Zafar Mah Noor, Pitt William G, Husseini Ghaleb A
Biomedical Engineering Program, College of Engineering, American University of Sharjah, Sharjah, P.O. Box. 26666, United Arab Emirates.
Department of Chemical Engineering, Brigham Young University, Provo, UT, 84602, USA.
Heliyon. 2024 Mar 13;10(6):e27882. doi: 10.1016/j.heliyon.2024.e27882. eCollection 2024 Mar 30.
Achieving an optimal therapeutic level is crucial in effectively eradicating cancer cells during treatment. However, conventional chemotherapy-associated systemic administration of anticancer agents leads to many side effects. To achieve the desired control over the target site, active targeting of HER2-positive breast cancer cells can be achieved by conjugating liposomal vesicles with Human Epidermal growth factor Receptor 2 (HER2) and inducing release of the encapsulated drug using ultrasound. To further enhance the delivery efficiency, nanoemulsion droplets exhibiting responsiveness to low-frequency ultrasound are encapsulated within these lipid vesicles. In this study, we prepared four different liposomal formulations, namely pegylated liposomes, emulsion liposomes (eLiposomes), HER-conjugated liposomes, and HER-conjugated eLiposomes, each loaded with calcein and subjected to a thorough characterization process. Their sizes, phospholipid concentration, and amount of antibody conjugation were compared and analyzed. Cryogenic transmission electron microscopy was used to confirm the encapsulation of nanoemulsion droplets within the liposomes. The drug-releasing performance of Herceptin-conjugated eLiposomes was found to surpass that of other liposomal formulations with a notably higher calcein release and established it as a highly effective nanocarrier. The study showcases the efficacy of calcein-loaded and Herceptin-conjugated eLiposomes, which demonstrate rapid and efficient drug release among other liposomal formulations when subjected to ultrasound. This discovery paves the way for a more targeted, efficient, and humane approach to cancer therapy.
在治疗过程中达到最佳治疗水平对于有效根除癌细胞至关重要。然而，传统的与化疗相关的抗癌药物全身给药会导致许多副作用。为了实现对靶位点的理想控制，可以通过将脂质体囊泡与人表皮生长因子受体2（HER2）偶联，并使用超声诱导包封药物的释放，来实现对HER2阳性乳腺癌细胞的主动靶向。为了进一步提高递送效率，将对低频超声有响应的纳米乳液滴包封在这些脂质囊泡中。在本研究中，我们制备了四种不同的脂质体制剂，即聚乙二醇化脂质体、乳液脂质体（e脂质体）、HER偶联脂质体和HER偶联e脂质体，每种制剂都负载了钙黄绿素，并进行了全面的表征过程。比较并分析了它们的大小、磷脂浓度和抗体偶联量。低温透射电子显微镜用于确认脂质体内纳米乳液滴的包封情况。发现赫赛汀偶联e脂质体的药物释放性能优于其他脂质体制剂，钙黄绿素释放量显著更高，并将其确立为一种高效的纳米载体。该研究展示了负载钙黄绿素和赫赛汀偶联e脂质体的功效，当受到超声作用时，它们在其他脂质体制剂中表现出快速有效的药物释放。这一发现为癌症治疗开辟了一条更具针对性、高效且人道的途径。
