Drug Discov Ther. 2018;12(3):142-153. (DOI: 10.5582/ddt.2018.01017)

D-cycloserine nasal formulation development for anxiety disorders by using polymeric gels.

Shin Y, Kokate R, Desai V, Bhushan A, Kaushal G


D-cycloserine (DCS), a partial agonist at N-methyl-D-aspartate (NMDA) receptors, is used as an enhancer of exposure therapy for anxiety disorders. The purpose of the present study was to investigate the feasibility of using polymeric gels to increase the viscosity of the formulation and thereby increase the nasal residence time and sustained release of DCS in vitro. Hydroxypropyl methylcellulose (HPMC), hydroxypropyl cellulose (HPC), and methyl cellulose (MC) were prepared at concentrations of 0.5 to 5% w/v. Pluronic F-127 (PF-127) was prepared at concentrations of 15 to 35% w/v. pH, viscosity and in vitro DCS release behavior of the formulated gels were analyzed. All four gels that were tested, demonstrated sustained DCS release behavior over a 24-hour period, but with different rates. Based on the results of this study, HPMC, HPC, MC, and PF-127 are capable of increasing the viscosity of nasal gel formulations and of releasing DCS in sustained manner. Therefore, these polymeric gels can be suitable carriers for DCS nasal gel formulation.

KEYWORDS: D-cycloserine, polymeric gels, hydroxypropyl methyl cellulose, hydroxypropyl cellulose, methylcellulose, Pluronic F-127

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