Preparation of pH-Dependent and Enzyme-Triggered Baicalin Colon-Targeting Micropellets
Objective To prepare pH-dependent and enzyme-triggered baicalin colon-targeted micropellets and optimize the process prescription.Methods The target pellet yield and roundness were taken as comprehensive evaluation indicators,and the pellet preparation process was optimized by the orthogonal experiment.The cumulative in vitro release was taken as the evaluation indicator,and the Box-Behnken response surface methodology was used to optimize the coating process.Results The optimized process formula obtained by the orthogonal experiment was as follows:the dosage of baicalin was 18%,the ratio of microcrystalline cellulose to lactose was 5∶1,and the spheronization time was 5 minutes.The optimal coating process formula determined by Box-Behnken response surface methodology was:acrylic resinⅢ∶resistant starch RS3(2∶1),plasticizer dosage 17.1%,coating weight gain of 29.8%,and aging time of 1.6 hours.The samples prepared by the optimal process formula had a cumulative in vitro release rate of about 2.9%in artificial intestinal fluid(pH 6.8 phosphate buffer)and a cumulative in vitro release rate of about 93.0%in artificial colonic fluid(pH 7.6 phosphate buffer);the cumulative release in simulated intestinal fluid(containing trypsin)was 2.9%,and the cumulative release in simulated colonic fluid(prepared by 4%cecal content method)at 32h was 70.37%,proving that the microcapsules were pH-dependent and enzyme-triggered.Conclusion The orthogonal experiment combined with Box-Be-hnken response surface method can be used to prepare baicalin colon-targeted micropellets,and the optimal micropellets are pH-dependent and enzyme-triggered.
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