Abstract
Background. Betamethasone as a corticosteroid drug is commonly used for the treatment of rheumatoid arthritis. Unfortunately, betamethasone is a low water-soluble drug and its efficacy is low. So an attractive strategy is the targeted delivery of betamethasone to the damaged joint using polymeric micelle-based carriers. Methods. Inulin-grafted stearate (In-g-St) was synthesized via the reaction of stearoyl chloride and inulin, then characterized by FT-IR and H-NMR. In-g-St forms micelles in the presence of betamethasone. The prepared polymeric micelles were characterized for size, zeta potential, drug loading, particles’ morphology, critical micelle concentration (CMC), and encapsulation efficiency. So sustained release polymeric micelles of betamethasone were developed by employing In-g-St. Results. The measurement of particle size showed a mean diameter of 60 and 130 nm for 10% and 20% drug-loaded micelles, respectively, and SEM showed that the particle’s morphologies are spherical. Zeta potential measurement for the drug-containing micelles showed a value of -11.8 mV. Drug loading efficiency and the encapsulation efficiency were 6.36% and 63.6%, as well as 18.97% and 94.88% for 10% and 20%, respectively. 20% drug-loaded polymer showed a small burst release of betamethasone at the first 3 h which was followed by sustained release in the next 24 h. Furthermore, the formula with 10% exhibited good sustained release properties except for the minor initial burst release. Conclusion. Data from the zeta potential, CMC, drug loading capacity, and in vitro drug release studies indicated that In-g-St polymeric micelles can be suitable candidates for the efficient delivery of hydrophobic drugs like betamethasone.
Highlights
Rheumatoid arthritis (RA), as one of the autoimmune and chronic inflammatory diseases, has affected approximately 1% of the world’s population [1]
Compared to the inulin spectrum, a new weak band in 1737 cm-1 was assigned to the carbonyl group of an ester, which confirmed the grafting of the stearate group to the inulin via an esterification reaction
We synthesized a novel derivative of inulin via the reaction of stearoyl chloride and inulin
Summary
Rheumatoid arthritis (RA), as one of the autoimmune and chronic inflammatory diseases, has affected approximately 1% of the world’s population [1]. Early diagnosis and treatment strategies that are based on glucocorticoids and nonsteroidal anti-inflammatory drugs could improve the RA patient’s quality of life [3]. Glucocorticoids or corticosteroids such as prednisone prednisolone, dexamethasone, and betamethasone as synthetic compounds similar to cortisol hormone can help to reduce the inflammation, stiffness, and pain of the swollen joints [4]. The prepared polymeric micelles were characterized for size, zeta potential, drug loading, particles’ morphology, critical micelle concentration (CMC), and encapsulation efficiency. Data from the zeta potential, CMC, drug loading capacity, and in vitro drug release studies indicated that In-g-St polymeric micelles can be suitable candidates for the efficient delivery of hydrophobic drugs like betamethasone
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