Novel Obesity Treatment Using Metformin Transdermal Patch

Autor: Shu Wang, Mehrnaz Abbasi
Jazyk: angličtina
Rok vydání: 2021
Předmět:
Zdroj: Curr Dev Nutr
Popis: OBJECTIVES: Metformin is the most commonly used FDA approved antidiabetic drug. Emerging evidence suggest that metformin can induce browning of white adipose tissue (WAT). However, oral administration of metformin has a low level of oral bioavailability, a high level of gastrointestinal side effects, and fast renal clearance, these lower its browning WAT efficacy. Hence, localized delivery of metformin directly to subcutaneous WAT (SubQ WAT) using transdermal delivery approach is an attractive alternative. The objectives of this study are to develop metformin transdermal patch and to evaluate its anti-obesity effects in mice. METHODS: We developed a metformin-loaded patch using the combination of microneedle (MN) and Iontophoresis. Thirty male C57BL/6J mice were fed a high fat diet for 4 weeks. Then, mice were randomly divided into one of the following six groups (5/group): 1. MN + Iontophoresis (Metformin), 2. MN + Iontophoresis (Blank), 3. MN alone, 4. Iontophoresis alone, 5. Gavage (Metformin), and 6. Gavage (Saline). Metformin dose was 3 mg/kg body weight/day. All treatments were given 3 times/week for additional 5 weeks. RESULTS: As compared to those in other treatment groups, MN + Iontophoresis (Metformin)-treated mice had 3.6- and 7.5-fold lower changes in body weight and body fat % (P 3.5-fold), (PGC-1α, >1.3-fold), (CIDEA, >1.9-fold), (TMEM26, 2.6-fold) and UCP1 and phosphorylated AMPK protein expression levels (>9.5- and 9.7-fold), and lower IgWAT mRNA levels of ACC1 (1.5-), leptin (1.2-), MCP1 (1.4-) and TNFα (1.36-fold) (P
Databáze: OpenAIRE