Modulation of Entrapment Efficiency and In Vitro Release Properties of BSA-Loaded Chitosan Microparticles Cross-Linked with Citric Acid as a Potential Protein–Drug Delivery System

Materials

卷:13

Natalia Sedyakina¹  Sergey Lutsenko¹  Nataliya Feldman¹  Kelly Velonia²  Andrey Kuskov³  Grigory Avramenko³ 

[1] Department of Biotechnology, I.M. Sechenov First Moscow State Medical University (Sechenov University), Moscow 119991, Russia;

[2] Department of Materials Science and Technology, University of Crete, 70013 Heraklion, Greece;

[3] Department of Technology of Chemical Pharmaceutical and Cosmetic Substances, D. Mendeleev University of Chemical Technology of Russia, Moscow 125047, Russia;

关键词: chitosan microparticles;    citric acid;    cross-linker;    polyglycerol polyricinoleate;    controlled release;    protein delivery;   

DOI  :  10.3390/ma13081989

来源: DOAJ

【 摘 要 】

Microparticles, aimed for oral protein and peptide drug delivery, were prepared via emulsion cross-linking using citric acid as cross-linker and polyglycerol polyricinoleate as surfactant. A comparative study of the interaction between chitosan and citric acid and its effect on the resulting microparticle properties was performed using different chitosan-to-cross-linker mass ratios and pH-values during fabrication of the microparticles. Non-cross-linked and cross-linked microparticles were studied in terms of size (4–12 μm), zeta potential (−15.7 to 12.8 mV), erosion (39.7–75.6%), a model protein encapsulation efficiency (bovine serum albumin) (6.8–27.6%), and loading capacity (10.4–40%). Fourier transform infrared spectroscopy and X-ray diffraction confirmed the ionic interaction between the protonated amine groups of chitosan and the carboxylate ions of the cross-linking agent. Scanning electron microscopy revealed that the non-cross-linked microparticles had an uneven shape with wrinkled surfaces, while the cross-linked formulations were spherical in shape with smooth surfaces. On the basis of these data, the role of the surfactant and microparticle structure on the release mechanism was proposed. Control of the microparticle shape and release mechanisms is expected to be crucial in developing carriers for the controlled delivery of proteins and peptides.

【 授权许可】

Unknown