Co-assembly of block copolymers as a tool for developing novel micellar carriers of insulin for controlled drug delivery. (July 2018)

• Record Type: Journal Article
• Authors: Kamenova, Katya; Haladjova, Emi; Grancharov, Georgy; Kyulavska, Mariya; Tzankova, Virginia; Aluani, Denitsa; Yoncheva, Krassimira; Pispas, Stergios; Petrov, Petar
• Is Part Of: European polymer journal. Volume 104(2018)
• Page Start: 1
• Page End: 9
• Publication Date: 2018-07
• Subjects: Block copolymers -- Mixed micelles -- Insulin -- Nanocarriers -- Drug delivery; Polymers -- Periodicals; Polymerization -- Periodicals; Polymères -- Périodiques; Polymérisation -- Périodiques; Polymerization; Polymers; Periodicals; Electronic journals; 547.705
• DOI: 10.1016/j.eurpolymj.2018.04.039
• Languages: English
• ISSNs: 0014-3057

Abstract

Graphical abstract: Highlights: Novel polymeric nanocarriers of insulin are developed by co-assembly approach. PDMAEMA short chains of mixed micellar corona form complex with insulin. Large PEO chains of mixed micellar corona provide superior solubility of carriers. Sustained release of insulin over the period of 24 h is achieved. Abstract: In this study the co-assembly of two amphiphilic block copolymers with tailored composition and molecular characteristics, poly(ethylene oxide)-poly(ε-caprolactone)-b-poly(ethylene oxide) (PEO113 -b-PCL35 -b-PEO113 ) and poly(2-(dimethylamino)ethyl methacrylate)-b-poly(ε-caprolactone)-b-poly(2-(dimethylamino)ethyl methacrylate) (PDMAEMA20 -b-PCL70 -b-PDMAEMA20 ), was employed for preparation of a novel micellar system for controlled delivery of insulin. Mixed block copolymer micelles (MBCMs) of three different compositions were prepared by blending the two copolymers at molar ratios of 7:3, 1:1 and 3:7. Next, the electrostatic complexation between insulin and MBCMs with a focus on particle size, morphology, zeta potential and colloid stability as a function of insulin concentration in the aqueous solution was investigated by dynamic and electrophoretic light scattering as well as atomic force microscopy. The properties of systems were proven to depend on MBCMs composition and protein concentration. In vitro cytotoxicity of blank and insulin-loaded carriers was assessed by standard MTT (3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide) test. The release profile of insulin from selected carriers in phosphate buffer (pH 7.4) was also studied.