Department of Pharmaceutical Sciences, College of Clinical Pharmacy, King Faisal University , Al-Ahsa, Hufof , Saudi Arabia and.
Pharm Dev Technol. 2014 Sep;19(6):748-54. doi: 10.3109/10837450.2013.829095. Epub 2013 Aug 22.
The objective of this work was to formulate and characterize non-ionic surfactant vesicles (niosomes) as an ocular carrier of dorzolamide hydrochloride (Dorzo); one of the antiglaucoma drugs. Niosomes were prepared of Cholesterol (Chol) with sorbitan monoesters (Span 20, 40, 60) or sorbitan trioleate (Span 85) in a molar ratio of 40:150. Those prepared from Span 40 were selected for further investigation on the effect of addition of dicetylphosphate (DCP) and polyoxyethylene fatty acid esters (either Tween 20, 40 or 80). All The batches were prepared using mechanical shaking technique, followed by sonication and then characterized using Zetasizer, transmission electron microscopy (TEM), calculating percent drug entrapment efficiency and cumulative percent released. Z-average sizes of the niosomes were between 25.9 and 165.5 nm. All niosomal formulations showed negative zeta potential charge. Dorzo was successfully entrapped in all of the formulations with entrapment efficiencies ranging between 34.81% and 97.66%. With reference to release profiles, Dorzo-loaded niosomal formulations showed significant reduction in cumulative percent drug released than Dorzo solution. High entrapment efficiencies, biphasic prolonged release rate and small particles size highlight Dorzo-loaded niosomal preparations as a promising ophthalmic carrier to prolong the drug lowering effect on the intraocular pressure.
本工作旨在将非离子表面活性剂囊泡(niosomes)制成盐酸多佐胺(Dorzo)的眼部载体,Dorzo 是一种青光眼药物。囊泡由胆固醇(Chol)与山梨醇单酯(Span 20、40、60)或山梨醇三油酸酯(Span 85)以摩尔比 40:150 制成。从 Span 40 制备的囊泡被选中进行进一步研究,研究添加双十六烷基磷酸酯(DCP)和聚氧乙烯脂肪酸酯(吐温 20、40 或 80)的效果。所有批次均采用机械搅拌技术制备,然后进行超声处理,再使用 Zetasizer、透射电子显微镜(TEM)进行表征,计算药物包封效率和累积释放百分比。囊泡的 Z 均粒径在 25.9nm 至 165.5nm 之间。所有囊泡制剂均显示负的 Zeta 电位电荷。多佐胺成功包封在所有制剂中,包封效率在 34.81%至 97.66%之间。参考释放曲线,多佐胺载药囊泡制剂的累积药物释放百分比显著低于多佐胺溶液。高包封效率、双相延长释放速率和小粒径突出了多佐胺载药囊泡制剂作为一种有前途的眼部载体,可延长药物对眼压的降低作用。