Caffeic Acid-PLGA Conjugate to Design Protein Drug Delivery Systems Stable to Irradiation

Journal of Functional Biomaterials

Francesca Selmin¹  Francesco Puoci²  Ortensia I. Parisi²  Silvia Franzé¹  Umberto M. Musazzi¹  Francesco Cilurzo¹ 

[1] Università degli Studi di Milano, Department of Pharmaceutical Sciences—via Giuseppe Colombo, 71-20133 Milano, Italy; E-Mails:;Università degli Studi della Calabria, Department of Pharmacy, Health and Nutritional Sciences, 87036 Arcavacata di Rende, Italy; E-Mails:

关键词: anti-oxidant;    microencapsulation;    drug release;    caffeic acid;    grafting;    γ-irradiation;    microspheres;    ovalbumin;    poly(lactide-co-glycolide);    sterilization;   

DOI  :  10.3390/jfb6010001

来源: mdpi

【 摘 要 】

This work reports the feasibility of caffeic acid grafted PLGA (g-CA-PLGA) to design biodegradable sterile microspheres for the delivery of proteins. Ovalbumin (OVA) was selected as model compound because of its sensitiveness of γ-radiation. The adopted grafting procedure allowed us to obtain a material with good free radical scavenging properties, without a significant modification of M_w and T_g of the starting PLGA (M_{w PLGA} = 26.3 ± 1.3 kDa vs. M_{w g-CA-PLGA} = 22.8 ± 0.7 kDa; T_{g PLGA} = 47.7 ± 0.8 °C vs. T_{g g-CA-PLGA} = 47.4 ± 0.2 °C). By using a W₁/O/W₂ technique, g-CA-PLGA improved the encapsulation efficiency (EE), suggesting that the presence of caffeic residues improved the compatibility between components (EE_PLGA = 35.0% ± 0.7% vs. EE_g-CA-PLGA = 95.6% ± 2.7%). Microspheres particle size distribution ranged from 15 to 50 µm. The zeta-potential values of placebo and loaded microspheres were −25 mV and −15 mV, respectively. The irradiation of g-CA-PLGA at the dose of 25 kGy caused a less than 1% variation of M_w and the degradation patterns of the non-irradiated and irradiated microspheres were superimposable. The OVA content in g-CA-PLGA microspheres decreased to a lower extent with respect to PLGA microspheres. These results suggest that g-CA-PLGA is a promising biodegradable material to microencapsulate biological drugs.

【 授权许可】

CC BY   
© 2015 by the authors; licensee MDPI, Basel, Switzerland.