Microneedle-Assisted Percutaneous Delivery of Paeoniflorin-Loaded Ethosomes
Microneedle-Assisted Percutaneous Delivery of Paeoniflorin-Loaded Ethosomes
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微针辅助经皮递送载有芍药苷的醇质体。
DOI：
10.3390/molecules23123371
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发表时间：
2018-12-01
期刊：
影响因子：
4.6
通讯作者：
Du, Shouying
中科院分区：
文献类型：
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作者：
Cui, Yahua;Mo, Yujia;Du, Shouying
芍药苷是白芍总苷（TGP）的主要成分，在关节炎治疗中显示出良好疗效，但口服时生物利用度较低。避免这一缺陷而采用局部给药方式将扩大其临床应用。本研究旨在通过纳米技术（醇质体）和物理方法（微针）来克服这些局限。对载芍药苷醇质体制剂（TGP - E）进行了优化，并从包封率（EE）、粒径（PS）、zeta电位（ZP）、多分散指数（PDI）及形态等方面进行了评估。TGP - E采用热注入法制备，并通过单因素试验和正交试验设计进行优化。优化后的载芍药苷醇质体包封率为27.82 ± 1.56%，粒径为137.9 ± 7.57 nm，多分散指数为0.120 ± 0.005，zeta电位为 - 0.74 ± 0.43 mV。在透射电子显微镜（TEM）下，醇质体呈近似球形。最佳微针辅助（MN辅助）条件为微针长度500μm、压力3 N、作用时间3 min。TGP溶液透皮（ST）和MN辅助TGP溶液透皮（MST）的累积渗透量（Q(n)）分别为24.42 ± 8.35 μg/cm²和548.11 ± 10.49 μg/cm²。TGP - E透皮（PT）和MN辅助TGP - E透皮（MPT）的Q(n)分别为54.97 ± 4.72 μg/cm²和307.17 ± 26.36 μg/cm²。这些研究结果表明，醇质体和微针均可增强芍药苷的渗透，但对于水溶性药物而言，在透皮给药系统中，纳米技术与微针在增强渗透方面并无明显协同作用。
Paeoniflorin, the main component of total glucosides of paeony (TGP), shows good therapeutic effects in arthritis, but has low bioavailability when administered orally. Avoiding such a deficiency for topical administration would expand its clinical application. This study aimed to avoid these limitations by using nanotechnology (ethosomes) and a physical approach (microneedles). Paeoniflorin-loaded ethosomal formulation (TGP-E) was optimized and evaluated in terms of entrapment efficiency (EE), particle size (PS), zeta potential (ZP), polydispersity index (PDI) and morphology. TGP-E was prepared by the hot injection method and optimized by single-factor tests and an orthogonal experimental design. The optimized paeoniflorin-loaded ethosomes had EE of 27.82 +/- 1.56%, PS of 137.9 +/- 7.57 nm with PDI of 0.120 +/- 0.005, ZP of -0.74 +/- 0.43 mV. Ethosomes showed a nearly spherical shape under the transmission electron microscope (TEM). The optimal microneedle-assisted (MN-assisted) conditions were obtained at a microneedle length of 500 m, a pressure of 3 N and an action time of 3 min. The cumulative penetration amounts (Q(n)) of TGP solution transdermal (ST) and MN-assisted TGP solution transdermal (MST) were 24.42 +/- 8.35 g/cm(2) and 548.11 +/- 10.49 g/cm(2), respectively. Q(n) of TGP-E transdermal (PT) and MN-assisted TGP-E transdermal (MPT) were 54.97 +/- 4.72 g/cm(2) and 307.17 +/- 26.36 g/cm(2), respectively. These findings indicate that use of ethosomes and microneedles can both enhance the penetration ofpaeoniflorin, but for the water-soluble drug, there is no obvious synergism between nanotechnology and microneedles for enhancing penetration in a transdermal drug delivery system.