Esposito Elisabetta, Cortesi Rita, Drechsler Markus, Paccamiccio Lydia, Mariani Paolo, Contado Catia, Stellin Elisa, Menegatti Enea, Bonina Francesco, Puglia Carmelo
Dipartmento di Scienze Farmaceutiche, Universitá di Ferrara, Via Fossato di Mortara, 19, 44100 Ferrara, Italy.
Pharm Res. 2005 Dec;22(12):2163-73. doi: 10.1007/s11095-005-8176-x.
The present study concerns the production and characterization of monooleine (MO) dispersions as drug delivery systems for indomethacin, taken as model anti-inflammatory drug.
Dispersions were produced by emulsification and homogenization of MO and poloxamer in water. Morphology and dimensional distribution of the disperse phase have been characterized by cryo-transmission electron microscopy and photon correlation spectroscopy, respectively. X-ray diffraction has been performed to determine the structural organization of the disperse phase. Sedimentation field flow fractionation (SdFFF) has been performed to investigate drug distribution in the dispersion. An in vitro diffusion study was conducted by Franz cell associated to stratum corneum epidermis membrane on cubosome dispersions viscosized by carbomer. In vivo studies based on skin reflectance spectrophotometry and tape stripping were performed to better investigate the performance of cubosome as indomethacin delivery system.
Microscopy studies showed the coexistence of vesicles and cubosomes. X-ray diffraction revealed the presence of a bicontinuous cubic phase of spatial symmetry Im3m (Q229). SdFFF demonstrated that no free drug was present in the dispersion. Indomethacin incorporated in viscosized MO dispersions exhibited a lower flux with respect to the analogous formulation containing the free drug in the aqueous phase and to the control formulation based on carbomer gel. Reflectance spectroscopy demonstrated that indomethacin incorporated into MO dispersions can be released in a prolonged fashion. Tape-stripping experiments corroborated this finding.
MO dispersions can be proposed as nanoparticulate systems able to control the percutaneous absorption of indomethacin.
本研究关注单油酸甘油酯（MO）分散体作为吲哚美辛药物递送系统的制备及特性，吲哚美辛作为模型抗炎药物。
通过在水中乳化和均质化MO与泊洛沙姆来制备分散体。分别采用低温透射电子显微镜和光子相关光谱对分散相的形态和尺寸分布进行了表征。进行X射线衍射以确定分散相的结构组织。采用沉降场流分级法（SdFFF）研究药物在分散体中的分布。通过与卡波姆增稠的立方液晶分散体上的角质层表皮膜相关联的Franz扩散池进行体外扩散研究。基于皮肤反射分光光度法和胶带剥离法进行体内研究，以更好地研究立方液晶作为吲哚美辛递送系统的性能。
显微镜研究显示囊泡和立方液晶共存。X射线衍射显示存在空间对称Im3m（Q229）的双连续立方相。SdFFF表明分散体中不存在游离药物。与含有游离药物的水相类似制剂以及基于卡波姆凝胶的对照制剂相比，加入增稠MO分散体中的吲哚美辛通量较低。反射光谱表明，加入MO分散体中的吲哚美辛能够以延长释放的方式释放。胶带剥离实验证实了这一发现。
MO分散体可被提议作为能够控制吲哚美辛经皮吸收的纳米颗粒系统。
