Preparation and quality evaluation of sempervir in echitosan thermosensitive microemulsion-based hydrogel
OBJECTIVE To optimize the formulation and evaluate the quality of sempervirine chitosan thermosensitive microemulsion-based hydrogel(SPV-CTMH).METHODS The formulation of SPV-TMH was optimized by combining single-factor experiments with central composite design-response surface method using gelling temperature as an index.Franz dif-fusion cell method was utilized for examining mucosal permeation profile and cytotoxicity of SPV-CTMH after adding chitosan at different concentrations for determining an appropriate concentration.Furthermore,appearance,pH,viscosity and mucosal per meation propenies of optimized SPV-CTMH were examined.RESULTS The optimal formulation of SPV-TMH contained 4.21％(W/V)for poloxamer 188 and 16.92％(W/V)for poloxamer 407.With the addition of not less than 0.2％chitosan,mucosal permeation of the drug improved markedly and there was a greater inhibition of U251 cell proliferation.Therefore 0.2％chitosan was selected as an optimal formulation.The prepared SPV-CTMH contained(1.099±0.001)mg·mL-1 of drug with a pH of(6.03±0.05),a zeta potential of(24.09±1.37)mV and a particle size of(32.7±1.9)nm.SPV-CTMH demonstrated a smooth flow before gelation and marked increases in both viscosity after gelation and mucous membrane permeation of semper-virine.CONCLUSION The prepared SPV-CTMH has desirable characteristics and its application for nasal drug delivery is expected to enhance the therapeutic efficacy.
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