Bseiso Eman A, Nasr Maha, Sammour Omaima A, Abd El Gawad Nabaweya A
a Department of Pharmaceutics , Faculty of Pharmacy, October 6 University , Cairo , Egypt.
b Department of Pharmaceutics and Industrial Pharmacy , Faculty of Pharmacy, Ain Shams University , Cairo , Egypt , and.
Drug Deliv. 2016 Oct;23(8):2813-2819. doi: 10.3109/10717544.2015.1099059. Epub 2015 Oct 8.
The systemic treatment of onychomycosis has been hampered by the reported side effects of antifungals in addition to the limited blood circulation to the affected nails. Topical ungual treatment would circumvent the limitations of systemic onychomycosis treatment.
Preparation and characterization of nail penetration enhancer containing nanovesicles (nPEVs) loaded with sertaconazole for topical treatment of onychomycosis.
nPEVs were prepared using different nail penetration enhancers (N-acetyl-L-cysteine, thioglycolic acid, thiourea and ethanol) by the thin film hydration method, and characterized for their particle size, zeta potential, entrapment efficiency (EE%), elasticity, viscosity, physical stability and morphology. The selected nPEVs formula and the marketed Dermofix® cream were compared in terms of nail hydration, transungual drug uptake and antifungal activity against Trichophyton rubrum.
N-acetyl-l-cysteine was the optimum nail penetration enhancer for incorporation within vesicles. nPEVs showed high EE% of sertaconazole ranging from 77 to 95%, a size ranging from 38-538 nm and a zeta potential ranging from +48 to +72 mV. The selected nPEVs formula displayed spherical morphology and good storage stability. Compared to the conventional marketed cream, the selected nPEVs formula showed 1.4-folds higher hydration and drug uptake enhancement into nail clippings. Furthermore, it showed significantly higher zone of inhibition for Trichophyton rubrum (20.9 ± 0.25 mm) than the marketed cream (11.6 ± 0.44 mm).
Nail penetration enhancer containing nanovesicles (nPEVs) present a very promising option, worthy of clinical experimentation on onychomycotic patients.
除了受感染指甲的血液循环有限外，抗真菌药物报告的副作用也阻碍了甲癣的全身治疗。局部指甲治疗将规避全身甲癣治疗的局限性。
制备并表征负载舍他康唑的含纳米囊泡的指甲渗透促进剂（nPEV），用于甲癣的局部治疗。
采用不同的指甲渗透促进剂（N-乙酰-L-半胱氨酸、巯基乙酸、硫脲和乙醇）通过薄膜水化法制备nPEV，并对其粒径、zeta电位、包封率（EE%）、弹性、粘度、物理稳定性和形态进行表征。将选定的nPEV配方与市售的Dermofix®乳膏在指甲水化、经指甲药物摄取以及对红色毛癣菌的抗真菌活性方面进行比较。
N-乙酰-L-半胱氨酸是纳入囊泡的最佳指甲渗透促进剂。nPEV显示舍他康唑的高EE%，范围为77%至95%，粒径范围为38 - 538 nm，zeta电位范围为 +48至 +72 mV。选定的nPEV配方呈现球形形态且具有良好的储存稳定性。与传统市售乳膏相比，选定的nPEV配方在指甲水化和药物摄取增强方面显示出高1.4倍的效果。此外，它对红色毛癣菌的抑菌圈（20.9 ± 0.25 mm）明显高于市售乳膏（11.6 ± 0.44 mm）。
含纳米囊泡的指甲渗透促进剂（nPEV）是一个非常有前景的选择，值得在甲癣患者身上进行临床试验。
