Nanocarrier-based topical drug delivery for an antifungal drug
Nanocarrier-based topical drug delivery for an antifungal drug
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DOI：
10.3109/03639045.2013.771647
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发表时间：
2014-04-01
影响因子：
3.4
通讯作者：
Ahmed, Farhan Jalees
中科院分区：
文献类型：
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作者：
Hussain, Afzal;Samad, Abdus;Ahmed, Farhan Jalees
目的：传统的脂质体两性霉素 B 会引起许多不良副作用，如血液紊乱、肾毒性、剂量依赖性副作用、口服吸收高度可变以及制剂相关的不稳定性。本研究的目的是开发具有成本效益的纳米乳液作为纳米载体，以增强和持续地将两性霉素 B 输送到皮肤中。方法和表征：通过自发滴定法改变亲水性 (Tween (R) 80) 表面活性剂和辅助表面活性剂的组成，开发了不同的水包油纳米乳液。对开发的制剂进行了表征、优化、评估，并与商业制剂（真菌体 0.01% w/w）的皮肤渗透性进行了比较。根据三元相图，使用不同浓度的表面活性剂和助表面活性剂筛选负载两性霉素 B 的优化制剂。结果与讨论：优化制剂 F-I、F-III 和 F-VI 获得的最大透光率百分比分别为 96.9 +/- 1.0%、95.9 +/- 3.0% 和 93.7 +/- 1.2%。对这些优化的纳米乳液进行热力学稳定性研究，以获得最稳定的纳米乳液（F-I）。最终优化的纳米乳液 F-I 的粒径和 zeta 电位值为 67.32 +/- 0.8 nm 和 -3.7 +/- 1.2mV，具有透明度和稳定的纳米乳液，具有更好的皮肤渗透性。对于 F-I，观察到制剂的稳态透皮通量在 5.89 +/- 2.06 和 18.02 +/- 4.3 mu g/cm(2)/h 之间，而最大增强率分别比真菌体和药物溶液高 1.85 倍和 3.0 倍。皮肤沉积研究结果表明，优化的纳米乳F-I可沉积231.37+/-3.6μg/cm(2)的药物，与真菌体相比，增强率高2.11倍。还尝试了优化的表面活性剂和助表面活性剂组合介导的药物通过皮肤的转运，结果显示促进了药物渗透和皮肤扰动 (SEM)。结论：综合结果表明，两性霉素 B 纳米乳可能是局部局部药物递送的更好选择，并且作为一种有效、高效和安全的方法具有更大的潜力。
Objective: The conventional liposomal amphotericin B causes many unwanted side effects like blood disorder, nephrotoxicity, dose-dependent side effects, highly variable oral absorption and formulation-related instability. The objective of the present investigation was to develop cost-effective nanoemulsion as nanocarreir for enhanced and sustained delivery of amphotericin B into the skin.Methods and characterizations: Different oil-in-water nanoemulsions were developed by varying the composition of hydrophilic (Tween (R) 80) surfactants and co-surfactant by the spontaneous titration method. The developed formulation were characterized, optimized, evaluated and compared for the skin permeation with commercial formulation (fungisome 0.01% w/w). Optimized formulations loaded with amphotericin B were screened using varied concentrations of surfactants and co-surfactants as decided by the ternary phase diagram.Results and discussion: The maximum % transmittance obtained were 96.9 +/- 1.0%, 95.9 +/- 3.0% and 93.7 +/- 1.2% for the optimized formulations F-I, F-III and F-VI, respectively. These optimized nanoemulsions were subjected to thermodynamic stability study to get the most stable nanoemulsions (F-I). The results of the particle size and zeta potential value were found to be 67.32 +/- 0.8 nm and -3.7 +/- 1.2mV for the final optimized nanoemulsion F-I supporting transparency and stable nanoemulsion for better skin permeation. The steady state transdermal flux for the formulations was observed between 5.89 +/- 2.06 and 18.02 +/- 4.3 mu g/cm(2)/h whereas the maximum enhancement ratio were found 1.85- and 3.0-fold higher than fungisome and drug solution, respectively, for F-I. The results of the skin deposition study suggests that 231.37 +/- 3.6 mu g/cm(2) drug deposited from optimized nanoemulsion F-I and 2.11-fold higher enhancement ratio as compared to fungisome. Optimized surfactants and co-surfactant combination-mediated transport of the drug through the skin was also tried and the results were shown to have facilitated drug permeation and skin perturbation (SEM).Conclusion: The combined results suggested that amphotericin B nanoemulsion could be a better option for localized topical drug delivery and have greater potential as an effective, efficient and safe approach.