通过聚合物涂层制成的纳米胶体载体,用于口服异拉地平。

Vikash Kumar, Hema Chaudhary, Anjoo Kamboj
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摘要

我们的研究目标是开发、表征和优化稳定形式的纳米胶体载体,即 Eudragit 包覆的固体脂质纳米生物颗粒(SLNbp),用于口服给药异拉地平(ISR)。为了实现这一目标,在 ISR 和芦丁比例不变的情况下,采用响应面方法在三个水平(质量中心水平的 -1 和 +1 水平)上应用三个因子,即脂质与表面活性剂的比例(A,% w/w)、Eudragit L100(B,% w/w)和超声时间(C,分钟)来开发 SLNbp。构建了反应[R1、R2 和 R3;包埋效率(EE)、粒度和药物释放]的二阶多项式二次方程,并绘制了反应曲面(二维和三维)图。得出的多项式方程以及二维和三维模型显示了所选自变量(A、B 和 C)之间的响应关系。通过数值检查点分析对模型进行了验证和优化,以预测优化的固体脂质纳米生物颗粒配方(ONbp 1-10)。制备出的优化配方ONbp 3粒径更小(106 nm),可持续释放率更高(40 h内释放率达95.61%),EE更高(97.85%),药物含量更高(99.92% ± 0.08%),在3个月的储存期间表现出良好的稳定性。因此,它的性能可用于进一步开发稳定的 ISR 口服给药系统。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

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Nano-colloidal carrier via polymeric coating for oral delivery of isradipine.

Our research objective was to develop, characterize, and optimize stable form of nano-colloidal carrier with Eudragit-coated solid lipid nanobioparticles (SLNbp) for oral delivery of isradipine (ISR). To achieve, a three factors, i.e., lipid-to-surfactant ratio (A, % w/w), Eudragit L100 (B, % w/w), and sonication time (C, minutes) at three levels (-1 and +1 levels of quality central level) was applied to develop SLNbp using response surface methodology at constant ratio of ISR and rutin. The second-order polynomial quadratic equations of responses [R1, R2, and R3; entrapment efficiency (EE), particle size, and drug release] were constructed and also plotted response surface (two- and three-dimensional) plots. The derived polynomial equation and 2D and 3D model were showed the relationship between the responses of the selected independent variables (A, B, and C). The model validation and optimization was performed by numerical checkpoint analysis to predict the optimized solid lipid nanobioparticle formulas (ONbp 1-10). The optimized formulations prepared and during evaluation ONbp 3 has better smaller particle size (106 nm), sustainable release (95.61% up to 40 h), higher EE (97.85%), and drug content (99.92% ± 0.08%) during 3-month storage showed good stability. Therefore, its performance can be considered for further development of stable oral drug delivery system of ISR.

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来源期刊
Interventional Medicine and Applied Science
Interventional Medicine and Applied Science MEDICINE, GENERAL & INTERNAL-
CiteScore
1.60
自引率
0.00%
发文量
0
审稿时长
15 weeks
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