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含姜黄素的单油酸甘油酯水基分散体:制剂前研究。

Curcumin containing monoolein aqueous dispersions: a preformulative study.

机构信息

Department of Life Sciences and Biotechnology, University of Ferrara, I-44121 Ferrara, Italy.

出版信息

Mater Sci Eng C Mater Biol Appl. 2013 Dec 1;33(8):4923-34. doi: 10.1016/j.msec.2013.08.017. Epub 2013 Aug 27.

DOI:10.1016/j.msec.2013.08.017
PMID:24094206
Abstract

The present study describes the production and characterization of monoolein aqueous dispersions (MAD) as drug delivery systems for curcumin (CR). MAD based on monoolein and different emulsifiers have been produced and characterized. Morphology and dimensional distribution have been investigated by Cryogenic Transmission Electron Microscopy (cryo-TEM), X-ray and Photon Correlation Spectroscopy (PCS). Monoolein in different mixtures with sodium cholate, sodium caseinate, bentonite and poloxamer resulted in heterogeneous dispersions constituted of unilamellar vesicles, cubosomes and sponge type phases, depending on the employed components, as found by cryo-TEM and X-ray studies. CR was encapsulated with entrapment efficiencies depending on the MAD composition, particularly the highest was reached in the case of monoolein/poloxamer/sodium cholate mixture. The same mixture was able to maintain CR stability also after 6 months. CR release modalities were in vitro investigated in order to mimic a possible subcutaneous administration of MAD. It was found that MAD constituted of monoolein/poloxamer and monoolein/poloxamer/sodium cholate mixtures were able to sustain CR release. MAD viscous vehicles were produced by xanthan gum. CR percutaneous absorption has been studied in vitro using excised human skin membranes [stratum corneum epidermis (SCE)] mounted into Franz cells. It was found that fluxes (Fn) of CR incorporated in MAD are influenced by the presence of monoolein based nanosystems. In particular xanthan gum based MAD better control CR diffusion from MAD.

摘要

本研究描述了单油酸甘油酯水基分散体(MAD)作为姜黄素(CR)药物传递系统的制备和特性。已经制备和表征了基于单油酸甘油酯和不同乳化剂的 MAD。通过低温透射电子显微镜(cryo-TEM)、X 射线和光子相关光谱(PCS)研究了形态和尺寸分布。单油酸甘油酯与胆酸钠、酪蛋白酸钠、膨润土和泊洛沙姆在不同混合物中形成了不均匀的分散体,由单层囊泡、立方相和海绵相组成,这取决于所使用的成分,如 cryo-TEM 和 X 射线研究所示。CR 的包封效率取决于 MAD 的组成,特别是在单油酸甘油酯/泊洛沙姆/胆酸钠混合物的情况下达到最高。相同的混合物在 6 个月后仍能保持 CR 的稳定性。为了模拟 MAD 的皮下给药,对 CR 的体外释放模式进行了研究。结果发现,由单油酸甘油酯/泊洛沙姆和单油酸甘油酯/泊洛沙姆/胆酸钠混合物组成的 MAD 能够持续释放 CR。通过黄原胶制备了 MAD 粘性载体。使用Franz 细胞将人离体皮肤膜(角质层表皮(SCE))安装到体外研究了 CR 的经皮吸收。结果发现,掺入 MAD 中的 CR 的通量(Fn)受单油酸甘油酯基纳米系统的存在影响。特别是黄原胶基 MAD 能更好地控制 MAD 中 CR 的扩散。

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