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Issue 103, 2016
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Nanonization of andrographolide by a wet milling method: the effects of vitamin E TPGS and oral bioavailability enhancement

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Abstract

Andrographolide (AND) has wide prospects in clinical use, but suffers from the restriction of poor oral bioavailability, due to its low solubility, rapid and extensive metabolism and efflux by P-glycoprotein (P-gp). In this study, for the first time, nanocrystals of AND, a model of BCS class II, were obtained via the wet milling method, with TPGS as a stabilizer to enhance the bioavailability of AND; HPMC E5 nanocrystals (E5NCs) were fabricated as the negative control. Using the optimized formulation, AND/TPGS nanocrystals (TNCs) and E5NCs were prepared. Physical characterizations demonstrated that the two nanocrystals shared similar particle size, the same crystallinity and identical morphology. Both nanocrystals were physically stable at 4 °C and 25 °C, respectively, for at least 1 month. Significant increases in cumulative dissolution (90% and 70%) were obtained after the TNCs and E5NCs dissolved at 60 min, which were higher than for coarse AND (no more than 40%), indicating that TNCs were superior to E5NCs in dissolution. As elucidated in the single-pass intestinal perfusion studies of AND, the nanocrystals could facilitate intestinal uptake, and TPGS possessed improved intestine absorption properties. Oral administration of AND nanocrystals produced a substantial improvement in oral absorption, compared to the AND coarse suspension. Compared to E5NCs, there was a significant difference in AUC0–24h after the oral administration of TNCs. Compared to the model group, the TNCs and E5NCs inhibited xylene induced ear swelling by 59.98 and 48.06%, respectively. These results corroborated that TNCs were a promising formulation choice for the oral delivery of AND.

Graphical abstract: Nanonization of andrographolide by a wet milling method: the effects of vitamin E TPGS and oral bioavailability enhancement

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Publication details

The article was received on 20 Jun 2016, accepted on 05 Oct 2016 and first published on 11 Oct 2016


Article type: Paper
DOI: 10.1039/C6RA16002F
Citation: RSC Adv., 2016,6, 101404-101414
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    Nanonization of andrographolide by a wet milling method: the effects of vitamin E TPGS and oral bioavailability enhancement

    P. Du, Q. Jiang, R. Yang, C. Liu, Y. Li, L. Wang, P. Xue, Q. Fu and T. Zhang, RSC Adv., 2016, 6, 101404
    DOI: 10.1039/C6RA16002F

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