Development and evaluation of 1‐deoxynojirimycin sustained‐release delivery system: In vitro and in vivo characterization studies

Abstract We aimed to establish a 1‐Deoxynojirimycin (DNJ) sustained‐release delivery system to improve the hypoglycemic effect of DNJ. We used a transdermal diffusion meter in an in vitro orthogonal experiment to determine the optimal composition of the DNJ sustained‐release transdermal system. Based on the in vitro analysis results, a sustained‐release patch was prepared, and its pharmacokinetics and other properties were determined in vivo. The results showed that 30% hydroxypropyl methylcellulose (K 100M ), 14% carboxymethyl cellulose sodium and 26% oleic acid‐azone compound as the matrix material, drug excipient, and penetration enhancer, respectively, produced an optimal DNJ sustained‐release delivery system. In vitro release tests showed that the system slowly released DNJ within 12 hr, conforming to the Higuchi equation. In vivo experiments showed that the prepared patch had good hypoglycemic activity and continuously released DNJ within 10 hr. In vivo pharmacokinetic study results showed that compared to conventional patches, the prepared patch exhibited significantly different maximum concentration ( C max ), time to achieve C max ( T max ), and area under the curve from 0 to time t (AUC [0‐ t ] ) as well as improved pharmacokinetics. In conclusion, the prepared DNJ patch has high stability, a sustained‐release effect, and relatively good pharmacokinetics and is a safe dosage form that does not cause skin irritation.