Potential Lipolytic Effect of Panduratin A Loaded Microspicule Serum as a Transdermal Delivery Approach for Subcutaneous Fat Reduction

• Published in: Biological & pharmaceutical bulletin Vol. 46; no. 12; pp. 1761 - 1768
• Main Authors: Jitsaeng, Kusuma, Duangjit, Sureewan, Sritananuwat, Phaijit, Tansathien, Kritsanaporn, Opanasopit, Praneet, Rangsimawong, Worranan
• Format: Journal Article
• Language: English
• Published: Tokyo The Pharmaceutical Society of Japan 01-12-2023; Japan Science and Technology Agency
• Subjects: Adipogenesis; antiadipogenesis; Bioactive compounds; Biological activity; Body fat; Boesenbergia rotunda extract; Drug delivery; Erythema; Hydration; Lipolysis; lipolytic body product; microspicule; panduratin A; Skin
• ISSN: 0918-6158; 1347-5215
• DOI: 10.1248/bpb.b23-00491

Boesenbergia rotunda (L.) Mansf contained a potent anti-obesity agent. The objectives of this study were to investigate the anti-adipogenesis and lipolysis effects of panduratin A from B. rotunda extract and develop extract-loaded lipolytic body microspicule (MS) serum. Panduratin A that was separated from the ethanolic extract of B. rotunda in fraction 3 (BP-3) were studied the bioactivity of 3T3-L1 preadipocyte cells. The extract-loaded MS serum was formulated and evaluated for safety and efficacy. The BP-3 extract containing panduratin A at 0.29 g per g of the extract was not toxic to the cells at concentrations lower than 10 µg/mL, and the antiadipogenesis and lipolysis effects of the BP-3 extract were strong at 10 µg/mL. To deliver bioactive panduratin A into and through the skin, MS serum was successfully formulated. Application of BP-3 extract-loaded MS serum to the human thigh for 14 d reduced the thigh circumference and increased skin hydration and firmness. Although the skin erythema was increased, no severe redness or pain was found. In conclusion, BP-3 extract acts as a potent bioactive compound to inhibit adipocyte cells, and the antiadipogenesis and lipolysis effects of BP-3 extract in MS serum might play an important role as a potential lipolytic body product for reducing human subcutaneous fat mass.