Pharmaceutical Research

, Volume 30, Issue 1, pp 238–246

Electrospun Formulations Containing Crystalline Active Pharmaceutical Ingredients

Authors

  • Blair Kathryn Brettmann
    • Department of Chemical EngineeringMassachusetts Institute of Technology
  • Kamyu Cheng
    • Department of Chemical EngineeringMassachusetts Institute of Technology
  • Allan S. Myerson
    • Department of Chemical EngineeringMassachusetts Institute of Technology
    • Department of Chemical EngineeringMassachusetts Institute of Technology
Research Paper

DOI: 10.1007/s11095-012-0868-4

Cite this article as:
Brettmann, B.K., Cheng, K., Myerson, A.S. et al. Pharm Res (2013) 30: 238. doi:10.1007/s11095-012-0868-4

ABSTRACT

Purpose

To investigate the use of electrospinning for forming solid dispersions containing crystalline active pharmaceutical ingredients (API) and understand the relevant properties of the resulting materials.

Method

Free surface electrospinning was used to prepare nanofiber mats of poly(vinyl pyrrolidone) (PVP) and crystalline albendazole (ABZ) or famotidine (FAM) from a suspension of the drug crystals in a polymer solution. SEM and DSC were used to characterize the dispersion, XRD was used to determine the crystalline polymorph, and dissolution studies were performed to determine the influence of the preparation method on the dissolution rate.

Results

The electrospun fibers contained 31 wt% ABZ and 26 wt% FAM for the 1:2 ABZ:PVP and 1:2 FAM:PVP formulations, respectively, and both APIs retained their crystalline polymorphs throughout processing. The crystals had an average size of about 10 μm and were well-dispersed throughout the fibers, resulting in a higher dissolution rate for electrospun tablets than for powder tablets.

Conclusions

Previously used to produce amorphous formulations, electrospinning has now been demonstrated to be a viable option for producing fibers containing crystalline API. Due to the dispersion of the crystals in the polymer, tablets made from the fiber mats may also exhibit improved dissolution properties over traditional powder compression.

KEY WORDS

crystalselectrospinningformulationsolid dispersion

ABBREVIATIONS

ABZ

albendazole

API

active pharmaceutical ingredient

DSC

differential scanning calorimetry

FAM

famotidine

PVP

poly(vinyl pyrrolidone)

SEM

scanning electron microscopy

XRD

X-ray diffraction

A

surface area for diffusion

C

concentration in solution

Csat

solubility

D

diffusion coefficient

\( \frac{{dm}}{{dt}} \)

dissolution rate

g

gravitational acceleration

h

diffusional path length

ρf

density of the fluid

ρp

density of the particle

R

radius of the particle

μ

viscosity of the fluid

vs

settling velocity

Copyright information

© Springer Science+Business Media, LLC 2012