Stable formulation of protein-type drug in electrospun polymeric fiber followed by tableting and scaling-up experiments

Suitability of electrospinning for biodrug formulation was investigated in order to develop an electrospinning‐based method for producing oral dosage form of β‐galactosidase. β‐Galactosidase‐loaded polymeric (polyvinyl alcohol, polyvinylpyrrolidones with two different molar masses, and polyethylene glycol) nanofibers were prepared by electrospinning in order to lengthen the shelf life of the enzyme (providing an alternative technology to drying). Based on the activity of the encapsulated β‐galactosidase, the most suitable polymer was polyvinylpyrrolidone with higher molecular weight (1,200,000 Da), because 97% of the original activity remained in this case. Kinetic behavior of β‐galactosidase did not show any alteration after encapsulation, and the pH and temperature profiles were not changed either. Time course of viability testing showed that the nanofibrous formulation can provide long‐term stability for β‐galactosidase; the activity of the enzyme decreased only 4% after a year. Furthermore, scaling‐up and tableting had no influence on activity and long‐term stability; thus, the developed drying technology and tablets, containing enzyme‐loaded nanofibers, can provide a new promising way of oral biodrug delivery. Copyright © 2015 John Wiley & Sons, Ltd.