Development of aqueous ternary nanomatrix films: A novel 'green' strategy for the delivery of poorly soluble drugs

作者：Kola Mustapha Adeola T; Armitage David; Abioye Amos Olusegun^*

来源：International Journal of Pharmaceutics, 2016, 515(1-2): 616-631.

DOI：10.1016/j.ijpharm.2016.11.017

• Aqueous nanomatrix film
• Controlled polymeric self-assembly
• Tuneable polymeric nanodomain
• Ternary nanoconjugate
• Green strategy for drug delivery
• Mechanism of drug release

Aqueous polymeric films have potentially great values in drug development, particularly in controlled drug release and taste masking strategies. However the progressive polymer-particle coalescence that occurs randomly during film formation, curing and storage may render the film less permeable leading to erratic and unpredictable drug release profile. The focus of this study was to investigate the impacts of the in situ formation of polymer-drug nanoconjugate, at the interfacial nano-domains of two oppositely charged polymers, on the mechanism of film formation and to prepare aqueous ternary polymer-drugpolymer nanomatrix films as a novel green strategy for the delivery of ibuprofen, a model poorly soluble drug. Composite and Layer-by-Layer films were prepared by aqueous casting technique using the concept of combined polymer-drug self-assembly and polyelectrolyte complexation. The plain and drug-loaded nanomatrix films were characterized using SEM, AFM, FTIR, DSC and TGA. Ibuprofen formed spherical core-shell microstructures (4.55-9.73 mu m) in gellan film. However in the presence of cationic dextran (Ddex), nanoconjugates (61.49 + 5.97-447.52 + 37.51 nm) were formed within the core of the film matrix. The composite films exhibited reduced tensile strength and lower elastic modulus with optimal conjugation efficiency of 98.14 +/- 1.19%, which correlates with higher dissolution efficiency (99.76%) compared to 47.37% in layer-by-layer (LbL) films, dictated by Ddex concentration. Generally, the mechanism of drug release was by Fickian diffusion, however anomalous transport or polymer relaxation was also observed at higher concentration of Ddex. This study demonstrated the potential application of aqueous drug-loaded nanomatrix films as controlled drug delivery strategy for ibuprofen, a model poorly soluble drug.

• 出版日期2016-12-30