Pharmacy Department, Faculty of Technology & Engineering, The Maharaja Sayajirao University of Baroda, Kalabhavan, Vadodara 390001, Gujarat State, India.
Pharmacy Department, Faculty of Technology & Engineering, The Maharaja Sayajirao University of Baroda, Kalabhavan, Vadodara 390001, Gujarat State, India.
Colloids Surf B Biointerfaces. 2014 Apr 1;116:351-8. doi: 10.1016/j.colsurfb.2014.01.014. Epub 2014 Jan 19.
The present studies were designed to develop a microemulsion (ME) formulation of Amphotericin B (Amp B) for the treatment of invasive fungal infections. The oil phase was selected on the basis of drug solubility whereas the surfactant and co-surfactant were screened and selected on the basis of their oil solubilizing capacity as well as their efficiency to form ME. Pseudo-ternary phase diagrams were constructed and on the basis of ME existence ranges various formulations of Amp B were developed. The influence of surfactant and co-surfactant mass ratio (Smix) on the ME formation and permeation of ME through excised rat skin was studied. The optimized formulation (ME 7) consisting of 0.1% (w/w) Amp B, 5% (w/w) Isopropyl Myristate and 35% (w/w) Smix (3:1, Tween 80 and Propylene glycol), has shown a globule size of 84.20 ± 2.13 nm, a polydispersity index of 0.164 ± 0.031, pH 7.36 ± 0.02 and conductance of 229.3 ± 1.95 μS. ME 7 exhibited 2-fold higher drug permeation as compared to plain drug solution. Besides this, the formulation was also evaluated for drug content, stability, skin retention, skin sensitivity and anti-fungal activity. In vitro anti-fungal activity in Trichophyton rubrum fungal species have shown that ME7 has higher zone of inhibition and the formulation was found stable at 2-8°C and at room temperature (25 ± 2°C) for the period of three months. The results indicate that, the investigated ME may be used as a promising alternative for Amp B therapy.
本研究旨在开发一种两性霉素 B（Amp B）的微乳（ME）制剂，用于治疗侵袭性真菌感染。油相是根据药物溶解度选择的，而表面活性剂和助表面活性剂则是根据其油溶性以及形成 ME 的效率进行筛选和选择的。构建了伪三元相图，并根据 ME 的存在范围开发了各种 Amp B 制剂。研究了表面活性剂和助表面活性剂质量比（Smix）对 ME 形成以及 ME 通过大鼠离体皮肤渗透的影响。由 0.1%（w/w）Amp B、5%（w/w）肉豆蔻异丙酯和 35%（w/w）Smix（3:1，吐温 80 和丙二醇）组成的优化制剂（ME7），其粒径为 84.20 ± 2.13nm，多分散指数为 0.164 ± 0.031，pH 值为 7.36 ± 0.02，电导率为 229.3 ± 1.95μS。与普通药物溶液相比，ME7 的药物渗透提高了 2 倍。此外，还对该制剂的药物含量、稳定性、皮肤滞留、皮肤敏感性和抗真菌活性进行了评价。在体外抗红色毛癣菌真菌物种中的抗真菌活性表明，ME7 具有更高的抑菌区，并且该制剂在 2-8°C 和室温（25±2°C）下在三个月的时间内保持稳定。结果表明，所研究的 ME 可能作为 Amp B 治疗的一种有前途的替代方法。
