Self-assembled liposome from core-sheath chitosan-based fibres for buccal delivery of carvedilol: formulation, characterization and in vitro and ex vivo buccal absorption

Objectives: A novel drug delivery system based on self-assembled liposome from core-sheath nanofibres for buccal delivery of Carvedilol (Car) was explored.

Methods: The Car-loaded PVP/PC (phospholipids) layer was coated with chitosan-PVA (CS-PVA) or CS-PVP to increase retention period in the mouth. SEM, confocal laser scanning microscopy (CLSM), XRD and Fourier transform infrared spectroscopy were applied to characterize fibre diameter and drug state. Appearance, particle size and encapsulation efficiency of self-assembled liposome were investigated by transmission electron microscopy (TEM) and Zeta-sizer Nano. The dissolution test and permeation tests across porcine buccal mucosa and TR146 cell model also were run.

Key findings: Confocal laser scanning microscopy and XRD confirmed the core-sheath structure of coaxial fibre and non-crystalline form of Car, separately. TEM demonstrated the sphere morphology of self-assembled liposome from spun fibres after contacting water. The dissolution test implied the ratio of PC to Car had a huge impact on drug release. The permeation tests across porcine buccal mucosa and TR146 cell model showed similar result, namely our formulation having a better permeation performance than Car suspension. The indirect toxicity against TR146 cells presented 5 mg/ml (or lower) of fibre extraction was safe for cells.

Conclusions: These researches exhibited this drug delivery system was promising and advantageous for Car buccal delivery.