Amity Institute of Biotechnology, Amity University, Uttar Pradesh, Sector-125, Noida, 201313, India.
All India Institute of Medical Sciences, Ansari Nagar, New Delhi, 110029, India.
Colloids Surf B Biointerfaces. 2021 Jun;202:111670. doi: 10.1016/j.colsurfb.2021.111670. Epub 2021 Mar 3.
Carbenoxolone (CBX) is a semi-synthetic plant derivative with pleiotropic pharmacological properties like anti-microbial and anti-inflammatory activities. Though approved for treatment of gastric ulcers, its use is limited due to adverse effects such as cytotoxicity. Bovine serum albumin (BSA) is a natural, non-toxic protein with high water-solubility and low immunogenicity, and is widely used as a nanocarrier for targeted drug delivery. In the present study, controlled release BSA-CBX nanoparticles (NPs) were synthesized by desolvation method to reduce drug cytotoxicity. These NPs showed desirable physicochemical properties such as particle size (∼240 nm), polydispersity index (0.08), zeta potential (-7.12 mV), drug encapsulation efficiency (72 %), and were stable for at least 3 months at room temperature. The drug was released from the BSA-CBX NPs in a biphasic manner in vitro following non-fickian diffusion. Computational analysis determined that the binding between BSA and CBX occurred through van der Waals forces, hydrophobic interactions, and hydrogen bonds with 93 % steric stability. Further, the cytotoxic assays demonstrated ∼1.8-4.9-fold reduction in cytotoxicity using three human cell lines (A549, MCF-7, and U-87). Subsequently, this novel CBX formulation with BSA as an efficient carrier can potentially be used for diverse biomedical applications.
卡波氯铵（CBX）是一种具有多种药理学特性的半合成植物衍生物，具有抗菌和抗炎活性。尽管已被批准用于治疗胃溃疡，但由于其细胞毒性等不良反应，其应用受到限制。牛血清白蛋白（BSA）是一种天然、无毒的蛋白质，具有高水溶性和低免疫原性，广泛用作靶向药物递送的纳米载体。在本研究中，通过去溶剂化法合成了具有缓释作用的 BSA-CBX 纳米颗粒（NPs），以降低药物的细胞毒性。这些 NPs 具有理想的物理化学性质，如粒径（约 240nm）、多分散指数（0.08）、Zeta 电位（-7.12mV）、药物包封效率（72%），在室温下至少稳定 3 个月。体外实验表明，BSA-CBX NPs 中的药物以非菲克扩散方式呈两相释放。计算分析表明，BSA 与 CBX 之间的结合是通过范德华力、疏水相互作用和氢键实现的，具有 93%的空间稳定性。此外，细胞毒性试验表明，三种人类细胞系（A549、MCF-7 和 U-87）的细胞毒性降低了 1.8-4.9 倍。因此，这种新型的以 BSA 为载体的 CBX 制剂可能具有广泛的生物医学应用前景。
