Department of Pharmaceutics, Rajiv Academy for Pharmacy, Mathura, Uttar Pradesh, India.
Pharm Dev Technol. 2011 Aug;16(4):367-76. doi: 10.3109/10837451003739289. Epub 2010 Mar 31.
The present study was carried out to exploit the feasibility of using polymeric nanosponges as an alternative carrier for targeting econazole nitrate (EN) to the skin through topical hydrogel formulation. Nanosponges prepared by emulsion solvent diffusion method were evaluated for various physicochemical parameters and in vitro drug release. The nanosponges of EN were discrete free flowing nanosized particles with perforated orange peel like morphology as visualized by SEM. The nanosponge formulated using PVA:EC (3:2) displayed highest in vitro release after 12?h in phosphate buffer (pH 6.8) that fitted matrix model. Selected nanosponge was formulated as Carbopol 934 NF hydrogel using varying concentrations of permeation enhancers propylene glycol and N-methyl-2-pyrrolidone. The EN nanosponge-loaded hydrogels (F0?F7) were evaluated for pharmacotechnical properties and irritation studies on rat skin. On the basis of various evaluation parameters F7 with an equilibrium swelling of 0.944?g/g after 4?h, low firmness and high adhesiveness, a flux rate of 1540.2 (?g/cm(2).h) and that exhibited a controlled release of EN for 12?h was selected as best hydrogel. The DRS and DSC spectra of F7 confirmed stability of drug in the delivery system and absence of drug polymer interaction in nanosponges.
本研究旨在探索将聚合纳米海绵作为一种替代载体,通过局部水凝胶制剂将硝酸益康唑(EN)靶向皮肤的可行性。采用乳化溶剂扩散法制备的纳米海绵,对其各种物理化学参数和体外药物释放进行了评价。EN 的纳米海绵是离散的自由流动的纳米尺寸颗粒,具有 SEM 观察到的穿孔桔皮样形态。在磷酸盐缓冲液(pH6.8)中,以 PVA:EC(3:2)为基础的纳米海绵在 12 小时后显示出最高的体外释放,符合基质模型。选择的纳米海绵用不同浓度的渗透促进剂丙二醇和 N-甲基-2-吡咯烷酮作为 Carbopol 934 NF 水凝胶进行配方。对载有 EN 的纳米海绵水凝胶(F0-F7)进行了药代动力学性质和大鼠皮肤刺激性研究。根据各种评价参数,F7 在 4 小时后达到 0.944?g/g 的平衡溶胀,硬度低、粘性高、通量为 1540.2 (?g/cm(2).h),并能在 12 小时内控制释放 EN,被选为最佳水凝胶。F7 的 DRS 和 DSC 图谱证实了药物在给药系统中的稳定性,以及纳米海绵中不存在药物-聚合物相互作用。