Abstract

The aim of the present study was to prepare mucoadhesive nasal gels from mucilage isolated from seeds of Linum usitatissimum L. containing midazolam hydrochloride. Characterization of the isolated mucoadhesive agent was carried out, including determination of pH, swelling property, viscosity and mucoadhesive strength. The results were compared with synthetic polymers (HPMC and carbopol 934). Nasal gels of midazolam were prepared with and without enhancers and the permeation study was carried out using excised goat nasal mucosa. Permeation profiles were evaluated and histological study of nasal mucosae before and after permeation study was also conducted to determine histological change, if any.

Highlights

  • Nasal drug delivery system has emerged to be an important area in the field of pharmaceutical research

  • The nasal mucosa being a highly vascularised area helps in rapid systemic absorption of the drug, thereby avoiding hepatic “first-pass effect” of drugs leading to quicker onset of action, which could be especially important in the management of crisis situations like cardiac arrest, epileptic seizures, severe nausea and vomiting [1,2,3]

  • The mucoadhesive agents make intimate contact with the mucin of mucosa, thereby, prolonging residence time of the drug in nasal cavity enhancing the period of contact with nasal mucosa, which may improve drug absorption [1,2,3,4]

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Summary

Introduction

Nasal drug delivery system has emerged to be an important area in the field of pharmaceutical research. Rapid mucociliary clearance of drug formulations is an important factor that is responsible for the underlying low bioavailability of drugs administered via nasal route [2,3,4,5,6]. To overcome this problem, a platform for drug delivery is required which can be effectively provided by mucoadhesive gels. Midazolam hydrochloride (8-chloro-6-(2-fluorophenyl)-1-methyl-4H-imidazo[1,5-a][1,4]benzodiazepine hydrochloride) is a potent water soluble benzodiazepine [7] It has powerful anxiolytic, amnestic, hypnotic, anticonvulsant, skeletal muscle relaxant and sedative properties [8]. Mucoadhesive material extracted from Linum usitatissimum L. seeds was used in the formulation because of its edibility, biodegradability and biocompatibility [12]

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