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Development of Nanostructured Liquid Crystalline Formulation of Anti-Cancer Drug as a New Drug Delivery System

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Abstract

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.

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Abbreviations

GMO:

Glycerol-mono-oleate

PF127:

Poloxamer 407

Cubs:

Cubosomes

Et:

Ethanol

EE:

Entrapping efficiency

PS:

Particle size

BH:

Berberine hydrochloride

AA:

Arachidonic acid

BH-cubs:

Cubosomal berberine hydrochloride

S-BH:

Solid BH-cubosome

NDDS:

New drug delivery systems

PBS:

Phosphate-buffered saline

PdI:

Polydispersity index

MCF-7:

Human breast cancer cell line

Malt:

Maltodextrin

PVA:

Polyvinyl alcohol

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Acknowledgments

The author thanks the Taif University-Deanship of research for its financial support to complete this project. The author also thanks Dr. Reem El Namary and Mrs. Rabab for their help to complete this project.

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Authors and Affiliations

  1. Pharmaceutics Department, Faculty of Pharmacy, Taif University, Taif, Saudi Arabia

    Hadel A. Abo El-Enin

  2. Pharmaceutics Department, National Organization of Drug Control and Research (NODCAR), 7 Abou Hazem St., Pyramids, Giza, Egypt

    Hadel A. Abo El-Enin

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Abo El-Enin, H.A. Development of Nanostructured Liquid Crystalline Formulation of Anti-Cancer Drug as a New Drug Delivery System. J Pharm Innov 15, 80–93 (2020). https://doi.org/10.1007/s12247-019-09371-x

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