Title:
Development of a Mucoadhesive Sublingual Spray of Palonosetron Hydrochloride: A Patient-Friendly Approach to Chemotherapy-Induced Nausea and Vomiting

Authors:
Ms Bhakti Shah*, Dr. Jingnesh Modi, India

Abstract:

Chemotherapy-induced nausea and vomiting (CINV) is a common complication of cancer therapy, and rapid-onset antiemetic drug delivery may improve therapeutic convenience. Palonosetron hydrochloride (PAL HCl), a potent 5-HT3 receptor antagonist with a prolonged half-life, was formulated as a mucoadhesive sublingual spray to facilitate rapid drug release and transmucosal permeation while reducing gastrointestinal exposure.

The spray formulations were prepared by a simple mixing method using trimethyl chitosan (TMC) as a mucoadhesive and permeation-enhancing polymer, with propylene glycol (PG) and PEG-400 as formulation variables. Nine formulations (F1–F9) were prepared using a 3² full factorial design and evaluated for physicochemical characteristics, spray performance, drug release, and ex-vivo permeation. The optimized formulation, F1, exhibited clear appearance, pH 6.2 ± 0.1, drug content of 99.4 ± 0.5%, viscosity of 20 ± 2 cP, uniform spray pattern, droplet size of 60 ± 2 µm, and mucoadhesion time of 90 ± 5 min. F1 showed 88.9% cumulative drug release at 10 min and 98.6% at 60 min.

The cumulative drug permeation of F1 was 79.6% at 60 min. In the ex-vivo permeation study, cumulative permeation increased from 42.96 ± 1.12% at 10 min to 81.45 ± 1.28% at 60 min. The findings demonstrate that the developed TMC-based PAL HCl sublingual spray exhibited satisfactory formulation characteristics, rapid drug release, and enhanced ex-vivo permeation.

DOI: http://dx.doi.org/10.51505/ijmshr.2026.10506