Preparation and characteristics of monostearin nanostructured lipid carriers.
Nanostuctured lipid carriers (NLC) consisted of solid lipid and liquid lipid are a new type of lipid nanoparticles, which offer the advantage of improved drug loading capacity and release properties. In this study, solvent diffusion method was employed to produce NLC. Monostearin (MS) and caprylic/capric triglycerides (CT) were chosen as the solid lipid and liquid lipid. Clobetasol propionate used as a model drug was incorporated into the NLC. The influences of preparation temperature and CT content on physicochemical properties of the NLC were characterized. As a result, monostearin solid lipid nanoparticles (without CT content, SLN) obtained at higher temperature (70 degrees C) exhibited slightly higher drug loading capacity than that of 0 degrees C (P < 0.05). In contrast, the production temperature made little effect on NLC drug loading capacity (P > 0.05). The improved drug loading capacity was observed for NLC and it enhanced with increasing the CT content in NLC. The results were explained by differential scanning calorimetry (DSC) measurement for NLC. The incorporation of CT to NLC led to crystal order disturbance and thus left more space to accommodate drug molecules. NLC displayed a good ability to reduce the drug expulsion in storage compared to SLN. The in vitro release behaviors of NLC were dependent on the production temperature and CT content. NLC obtained at 70 degrees C exhibited biphasic drug release pattern with burst release at the initial 8h and prolonged release afterwards, whereas NLC obtained at 0 degrees C showed basically sustained drug release throughout the release time. The drug release rates were increased with increasing the CT content. These results indicated that the NLC produced by solvent diffusion method could potentially be exploited as a carrier with improved drug loading capacity and controlled drug release.
School of Pharmaceutical Science, Zhejiang University, 353 Yanan Road, Hangzhou 310031, PR China. hufq@zju.edu.cn
Fu-Qiang
FQ
Hu
Sai-Ping
SP
Jiang
Yong-Zhong
YZ
Du
Hong
H
Yuan
Yi-Qing
YQ
Ye
Su
S
Zeng
D002152:Calorimetry, Differential Scanning; D002990:Clobetasol / Q000008:administration & dosage / Q000031:analogs & derivatives / Q000737:chemistry; D003692:Delayed-Action Preparations; D004337:Drug Carriers / Q000737:chemistry*; D004355:Drug Stability; D004356:Drug Storage; D005989:Glycerides / Q000737:chemistry; D008055:Lipids / Q000737:chemistry*; D049329:Nanostructures / Q000737:chemistry*; D010316:Particle Size; D012995:Solubility; D013696:Temperature; D014280:Triglycerides / Q000737:chemistry
D003692:Delayed-Action Preparations; D004337:Drug Carriers; D005989:Glycerides; D008055:Lipids; D014280:Triglycerides; C048159:glyceryl monostearate; D002990:Clobetasol