Design and Characterization of Thermosensitive Mucoadhesive Nasal Gel for Meclizine Hydrochloride

Abstract

Background: The current study was to develop a thermoreversible nasal in-situ gel  for meclizine hydrochloride. As meclizine hydrochloride is water-insoluble and is  having a hepatic first-pass metabolism it becomes necessary to prepare a  formulation that will enhance the absorption of the drug and gives sustained action  in the body.   Method: The FT-IR and DSC study revealed that there was no incompatibility  between the drug and the excipient. The inclusion complex of meclizine  hydrochloride was prepared by employing Sulfobutyl-ether- β- Cyclodextrin  (SBEβCD) and then using this complex the thermoreversible gel was prepared by  using the cold method. The thermoreversible gel was prepared by incorporating  various types of polymers like Carrageenan, HPMC, carbopol-934, and Sodium  Alginate in different concentrations and was evaluated for the various evaluation  parameters to identify the optimized formulation from the batches B1-B8.   Result: From the prepared formulation B6 was found to be optimized as it was  having a higher drug concentration of 98.33±2.1547%, the mucoadhesive strength  of 28.98±1.5692 dyne/cm2 in B6 showed that more drug can be retained in the body  as compared with other formulations, more sustained release of drug was seen i.e.  87.42±1.4113% of drug release in 8 hours than compared with the other prepared  formulation. The kinetics study reveals peppas model was best fitted to the  optimized formulation with the regression coefficient of 0.9832. From the stability  study, it was concluded that the prepared formulation was stable during the full time study and does not change its property with time.   Conclusion: The concentration of polymers was a significant factor in the % drug  release in the formulation and also in the mucoadhesive strength of the  formulation. Hence, it was concluded that the prepared thermoreversible nasal in situ gel was a successful approach in increasing the drug absorption in the body.