固体脂质纳米粒(SLN)已广泛应用于多种给药途径,在药物控释方面具有突出的优势。SLN的释放受多种因素支配,其中SLN的粒径是一个关键的粒径。该项目的目的是探索药物释放曲线与SLN粒径之间的关系。通过热高压均质化（HPH）方法合成了SLN，布地奈德（BUD）作为模型药物，并得到粒径增大的BUD-SLN1-BUD-SLN4,即120、240、360和480nm。制备的SLN具有良好的封装效率,载药量,和稳定性。体外释放行为研究表明，BUD-SLN在Tris-Maleate（Tris-M）培养基中的累积释放量可以忽略不计，而在Tris-M加胰酶培养基或Tris-M-乙醇培养基中，服从Ritger-Peppas模型或一级动力学模型，分别。值得注意的是，SLN的释放行为在一定程度上与SLN的平均粒径有关，但当粒径分布的交叉程度较大时，相关性不明显。本研究为了解SLN的体外释放提供了新的思路,对新型纳米药物的研发具有一定的参考价值。
Solid lipid nanoparticles (SLN) have been widely used in a variety of drug delivery routes, which have the outstanding advantage of controlled drug release. The release of SLN is dominated by many factors, among which the particle size of SLN is a critical one. The aim of this project was to explore the relationship between drug release profile and particle size of SLN. SLN were synthesized via the hot high-pressure homogenization (HPH) method, budesonide (BUD) was used as the model drug, and BUD-SLN1-BUD-SLN4 with increasing particle size was obtained, i.e. 120, 240, 360, and 480 nm. The prepared SLN has good encapsulation efficiency, drug loading capacity, and stability. In vitro release behavior studies showed that the cumulative release of BUD-SLN in Tris-Maleate (Tris-M) media was negligible, while that in Tris-M plus pancreatin media or Tris-M-ethanol media obeyed Ritger-Peppas model or first-order kinetic model, respectively. Noticeably, the release behavior of SLN was to some extent related to the average particle size of SLN, but the correlation was insignificant when the intersection degree of particle size distribution was great. This study provides a new idea for the understanding of in vitro release of SLN and has a certain referencing value for the research and development of novel nanomedicines.
