口服可生物降解的姜黄素纳米颗粒在糖尿病患者持续治疗方案中的体内外相关性

IF 0.2 Q4 PHARMACOLOGY & PHARMACY Asian Journal of Pharmaceutical Research and Health Care Pub Date : 2023-04-01 DOI:10.4103/ajprhc.ajprhc_46_23
K. Shailaja, K. Senthilkumaran, Ubaidulla Uthumansha
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引用次数: 0

摘要

背景:姜黄素(Curcumin, CUR)具有治疗糖尿病的潜力,但其低口服生物利用度使其难以用于慢性疾病的治疗。目的:探讨口服可生物降解CUR纳米颗粒(NPs)在糖尿病患者持续治疗方案中的体内外相关性(IVIVC)。材料与方法:本研究采用Box-Behnken设计,对聚合物的浓度和工艺参数进行优化,制备了CUR可生物降解NPs。结果:采用Box-Behenken法,在聚合物质量分数为2.5% w/v、TPP质量分数为3% w/v、搅拌转速为2534 rpm的条件下,制备出最佳配方,实际反应粒径为192.31±6.82 nm,包封效率为84.26±2.87%,释药量(Q24 h)为95.22±1.81%,期望函数为0.910,表明该模型有效。与普通CUR相比,口服CUR- nps具有更长的Tmax、更高的Cmax、更大的AUC和更大的MRT。通过绘制CUR- nps的吸收百分比与溶解百分比的曲线,得到了IVIVC模型线性回归图(R2= 0.9949)。为了证明体内吸收和体外释放之间的关系,我们建立了ivivc。结论:从结果可以看出,这种新型的cur负载NPs具有提高其治疗效果的潜力。
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In vitro‒in vivo correlation of oral biodegradable curcumin nanoparticles for sustained treatment regimen of diabetics
Background: Curcumin (CUR) has the potential to treat diabetes, but its low oral bioavailability makes it challenging to use in the treatment of chronic conditions. Objectives: To investigate in vitro–in vivo correlation (IVIVC) of oral biodegradable CUR nanoparticles (NPs) for sustained treatment regimen of diabetics. Materials and Methods: In this study, CUR biodegradable NPs were prepared using Box–Behnken design to optimize the concentration of polymer and process parameters. Results: The optimized formulation was prepared using the values obtained from the Box-Behenken method, 2.5 %w/v of polymer, 3 % w/v of TPP, and 2534 rpm of stirring speed and the actual response was observed 192.31±6.82 nm particle size, 84.26±2.87 % of entrapment efficiency, and 95.22±1.81 % of drug release (Q24 h) with the desirability function of 0.910 which indicated that the model is valid. In vitro release of curcumin from nanoparticles showed prolonged drug release up to 24 h. CUR-NPs administered orally were found to have longer Tmax, higher Cmax, larger AUC, and larger MRT compared to plain CUR. IVIVC model linear regression plots (R2= 0.9949) were obtained by plotting the graph with percent absorbed versus percent dissolved for CUR-NPs. IVIVCs were established for demonstrating the relationship between in vivo absorption and in vitro release. Conclusions: From the results, it can be concluded that this novel CUR-loaded NPs have potential to improve its therapeutic efficacy.
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