Microemulsion-Based Mucoadhesive Buccal Wafers: Wafer Formation, In Vitro Release, and Ex Vivo Evaluation

AAPS PharmSciTech. 2017 Oct;18(7):2727-2736. doi: 10.1208/s12249-017-0754-9. Epub 2017 Mar 15.

Abstract

Microemulsion has the potentials to enhance dissolution as well as facilitate absorption and permeation of poorly water-soluble drugs through biological membranes. However, its application to govern a controlled release buccal delivery for local treatment has not been discovered. The aim of this study is to develop microemulsion-based mucoadhesive wafers for buccal delivery based on an incorporation of the microemulsion with mucoadhesive agents and mannitol. Ratio of oil to surfactant to water in the microemulsion significantly impacted quality of the wafers. Furthermore, the combination of carbopol and mannitol played a key role in forming the desired buccal wafers. The addition of an extra 50% of water to the formulation was suitable for wafer formation by freeze-drying, which affected the appearance and distribution of carbopol in the wafers. The amount of carbopol was critical for the enhancement of mucoadhesive properties and the sustained drug release patterns. Release study presented a significant improvement of the drug release profile following sustained release for 6 h. Ex vivo mucoadhesive studies provided decisive evidence to the increased retention time of wafers along with the increased carbopol content. The success of this study indicates an encouraging strategy to formulate a controlled drug delivery system by incorporating microemulsions into mucoadhesive wafers.

Keywords: buccal wafer; freeze-drying; microemulsion; mucoadhesive.

MeSH terms

  • Administration, Buccal
  • Animals
  • Delayed-Action Preparations
  • Drug Delivery Systems*
  • Drug Liberation*
  • Emulsions
  • Mouth Mucosa / metabolism*
  • Solubility
  • Swine

Substances

  • Delayed-Action Preparations
  • Emulsions