Purpose

This study is concerned with encapsulation of the anti-cancer drug (berberine hydrochloride (BH)) in nanocarriers as cubosomes, which is, then, formulated in solid form to ease its incorporation into different drug delivery systems, improve its solubility, and improve its anti-cancer activity.

Methods

BH cubosomes were prepared using glyceryl mono-oleate (GMO) and poloxamer 407 (PF127). Polyvinyl alcohol (PVA) was added as a stabilizer. The well-characterized cubosome formula via particle size, entrapment efficiency, and in vitro release study was converted into free-flowing powder (S-BH) using sugar carriers at different mass ratios. The prepared powdered cubosome S-BH was subjected to in vitro characterization, such as flowability, compressibility, drug solubility, and drug release studies. The prepared formula’s cytotoxic effects on human breast cancer cell line (MCF-7) were studied.

Results and Discussion

The prepared cubosome formula has an average particle size of 220.8 nm with a polydispersity index (PdI) < 1 and a high drug EE value (64.75%). The BH release rate begins relatively fast followed by a slower release rate. S-BH has good flowability and compressibility as evidenced by decreased repose angle (31.53 ± 0.31) and lowered required pressure for compression (60.07 ± 6.16). Enhanced dissolution rate and increased drug solubility relate to the increased particle surface area as a result of decreased particle size. It also provides high anti-proliferative and apoptotic activities against breast cancer cells.

Conclusion

The prepared solid cubosomal BH can be utilized for the preparation of different solid dosage forms, like tablets and capsules.

中文翻译：

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新型抗癌药物纳米结构液晶制剂的开发

目的

这项研究涉及将抗癌药（盐酸小ber碱（BH））包裹在纳米载体中作为立方脂质体，然后将其制成固体形式，以易于将其掺入不同的药物递送系统，提高其溶解度并改善其抗癌活性。

方法

BH cusomesomes使用甘油单油酸酯（GMO）和泊洛沙姆407（PF127）制备。加入聚乙烯醇（PVA）作为稳定剂。通过粒径，包封率和体外释放研究，表征良好的立方糖配方被转化为使用不同质量比的糖载体的自由流动粉末（S-BH）。对制得的粉状立方体S-BH进行体外表征，例如流动性，可压缩性，药物溶解度和药物释放研究。研究了制备的配方对人乳腺癌细胞系（MCF-7）的细胞毒性作用。

结果与讨论

制备的立方微粒配方的平均粒径为220.8 nm，多分散指数（PdI）<1，药物EE值较高（64.75％）。BH释放速率开始相对较快，然后释放速率较慢。S-BH具有良好的流动性和可压缩性，如减小的休止角（31.53±0.31）和降低的压缩所需压力（60.07±6.16）所证明。由于减小的粒度，提高的溶出速率和增加的药物溶解度与增加的颗粒表面积有关。它还提供了针对乳腺癌细胞的高抗增殖和凋亡活性。

结论

制备的固体cusosomal BH可用于制备不同的固体剂型，如片剂和胶囊剂。