十六烷基磷脂酰胆碱复合聚ε-己内酯电纺微球的制备及表征

Preparation and Characterizations of Hexadecyl Phosphatidyl Choline Hybrided Poly ε- caprolactone Electrospun Microspheres

目的用静电纺技术制备载表面活性剂型药物十六烷基磷脂酰胆碱的聚ε-己内酯微球并对其进行初步表征。方法将十六烷基磷脂酰胆碱、聚ε-己内酯和胆固醇共同溶解在二氯甲烷-乙酸-四氢呋喃混合溶剂中形成均相溶液后静电纺。将纺得物冻干后扫描电子显微镜进行形态观察,图形软件评价其粒度及分布。广角X-射线、差示热分析及热重分析考察十六烷基磷脂酰胆碱在微球中的存在状态。结果可由十六烷基磷脂酰胆碱、胆固醇与聚ε-己内酯所组成的溶液体系电纺得到微球,药物本身载量的增高和胆固醇的添加使得微球球形度变差。扫描电子显微镜下观察到小球周长<10μm和纤维直径<500 nm的珠串状微球-纤维复合体系。广角X-射线衍射和热分析可知十六烷基磷脂酰胆碱与聚ε-己内酯结合良好。结论静电纺有可能作为一种新的制备微球的理想方法进行开发。

Objective To prepare and characterize poly ε- caprolactone microsphere with surfactant loaded drug hexadecyl phosphatidyl choline. Methods Hexadecyl phosphatidyl choline,poly ε- caprolactone and cholesterol were co- dissolved in dichloromethane- acetic acid- tetrahydrofuran solution to obtain homogeneous solution that was sequently electrospun. The products were freeze- dried and observed morphologically by scanning electron microscope. Particle sizes and distribution were evaluated by graphics software. Hexadecyl phosphatidyl choline existing state in mirosphere was evaluated by wide angle X- ray diffraction,differential scanning calorimetry and thermogravimetric analysis. Results Microspheres could be obtained by electrospinning from Hexadecyl phosphatidyl choline,poly ε- caprolactone and cholesterol in organic solution. The addtion of hexadecyl phosphatidyl choline and the increase of cholesterol made the sphere not as round as only small amount of hexadecyl phosphatidyl choline. Under scanning electron microscope,beads- linked- by- fibers complexed system of microsphere- fiber could be observed with microsphere circumference 10 μm and fiber diameter 〈500 nm. Wide angle X- ray diffraction and thermo- analysis indicated that hexadecyl phosphatidyl choline integrated well with poly ε- caprolactone. Conclusion Electrospinning may be developed as a novel desirable method for preparing microsphere.