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

Abstract

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