Preparation and characterization of PEG-coated silica nanoparticles for oral insulin delivery

Author(s):Show less -

Andreani, Tatiana ^{[1, 2, 3]} ; de Souza, Ana Luiza R. ^[4] ; Kiill, Charlene P. ^[4] ; Lorenzon, Esteban N. ^[5] ; Fangueiro, Joana F. ^{[3, 6]} ; Cristina Calpena, Ana ^[7] ; Chaud, Marco V. ^[8] ; Garcia, Maria L. ^[9] ; Gremiao, Maria Palmira D. ^[4] ; Silva, Amelia M. ^{[1, 2]} ; Souto, Eliana B. ^{[3, 6, 10]}

Affiliation

^[1] Univ Tras Os Montes & Alto Douro, Dept Biol & Environm, UTAD, P-5001801 Vila Real - Portugal

^[2] UTAD, Ctr Res & Technol Agroenvironm & Biol Sci CITAB, Vila Real - Portugal

^[3] Fernando Pessoa Univ UFP, Res Ctr Biomed CEBIMED, P-4249004 Oporto - Portugal

^[4] Univ Estadual Paulista, Dept Pharmaceut Sci, UNESP, Sao Paulo - Brazil

^[5] Univ Estadual Paulista, Inst Chem, UNESP, Dept Biochem & Chem Technol, Sao Paulo - Brazil

^[6] Fernando Pessoa Univ, Fac Hlth Sci, P-4200150 Oporto - Portugal

^[7] Univ Barcelona, Sch Pharm, Pharm & Pharmaceut Technol Dept, Biopharm & Pharmacokicet Unit, Barcelona 8028 - Spain

^[8] Sorocaba Univ, UNISO, BR-18023000 Sorocaba - Brazil

^[9] Univ Barcelona, Fac Pharm, Dept Phys Chem, Barcelona 8028 - Spain

^[10] UTAD, Ctr Genom & Biotechnol, Inst Biotechnol & Bioengn, Vila Real - Portugal

• Document type: Journal article
• Source: International Journal of Pharmaceutics; v. 473, n. 1-2, p. 627-635, OCT 1 2014.
• Web of Science Citations: 35

Abstract

The present study reports the production and characterization of PEG-coated silica nanoparticles (SiNP-PEG) containing insulin for oral administration. High (PEG 20,000) and low (PEG 6000) PEG molecular weights were used in the preparations. SiNP were produced by sol gel technology followed by PEG adsorption and characterized for in vitro release by Franz diffusion cells. In vitro permeation profile was assessed using everted rat intestine. HPLC method has been validated for the determination of insulin released and permeated. Insulin secondary structure was performed by circular dichroism (CD). Uncoated SiNP allowed slower insulin release in comparison to SiNP PEG. The coating with high molecular weight PEG did not significantly (p>0.05) alter insulin release. The slow insulin release is attributed to the affinity of insulin for silanol groups at silica surface. Drug release followed second order kinetics for uncoated and SiNP PEG at pH 2.0. On the other hand, at pH 6.8, the best fitting was first-order for SiNP PEG, except for SiNP which showed a Boltzmann behavior. Comparing the values of half-live, SiNP PEG 20,000 showed a faster diffusion followed by Si-PEG 6000 and SiNP. CD studies showed no conformational changes occurring after protein release from the nanoparticles under gastrointestinal simulated conditions. (C) 2014 Elsevier B.V. All rights reserved. (AU)

• FAPESP's process: 12/10174-3 - EVALUATION OF CHITOSAN NANOPARTICLES FOR DELIVERY OF POTENTIALLY ACTIVE INTEGRINS INHIBITORS IN GLIOBLASTOMAS
• Grantee: Charlene Priscila Kiill
• Support Opportunities: Scholarships in Brazil - Doctorate