Synthesis and Statistical Optimization of Poly (Lactic-Co-Glycolic Acid) Nanoparticles Encapsulating GLP1 Analog Designed for Oral Delivery.
PURPOSE
To design and stabilize Liraglutide loaded poly (lactic-co-glycolic acid) nanoparticles (PLGA NPs) proper for oral administration.


METHODS
PLGA NPs were prepared by means of double emulsion solvent evaporation method and optimized by applying 7-factor 2-level Plackett-Burman screening design.


RESULTS
Spherical shaped NPs with homogeneous distribution, 188.95 nm particle size and 51.81% encapsulation efficiency were obtained. Liraglutide was successfully entrapped in the NPs while maintaining its native amorphous nature, and its structural integrity as well.


CONCLUSION
Lira-PLGA NPs with the required Critical Quality Attributes (CQAs) were successfully designed by implementing a 7-factor 8-run Plackett Burman design into the extended Quality by Design (QbD) model, to elucidate the effect of formulation and process variables on the particle size, size-distribution, encapsulation efficiency and surface charge. As the developed nanoparticles maintained the native structure of the active pharmaceutical ingredient (API), they are promising compositions for the further development for the oral delivery of Lira. Graphical Abstract.
['Ismail|Ruba|R|', 'Sovány|Tamás|T|', 'Gácsi|Attila|A|', 'Ambrus|Rita|R|', 'Katona|Gábor|G|', 'Imre|Norbert|N|', 'Csóka|Ildikó|I|']
D000284:Administration, Oral D004337:Drug Carriers D065546:Drug Liberation D004655:Emulsions D007004:Hypoglycemic Agents D000069450:Liraglutide D053758:Nanoparticles D010316:Particle Size D000077182:Polylactic Acid-Polyglycolic Acid Copolymer
oral delivery liraglutide plackett Burman design quality by design PLGA nanoparticles