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Formulation of Hydrophilic Non-Aqueous Gel: Drug Stability in Different Solvents and Rheological Behavior of Gel Matrices

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Abstract

Purpose

This study was aimed at formulating a hydrophilic non-aqueous gel for topical delivery of the model moisture-sensitive drug, minocycline hydrochloride (MH).

Methods

Stability study of MH dissolved in water and various hydrophilic non-aqueous solvents was performed over a period of four months in order to select a suitable non-aqueous solvent for MH gel. To improve MH stability, the effect of different cation additives on MH stability in the selected solvent was investigated. Non-aqueous gel matrices were prepared from three different types of hydrophilic polymers in glycerin-propylene glycol mixture with Mg2+ cation additive. Oscillatory shear rheometry was performed on the gel matrices using a cone-and-plate rheometer.

Results

MH stability was affected by the type of solvent employed and the duration of storage. Different cation additives affected the extent of MH stabilization through MH-cation complex formation. Rheological properties of the non-aqueous gel matrices were significantly affected by the type and concentration of polymer, and the vehicle ratios in the formulations.

Conclusions

MH stabilization could be achieved using the selected glycerin-propylene glycol mixture containing MgCl2. Gel matrix formulated using this solvent system and 3%w/w N-vinylacetamide/sodium acrylate copolymer had demonstrated the most favorable rheological properties as a gel for topical application.

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Author notes

  1. Keat Theng Chow

    Present address: Division of Pharmaceutics, College of Pharmacy, The University of Texas at Austin, 1 University Station, Mailstop A1920, Austin, Texas, 78712, USA

Authors and Affiliations

  1. Department of Pharmacy, Faculty of Science, National University of Singapore, 18 Science Drive 4, Singapore, 117543, Singapore

    Keat Theng Chow, Lai Wah Chan & Paul W. S. Heng

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Correspondence to Paul W. S. Heng.

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Chow, K.T., Chan, L.W. & Heng, P.W.S. Formulation of Hydrophilic Non-Aqueous Gel: Drug Stability in Different Solvents and Rheological Behavior of Gel Matrices. Pharm Res 25, 207–217 (2008). https://doi.org/10.1007/s11095-007-9457-3

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