Development, optimization and evaluation of solid lipid nanoparticles of Celecoxib.

固体脂质纳米粒 Zeta电位 生物利用度 溶解 溶解度 粒径 分散性 纳米颗粒 化学 化学工程 傅里叶变换红外光谱 色谱法 尼奥体 材料科学 动态光散射 塞来昔布 纳米技术 有机化学 药理学 生物化学 医学 小泡 物理化学 工程类
作者
Madhu Verma,Manish Gautam,Arun Nanda,Iti Chauhan,Mohd Yasir,Alok Pratap Singh,Sagarika Majhi,Raj Kumari,Meenakshi Sharma
出处
期刊:Pharmaceutical nanotechnology [Bentham Science Publishers]
卷期号:11
标识
DOI:10.2174/2211738511666230831143111
摘要

As indicated by the biopharmaceutical classification system, Celecoxib is a class II moiety. Many endeavors have been made to improve its solubility and consequently its dissolution rate, thus enhancing its overall bioavailability. In the present investigation, the nano-lipid technology was exploited to control the release of celecoxib (CXB) to overcome its dissolution problem. Solid lipid nanoparticles (SLNs) have a small particle size (50-1000 nm) that results in a large surface area-to-volume ratio, which further enhances the contact between the drug and the dissolution medium. This leads to improved drug release and absorption. Moreover, SLNs can solubilize hydrophobic drugs within the lipid matrix, increasing their effective solubility and facilitating their dissolution in an aqueous environment.The objective of the study was to enhance the solubility and bioavailability of a BCS Class-II drug-celecoxib formulating it as solid lipid nanoparticles. In order to overcome all its limitations, solid lipid nanoparticles of Celecoxib were developed, optimized, and evaluated for in-vitro and in-vivo parameters.The CXB loaded-SLNs were prepared by solvent emulsification-diffusion technique. SLN was characterized using Fourier transform infra spectroscopy (FTIR) and evaluated for entrapment efficiency, drug loading, particle size, Polydispersity index (PDI), zeta potential, In-vitro release studies as well as in- vivoanti-inflammatory studies using rat paw edema method. The SLN formulations were optimized by central composite design (Design Expert 11- trial version).On the basis of outcomes of CCD the optimized formulation OF1 was selected as a desirable formulation. Its particle size, PDI, and zeta potential were found to be 314 nm, 0.204, and -18.73 respectively. It exhibited high entrapment efficiency (79±0.18 %) and drug loading (44.38±0.21 %). In-vitro release studies of the optimized formulation displayed the Korsemeyer-Peppas model with a maximum drug release of 89.42 ±0.12 % in 24 h. In-vivo studies also revealed that OF1 formulation reduced the rat paw volume to a minimum (1±0.32) in 24 h when compared to pure API (2±0.62) and marketed preparation (2±0.42).The results revealed that in-vitro release studies of optimized formulation exhibited a sustained drug release delivery. In-vivo anti-inflammatory studies proved that the CXB-loaded SLNs enhance the oral bioavailability more than pure API.

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