Abstract


 CD-nanosponges were prepared by crosslinking B-CD with diphenylcarbonate (DPC) using ultrasound assisted technique. 5-FU was incorporated with NS by freeze drying, and the phase solubility study, complexation efficiency (CE) entrapment efficiency were performed. Also, the particle morphology was studied using SEM and AFM. The in-vitro release of 5-FU from the prepared nanosponges was carried out in 0.1N HCl.
 5-FU nanosponges particle size was in the nano size. The optimum formula showed a particle size of (405.46±30) nm, with a polydispersity index (PDI) (0.328±0.002) and a negative zeta potential (-18.75±1.8). Also the drug entrapment efficiency varied with the CD: DPC molar ratio from 15.6 % to 30%. The SEM and AFM showed crystalline and porous nature of the nanosponges. The in vitro drug release study of the selected formula 5-FUNS2 exhibited the fastest dissolution rate which is 56% in the first hr.
 Different molar ratios of (cyclodextrin to crosslinker) (CD: DPC) has a proficient effect on complexation efficiency (CE), apparent stability constant (Kst) and entrapment efficiency of 5-FU. 5-FUNS2 with (1:4) molar ratio showed the best result of CE, Kst and entrapment efficiency. 5-FUNS2 gave a higher release rate than the 5-FU-BCD inclusion complex and 5-FU solution. Surface morphology of the prepared nanosponges by SEM, AFM indicate that nanosized and highly porous nanosponges was obtained. The overall results suggest that cyclodextrin nanosponges could be a promising 5-FU delivery system utilizing the suitable formula.

Highlights

  • IntroductionChemotherapeutic agents can reduce tumor size and cancer remission and have a high potential to destroy cancer cells, they are not organ specific and can damage proliferative cells[1]

  • Chemotherapeutic agents can reduce tumor size and cancer remission and have a high potential to destroy cancer cells, they are not organ specific and can damage proliferative cells[1].One of the major goals of cancer therapeutics is to kill cancer cells without damaging normal tissues

  • Conventional chemotherapeutic agents work by destroying rapid dividing cells, which is the main property of neoplastic cells

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Summary

Introduction

Chemotherapeutic agents can reduce tumor size and cancer remission and have a high potential to destroy cancer cells, they are not organ specific and can damage proliferative cells[1]. One of the major goals of cancer therapeutics is to kill cancer cells without damaging normal tissues. Tissue and cell distribution of cancer therapeutic drugs can be controlled by the entrapment in sub-micron level (˂1 μm) colloidal systems, in other words known as nanoparticles. Conventional chemotherapeutic agents work by destroying rapid dividing cells, which is the main property of neoplastic cells. This is why chemotherapy damages normal healthy cells that divide rapidly such as cells in the bone marrow, macrophages, digestive tract, and hair follicles [3]

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