Formulation Development of Albendazole-Loaded Self-Microemulsifying Chewable Tablets to Enhance Dissolution and Bioavailability

• Published in: Pharmaceutics Vol. 11; no. 3; p. 134
• Main Authors: Sawatdee, Somchai, Atipairin, Apichart, Sae Yoon, Attawadee, Srichana, Teerapol, Changsan, Narumon, Suwandecha, Tan
• Format: Journal Article
• Language: English
• Published: Switzerland MDPI AG 20.03.2019; MDPI
• Subjects: albendazole; Bioavailability; chewable tablet; dissolution; Drug delivery systems; Drug dosages; Lactose; Microemulsions; Oral administration; Particle size; pharmacokinetics; self-microemulsion; Surfactants; Vegetable oils; Vortices; Thailand; United States > US; Bangkok Thailand; pharmacokinetics; self-microemulsion; albendazole; bioavailability; chewable tablet; dissolution
• ISSN: 1999-4923; 1999-4923
• DOI: 10.3390/pharmaceutics11030134

Albendazole is an anthelmintic agent with poor solubility and absorption. We developed a chewable tablet (200 mg drug equivalent), containing a self-microemulsifying drug delivery system (SMEDDS), with oral disintegrating properties. The emulsion was developed using sesame and soybean oils along with surfactant/co-surfactants, and the tablets were prepared by wet granulation using superdisintegrants and adsorbents. Infra-red (IR) spectral studies revealed no interaction between the drug and excipients, and all physical and chemical parameters were within acceptable limits. Stability studies for the formulation indicated no significant change over time. An in vitro release study indicated 100% drug release within 30 min, and in vivo plasma concentrations indicated that the area under the curve (AUC) of albendazole in rats administered SMEDDS chewable tablets was significantly higher than in those administered commercial tablets or powder ( -value < 0.05). The systemic bioavailability of albendazole achieved through the SMEDDS tablets was 1.3 times higher than that achieved by the administration of comparable quantities of albendazole commercial tablets. This was due to the higher dissolution of albendazole SMEDDS in the chewable tablets. We conclude that the SMEDDS chewable formulation can be used to improve the dissolution and systemic availability of poorly water-soluble drugs.