Preparation, development and in vitro release evaluation of amphotericin B-loaded amphiphilic block copolymer vectors

作者：Pippa Natassa; Mariaki Maria; Pispas Stergios; Demetzos Costas^*

来源：International Journal of Pharmaceutics, 2014, 473(1-2): 80-86.

DOI：10.1016/j.ijpharm.2014.07.001

• Amphiphilic block copolymer
• Amphotericin B
• Self-assembly
• Morphology
• Drug release

The aim of this work is to design and develop a suitable polymeric formulation incorporating amphotericin B (Ampho B) in order to overcome its water insolubility problem. To this end, we have chosen the poly(isoprene-b-ethylene oxide) amphiphilic block copolymer (IEO) family. We investigate the self assembly behavior and the stability kinetics of IEO copolymer based nanostructures formed in HPLC grade water and in phosphate buffer saline (PBS). The IEO block copolymer samples investigated have different molecular weights and compositions. A gamut of light scattering techniques (static, dynamic and electrophoretic) were used in order to extract information on the size, zeta-potential and morphological characteristics of the structures formed, as a function of the molar ratio of incorporated lipophilic drug Ampho B. The amphiphilic character and the colloidal stability of the particular polymeric drug vectors indicate that these nanostructures can be utilized as effective containers for the particular hydrophobic drug. The incorporation of Ampho B led to alteration of the physicochemical and morphological characteristics of the pure polymeric carriers. It is observed that the in vitro release of Ampho B from the prepared vectors IEO-b:Ampho B was quite slow, while the IEO-a carriers did not release Ampho B.

• 出版日期2014-10-1