Formulation and evaluation of dexamethasone loaded stearic acid nanoparticles by hot homogenization method.

S. Parvin, Abu Shuaib Rafshanjani, A. Kader
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引用次数: 2

Abstract

Dexamethasone is a type of steroid medication having anti-inflammatory and immunosuppressant effects. One of the major problems with this drug is its low solubility in water which results into poor bioavailability after oral administration. So the objective of the present work is to improve the solubility and dissolution rate of dexamethasone using its solid lipid nano particles (SLNPs) with stearic acid as solid lipid, lutrol F-68 as surfactant and tween-80 as stabilizer. SLNPs are prepared by hot homogenization method at different ratio of drug, lipid, surfactant and stabilizer and designated as DNP1 to DNP6. In vitro dissolution study was performed using the USP type II apparatus (paddle method) at 50 rpm to a temperature of 37°±0.5°C in distilled water containing 0.75% w/v SLS (sodium lauryl sulfate). The absorbance of sample was measured spectrophotometrically at λ max 239nm on a UV-Visible spectrophotometer. Release pattern of drug was found to follow zero order, first order and Korsmeyer-Peppas equations. Improvement of dissolution was observed in all the solid lipid nano particles as compared to pure drug. Pure drug showed only 27.25% release in 50 min whereas the dexamethasone SLNPs showed faster (66.19%) in vitro drug release. Hence, this finding indicates that dexamethasone SLNPs prepared by hot homogenization method can be used to enhance the dissolution rate and to show novel application to this drug delivery system. DOI:  http://dx.doi.org/10.3329/icpj.v3i12.20829 International Current Pharmaceutical Journal, November 2014, 3(12): 331-335
热均质法制备负载地塞米松的硬脂酸纳米颗粒。
地塞米松是一种类固醇药物,具有抗炎和免疫抑制作用。该药的主要问题之一是其在水中的溶解度低,导致口服给药后生物利用度差。以硬脂酸为固体脂质,lutrol F-68为表面活性剂,tween-80为稳定剂,利用固体脂质纳米颗粒(SLNPs)提高地塞米松的溶解度和溶出率。采用热均质法,以不同比例的药物、脂类、表面活性剂和稳定剂制备SLNPs,命名为DNP1 ~ DNP6。体外溶出研究采用USP II型仪器(桨叶法),在含有0.75% w/v十二烷基硫酸钠(SLS)的蒸馏水中,转速为50 rpm,温度为37°±0.5°C。用紫外可见分光光度计在λ max 239nm处测定样品的吸光度。药物释放模式遵循零阶、一阶和Korsmeyer-Peppas方程。与纯药物相比,所有固体脂质纳米颗粒的溶出度都有所提高。纯药50 min释放量为27.25%,地塞米松SLNPs的体外释放量为66.19%。由此可见,热均质法制备的地塞米松SLNPs可提高溶出率,在该给药系统中具有新的应用前景。DOI: http://dx.doi.org/10.3329/icpj.v3i12.20829国际现代医药杂志,2014年11月,3(12):331-335
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