Abstract

The controlled release of cyclosporine A (CsA) microencapsulated in alginate microbeads is a novel drug delivery system for the treatment of inflammatory diseases. In this study, CsA-loaded nanospheres encapsulated in alginate microbeads were applied to evaluate their controlled release profile and anti-inflammatory activity. Initially, a controlled-release drug delivery system was created by encapsulating CsA-loaded PLGA nanospheres within alginate microbeads. CsA-loaded PLGA nanospheres had a diameter of 418.70 ± 59.08 nm, a zeta potential of −22 ± 0.57 mV, and a polydispersity index of 0.517 ± 0.010. CsA-loaded nanosphere-encapsulated alginate microbeads were stable for 37 days. After encapsulating CsA-loaded PLGA nanospheres in the alginate microbeads, 5.60% of CsA was released after 24 h, and approximately 85.90% of the drugs were diffused until day 64. The cytotoxic and anti-inflammatory properties of the CsA released from the microbeads were evaluated in vitro using a murine macrophage cell line (RAW 264.7 cells). CsA-loaded nanosphere-encapsulated alginate microbeads inhibited 39.47 ± 1.71% of nitric oxide production from the RAW 264.7 cells on day 3, whereas nanosphere-encapsulated alginate microbeads inhibited 18.45 ± 1.56% only. CsA released from CsA-loaded nanosphere-encapsulated alginate microbeads had a RAW cell viability of 82.73 ± 5.58% on day 3 compared to 87.59 ± 0.69% of nanosphere-encapsulated alginate microbeads. The efficacy of the CsA-loaded nanosphere-encapsulated alginate microbeads in protecting the immune system via a controlled drug delivery system was established through anti-inflammatory and cell viability evaluation. Based on this research, the controlled release of CsA-loaded nanosphere-encapsulated alginate microbeads provides an innovative treatment for inflammatory diseases.