Development & Pharmaceutical Characterization of Isoniazid Loaded Solid Lipid Nanoparticle Drug Delivery Approach
Development & Pharmaceutical Characterization of Isoniazid Loaded Solid Lipid Nanoparticle Drug Delivery Approach
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作者：
S. Kushwaha;A. Rai;H. Parveen
结核病是世界上一个主要的公共卫生问题。
异烟肼是一种一线抗结核药物，对分枝杆菌有活性，
抑制分枝菌酸的合成。
本研究的目的是制备固体脂质纳米粒
含有异烟肼，以增加生物利用度，持续释放并降低毒性
通过增加渗透性。
异烟肼被纳入SLN用于持续药物递送，
渗透性和生物利用度。SLN通过乳化制备，然后通过乳化制备。
通过优化脂质、聚合物和表面活性剂的比例，
控制优化的工艺变量，即温度和搅拌速度。SLN是
表征粒度分析，在不同生理条件下的比较研究设计
用于体外药物释放和药物释放动力学的pH。
F7的最佳体外释放度在pH = 7.4时为80.2%，在pH = 1.5时为82.2%。
pH值-4.5。发现F7制剂的粒度在200 - 300 μ m的范围内。
600纳米。在所有3种优化的制剂中，即F3、F7和F8在两种pH下，F3
在pH-4.5下遵循非Fickian扩散机制，而在pH-4.5和pH-4.5下的所有制剂都遵循非Fickian扩散机制。
pH值遵循超级案例II扩散机制。进行了稳定性研究
根据ICH指导原则，这表明SLN在冷藏条件下稳定
条件
结果表明SLNs是一种很有前途的给药系统
抗结核药物输送的方法，因为它被证明是持续释放，增加
渗透性，提高生物利用度，从而降低给药频率。动力学
零阶、一阶、Higuchi和Korsmeyer-peppas的配方建模是
在这篇文章中解释。
Tuberculosis is a major public health problem in the world.
Isoniazid is a first line antitubercular drug active against Mycobacterium species which
inhibits mycolic acid synthesis.
The aim of the present investigation was the preparation of solid lipid nanoparticle
containing Isoniazid to increase bioavailability, sustained release and decrease toxicity
by increasing permeability.
Isoniazid was incorporated into SLN for sustained drug delivery, increasing
permeability and bioavailability. SLNs were prepared by emulsification followed by the
solvent evaporation technique by optimizing lipid, polymer and surfactant ratio under
controlled optimized process variables i.e. temperature and stirring speed. SLNs were
characterized for particle size analysis, comparative study design in different physiological
pH for in-vitro drug release and drug release kinetics.
The best in-vitro release for F7 was found to be 80.2% in pH-7.4 and 82.2% in
pH-4.5. The particle size of the F7 formulation was found to be in the range of 200-
600nm . Among all 3 optimized formulations, i.e. F3, F7 and F8 in both the pH, F3
followed non-fickian diffusion mechanism in pH-4.5 whereas all the formulations in both
pH followed super-case II diffusion mechanism. The stability studies were carried out
as per ICH guidelines which signify that the SLNs were found stable in the refrigerated
condition.
The results clearly demonstrated that SLNs drug delivery system is a promising
approach for antitubercular drug delivery as it proved to sustained release, increase
permeability, enhanced bioavailability and thus decreased dosing frequency. Kinetic
modelling of the formulation with zero, first order, Higuchi and Korsmeyer- peppas is
explained in this article.
影响因子：
3.1
作者：
Iyer R;Hsia CC;Nguyen KT
通讯作者：
Nguyen KT