Pharmaceutica Analytica Acta

A case study on tuning drug release dynamics facilitated by polymer surfactant interaction in microemulsion in-situ nasal gel

5^th International Conference and Exhibition on Pharmaceutics & Novel Drug Delivery Systems

March 16-18, 2015 Crowne Plaza, Dubai, UAE

Mukesh Sharma1, Atindra Shukla1, Vidhi Shah2, Radhika Pandya2, Rajesh K Parikh2 and B N Suhagia1

Posters & Accepted Abstracts: Pharm Anal Acta

Abstract:

Present work highlights a strategy to develop microemulsion based in situ nasal gel (MEG) to entrap Lorazepam (BCS II) for the treatment of various CNS diseases using Capmul MCM-in water media. The interaction between PBC 34 and Gellan gum with Carbopol in water was studied as a function of surfactant concentration. Pseudo-ternary phase diagrams were constructed and various formulations of Lorazepam were developed accordingly. Gellan gum and carbopol 934 P were used to decrease mucocilliary clearance of formulation. 32 factorial design was constructed using ratio of oil to surfactant/cosurfactant concentration (X1) and concentration of gellan gum (X2) as independent variables and their effect on response Y1 (drug release at 6 hrs) and Y2 (viscosity) were studied. The derived polynomial equation and contour graph aid in predicting the values of selected independent variables for optimization of MEG with desired properties. Carbopol dispersions showed a continuous decrease in transmittance, viscosity and mucoadhesive property when surfactant concentration were increased. The developed formulation showed no toxicity to goat nasal mucosa, which proves that it is safe for intranasal delivery for brain targeting. It is proposed that the surfactant-polymer interactions in form of a stoichiometric hydrogen bonding between oxyethylene and carboxylic groups of the polymers used, provides exceptional ME stability and adhesion properties. MEG showed higher flux and permeation across goat nasal mucosa. Pharmacodynamic activities were carried out and compared with marketed product, which showed superior performance. The investigated ME based in situ nasal gel could be a promising alternative for existing CNS therapies.