PLA/PEG-b-PLA particles: Promising peptide carriers

CHEVALIER, MERARI*; GARCÍA, MÓNICA C* (*SHARED FIRST AUTHORSHIP); GONZALEZ, DANIELA; JIMENEZ-KAIRUZ, ALVARO; ALVAREZ, VERA

Granada

Conferencia; XI Spanish-Portuguese Conference on Controlled Drug Delivery ?Revolutionary Approaches in Nanomedicine Development; 2016

Introduction: The last decade has seen significant technological progress in the development of new pharmaceutical platforms in order to improve the current available pharmacotherapy. In particular, therapeutically effective and patient-compliant drug delivery systems continuously lead researchers to design novel tools and strategies.The primary method of accomplishing drug controlled release has been through incorporating the actives within polymers. Particularly, polymeric micro and nanoparticles as carrier can be made from a wide variety of natural and synthetic polymers. Due to particle?s ability to improve the pharmacotherapy treatment, such devices are being extensively studied and used as drug carriers and controlled release systems in the field of biomaterials, medicine and pharmacy. Considering polylactic acid capability for high loading drugs and its ability to modulate drug release, this work attempts to study the physicochemical and biopharmaceutical properties of PLA/PEG-b-PLA polylisine particulated carriers.Materials and Methods: Microparticles were obtained by a proprietary electrohydrodynamic technology (Bio-Target Inc., Chigaco, IL, USA; LNK Chemsolutions LLC, Lincoln, Nebraska, USA). Briefly, a organic solution containing all the necessary components were processed using this technology resulting in a dry collection of the specified microparticles. The particles were characterized by scanning electron microscopy (SEM), thermo gravimetric analysis (TGA), differential scanning calorimetry (DSC), and Fourier transform infrared spectroscopy (FTIR). UV-Vis spectrophotometry was used to determine the encapsulation efficiency (EE) of the obtained system. The polylisine release from particles was performed in a bi-compartimental diffusion device (Franz´s cells) mounted with a semi synthetic cellulose membrane. The donor compartment was filled with 0.5 mL of particles dispersed in 1% BSA in PBS and kept in contact with 16 mL of receptor medium at 37 °C. Ringer solution was used as receptor media. Samples of 1.0 mL of receptor medium were withdrawn at predetermined time intervals and replaced with equal quantities of fresh medium. The amount of drug released was determined by high performance liquid chromatography (HPLC).Results and Discussion: The results obtained showed that the particles exhibit thermal stability. The TGA showed a thermal decomposition of the particles at 275 °C. The DSC showed an endothermic event at 58 ° C attributed to the glass transition temperature of PLA. There are not differences in the thermal analysis between particles loaded with polylisine and control. The particles have a high percentage of polylisine loaded; the EE calculations yielded a value of 81 %. Conclusions: The properties of these particles are encouraging for the design of controlled release systems for peptides that could improve existing therapies in the field of health.References:[1]Tiwari, G., Tiwari, R., Sriwastawa, B., Bhati, L., Pandey, S., Pandey, P., & Bannerjee, S. K. (2012). Drug delivery systems: An updated review. International Journal of Pharmaceutical Investigation, 2(1), 2-11. doi: 10.4103/2230-973X.96920