的Zeta电位范围为 - 25.80至 - 15.40mV。对于壳聚糖修饰的制剂(F6),这些值变为正值。药物含量和包封率分别在0.86±0.03至0.91±0.03mg/mL和68.95±0.03至83.68±0.04%之间。pH值为5.45至5.53表明它们适用于皮肤应用。随着表面活性剂浓度的增加,SLNs的表面张力降低,这可能会增加SLNs对皮肤的粘附性。与相应的SLN制剂相比,凝胶制剂中药物的释放显著延迟(≤0.05)。SLNs及其相应的凝胶实现了相同水平的药物渗透,但由于其更高的生物粘附性,将SLNs转化为相应的凝胶制剂后,药物的保留率显著提高(≤0.05)。
Colloids Surf B Biointerfaces. 2015-4-1
Int J Pharm Investig. 2014-4
Pharmaceuticals (Basel). 2025-6-27
Naunyn Schmiedebergs Arch Pharmacol. 2025-3-13
Asian J Pharm Sci. 2025-2
Int J Pharm X. 2024-9-15