Montelukast sodium (MS) as an anti-inflammatory agent in asthma requires a drug delivery system to sustain release at specific doses. ZIF-8 commonly used in drug delivery systems due to its low cytotoxicity and biodegradability was functionalized with 3-aminopropyltrimethoxysilane (APTES) as a carrier (ZIF-8@APTES) for MS. The particles were characterized with Field emission scanning electron microscopy (FE-SEM), Fourier transform infrared (FTIR), X-ray diffraction (XRD), BrunauerEmmett-Teller (BET) method, and thermogravimetric analysis (TGA). Furthermore, the biocompatibility of ZIF-8@APTES-MS on a normal murine cell line (L929) and its antioxidant activity were investigated. The results showed that MS was gradually released from ZIF-8@APTES-MS in phosphate buffer solution (pH 7.4) over 6 hours. ZIF-8@APTES and ZIF-8@APTES-MS also had good biocompatibility properties, and significantly (P� 0.05) enhanced total antioxidant activity at high doses (32 μg/ mL). In conclusion ZIF-8@APTES-MS can be a promising drug delivery system for MS