Poly(glycerol sebacate) nanoparticles for ocular delivery of sunitinib: physicochemical,cytotoxic and allergic studies |
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| Authors: | Sana Pirmardvand Chegini Jaleh Varshosaz Hamid Mirmohammad Sadeghi Alireza Dehghani Mohsen Minayian |
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| Affiliation: | 1. Department of Pharmaceutics, Faculty of Pharmacy and Novel Drug Delivery Systems Research Centre, Isfahan University of Medical Sciences, Isfahan Iran ; 2. Department of Pharmaceutical Biotechnology, Faculty of Pharmacy, Isfahan University of Medical Sciences, Isfahan Iran ; 3. School of Medicine, Isfahan Eye Research Centre, Isfahan University of Medical Sciences, Isfahan Iran ; 4. Department of Pharmacology, Faculty of Pharmacy, Isfahan University of Medical Sciences, Isfahan Iran |
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| Abstract: | 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 (S1 G0.7 D21.2) 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.Inspec keywords: polymers, differential scanning calorimetry, toxicology, drug delivery systems, solvation, eye, encapsulation, particle size, drugs, biodegradable materials, nanofabrication, nanomedicine, nanoparticles, gelatin, Fourier transform infrared spectraOther keywords: gelatine‐to‐PGS ratio, glycerine‐to‐sebacate ratio, particle size, zeta potential, sunitinib‐loaded nanoparticles, biodegradable polymer, retinal delivery, differential scanning calorimetry, drug‐to‐carrier ratio, allergic reactions, physicochemistry, cytotoxicity, poly(glycerol sebacate) nanoparticles, sunitinib ocular delivery, drug delivery, sunitinib‐loaded PGS‐gelatine nanoparticles, Fourier‐transform, in vitro cytotoxicity, biocompatibility, Draize test, rabbit eyes, 3‐(4,5‐dimethylthuazol‐2‐yl)‐2,5‐diphenyltetrazolium bromide assay |
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