Synthesis and Statistical Optimization of Poly (Lactic-Co-Glycolic Acid) Nanoparticles Encapsulating GLP1 Analog Designed for Oral Delivery

• Published in: Pharmaceutical research Vol. 36; no. 7; pp. 99 - 16
• Main Authors: Ismail, Ruba, Sovány, Tamás, Gácsi, Attila, Ambrus, Rita, Katona, Gábor, Imre, Norbert, Csóka, Ildikó
• Format: Journal Article
• Language: English
• Published: New York Springer US 01-07-2019; Springer; Springer Nature B.V
• Subjects: Analysis; Biochemistry; Biomedical and Life Sciences; Biomedical Engineering and Bioengineering; Biomedicine; Design; Encapsulation; Evaporation; Glycolic acid; Liraglutide; Medical Law; Nanoparticles; Optimization; Oral administration; Particle size; Pharmacology/Toxicology; Pharmacy; Polylactide-co-glycolide; Research Paper; Surface charge; liraglutide; quality by design; plackett Burman design; PLGA nanoparticles; oral delivery
• ISSN: 0724-8741; 1573-904X
• DOI: 10.1007/s11095-019-2620-9

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