Two types of core/shell fibers based on carboxymethyl chitosan and Sodium carboxymethyl cellulose with self-assembled liposome for buccal delivery of carvedilol across TR146 cell culture and porcine buccal mucosa.

Abstract

Two novel core-shell fibers which could self-assemble liposome were fabricated based on bioadhesive polymer carboxymethyl chitosan (CMCS) and Sodium carboxymethyl cellulose (CMC-Na), separately. The shell layers were CMCS/PVA and CMC-Na/PVA, respectively, and the core layer was mixture of PVP, Phospholipids (PC) and Carvedilol (Car). The diameter distribution and core/shell structure were examined by SEM and CLSM. FTIR and XRD were also used to characterize the fiber. Self-assembled liposome was observed by TEM, and other parameters like drug encapsulation efficiency was also determined. In vitro adhesive force was conducted to evaluate bioadhesive property of fibers. Dissolution test demonstrated Car was almost completely released within 2 h and presented linear release. The permeation studies across porcine TR146 cell culture and buccal mucosa were carried out, indicating self-assembled liposome and bioadhesive polymer both promoted drug penetration. MTT test showed TR146 cells were safe after incubation with fibers' extraction medium under the concentration of 10 mg/mL. In summary, this design based on self-assembled liposome and core/shell fiber using water-soluble bioadhesive polymer was desirable for Car buccal absorption.