Formulation optimization of pH-sensitive liposomes based drug delivery of Carboplatin and anti-proliferative evaluation against A549 (human lung carcinoma) cell lines

IF 1.3 4区化学 Q3 CHEMISTRY, MULTIDISCIPLINARY

Main Group Chemistry Pub Date : 2023-02-09 DOI:10.3233/mgc-220078

Preeti Aneja, Prabha Negi, Shivali Aneja, Suyog Rajendra Garad, Sunil Kumar

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引用次数: 0

Abstract

The developments of pH–sensitive liposomes which are stable at physiological pH i.e. (6.8–7.4) have not explored much up until now. These lipid vesicles will go through destabilization and attain fusogenic properties in acidic conditions leading to liberation of aqueous contents. Carboplatin, included in the family of alkylating agent was found to exhibit adverse effects like myelo suppression, ion thrombocytopenia and leucopenia. Therefore, in order to circumvent these effects, carboplatin pH-sensitive liposomes for specific delivery is the ideal criteria and it poses a great challenge since the water-soluble drugs exhibited very low entrapment efficiency. The essential portion of study was evaluated using the Design Expert software 8. The pH-sensitive liposomes were optimized using Central composite design and one factor Response surface model design method and were prepared by film hydration method. Two formulation variables like drug: lipid ratio (X1) and volume of hydration media (X2) used to vary at three different levels and the other three variables viz. temperature, speed of rotation and vacuum applied were kept constant. The Response surface and contour plots were figured to elicit the effects of interaction of variables on the overall entrapment efficiency. pH-sensitive liposomes of carboplatin have been regarded as a promising delivery systematic approach in order to target tumor tissue as evaluated by the pre-clinical studies in both in vitro and ex-vivo conditions.

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基于ph敏感脂质体的卡铂给药配方优化及对A549(人肺癌)细胞系的抗增殖评价

在生理pH值(6.8-7.4)稳定的pH敏感脂质体的研究进展至今尚未见进展。这些脂质囊泡将在酸性条件下经历不稳定并获得促聚变特性，从而导致水内容物的释放。卡铂属于烷基化剂家族，研究发现其不良反应包括骨髓抑制、离子性血小板减少和白细胞减少。因此，为了规避这些影响，卡铂ph敏感脂质体是用于特异性递送的理想标准，但由于水溶性药物的包封效率非常低，因此它提出了很大的挑战。使用Design Expert软件对研究的重要部分进行了评估。采用中心复合设计和单因素响应面模型设计对ph敏感脂质体进行优化，并采用膜水化法制备脂质体。药物脂质比(X1)和水化介质体积(X2)这两个配方变量在三个不同的水平上变化，其他三个变量温度、旋转速度和真空度保持不变。绘制响应面和等高线图，揭示各变量交互作用对整体捕获效率的影响。通过体外和离体的临床前研究，卡铂的ph敏感性脂质体已被认为是一种有前途的靶向肿瘤组织的系统递送方法。

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来源期刊

Main Group Chemistry 化学-化学综合

CiteScore

2.00

自引率

26.70%

发文量

审稿时长

>12 weeks

期刊介绍： Main Group Chemistry is intended to be a primary resource for all chemistry, engineering, biological, and materials researchers in both academia and in industry with an interest in the elements from the groups 1, 2, 12–18, lanthanides and actinides. The journal is committed to maintaining a high standard for its publications. This will be ensured by a rigorous peer-review process with most articles being reviewed by at least one editorial board member. Additionally, all manuscripts will be proofread and corrected by a dedicated copy editor located at the University of Kentucky.