Solidification of Nanostructured Lipid Carriers Loaded Testosterone Undecanoate: In Vivo and In Vitro Study
Solidification of Nanostructured Lipid Carriers Loaded Testosterone Undecanoate: In Vivo and In Vitro Study
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负载十一酸睾酮的纳米结构脂质载体的固化：体内和体外研究
DOI：
10.1055/a-0573-9132
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发表时间：
2018-03
期刊：
影响因子：
2.2
通讯作者：
Aiping Zheng
中科院分区：
文献类型：
--
作者：
Yabing Hua;Wanqing Li;Zhou Cheng;Ziming Zhao;Xiaoxing Yin;Ying Li;Jianxu Sun;Jing Gao;Hui Zhang;Aiping Zheng
为了提高十一酸睾酮（TU）的生物利用度，克服目前软胶囊（Andriol Testocaps®）的问题，开发了十一酸睾酮纳米结构脂质载体（NLC）。首先，采用高压均质法制备TU-NLC悬浮液（TU-NLC）；然后用吸附剂或保护剂β-环糊精对悬浮液进行真空固化；最后将TU-NLC的固体粉末（固体TU-NLC）填充到硬胶囊中。研究了固体TU-NLC在体外和体内的特性。TU-NLC的粒径约为273.3 nm，电势为0.156±0.04。透射电子显微镜（TEM）显示NLC呈球形，均匀。差示扫描量热法（DSC）显示药物已被包裹在NLC脂质基质中。释药结果表明，固体TU-NLC具有较高的体外溶出度。CaCO-2细胞通透性表明，TU- nlc固体制剂能增强TU的跨膜吸收，且其AUC（4304±550.50μg/L*min）高于市售Andriol Testocaps®（3075±372.50 μg/L*min）。综上所述，固体TU-NLC可以提高溶出率，并且相对于Andriol Testocaps®具有较高的体内生物利用度
To enhance the bioavailability of testosterone undecanoate(TU) and overcome the current problem of soft capsules(Andriol Testocaps®), Nano-structured lipid carriers (NLC)for TU was developed. First, suspension of TU-loaded NLC(TU-NLC) was prepared by high pressure homogenization; then adsorbent or a protective agent β-cyclodextrin was used to solidify the suspension through a vacuum system; finally, the solid powder of TU-loaded NLC (solid TU-NLC) was filled into hard capsules. The characteristics of solid TU-NLC, were investigated in vitro and vivo. The particle size of TU-NLC was about 273.3 nm, the potential was 0.156 ± 0.04. Transmission electron microscope (TEM) revealed that the NLC was spherical and uniform. Differential scanning calorimetry (DSC) suggested the drug had been encapsulated into NLC lipid matrix. The drug release proved that solid TU-NLC showed a higher dissolution in vitro. The CaCO-2 cell permeability showed that solid TU-NLC could enhance trans-membrane absorption of the TU. Moreover, the AUC of solid TU-NLC formulations(4304±550.50μg/L*min) was higher than commercial product Andriol Testocaps® (3075 ± 372.50 μg/L * min). In conclusion,solid TU-NLC could enhance the rate of dissolution, and had a relatively higher bioavailability than Andriol Testocaps® in vivo
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影响因子：
--
作者：
Zirkin BR;Tenover JL
通讯作者：
Tenover JL
影响因子：
1.7
作者：
S. Song;Kyung Min Lee;Jong Boo Kang;Sang Gon Lee;M. Kang;Y. Choi
通讯作者：
S. Song;Kyung Min Lee;Jong Boo Kang;Sang Gon Lee;M. Kang;Y. Choi
DOI：
10.3109/13685538.2015.1032925
发表时间：
2015-06
期刊：
The Aging Male
影响因子：
--
作者：
E. Meuleman;J. Legros;P. Bouloux;A. Johnson-Levonas;Marion J. G. H. Kaspers;J. Elbers;T. Geurts;A. Meehan
通讯作者：
E. Meuleman;J. Legros;P. Bouloux;A. Johnson-Levonas;Marion J. G. H. Kaspers;J. Elbers;T. Geurts;A. Meehan
影响因子：
2.6
作者：
Bouloux, Pierre M. G.;Legros, Jean-Jacques;Meuleman, Eric J. H.
通讯作者：
Meuleman, Eric J. H.
影响因子：
2.8
作者：
Surampudi PN;Wang C;Swerdloff R
通讯作者：
Swerdloff R