| 摘要: |
| \[摘要\]目的考察微针阵列对纳米粒经皮给药的促渗作用,以及纳米粒在接收液和皮肤中的分布。方法采用双荧光探针指示纳米粒的经皮过程,采用Franz扩散池法,将裸鼠皮肤置于扩散池间,微针组供给室加入纳米粒混悬液,皮肤采用微针阵列作用；对照组皮肤无微针作用。采用共聚焦显微镜观察纳米粒在皮肤内的渗透过程,采用HPLC法测定纳米粒的分布。结果共聚焦显微镜观察显示纳米粒经由微针作用皮肤后产生的微孔渗透进入皮肤。 48 h后测定显示没有纳米粒进入接收液,皮肤中纳米粒的滞留量如下：微针组表皮125.99 μg/cm2,真皮55.31 μg/cm2,皮肤中总量181.30 μg/cm2；对照组表皮42.15 μg/cm2,真皮32.76 μg/cm2,皮肤中总量74.91 μg/cm2。微针可以增加纳米粒在皮肤内的滞留量(P<0.01),并且纳米粒在表皮层中的滞留量大于真皮层(P<0.01)。结论微针作用于皮肤后可显著增加纳米粒的皮肤内递送量,纳米粒沉积在皮肤中缓慢释放药物,有利于局部皮肤给药。 |
| 关键词: 皮肤 微针 聚乳酸-羟基乙酸共聚物 纳米粒 皮肤投药 |
| DOI：10.3724/SP.J.1008.2010.01341 |
| 投稿时间：2010-07-11修订日期：2010-11-26 |
| 基金项目:国家自然科学基金(81000689),上海市自然科学基金(10ZR1437300). |
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| Study on microneedle technique in enhancement of transdermal nanoparticle delivery |
| ZHANG Wei1 , GAO Jing2 , ZHU Quan-gang1 , ZHANG Min1 , WANG Xiao-yu1, GAO Shen1* |
| (1.Department of Pharmaceutics, Changhai Hospital, Second Military Medical University, Shanghai 200433, China; 2.Department of Pharmaceutics, School of Pharmacy, Second Military Medical University, Shanghai 200433, China) |
| Abstract: |
| \[Abstract\]ObjectiveTo investigate the microneedle technique in enhancement of transdermal nanoparticle delivery and the distribution of poly (D,L-lactic-co-glycolic acid) (PLGA) nanoparticles in the skin and the transdermal microconduits. MethodsDouble fluorescent PLGA nanoparticles were used to show the transdermal transport process.Franz diffusion cell was used for the transdermal study.The nanoparticle suspension was added to the donor chamber.The hairless mouse skin in the microneedle group was treated by microneedle technique and that in the control group was not treated.Penetration of nanoparticles was visualized by confocal laser scanning microscopy (CLSM).Distribution of nanoparticle diameter was quantified by HPLC.ResultsThe CLSM images revealed that the nanoparticles were delivered into the microconduits created by microneedles and entered the epidermis and the dermis.The quantitative results showed that no nanoparticles reached the receptor compartment 48 h after addition of the nanoparticles in both groups.In microneedle group the nanoparticle amount was 125.99 μg/cm2 in the epidermis and 55.31 μg/cm2 in the dermis,with the total amount in the skin being 181.30 μg/cm2；in the the control group ,the nanoparticle amount was 42.15 μg/cm2 in the epidermis and 32.76 μg/cm2 in the dermis,with the total amount in the skin being 74.91 μg/cm2.Microneedle technique significantly increased the amount of nanoparticles entering the skin (P<0.01),and the amount in the epidermis was significantly more than that in the dermis (P<0.01).ConclusionOur results suggest that microneedles can enhance the intradermal PLGA nanoparticle delivery,and the nanoparticles deposit in the skin to achieve sustainable drug release,which is beneficial for topical drug administration. |
| Key words: skin microneedles poly (D,L-lactic-co-glycolic acid) nanoparticles cutaneous administration |
