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

Abstract

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 coresheath 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.Core-sheath fiber for buccal permeation Jianting Chen et al.

Intranasal Delivery of Carvedilol- and Quercetin-Encapsulated Cationic Nanoliposomes for Cardiovascular Targeting: Formulation and In Vitro and Ex Vivo Studies

“…7 Similar outcomes were also reported by Chen et al, where peaks were observed at 3350 cm −1 representing O−H or N−H stretching, 1606, 1589, and 1501 cm −1 for C�C aromatic stretching, and 1253 and 1099 cm −1 stretching of aliphatic−aromatic ether C−O. 55 The IR spectra of QC show characteristic peaks at 3343 cm −1 (−OH stretching) with a transmittance of 90.17%, and 2879 cm −1 with a % transmittance of 84.11%, and 1651 cm −1 (bending in ketone and C�O bands) at transmittance of 89.98%, which were observed to retain in the IR spectra of physical mixtures X 3 and X 4 and in the optimized nasal gel CVD/QC-L.O.F. (16.25%w/v) as well.…”

“…reported similar IR peaks of CVD at 3345 cm –1 for N–H and O–H stretching, with 3059 and 2994 cm –1 representing aromatic C–H stretching, 2848 cm –1 for methyl C–H stretching, 1590 cm –1 representing N–H bending, 1505 cm –1 for aromatic CC stretching, 1254 and 1099 cm –1 representing aliphatic–aromatic ether C–O stretching, 1212.31 cm –1 for C–N stretching, and 718 and 753 cm –1 for out-of-plane C–H bending . Similar outcomes were also reported by Chen et al., where peaks were observed at 3350 cm –1 representing O–H or N–H stretching, 1606, 1589, and 1501 cm –1 for CC aromatic stretching, and 1253 and 1099 cm –1 stretching of aliphatic–aromatic ether C–O . The IR spectra of QC show characteristic peaks at 3343 cm –1 (−OH stretching) with a transmittance of 90.17%, and 2879 cm –1 with a % transmittance of 84.11%, and 1651 cm –1 (bending in ketone and CO bands) at transmittance of 89.98%, which were observed to retain in the IR spectra of physical mixtures X 3 and X 4 and in the optimized nasal gel CVD/QC-L.O.F.…”

Development, Characterization, and Ex Vivo Assessment of Elastic Liposomes for Enhancing the Buccal Delivery of Insulin

“…Herein, we selected the porcine buccal tissue owing to its morphology, which is consistent with that of the human buccal cheek [29]. Porcine buccal tissue is widely used as an ex vivo model to study the transbuccal permeation of drugs [45,46]. Figure 5 shows the buccal permeability profiles of the insulin-loaded elastic liposomes (SC-EL and SGDC-EL), and the combination of insulin and surfactants (insulin + SC and insulin + SGDC).…”

Bitterness-masking assessment of luteolin encapsulated in whey protein isolate-coated liposomes

“…This indicated that the crystal morphology of uncoated liposomes was a blend of crystalline and amorphous forms. 51 This blended form significantly reduced the bitterness of luteolin.…”