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Molecules 2017, 22(2), 246; doi:10.3390/molecules22020246

Poloxamer-Based Thermoreversible Gel for Topical Delivery of Emodin: Influence of P407 and P188 on Solubility of Emodin and Its Application in Cellular Activity Screening

College of Pharmacy, CHA University, 521 CHA Bio Complex, 335 Pangyo-ro, Bundang-gu, Seongnam 463-400, Korea
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Author to whom correspondence should be addressed.
Academic Editor: Guy Van den Mooter
Received: 27 December 2016 / Revised: 29 January 2017 / Accepted: 2 February 2017 / Published: 7 February 2017
(This article belongs to the Collection Poorly Soluble Drugs)
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Abstract

Emodin is a component in a Chinese herb, Rheum officinale Baill, traditionally used for diabetes and anticancer. Its poor solubility is one of the major challenges to pharmaceutical scientists. We previously reported on thermoreversible gel formulations based on poloxamer for the topical delivery of emodin. The present study was to understand the effect of poloxamer type on emodin solubility and its application in cellular activity screening. Various gel formulations composed of poloxamer 407 (P407), poloxamer 188 (P188) and PEG400 were prepared and evaluated. Major evaluation parameters were the gelation temperature (Tgel) and solubility of emodin. The emodin solubility increased with increasing poloxamer concentration and the Tgel was modulated by the proper combination of P407. In particular, this study showed that the amount of P407 in thermoreversible poloxamer gel (PG) was the dominant factor in enhancing solubility and P188 was effective at fixing gelation temperature in the desired range. A thermoreversible emodin PG was selected as the proper composition with the liquid state at room temperature and gel state at body temperature. The gel showed the solubility enhancement of emodin at least 100-fold compared to 10% ethanol or water. The thermoreversible formulation was applied for in vitro cellular activity screening in the human dermal fibroblast cell line and DLD-1 colon cancer cell line after dilution with cell culture media. The thermoreversible gel formulation remained as a clear solution in the microplate, which allowed reliable cellular activity screening. In contrast, emodin solution in ethanol or DMSO showed precipitation at the corresponding emodin concentration, complicating data interpretation. In conclusion, the gel formulation is proposed as a useful prototype topical formulation for testing emodin in vivo as well as in vitro. View Full-Text
Keywords: thermoreversible; poloxamer; emodin; solubility; in vitro cellular activity screening thermoreversible; poloxamer; emodin; solubility; in vitro cellular activity screening
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MDPI and ACS Style

Ban, E.; Park, M.; Jeong, S.; Kwon, T.; Kim, E.-H.; Jung, K.; Kim, A. Poloxamer-Based Thermoreversible Gel for Topical Delivery of Emodin: Influence of P407 and P188 on Solubility of Emodin and Its Application in Cellular Activity Screening. Molecules 2017, 22, 246.

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