Hyperbranched cellulose polyester of oral thin film and nanofiber for rapid release of donepezil; preparation and in vivo evaluation

Abstract

Cellulose blended hyperbranched polyester (CHP) and hyperbranched cellulose polyester (HPC) were synthesized by melt condensation method using 2,2-bis (methylol) propionic acid and p-TSA. Obtained polymers were utilized for the preparation of various donepezil loaded thinfilm (CHPF, HPCF) and nanofibers (CHPN, HPCN) using solvent casting and electrospinning technique respectively. Formulated thinfilms and nanofibers were subjected to thermal analysis and microscopic evaluations. Compared with thinfilm formulations, hyperbranched nanofiber has shown lower particle size about 50–100 nm. This might be helped in releasing 98% of drug in the span of 10 min in in vitro studies for HPCN 4 formulation. Further investigation of in vivo bioavailability studies, peak plasma concentration was observed at 3 to 3.5 h for HPCN formulation. Hyperbranched cellulose formulations (HPCN 4) have significantly higher absorption (AUC 0–∞) (1294.1 ± 5.4 ng/mL) than cellulose blended hyperbranched polymer formulations (876.1 ± 6.1 ng/mL). These studies revealed that the hyperbranched nanofiber formulations possess high mechanical strength and good drug release properties. Current study concludes prepared Hyperbranched cellulose nanofiber will be good alternative for commercially available dosage forms for the treatment of Alzheimer's diseases.