Abstract
Although glucocorticoids are highly effective in treating various types of inflammation such as skin disease, rheumatic disease, and allergic disease, their application have been seriously limited for their high incidence of side effects, particularly in long term treatment. To improve efficacy and reduce side effects, we encapsulated betamethasone phosphate (BSP) into biocompatible red blood cells (RBCs) and explored its long acting-effect. BSP was loaded into rat autologous erythrocytes by hypotonic preswelling method, and the loading amount was about 2.5 mg/mL cells. In vitro, BSP loaded RBCs (BSP-RBCs) presented similar morphology, osmotic fragility to native RBCs (NRBCs). After the loading process, the loaded cells can maintain around 70% of Na+/K+-ATPase activity of natural cells. In vivo, a series of tests including survival, pharmacokinetics, and anti-inflammatory effect were carried out to examine the long-acting effect of BSP-RBCs. The results shown that the loaded cells could circulate in plasma for over nine days, the release of BSP can last for over seven days and the anti-inflammatory effect can still be observed on day 5 after injection. Totally, BSP-loaded autologous erythrocytes seem to be a promising sustained releasing delivery system with long anti-inflammatory effect.
Highlights
Glucocorticoids are one kind of the most effective drugs for treating various inflammation such as skin disease, rheumatic disease, and allergic disease
The loading amount of the prepared betamethasone phosphate (BSP)-Red blood cells (RBCs) was about 2.5 mg/mL cells, which was promising for the treatment of inflammatory [30]. 1 mL cells were collected from 2–3 mL whole blood by centrifuging at 600× g for 5 min
Betamethasone phosphate was successfully loaded into autologous erythrocytes by hypotonic preswelling method, thephosphate loading amount about 2.5 loaded mg/mL into cells. autologous
Summary
Glucocorticoids are one kind of the most effective drugs for treating various inflammation such as skin disease, rheumatic disease, and allergic disease. Their system applications should be used only when necessary and in as low a dose as possible for their high incidence of adverse effects, in long term treatment. Betamethasone is a kind of classic glucocorticoids which plays an important role in controlling many inflammations. To prolong the release of betamethasone phosphate (BSP), the administration of drug encapsulated in biodegradable polymeric particles has been investigated. Ishihara et al [5] firstly developed betamethasone disodium 21-phosphate (BP) encapsulated in nanoparticles of poly(D,L-lactic acid (PLA)) homopolymers, which had strong anti-inflammatory activity. Other nanoparticles for BSP loading include poly(D,L-lactic/glycolic acid) (PLGA) nanoparticle, and polyethylene glycol
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