α-Linolenic acid-modified pluronic 127-CS copolymeric micelles for the skin targeted delivery of amphotericin B,New Journal of Chemistry

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α-Linolenic acid-modified pluronic 127-CS copolymeric micelles for the skin targeted delivery of amphotericin B
New Journal of Chemistry ( IF 2.7 ) Pub Date : 2018-11-20 00:00:00 , DOI: 10.1039/c8nj03847c
Feilong Zhou _{1,

2,

3,

4} , Hongmei Xu _{1,

2,

3,

4} , Zhimei Song _{1,

2,

3,

4} , Li Zhu _{1,

2,

3,

4} , Sijia Feng _{4,

5,

6,

7} , Runliang Feng _{1,

2,

3,

4}

Affiliation

In this study, an α-linolenic acid modified pluronic F127-block-chitosan (F127-(CS-LNA)₂) copolymer was synthesized to prepare topical amphotericin B (AMB)-loaded micelles (AMB-M) via a dialysis technique. The drug encapsulation efficiency, particle size and zeta potential of AMB-M were 97.26 ± 2.85%, 140.00 ± 0.36 nm and 7.00 ± 0.54 mV, respectively. Characterization of AMB-M by Fourier transform infrared spectroscopy and powder X-ray diffraction revealed the presence of an interaction between AMB and the copolymer, and that AMB was present in AMB-M without any crystallization. AMB-M exhibited in vitro antifungal activity comparable to that of a commercial AMB injection (AMB-I), although it showed a slower AMB release than that of AMB-I. AMB-M showed a 310-fold increase in the drug skin deposition and better in vivo activity against a fungal infection of the skin as compared to commercial AMB liposomal gel, a topical formulation, which shows no AMB penetration through the skin. In addition, AMB-M showed inconspicuous skin irritation, and was stable at 4 °C for 30 days. In conclusion, F127-(CS-LNA)₂ may be a promising and safe drug delivery vehicle for AMB in the treatment of topical skin fungal infections.

中文翻译：

α-亚麻酸修饰的普卢尼克127-CS共聚胶束，用于两性霉素B的皮肤靶向递送

在这项研究中，合成了一种α-亚麻酸修饰的普卢尼克F127-嵌段-壳聚糖（F127-（CS-LNA）₂）共聚物，通过透析技术制备了负载有两性霉素B（AMB）的胶束（AMB-M）。AMB-M的药物包封效率，粒径和Zeta电位分别为97.26±2.85％，140.00±0.36 nm和7.00±0.54 mV。通过傅立叶变换红外光谱和粉末X射线衍射对AMB-M进行表征，揭示了AMB与共聚物之间存在相互作用，并且AMB存在于AMB-M中而没有任何结晶。AMB-M在体外展示其抗真菌活性与市售AMB-1相当，尽管它显示出的AMB释放速度比AMB-1慢。与市售AMB脂质体凝胶（一种局部制剂）相比，AMB-M的药物皮肤沉积增加了310倍，并且对皮肤的真菌感染的体内活性更高，后者没有AMB穿透皮肤。另外，AMB-M表现出不起眼的皮肤刺激，并在4°C下稳定30天。总之，F127-（CS-LNA）₂可能是AMB用于治疗局部皮肤真菌感染的有前途和安全的药物输送工具。

更新日期：2018-11-20

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