Optimization and physicochemical characterization of thermosensitive poloxamer gel containing puerarin for ophthalmic use.

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Qi H, Li L, Huang C, Li W, Wu C

Optimization and physicochemical characterization of thermosensitive poloxamer gel containing puerarin for ophthalmic use.

Chem Pharm Bull (Tokyo). 2006 Nov;54(11):1500-7.

PubMed ID
17077546 [ View in PubMed
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Abstract

The purpose of this study was to systematically optimize an ophthalmic thermosensitive poloxamer analogs gel containing puerarin that was a free flowing liquid below the room temperature and could shift to a gel with an eligible gel strength and bioadhesive force in physiological condition (dilution by the simulated tear fluid and at 35.0 degrees C). A two-factor, five-level central composite design (CCD) was employed to the optimization procedure. The effect of formulation variables (the w/v concentration of poloxamer 407 (X1) and poloxamer 188 (X2)) on a number of response variables (the gelation temperature before (Y1) and after (Y2) the simulated tear fluid diluted, the difference between them (Y3)) was systemically investigated. A second order polynomial equation was fitted to the data. The resulting equation and response surface plots were used to predict the responses in the optimal region. Finally, 21.0% (w/v) poloxamer 407 and 5.0% (w/v) poloxamer188 were chosen as the optimal poloxamer gel matrix. The influence of the other ingredients on the physicochemical properties of the formulation was also investigated. Hydroxypropyl-beta-cyclodextrin (HPCD) enhanced the gelation temperature and reduced the gel strength and the bioadhesive force, while puerarin and benzalkonium chloride (BC) had a comparatively smaller influence. All the isotonicity agents studied had the gelation temperatures lowered, and the gel strengths and the bioadhesive forces enhanced. But only sodium chloride appears to be a promising isotonicity agent for the poloxamer gel containing puerarin, HPCD and BC.

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