Abstract
ABSTRACTChitosan (CS)-acetylsalicylic acid (ASA) nanoparticles, which are well dispersed and stable in aqueous solution, have been prepared by interpolymer complexation of ASA in CS solution. The physicochemical properties of nanoparticles were investigated by using FT-IR, 1H NMR, scanning electron microscope（SEM）, dynamic light scattering, and UV spectrophotometer. It was found that the carboxyl group of the ASA had firmly integrated on the amino group of CS and the ASA-CS nanoparticles were almost spherical in shape with an average diameter of less than (79.3 ± 24.6) nm in high reproducibility and showed high chemical stability against environmental changes. It was also found that the prepared nanoparticles carried a positive charge and showed the size in the range from 700 to 150 nm. The surface structure and zeta potential of nanoparticles can be controlled by different preparation processes. The factor experiment results indicated that the ASA-CS nanoparticles had satisfactory loading capacity (LC) and encapsulation efficiency (EE), 27.27% and 46.88% (data not shown), respectively. The experiments of in vitro ASA release showed that these nanoparticles provided a sustained and pH-dependent drug release manner, and the release behavior was influenced by the pH value of the medium. Preliminary pharmacology experiment exhibited prolonged circulation and higher bioavailability than that of ASA. All the results indicated that ASA/CS nanoparticles may have promising pharmaceutical application, and further pharmacological research is needed to confirm these beneficial effects.
Highlights
Acute myocardial infarction (AMI) and thromboembolic disease are a major cause of morbidity and mortality worldwide, so the development of effective drugs for the prevention and treatment of such diseases has increasingly attracted worldwide attention
The – NH2 bending vibration shifted from 1646 cm−1 to 1630 cm−1 and a new peak at 1595 cm−1 appeared, which indicated that some interaction between acetylsalicylic acid (ASA) and CS have occurred within the nanoparticles
Comparison of the 1H NMR data among acetylsalicylic acid, chitosan and ASA-CS nanoparticles, it showed that the acetylsalicylic acid acyl had replaced the -NH of chitosan,which indicated that the acetylsalicylic acid acyl had combined into the chitosan amino
Summary
Acute myocardial infarction (AMI) and thromboembolic disease are a major cause of morbidity and mortality worldwide, so the development of effective drugs for the prevention and treatment of such diseases has increasingly attracted worldwide attention. Acetylsalicylic acid (ASA) had significant anti-platelet aggregation function [1] and it had been used for the prevention and treatment of AMI and thrombosis diseases from 1970s [2]. Evidencebased studies had proved that ASA could reduce the incidence rate of 25% of heart and brain and peripheral thromboembolic disease [3,4]. For myocardial infarction and stroke, long-term use of the low-dose acetylsalicylic acid (ASA) could significantly reduce the incidence of this diseases. Many studies found that some patients would get aspirin resistance (AR) or aspirin failure (AF) [5]. All of these limited the application of ASA. To improve the pharmacological properties of ASA, lots of research work has been done around the world [6,7,8,9], but little progress has been made
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