Preparation of triptolide-loaded dissolving microneedles and its transdermal penetration.
10.19540/j.cnki.cjcmm.20210330.303
- Author:
Xin CHEN
1
;
Yong-Ping ZHANG
2
;
Jian XU
2
;
Xin-Li SONG
3
;
Yao LIU
2
;
Ling GUO
3
;
Zu-Hua WANG
3
Author Information
1. Guizhou University of Traditional Chinese Medicine Guiyang 550025, China.
2. Guizhou University of Traditional Chinese Medicine Guiyang 550025, China Guizhou Engineering Research Center for Traditional Chinese Medicine and Ethnic Medicine Processing and Preparation Guiyang 550025, China National Engineering Research Center of Miao's Medicines Guiyang 550025, China.
3. Guizhou University of Traditional Chinese Medicine Guiyang 550025, China Guizhou Engineering Research Center for Traditional Chinese Medicine and Ethnic Medicine Processing and Preparation Guiyang 550025, China.
- Publication Type:Journal Article
- Keywords:
dissolving microneedles;
transdermal drug delivery system;
transdermal properties in vitro;
triptolide;
two-step centrifugation method
- MeSH:
Administration, Cutaneous;
Diterpenes;
Drug Delivery Systems;
Epoxy Compounds;
Needles;
Phenanthrenes;
Skin
- From:
China Journal of Chinese Materia Medica
2021;46(20):5278-5283
- CountryChina
- Language:Chinese
-
Abstract:
Triptolide(TP), the main active and toxic component of Tripterygium wilfordii, has the limitations of low bioavailability, poor absorption, low concentration in plasma, and small lethal dose. Microneedle(MN), the hybrid of hypodermic needle and transdermal patch, is a physical penetration-enhancing system. Dissolving microneedles(DMNs) can be tailored to specific needs of degradation rate. In this study, the TP-loaded DMNs(DMNs-TP) were prepared with the two-step centrifugation method. The optimal ratio of PVA to PVP K30, water content in matrix solution, demoulding method, and plasticizer for preparing DMNs were investigated with the indexes of formability and mechanical strength. The drug loading capacity was determined by HPLC and morphological characteristics were observed under an optical microscope. The mechanical properties were investigated by H&E staining and Franz diffusion cell was used to detect the in vitro skin permeation characteristics. Through the experiment, we confirmed that the optimal backing material should be PVA and PVP K30(3∶1) and the optimal ratio of matrix material to water should be 3∶4. The prepared DMNs-TP were pyramidal with smooth surface and length of approximately 550 μm. Each patch(2.75 cm~2) had the drug loading capacity of(153.41±2.29) μg, and TP was located in the upper part of the needle. The results of in vitro skin permeation assay demonstrated that the cumulative penetration of TP in DMNs-TP reached 80% in 24 h, while little TP solution penetrated the skin, which proved that DMNs promoted the transdermal delivery of TP.
