Dually Active Apigenin-Loaded Nanostructured Lipid Carriers for Cancer Treatment

Abstract

Cancer is one of the major causes of death worldwide affecting more than 19 million people. Traditional cancer therapies have many adverse effects and often result in unsatisfactory outcomes. Natural flavones, such as apigenin (APG), have demonstrated excellent antitumoral properties. However, they have a low aqueous solubility. To overcome this drawback, APG can be encapsulated in nanostructured lipid carriers (NLC). Therefore, we developed dual NLC encapsulating APG (APG-NLC) with a lipid matrix containing rosehip oil, which is known for its anti-inflammatory and antioxidant properties. Methods: Optimisation, physicochemical characterisation, biopharmaceutical behaviour, and therapeutic efficacy of this novel nanostructured system were assessed. Results: APG-NLC were optimized obtaining an average particle size below 200 nm, a surface charge of −20 mV, and an encapsulation efficiency over 99%. The APG-NLC released APG in a sustained manner, and the results showed that the formulation was stable for more than 10 months. In vitro studies showed that APG-NLC possess significant antiangiogenic activity in ovo and selective antiproliferative activity in several cancer cell lines without exhibiting toxicity in healthy cells. Conclusion: APG-NLC containing rosehip oil were optimised. They exhibit suitable physicochemical parameters, storage stability for more than 10 months, and prolonged APG release. Moreover, APG-NLC were internalised inside tumour cells, showing the capacity to cause cytotoxicity in cancer cells without damaging healthy cells.

Combination of Indomethacin with Nanostructured Lipid Carriers for Effective Anticancer Therapy

“…These observations are in accordance with the results obtained from Turbiscan ® as well as with literature data, which indicates that nanoparticles are more stable at 4 °C than at 25 °C. 53 …”

Fresh Carrier for an Old Topical Local Anesthetic: Benzocaine in Nanostructured Lipid Carriers

“…Differential scanning calorimetry (DSC) thermograms of the optimized NLC formulation were obtained in a TA 2910 calorimeter and analyzed with Thermal Solutions v.125 software (TA Instruments, Delaware). The samples were dried and heated at a rate of 10 °C min –1 from 30 to 200 °C. , Optimized nanoparticles (NLC BZC ) and their control without benzocaine (NLC), besides their main ingredients (CP, P68, and BZC), were run.…”

“…The samples were dried and heated at a rate of 10 °C min −1 from 30 to 200 °C. 22,23 Optimized nanoparticles (NLC BZC ) and their control without benzocaine (NLC), besides their main ingredients (CP, P68, and BZC), were run.…”

Apigenin: A Bioflavonoid with a Promising Role in Disease Prevention and Treatment

“…Dual nanostructured lipid carriers (NLC) encapsulating apigenin (APG-NLC) with a lipid matrix containing rosehip oil, which is identified for its antioxidant and anti-inflammatory properties, were prepared. According to the in vitro studies, APG-NLC exhibited significant anti-angiogenic activity in ovo and selective antiproliferative activity in various cancer cell lines, without showing any toxicity in healthy cells [ 216 ]. Apigenin-loaded Cs/Gel membranes were made.…”

“…The nanoformulation that has been prepared shows antiangiogenic activity and selective antiproliferative activity in multiple cancer cell lines [216] Apigenin-loaded chitosan/gelatin membranes In vitro…”