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透皮传递体载药巴布剂的制备、表征及体外透皮研究。

Preparation, Characterization and Permeation Study of Topical Gel Loaded with Transfersomes Containing Asiatic Acid.

机构信息

Pharmaceutical Sciences and Technology Program, Faculty of Pharmaceutical Sciences, Chulalongkorn University, Bangkok 10330, Thailand.

Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmaceutical Sciences, Chulalongkorn University, Bangkok 10300, Thailand.

出版信息

Molecules. 2022 Jul 29;27(15):4865. doi: 10.3390/molecules27154865.

Abstract

The objective of this study is to investigate the in vitro permeation of asiatic acid (AA) in the form of a topical gel after entrapment in transfersomes by Franz diffusion cells. Transfersomes composed of soybean lecithin and three different edge activators including Tween 80 (TW80), Span 80 (SP80) and sodium deoxycholate (SDC) at the ratio of 50:50, 90:10 and 90:10, respectively, together with 0.3% / of AA, were prepared by a high-pressure homogenization technique and further incorporated in gels (TW80AATG, SP80AATG and SDCAATG). All transfersomal gels were characterized for their AA contents, dynamic viscosity, pH and homogeneity. Results revealed that the AA content, dynamic viscosity and pH of the prepared transfersomal gels ranged from 0.272 ± 0.006 to 0.280 ± 0.005% /, 812.21 ± 20.22 to 1222.76 ± 131.99 Pa.s and 5.94 ± 0.03 to 7.53 ± 0.03, respectively. TW80AATG gave the highest percentage of AA penetration and flux into the Strat-M membrane at 8 h (8.53 ± 1.42% and 0.024 ± 0.008 mg/cm/h, respectively) compared to SP80AATG (8.00 ± 1.70% and 0.019 ± 0.010 mg/cm/h, respectively), SDCAATG (4.80 ± 0.50% and 0.014 ± 0.004 mg/cm/h, respectively), non-transfersomal gels (0.73 ± 0.44 to 3.13 ± 0.46% and 0.002 ± 0.001 to 0.010 ± 0.002 mg/cm/h, respectively) and hydroethanolic AA solution in gel (1.18 ± 0.76% and 0.004 ± 0.003 mg/cm/h, respectively). These findings indicate that the TW80AATG might serve as a lead formulation for further development toward scar prevention and many types of skin disorders.

摘要

本研究旨在通过 Franz 扩散池研究以传递体形式包封的积雪草酸(AA)的体外渗透。传递体由大豆卵磷脂和三种不同的边缘活性剂(Tween 80(TW80)、Span 80(SP80)和脱氧胆酸钠(SDC))组成,比例分别为 50:50、90:10 和 90:10,以及 0.3%/的 AA,采用高压匀质技术制备,并进一步掺入凝胶(TW80AATG、SP80AATG 和 SDCAATG)中。所有传递体凝胶均对 AA 含量、动态粘度、pH 值和均匀性进行了表征。结果表明,制备的传递体凝胶的 AA 含量、动态粘度和 pH 值范围分别为 0.272±0.006 至 0.280±0.005%/、812.21±20.22 至 1222.76±131.99 Pa.s 和 5.94±0.03 至 7.53±0.03。与 SP80AATG(8.00±1.70%和 0.019±0.010 mg/cm/h)、SDCAATG(4.80±0.50%和 0.014±0.004 mg/cm/h)、非传递体凝胶(0.73±0.44 至 3.13±0.46%和 0.002±0.001 至 0.010±0.002 mg/cm/h)和水醇 AA 溶液相比,TW80AATG 在 Strat-M 膜中的 8 小时 AA 渗透和通量最高(8.53±1.42%和 0.024±0.008 mg/cm/h)。这些发现表明,TW80AATG 可能成为预防疤痕和多种皮肤疾病的进一步开发的先导配方。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/777b/9369753/a8445d28da00/molecules-27-04865-g001.jpg

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