
Poly(glycerol sebacate) nanoparticles for ocular delivery of sunitinib: physicochemical, cytotoxic and allergic studies
Author(s) -
Chegini Sana Pirmardvand,
Varshosaz Jaleh,
Sadeghi Hamid Mirmohammad,
Dehghani Alireza,
Minayian Mohsen
Publication year - 2019
Publication title -
iet nanobiotechnology
Language(s) - English
Resource type - Journals
ISSN - 1751-875X
DOI - 10.1049/iet-nbt.2019.0002
Subject(s) - zeta potential , nanoparticle , biocompatibility , nuclear chemistry , sebacic acid , particle size , drug delivery , chemistry , cytotoxicity , hela , materials science , nanotechnology , polymer chemistry , organic chemistry , in vitro , biochemistry
Poly(glycerol sebacate) (PGS) is a new biodegradable polymer with good biocompatibility used in many fields of biomedicine and drug delivery. Sunitinib‐loaded PGS/gelatine nanoparticles were prepared by the de‐solvation method for retinal delivery and treatment of diabetic retinopathy. The nanoparticles were characterised by Fourier‐transform infrared and differential scanning calorimetry. The effects of different formulation variables including drug‐to‐carrier ratio, gelatine‐to‐PGS ratio, and glycerine‐to‐sebacate ratio were assessed on the encapsulation efficiency (EE%), particle size, release efficiency (RE), and zeta potential of the nanoparticles. The in vitro cytotoxicity of PGS/gelatine nanoparticles was studied on L929 cells. Draize test on rabbit eyes was also done to investigate the possible allergic reactions caused by the polymer. Glycerine/sebacic acid was the most effective parameter on the EE and RE. Gelatine‐to‐PGS ratio had the most considerable effect on the particle size while the RE was more affected by the glycerine/sebacic acid ratio. The optimised formulation (S 1 G 0.7 D 21.2 ) exhibited a particle size of 282 nm, 34.6% EE, zeta potential of −8.9 mV, and RE% of about 27.3% for drug over 228 h. The 3‐(4,5‐dimethylthuazol‐2‐yl)‐2,5‐diphenyltetrazolium bromide assay indicated PGS/gelatine nanoparticles were not cytotoxic and sunitinib‐loaded nanoparticles were not toxic at concentrations <36 nM.