Transdermal Delivery of Anti‐Obesity Compounds to Subcutaneous Adipose Tissue with Polymeric Microneedle Patches. Issue 11 (13th October 2017) - Than, Aung
Abstract: Excess white adipose tissue (WAT), or obesity, is the leading cause of many diseases. Combating obesity is, however, challenging due to the fact that laboratory‐proven anti‐obesity compounds lose effectiveness or/and cause severe side‐effects while being delivered via conventional routes. Here, a new strategy is reported using disposable transdermal patches equipped with detachable polymeric microneedle (MN) arrays for painless and bloodless drug delivery to subcutaneous WAT. In contrast to the current methods to reduce energy intake, MN‐patches are used to deliver anti‐obesity compounds to increase energy expenditure by transforming calorie‐storing white fat into calorie‐burning brown fat. Specifically, prominent WAT browning and reduction effects are demonstrated by β3‐adrenoceptor agonist and thyroid hormone T3 transdermally delivered from rapidly dissolving MNs on mice. Furthermore, using a diet‐induced obese mouse model, it is shown that β3‐adrenoceptor agonist released by slowly dissolving MNs can effectively promote WAT browning and suppress gaining of body fat and weight, without the need of daily administration. Such an MN approach can achieve a much lower effective dose as compared to systemic administration and enables long‐term home‐based treatment. Abstract : A new anti‐obesity strategy using transdermal patches equipped with a detachable polymeric microneedle array is developed for localized drug‐delivery targeting on subcutaneous fat and nudging it toward energy‐burning brown‐like adipose tissue. This painless and bloodless delivery strategy promises high drug integrity, low therapeutic dose, low side‐effects, and amenability for home‐based long‐term management of obesity and associated metabolic diseases.