Topical administration is a promising clinical strategy to avoid serious gastrointestinal adverse reactions of loxoprofen sodium (LOX), a new non-steroidal anti-inflammatory drug. Small molecule organic acids had been reported with the ability of promoting transdermal rate of several drugs. In this article, the effect of small molecule organic acids on the transdermal delivery of LOX was studied, and the possible mechanism was also explored by Fourier infrared spectroscopy , differential scanning calorimetry , tape stripping, etc. The results showed that lactic acid and fumaric acid could significantly increase the penetration rate of LOX and reduce time lag even without the help of acidic environment. The preliminary mechanism investigation inferred that fumaric acid could increase LOX’s distribution in stratum corneum and might change its complexation state, but had little effect on the drug structure and skin’s lipids and proteins configuration. The topical LOX gel using fumaric acid as penetration enhancer had higher transdermal rate, significant anti-inflammatory effect and no obvious skin irritation . This study proved the promising application of small molecule organic acids in transdermal enhancing and provided a potential strategy for transdermal delivery of LOX combined with fumaric acid.
Strontium-doped mesoporous bioactive glass microspheres (Sr-MBGMs) were prepared by sol–gel method for delivering loxoprofen sodium (LX) drug. The loading capacity of the prepared Sr-MBGMs for LX drug was affected by the initial concentration of the drug solution and adsorption time. The LX-loaded Sr-MBGMs obtained under optimum conditions were coated with polydopamine (LX/Sr-MBGMs@PDA) and incorporated into the aminated modified poly-l-lactic acid nanofibrous matrix to develop a functional composite scaffold for bone tissue engineering applications. The in vitro studies revealed that the incorporation of the LX/Sr-MBGMs@PDA could promote cell proliferation and biomineralization, indicating that the as-developed composite scaffolds possessed an improved cell viability and osteogenic ability.
Oxidative stress is a key factor in the development of inflammatory diseases. Elimination of reactive oxygen species (ROS) in the inflamed colon has been confirmed as an effective strategy to alleviate inflammatory bowel disease (IBD). The conventional approaches will cause systemic absorption and potential side effects. To address these issues, we develop a nanomedicine ( [email protected] NPs) that is capable of delivering to target inflammatory lesions by electrostatic adsorption, subsequently effectively scavenging the excess ROS and alleviating inflammation to ameliorate ulcerative colitis (UC). In the DSS induced acute colitis mice model, [email protected] NPs can significantly reduce the production of pro-inflammatory cytokines, alleviate oxidative stress, and promote the favorable recovery of the damaged colonic tissue. These results indicate that [email protected] NPs are able to effectively alleviate intestinal inflammation and provide strong theoretical support for the treatment of other inflammatory diseases.
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