Development and Characterization of Mucoadhesive In Situ Nasal Gel of Midazolam Prepared with Ficus carica Mucilage
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The objective of the present study was to prepare mucoadhesive in situ nasal gels with mucilage isolated from fig fruits (Ficus carica, family: Moraceae) containing midazolam hydrochloride. Nasal gels of midazolam were prepared using three different concentrations (0.5%, 1.0% and 1.5% w/v) of F. carica mucilage (FCM) and synthetic polymers (hydroxypropylmethyl cellulose and Carbopol 934). Evaluation of FCM showed that it was as safe as the synthetic polymers for nasal administration. In situ gels were prepared with mixture Pluronic F127 and mucoadhesive agents. Evaluation of the prepared gels was carried out, including determination of viscosity, texture profile analysis and mucoadhesive strength. In vitro drug permeation study was conducted with the gels prepared with and without permeation enhancer (0.5% w/v sodium taurocholate) using excised goat nasal mucosa. In vitro permeation profiles were evaluated, and histological study of nasal mucosae before and after permeation study was also conducted to determine histological change, if any. In vivo experiments conducted in rabbits further confirmed that in situ nasal gels provided better bioavailability of midazolam than the gels prepared from synthetic mucoadhesive polymers. It was observed that the nasal gel containing 0.5% FCM and 0.5% sodium taurocholate exhibited appropriate rheological, mechanical and mucoadhesive properties and showed better drug release profiles. Moreover, this formulation produced no damage to the nasal mucosa that was used for the permeation study, and absolute bioavailability was also higher compared to gels prepared from synthetic polymers.
KEY WORDSmidazolam hydrochloride mucoadhesive nasal permeation enhancer
The authors are grateful to AICTE National Doctoral Fellowship for providing financial assistance for carrying out the research work.
- 1.Wikipedia. The free encyclopedia. http://en.wikipedia.org/wiki/. Accessed 20 July 2007.
- 22.Miyazaki S, Takeuchi S, Yokouchi C, Takada M. Pluronic F-127 gels as a vehicle for topical administration of anticancer agents. Chem Pharm Bull. 1984;10:4205–8.Google Scholar
- 24.Majithiya RJ, Ghosh, PK, Umrethia ML, Murthy RS. Thermoreversible-mucoadhesive gel for nasal delivery of sumatriptan. AAPS PharmSciTech. 2006;7(3):Article 67.Google Scholar
- 26.Tease WB. Trease and Evans’ pharmacognosy. 15th ed. London: WB Saunders Company Ltd; 2002.Google Scholar
- 35.Tan YTF, Peh KK, Al-Hanbali O. Effect of Carbopol and polyvinylpyrrolidone on the mechanical, rheological and release properties of bioadhesive polyethylene glycol gels. AAPS PharmSciTech. 2000;1:Article 24.Google Scholar