Fabrication of tri-layered electrospun polycaprolactone mats with improved sustained drug release profile

S Manjunath Kamath,S Padmapriya,V Gopinath,B K Mohamed Ibrahim,A Sundaram,Nilkantha Gupta,P Sivaperumal,D Jaison,S Shantanu Patil,K Sridhar

doi:10.1038/s41598-020-74885-1

Abstract

Modulation of initial burst and long term release from electrospun fibrous mats can be achieved by sandwiching the drug loaded mats between hydrophobic layers of fibrous polycaprolactone (PCL). Ibuprofen (IBU) loaded PCL fibrous mats (12% PCL-IBU) were sandwiched between fibrous polycaprolactone layers during the process of electrospinning, by varying the polymer concentrations (10% (w/v), 12% (w/v)) and volume of coat (1 ml, 2 ml) in flanking layers. Consequently, 12% PCL-IBU (without sandwich layer) showed burst release of 66.43% on day 1 and cumulative release (%) of 86.08% at the end of 62 days. Whereas, sandwich groups, especially 12% PCLSW-1 & 2 (sandwich layers—1 ml and 2 ml of 12% PCL) showed controlled initial burst and cumulative (%) release compared to 12% PCL-IBU. Moreover, crystallinity (%) and hydrophobicity of the sandwich models imparted control on ibuprofen release from fibrous mats. Further, assay for cytotoxicity and scanning electron microscopic images of cell seeded mats after 5 days showed the mats were not cytotoxic. Nuclear Magnetic Resonance spectroscopic analysis revealed weak interaction between ibuprofen and PCL in nanofibers which favors the release of ibuprofen. These data imply that concentration and volume of coat in flanking layer imparts tighter control on initial burst and long term release of ibuprofen.

Highlights

ObjectivesThe major objective of the present work are as follows (i) electrospinning of fibers eluting IBU flanked between PCL fibers for sustained and prolonged release of IBU during the process of electrospinning
Earlier reports suggest the importance of crystallinity (%) of polymer in drug release modulation patterns[34,40,50] by virtue of its highly arranged crystalites barricading the peneteration of aqueous medium. These results suggest that initial burst and long term sustained release of IBU are tightly controlled by concentration and volume of PCL coat in the flanking layers as reported e arlier[26]
X-Ray Diffraction (XRD) results confirmed that lipophilic drug IBU was amorphized during fabrication process which eventually enhanced the dissolution properties

Summary

Objectives

The major objective of the present work are as follows (i) electrospinning of fibers eluting IBU flanked between PCL fibers for sustained and prolonged release of IBU during the process of electrospinning. (ii) Physicochemical characterization to study chemical changes during fabrication. (iii) Cumulative(%) release and drug release kinetics evaluation.

Results

Discussion

Conclusion