Formulation of Quaternized Aminated Chitosan Nanoparticles for Efficient Encapsulation and Slow Release of Curcumin.

Ahmed M Omer,Randa E Khalifa,Mohamed S Mohy-Eldin,Zyta M Ziora,Mark A T Blaskovich,Tamer M Tamer,Mohamed A Hassan

doi:10.3390/molecules26020449

Abstract

An effective drug nanocarrier was developed on the basis of a quaternized aminated chitosan (Q-AmCs) derivative for the efficient encapsulation and slow release of the curcumin (Cur)-drug. A simple ionic gelation method was conducted to formulate Q-AmCs nanoparticles (NPs), using different ratios of sodium tripolyphosphate (TPP) as an ionic crosslinker. Various characterization tools were employed to investigate the structure, surface morphology, and thermal properties of the formulated nanoparticles. The formulated Q-AmCs NPs displayed a smaller particle size of 162 ± 9.10 nm, and higher surface positive charges, with a maximum potential of +48.3 mV, compared to native aminated chitosan (AmCs) NPs (231 ± 7.14 nm, +32.8 mV). The Cur-drug encapsulation efficiency was greatly improved and reached a maximum value of 94.4 ± 0.91%, compared to 75.0 ± 1.13% for AmCs NPs. Moreover, the in vitro Cur-release profile was investigated under the conditions of simulated gastric fluid [SGF; pH 1.2] and simulated colon fluid [SCF; pH 7.4]. For Q-AmCs NPs, the Cur-release rate was meaningfully decreased, and recorded a cumulative release value of 54.0% at pH 7.4, compared to 73.0% for AmCs NPs. The formulated nanoparticles exhibited acceptable biocompatibility and biodegradability. These findings emphasize that Q-AmCs NPs have an outstanding potential for the delivery and slow release of anticancer drugs.

Highlights

Drug delivery systems (DDSs) are pharmaceutical formula or devices designed to overcome the present limitations of conventional therapeutics [1]
The bands at 1645–1649 cm−1 and 1560 cm−1 were assigned to the stretching vibration of the amide-I (C=O of NH-C=O) groups and the N-H bending of amide-II
The results revealed that the aminated chitosan (AmCs) and quaternized aminated chitosan (Q-AmCs) nanoparticles had high positive charges on their entire surfaces

Summary

Introduction

Drug delivery systems (DDSs) are pharmaceutical formula or devices designed to overcome the present limitations of conventional therapeutics [1]. DDSs have the ability to improve the biological activity, enhance the therapeutic index or extend the biological half-life of drugs [2,3]. A wide range of nanoparticles are being advanced to serve as potential carriers for delivering drugs in a controlled mode to specific-targeted sites in the human body [5,6,7,8]. These nano-sized systems have a remarkable aptitude for the targeted delivery of a specific drug dose to specific cells (such as cancer cells), without disturbing the physiology of the normal cells [9]. The targeted nano systems are able to ameliorate poor drug diffusion/release profiles, improve drug solubility, and boost bio-distribution and immunogenicity [10]

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